We previously prepared nerve growth factor poly-lactide co-glycolid sustained-release microspheres to treat rat sciatic nerve injury using the small gap sleeve technique.Multiple growth factors play a synergistic role...We previously prepared nerve growth factor poly-lactide co-glycolid sustained-release microspheres to treat rat sciatic nerve injury using the small gap sleeve technique.Multiple growth factors play a synergistic role in promoting the repair of peripheral nerve injury;as a result,in this study,we added basic fibroblast growth factors to the microspheres to further promote nerve regeneration.First,in an in vitro biomimetic microenvironment,we developed and used a drug screening biomimetic microfluidic chip to screen the optimal combination of nerve growth factor/basic fibroblast growth factor to promote the regeneration of Schwann cells.We found that 22.56 ng/mL nerve growth factor combined with 4.29 ng/mL basic fibroblast growth factor exhibited optimal effects on the proliferation of primary rat Schwann cells.The successfully prepared nerve growth factor-basic fibroblast growth factor-poly-lactide-co-glycolid sustained-release microspheres were used to treat rat sciatic nerve transection injury using the small gap sleeve bridge technique.Compared with epithelium sutures and small gap sleeve bridging alone,the small gap sleeve bridging technique combined with drug-free sustained-release microspheres has a stronger effect on rat sciatic nerve transfection injury repair at the structural and functional level.展开更多
The management of diabetes mellitus is based on lifestyle and dietary measures suggesting the consumption of foods with a low glycemic index. The present study was conducted in order to propose food formulas based on ...The management of diabetes mellitus is based on lifestyle and dietary measures suggesting the consumption of foods with a low glycemic index. The present study was conducted in order to propose food formulas based on white rice and white beans resulting in a lower glycemic response. For this, food formulations based on these foods were first made, in particular the formulation [75% white rice + 25% white beans] and the formulation [50% rice + 50% white beans]. Then, the biochemical composition of white rice, white bean and these two formulations was determined by the usual methods. Finally, their glycemic responses over 120 minutes were studied by the FAO/ WHO 1998 method. The results showed that white rice [100% white rice] had the highest carbohydrate content (54.61%) followed respectively by the formulation [75% white rice + 25% white bean] (45.69%), the white bean [100% white bean] (29.1%) and the formulation [50% white rice + 50% white bean] (26.16%). In terms of glycemic responses, the formulation [50% white rice + 50% white beans] presented the best evolution with a lower peak (6.041 mmol/L) observed at T45<sub>min</sub> and a lower postprandial glycemia (4.872 mmol/ L) at T120<sub>min</sub>. An increase in the proportion of beans is therefore recommended as it may suggest a beneficial metabolic effect.展开更多
Liposome is one of the most widely used carriers for drug delivery because of the great biocompatibility and biodegradability.Due to the complex formulation components and preparation process,formulation screening mos...Liposome is one of the most widely used carriers for drug delivery because of the great biocompatibility and biodegradability.Due to the complex formulation components and preparation process,formulation screening mostly relies on trial-and-error process with low efficiency.Here liposome formulation prediction models have been built by machine learning(ML)approaches.The important parameters of liposomes,including size,polydispersity index(PDI),zeta potential and encapsulation,are predicted individually by optimal ML algorithm,while the formulation features are also ranked to provide important guidance for formulation design.The analysis of key parameter reveals that drug molecules with logS[-3,-6],molecular complexity[500,1000]and XLogP3(≥2)are priority for preparing liposome with higher encapsulation.In addition,naproxen(NAP)and palmatine HCl(PAL)represented the insoluble and water-soluble molecules are prepared as liposome formulations to validate prediction ability.The consistency between predicted and experimental value verifies the satisfied accuracy of ML models.As the drug properties are critical for liposome particles,the molecular interactions and dynamics of NAP and PAL liposome are further investigated by coarse-grained molecular dynamics simulations.The modeling structure reveals that NAP molecules could distribute into lipid layer,while most PAL molecules aggregate in the inner aqueous phase of liposome.The completely different physical state of NAP and PAL confirms the importance of drug properties for liposome formulations.In summary,the general prediction models are built to predict liposome formulations,and the impacts of key factors are analyzed by combing ML with molecular modeling.The availability and rationality of these intelligent prediction systems have been proved in this study,which could be applied for liposome formulation development in the future.展开更多
A solid sustained-release energetic material sample,an eruption device and a complete test system were prepared further to analyse the combustion characteristics of solid sustainedrelease energetic materials.The high-...A solid sustained-release energetic material sample,an eruption device and a complete test system were prepared further to analyse the combustion characteristics of solid sustainedrelease energetic materials.The high-temperature heat flux generated by the combustion of the samples from the eruption device was used to penetrate the Q235 target plate.In addition,the meaning and calculation formula of energy density characterising the all-around performance of heat flux were proposed.The numerical simulation of the combustion effect of samples was carried out.According to the data comparison,the numerical simulation results agreed with the experimental results,and the maximum deviation between the two was less than 8.9%.In addition,the structure of the combustion wave and high-temperature jet was proposed and analysed.Based on theoretical analysis,experimental research and numerical simulation,the theoretical burning rate formula of the sample was established.The maximum error between the theoretically calculated mass burning rate and the experimental results was less than 9.8%.Therefore,using the gas-phase steady-state combustion model to study the combustion characteristics of solid sustained-release energetic materials was reasonable.The theoretical burning rate formula also had high accuracy.Therefore,the model could provide scientific and academic guidance for the theoretical research,system design and practical application of solid sustained-release energetic materials in related fields.展开更多
Difenoconazole(DIF)is a representative variety of broad-spectrum triazole fungicides and liposoluble pesticides.However,the water solubility of DIF is so poor that its application is limited in plant protection.In add...Difenoconazole(DIF)is a representative variety of broad-spectrum triazole fungicides and liposoluble pesticides.However,the water solubility of DIF is so poor that its application is limited in plant protection.In addition,the conventional formulations of DIF always contain abundant organic solvents,which may cause pollution of the environment.In this study,two DIF/cyclodextrins(CDs)inclusion complexes(ICs)were successfully prepared,which were DIF/β-CD IC and DIF/hydroxypropyl-β-CD IC(DIF/HP-β-CD IC).The effect of cyclodextrins on the water solubility and the antifungal effect of liposoluble DIF pesticide were investigated.According to the phase solubility test,the molar ratio and apparent stability constant of ICs were obtained.Fourier transform infrared spectroscopy,thermal gravity analysis,X-ray diffraction and scanning electron microscopy were used systematically to characterize the formation and characteristics of ICs.The results noted that DIF successfully entered the cavities of two CDs.In addition,the antifungal effect test proved the better performance of DIF/HP-β-CD IC,which exceeded that of DIF emulsifiable concentrate.Therefore,our study provides informative direction for the intelligent use of liposoluble pesticides with cyclodextrins to develop water-based environmentally friendly formulations.展开更多
BACKGROUND Diabetic retinopathy(DR)is the primary cause of visual problems in patients with diabetes.The Heyingwuzi formulation(HYWZF)is effective against DR.AIM To determine the HYWZF prevention mechanisms,especially...BACKGROUND Diabetic retinopathy(DR)is the primary cause of visual problems in patients with diabetes.The Heyingwuzi formulation(HYWZF)is effective against DR.AIM To determine the HYWZF prevention mechanisms,especially those underlying mitophagy.METHODS Human retinal capillary endothelial cells(HRCECs)were treated with high glucose(hg),HYWZF serum,PX-478,or Mdivi-1 in vitro.Then,cell counting kit-8,transwell,and tube formation assays were used to evaluate HRCEC proliferation,invasion,and tube formation,respectively.Transmission electron microscopy was used to assess mitochondrial morphology,and Western blotting was used to determine the protein levels.Flow cytometry was used to assess cell apoptosis,reactive oxygen species(ROS)production,and mitochondrial membrane potential.Moreover,C57BL/6 mice were established in vivo using streptozotocin and treated with HYWZF for four weeks.Blood glucose levels and body weight were monitored continuously.Changes in retinal characteristics were evaluated using hematoxylin and eosin,tar violet,and periodic acid-Schiff staining.Protein levels in retinal tissues were determined via Western blotting,immunohistochemistry,and immunostaining.RESULTS HYWZF inhibited excessive ROS production,apoptosis,tube formation,and invasion in hg-induced HRCECs via mitochondrial autophagy in vitro.It increased the mRNA expression levels of BCL2-interacting protein 3(BNIP3),FUN14 domain-containing 1,BNIP3-like(BNIP3L,also known as NIX),PARKIN,PTEN-induced kinase 1,and hypoxia-inducible factor(HIF)-1α.Moreover,it downregulated the protein levels of vascular endothelial cell growth factor and increased the light chain 3-II/I ratio.However,PX-478 and Mdivi-1 reversed these effects.Additionally,PX-478 and Mdivi-1 rescued the effects of HYWZF by decreasing oxidative stress and apoptosis and increasing mitophagy.HYWZF intervention improved the symptoms of diabetes,tissue damage,number of acellular capillaries,and oxidative stress in vivo.Furthermore,in vivo experiments confirmed the results of in vitro experiments.CONCLUSION HYWZF alleviated DR and associated damage by promoting mitophagy via the HIF-1α/BNIP3/NIX axis.展开更多
3 D printing is a method of rapid prototyping and manufacturing in which materials are deposited onto one another in layers to produce a three-dimensional object. Although 3 D printing was developed in the 1980 s and ...3 D printing is a method of rapid prototyping and manufacturing in which materials are deposited onto one another in layers to produce a three-dimensional object. Although 3 D printing was developed in the 1980 s and the technology has found widespread industrial applications for production from automotive parts to machine tools,its application in pharmaceutical area is still limited. However,the potential of 3 D printing in the pharmaceutical industry is now being recognized. The ability of 3 D printing to produce medications to exact specifications tailored to the needs of individual patients has indicated the possibility of developing personalized medicines. The technology allows dosage forms to be precisely printed in various shapes,sizes and textures that are difficult to produce using traditional techniques. However,there are various challenges associated with the proper application of3 D printing in the pharmaceutical sector which should be overcome to exploit the scope of this technology. In this review,an overview is provided on the various 3 D printing technologies used in fabrication of complex dosage forms along with their feasibility and limitations.展开更多
A dry flowable formulation of Clonostachys rosea with fungicidal activity against Sclerotinia sclerotiorum was prepared by spray drying. The formulation was optimized by a four-factor, three-level orthogonal experimen...A dry flowable formulation of Clonostachys rosea with fungicidal activity against Sclerotinia sclerotiorum was prepared by spray drying. The formulation was optimized by a four-factor, three-level orthogonal experiment to screen inert ingredients and spray-drying conditions. The optimal dry flowable formulation of C. rosea included 30% C. rosea (ratio of conidia powder and its fermentation broth is 1:3), 3% Morwet EFW, 4% K12, 10% Morwet D425, 9% sodium salt of polynaphthalene sulphonic acid (NNO), 5% croscarmellose sodium, 5% (NH4)2SO4, 0.5% carboxymethyl cellulose sodium (CMC-Na), 1% oxalic acid and palygorskite (carrier) up to 100%. The formulation exhibited good physical characteristics, such as high dispersibility, viability and a long shelf life. Plate antagonism tests and pot trials indicated that the dry flowable formulation was very effective against S. sclerotiorum, with control efficiency of up to 88.30%. This dry flowable formulation of C. rosea is a new potential commercial fungicide for spray drying to control S. sclerotiorum.展开更多
Oral disintegrating tablets(ODTs) are a novel dosage form that can be dissolved on thetongue within 3 min or less especially for geriatric and pediatric patients. Current ODT for-mulation studies usually rely on the p...Oral disintegrating tablets(ODTs) are a novel dosage form that can be dissolved on thetongue within 3 min or less especially for geriatric and pediatric patients. Current ODT for-mulation studies usually rely on the personal experience of pharmaceutical experts andtrial-and-error in the laboratory, which is inefficient and time-consuming. The aim of cur-rent research was to establish the prediction model of ODT formulations with direct com-pression process by artificial neural network(ANN) and deep neural network(DNN) tech-niques. 145 formulation data were extracted from Web of Science. All datasets were dividedinto three parts: training set(105 data), validation set(20) and testing set(20). ANN andDNN were compared for the prediction of the disintegrating time. The accuracy of the ANNmodel have reached 85.60%, 80.00% and 75.00% on the training set, validation set and testingset respectively, whereas that of the DNN model were 85.60%, 85.00% and 80.00%, respec-tively. Compared with the ANN, DNN showed the better prediction for ODT formulations.It is the first time that deep neural network with the improved dataset selection algorithmis applied to formulation prediction on small data. The proposed predictive approach couldevaluate the critical parameters about quality control of formulation, and guide researchand process development. The implementation of this prediction model could effectivelyreduce drug product development timeline and material usage, and proactively facilitatethe development of a robust drug product.展开更多
Nutritional evaluation of complementary food formulations from maize, soybean and peanut fortified with Moringa oleifera leaf powder was carried out. Maize, soybean and peanut were blended in a ratio of 60:30:10 to pr...Nutritional evaluation of complementary food formulations from maize, soybean and peanut fortified with Moringa oleifera leaf powder was carried out. Maize, soybean and peanut were blended in a ratio of 60:30:10 to produce a complementary food, which was then fortified. While the unfortified food product (sample A) served as control, the other three formulations were fortified with 5%, 10% and 15% Moringa leaf powder to give three samples (B, C and D respectively) of fortified food. Nutritional composition determination and feeding trials were then carried out, using two weeks old male albino rats to determine the performance of the food formulations. While the crude protein, crude fibre, and ash contents of the diets increased significantly (p with fortification, with values ranging from 16.04% to 17.59%, 2.25% to 4.42% and 1.40% to 2.50% respectively, crude fat and carbohydrate decreased significantly (p < 0.05), with concomitant decrease in energy, with values ranging from 23.48% to 20.80%, 49.32% to 47.63% and 472.76% to 448.08 kcal/100g respectively in samples A to D. PER values significantly (p < 0.05) improved up to 10% substitution, from 1.77 in unfortified (sample A) to 1.90 in 10% fortified (sample C), but declined at 15% substitution (sample D) to 1.69. Similarly, NPR values increased from 0.71 to 0.76 and 0.68. However, all the PER values including that of Nestle Cerelac (2.04) were lower than, though within the same range, with the value of 2.10 recommended by the Protein Advisory Group (PAG) for complementary foods. Sample C (10% Moringa flour blend) gave the best performance after rat feeding trials.展开更多
Liposome is one of the most successful drug delivery systems applying nanotechnology topotentiate the therapeutic efficacy and reduce toxicities of conventional medicines. Sincethe first doxorubicin-loaded liposome re...Liposome is one of the most successful drug delivery systems applying nanotechnology topotentiate the therapeutic efficacy and reduce toxicities of conventional medicines. Sincethe first doxorubicin-loaded liposome reached the market, numerous researches have beencarried out to develop new liposomal formulations over the past decade and have givenbirth to a series of commercial products. Therapeutic agents, most of which are anti-cancerdrugs, are encapsulated in the aqueous core or lipid bilayers of liposomes to improve theirdelivery to the targeted tissue. There are several liposomal formulations, such as EndoTAG-1 (paclitaxel-loaded cationic liposomes), Lipoplatin (cisplatin-loaded long circulating liposomes) and Stimuvax (a cancer vaccine), showing promising therapeutic value in clinicalstudies. Besides, new designs including environmentally sensitive liposomes, liposomaldrug combinations and liposomal vaccines are now tested in clinical trials.展开更多
Androgens have an intense consequence on the human scalp and body hair.Scalp hair sprouts fundamentally in awol of androgens whereas the body hair hike is vulnerable to the activity of androgens.Androgenetic alopecia(...Androgens have an intense consequence on the human scalp and body hair.Scalp hair sprouts fundamentally in awol of androgens whereas the body hair hike is vulnerable to the activity of androgens.Androgenetic alopecia(AGA)invoked as males emulate Alopecia due to the cause of the dynamic reduction of scalp hair.Androgens are medium of terminus growth of hair although the body.Local and system androgens convert the extensive terminal follicles into lesser vellus like structure.The out start of this type of alopecia is intensely irregular and the reason behind this existence of enough circulating steroidal hormones androgens and due to genetic predisposition.Effective treatments are available in the market as well as under clinical and preclinical testing.Many herbal formulations are also available but not FDA approved.Different conventional and NDDS formulations are already available in the market.To avoid various systemic side effects of both Finasteride and Minoxidil,topical formulations and natural products(nutrients,minerals,vitamins)now a days are being widely used to treat Androgenic alopecia.CAM(complementary and alternative medicine)provides the option to elect favorable,low-risk,adjuvant and alternative therapies.Herein,we offer a widespread review of topical marketed formulations,natural products,and CAM treatment options for AGA.展开更多
The Birkhoffian mechanics is more general than the Hamilton mechanics,but only some dynamical systems can be realized as a Birkhoffian formulation.This paper proposes a novel Birkhoffian formulation for the classical ...The Birkhoffian mechanics is more general than the Hamilton mechanics,but only some dynamical systems can be realized as a Birkhoffian formulation.This paper proposes a novel Birkhoffian formulation for the classical Bessel equation.Based on the first method of Santilli,the Birkhoffian formulation of Bessel equation is established under the assumption that the Birkhoffian describes the total physical energy of the corresponding conservative systems.Zero and n-th order classical Bessel equations are studied to verify the effectiveness of the proposed formulation.展开更多
Corticosteroids are widely used for the treatment of acute central nervous system injury. However, their bioactivity is limited by their short half-life. Sustained release of glucocorticoids can prolong their efficacy...Corticosteroids are widely used for the treatment of acute central nervous system injury. However, their bioactivity is limited by their short half-life. Sustained release of glucocorticoids can prolong their efficacy and inhibit scar formation at the site of nerve injury. In the present study, we wrapped the anastomotic ends of the rat sciatic nerve with a methylprednisolone sustained-release membrane. Compared with methylprednisone alone or methylprednisone microspheres, the methylprednisolone microsphere sustained-release membrane reduced tissue adhesion and inhibited scar tissue formation at the site of anastomosis. It also increased sciatic nerve function index and the thickness of the myelin sheath. Our findings show that the methylprednisolone microsphere sustained-release membrane effectively inhibits scar formation at the site of anastomosis of the peripheral nerve, thereby promoting nerve regeneration.展开更多
AIM:To investigate the quality of topical 2%diltiazem formulations extemporaneously compounded by retail pharmacies openly offering drug-compounding services.METHODS:A participating healthcare professional wrote 12 pr...AIM:To investigate the quality of topical 2%diltiazem formulations extemporaneously compounded by retail pharmacies openly offering drug-compounding services.METHODS:A participating healthcare professional wrote 12 prescriptions for compounded 2%diltiazem cream,with 2 refills allowed per prescription.The 12sets of prescriptions were filled,at intervals of 1-2 wk between refills,at 12 different independent retail pharmacies that openly offer drug-compounding services in a major metropolitan region.The 36 resultant preparations,provided as jars or tubes,were shipped,as soon as each was filled,at ambient temperature to the study core laboratory for high-performance liquid chromatography(HPLC)analysis,within 10 d of receipt.For the HPLC analysis,8 different samples of the topical diltiazem,each approximately 1 g in weight,were taken from prespecified locations within each container.To initiate the HPLC analysis,each sample was transferredto a 100 mL volumetric flask,to which methanol was added.The HPLC analysis was conducted in accordance with the laboratory-validated method for diltiazem in cream,ointment,and gel formulations.The main outcome measures were potency(percentage of label claim)and content uniformity of the compounded topical 2%diltiazem formulations.RESULTS:Of the 36 prescriptions filled,30 were packaged in jars and 6 were packaged as tubes.The prescriptions were specifically for cream formulations,but6 of the 12 pharmacies compounded 2%diltiazem as an ointment;for another pharmacy,which had inadequate labeling,the dosage form was unknown.The United States Pharmacopoeia(USP)standard for potency is 90%-115%of label claim.Of the 36 preparations,5(13.89%)were suprapotent and 13(36.11%)were subpotent.The suprapotent prescriptions ranged in potency from 117.2%to 128.5%of label claim,and the subpotent prescriptions ranged in potency from34.8%to 89.8%of label claim.Fourteen(38.9%)preparations lacked content uniformity according to the USP standard of 90%-110%potency and<6%relative standard deviation.Of the 30 formulations packaged in jars,12(40%)lacked content uniformity,while of the6 formulations packaged in tubes,2(33.3%)lacked content uniformity.Nine of the 12 pharmacies(75%)failed USP potency or content-uniformity specifications for at least 1 of the 3 prescription fills.For 5 of the 12pharmacies(41.7%),the mean potency across all three prescription fills was<90%of label claim.CONCLUSION:Patients prescribed topical 2%diltiazem for treatment of anal fissure frequently receive compounded formulations that are misbranded with respect to potency and that lack content uniformity.展开更多
Caffeine is present in products marketed for weight loss, with the purpose of increasing thermogenesis and lipid metabolism. The dosage declared by the product manufacturer, or even its presence, is not always correct...Caffeine is present in products marketed for weight loss, with the purpose of increasing thermogenesis and lipid metabolism. The dosage declared by the product manufacturer, or even its presence, is not always correctly described on the label. This work aimed to investigate the undeclared synthetic caffeine in weight loss formulations by a high-performance liquid chromatography with diode array detection(HPLC-DAD) method. From one hundred products purchased through Brazilian e-commerce, seventeen contained caffeine, either naturally or synthetically added to formulation. The caffeine-containing samples were confirmed by an ultra-high performance liquid chromatography-tandem mass spectrometry(UHPLC-MS/MS) method, and adulteration was clearly proven in five products. The content highest caffeine contained 448.8 mg per dose. Other irregularities were also found; nevertheless, the most serious was the addition of synthetic drugs without asking the consumers. Additional drugs expose the consumer to more possible side-effects as well as deleterious drug interactions. Intentional adulteration with any unlabeled substance is typically motivated by a desire to increase or alter the claimed effect of the marketed product to gain a commercial advantage.展开更多
A very simple, non-destructive, inexpensive and green strategy was applied for the simultaneous determination of ibu-profen (IBP) and paracetamol (PC) using transmission Fourier Transform Infrared (FTIR) spectroscopy ...A very simple, non-destructive, inexpensive and green strategy was applied for the simultaneous determination of ibu-profen (IBP) and paracetamol (PC) using transmission Fourier Transform Infrared (FTIR) spectroscopy in tablet formulations for routine quality control laboratories. For the determination of the active pharmaceutical ingredients (API), KBr pellets containing known amount of standards and samples were used for acquisition of the FTIR spectra. The partial least squares (PLS) calibration model was developed using the spectral region from 1781 - 1683 cm-1 for IBP and 1630 - 1530 cm-1 for PC. The excellent coefficients of determination (R2), 0.9999 and 0.9998 were achieved for IBP and PC, respectively. The accuracy of calibration model was also verified through root mean square error of cross validation (RMSECV) which was found to be 0.064. This work clearly shows the capability of transmission FTIR spectroscopy for assessment of exact quantity of API to control the quality of finished products as well as during processing in pharmaceutical industries without involvement of any solvent.展开更多
Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate(HEMA)and Methyl methacrylate(MMA)cross-linked copolymer(P(HEMA-co-MMA))was prepared to examine the potential use for preventing poste...Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate(HEMA)and Methyl methacrylate(MMA)cross-linked copolymer(P(HEMA-co-MMA))was prepared to examine the potential use for preventing posterior capsule opacification(PCO).The preparations were prepared by polymerizing the mixture of HEMA,MMA,cross-linking agent(EGDMA),initiator(AIBN)and docetaxel.The influence factors and mechanism of drug release were studied in the experiments.FT-IR,X-RD and SEM methods were used to characterize the polymer(P(HEMA-co-MMA))and docetaxel-loaded sustained-release preparations.Biocompatibility of P(HEMA-co-MMA)and in-vitro effect of docetaxel-loaded sustained-release preparations were also evaluated.The results showed that docetaxel could release sustainedly from these preparations prepared by cross-linking polymerization.And the release rate could be accelerated by increasing the MMA ratio or EGDMA ratio of the polymer.Release mechanism of docetaxel fitted the Higuchi model well.The results of IR and X-RD showed that only a hydrogen bond was formed between docetaxel and P(HEMA-co-MMA).Docetaxel dispersed in P(HEMA-co-MMA)in amorphous form.The elution test showed that P(HEMA-co-MMA)had good biocompatibility and the in-vitro pharmacodynamics study proved that docetaxel could release stably from the preparations and inhibit HLECs’proliferation.The docetaxel-loaded sustained-release preparations proved to be a promising therapy for preventing PCO.These results also lay a theoretical and experimental foundation for the future.展开更多
By the modified three-field Hu-Washizu principle, this paper establishes a theoretical founda- tion and general convenient formulations to generate convergent stable generalized hybrid/mixed cle- ment (GH/ME) model wh...By the modified three-field Hu-Washizu principle, this paper establishes a theoretical founda- tion and general convenient formulations to generate convergent stable generalized hybrid/mixed cle- ment (GH/ME) model which is invariant with respect to coordinate, insensitive to geometric distortion and suitable for improved stress computation. In the two proposed formulations, the stress equilibrium and orthogonality constraints are imposed through incompatible displacement and internal strain modes respectively. The proposed model by the general formulations in this paper is characterized by including as- sumed stress/strain, assumed stress, variable-node, singular, compatible and incompatible GH/ME models. When using regular meshes or the constant values of the isoparametric Jacobian Det in the assumed strain in- terpolation, the incompatible GH/ME model degenerates to the hybrid/mixed element model. Both general and concrete guidelines for the optimal selection of element shape functions are suggested. By means of the GH/ME theory in this paper, a family of new GH/ME can be and have been easily constructed. The software can also be developed conveniently because all the standard subroutines for the corresponding isoparametric displacement elements can be utilized directly.展开更多
Matrix metalloproteinases (MMPs) are known to be involved in a number of pathological processes including cancer, atherosclerosis, arthritis and neurodegenerative disease among others. The drive to develop MMP inhib...Matrix metalloproteinases (MMPs) are known to be involved in a number of pathological processes including cancer, atherosclerosis, arthritis and neurodegenerative disease among others. The drive to develop MMP inhibitors as therapeutics has been put forward for years by pharmaceutical companies as well as academicians. In an attempt to screen for MMP inhibitors from Traditional Chinese Medicines (TCMs) , a number of Chinese formulations used to treat inflammatory diseases such as nephritis and hepatitis have been studied. Strong inhibitory effects of three Chinese formulations toward the activity of MMP-16 have been discovered. These results suggest that these anti-inflammatory medicines contain some unknown MMP inhibitory compound(s) and provide reasonable molecular mechanisms for their theraoeutic effects.展开更多
基金supported by the National Key Research and Development Program of China, No. 2016YFC1101603 (to DYZ)the National Natural Science Foundation of China, Nos. 31640045 (to YHW), 81901251 (to ML)the Natural Science Foundation of Beijing of China, No. 7204323 (to ML)
文摘We previously prepared nerve growth factor poly-lactide co-glycolid sustained-release microspheres to treat rat sciatic nerve injury using the small gap sleeve technique.Multiple growth factors play a synergistic role in promoting the repair of peripheral nerve injury;as a result,in this study,we added basic fibroblast growth factors to the microspheres to further promote nerve regeneration.First,in an in vitro biomimetic microenvironment,we developed and used a drug screening biomimetic microfluidic chip to screen the optimal combination of nerve growth factor/basic fibroblast growth factor to promote the regeneration of Schwann cells.We found that 22.56 ng/mL nerve growth factor combined with 4.29 ng/mL basic fibroblast growth factor exhibited optimal effects on the proliferation of primary rat Schwann cells.The successfully prepared nerve growth factor-basic fibroblast growth factor-poly-lactide-co-glycolid sustained-release microspheres were used to treat rat sciatic nerve transection injury using the small gap sleeve bridge technique.Compared with epithelium sutures and small gap sleeve bridging alone,the small gap sleeve bridging technique combined with drug-free sustained-release microspheres has a stronger effect on rat sciatic nerve transfection injury repair at the structural and functional level.
文摘The management of diabetes mellitus is based on lifestyle and dietary measures suggesting the consumption of foods with a low glycemic index. The present study was conducted in order to propose food formulas based on white rice and white beans resulting in a lower glycemic response. For this, food formulations based on these foods were first made, in particular the formulation [75% white rice + 25% white beans] and the formulation [50% rice + 50% white beans]. Then, the biochemical composition of white rice, white bean and these two formulations was determined by the usual methods. Finally, their glycemic responses over 120 minutes were studied by the FAO/ WHO 1998 method. The results showed that white rice [100% white rice] had the highest carbohydrate content (54.61%) followed respectively by the formulation [75% white rice + 25% white bean] (45.69%), the white bean [100% white bean] (29.1%) and the formulation [50% white rice + 50% white bean] (26.16%). In terms of glycemic responses, the formulation [50% white rice + 50% white beans] presented the best evolution with a lower peak (6.041 mmol/L) observed at T45<sub>min</sub> and a lower postprandial glycemia (4.872 mmol/ L) at T120<sub>min</sub>. An increase in the proportion of beans is therefore recommended as it may suggest a beneficial metabolic effect.
基金supported by the Multi-Year Research Grants from the University of Macao(MYRG2019-00032-ICMS and MYRG2020-00113-ICMS)the Macao FDCT research grant(0108/2021/A)Molecular modeling was performed at the High-Performance Computing Cluster(HPCC),which is supported by the Information and Communication Technology Office(ICTO)of the University of Macao.
文摘Liposome is one of the most widely used carriers for drug delivery because of the great biocompatibility and biodegradability.Due to the complex formulation components and preparation process,formulation screening mostly relies on trial-and-error process with low efficiency.Here liposome formulation prediction models have been built by machine learning(ML)approaches.The important parameters of liposomes,including size,polydispersity index(PDI),zeta potential and encapsulation,are predicted individually by optimal ML algorithm,while the formulation features are also ranked to provide important guidance for formulation design.The analysis of key parameter reveals that drug molecules with logS[-3,-6],molecular complexity[500,1000]and XLogP3(≥2)are priority for preparing liposome with higher encapsulation.In addition,naproxen(NAP)and palmatine HCl(PAL)represented the insoluble and water-soluble molecules are prepared as liposome formulations to validate prediction ability.The consistency between predicted and experimental value verifies the satisfied accuracy of ML models.As the drug properties are critical for liposome particles,the molecular interactions and dynamics of NAP and PAL liposome are further investigated by coarse-grained molecular dynamics simulations.The modeling structure reveals that NAP molecules could distribute into lipid layer,while most PAL molecules aggregate in the inner aqueous phase of liposome.The completely different physical state of NAP and PAL confirms the importance of drug properties for liposome formulations.In summary,the general prediction models are built to predict liposome formulations,and the impacts of key factors are analyzed by combing ML with molecular modeling.The availability and rationality of these intelligent prediction systems have been proved in this study,which could be applied for liposome formulation development in the future.
文摘A solid sustained-release energetic material sample,an eruption device and a complete test system were prepared further to analyse the combustion characteristics of solid sustainedrelease energetic materials.The high-temperature heat flux generated by the combustion of the samples from the eruption device was used to penetrate the Q235 target plate.In addition,the meaning and calculation formula of energy density characterising the all-around performance of heat flux were proposed.The numerical simulation of the combustion effect of samples was carried out.According to the data comparison,the numerical simulation results agreed with the experimental results,and the maximum deviation between the two was less than 8.9%.In addition,the structure of the combustion wave and high-temperature jet was proposed and analysed.Based on theoretical analysis,experimental research and numerical simulation,the theoretical burning rate formula of the sample was established.The maximum error between the theoretically calculated mass burning rate and the experimental results was less than 9.8%.Therefore,using the gas-phase steady-state combustion model to study the combustion characteristics of solid sustained-release energetic materials was reasonable.The theoretical burning rate formula also had high accuracy.Therefore,the model could provide scientific and academic guidance for the theoretical research,system design and practical application of solid sustained-release energetic materials in related fields.
文摘Difenoconazole(DIF)is a representative variety of broad-spectrum triazole fungicides and liposoluble pesticides.However,the water solubility of DIF is so poor that its application is limited in plant protection.In addition,the conventional formulations of DIF always contain abundant organic solvents,which may cause pollution of the environment.In this study,two DIF/cyclodextrins(CDs)inclusion complexes(ICs)were successfully prepared,which were DIF/β-CD IC and DIF/hydroxypropyl-β-CD IC(DIF/HP-β-CD IC).The effect of cyclodextrins on the water solubility and the antifungal effect of liposoluble DIF pesticide were investigated.According to the phase solubility test,the molar ratio and apparent stability constant of ICs were obtained.Fourier transform infrared spectroscopy,thermal gravity analysis,X-ray diffraction and scanning electron microscopy were used systematically to characterize the formation and characteristics of ICs.The results noted that DIF successfully entered the cavities of two CDs.In addition,the antifungal effect test proved the better performance of DIF/HP-β-CD IC,which exceeded that of DIF emulsifiable concentrate.Therefore,our study provides informative direction for the intelligent use of liposoluble pesticides with cyclodextrins to develop water-based environmentally friendly formulations.
基金Supported by the National Key Research and Development Project of China,No.2019YFC1711605National Natural Science Foundation of China,No.81904257Medical Innovation Research Project of Science and Technology Commission of Shanghai Municipality,No.21Y11923100.
文摘BACKGROUND Diabetic retinopathy(DR)is the primary cause of visual problems in patients with diabetes.The Heyingwuzi formulation(HYWZF)is effective against DR.AIM To determine the HYWZF prevention mechanisms,especially those underlying mitophagy.METHODS Human retinal capillary endothelial cells(HRCECs)were treated with high glucose(hg),HYWZF serum,PX-478,or Mdivi-1 in vitro.Then,cell counting kit-8,transwell,and tube formation assays were used to evaluate HRCEC proliferation,invasion,and tube formation,respectively.Transmission electron microscopy was used to assess mitochondrial morphology,and Western blotting was used to determine the protein levels.Flow cytometry was used to assess cell apoptosis,reactive oxygen species(ROS)production,and mitochondrial membrane potential.Moreover,C57BL/6 mice were established in vivo using streptozotocin and treated with HYWZF for four weeks.Blood glucose levels and body weight were monitored continuously.Changes in retinal characteristics were evaluated using hematoxylin and eosin,tar violet,and periodic acid-Schiff staining.Protein levels in retinal tissues were determined via Western blotting,immunohistochemistry,and immunostaining.RESULTS HYWZF inhibited excessive ROS production,apoptosis,tube formation,and invasion in hg-induced HRCECs via mitochondrial autophagy in vitro.It increased the mRNA expression levels of BCL2-interacting protein 3(BNIP3),FUN14 domain-containing 1,BNIP3-like(BNIP3L,also known as NIX),PARKIN,PTEN-induced kinase 1,and hypoxia-inducible factor(HIF)-1α.Moreover,it downregulated the protein levels of vascular endothelial cell growth factor and increased the light chain 3-II/I ratio.However,PX-478 and Mdivi-1 reversed these effects.Additionally,PX-478 and Mdivi-1 rescued the effects of HYWZF by decreasing oxidative stress and apoptosis and increasing mitophagy.HYWZF intervention improved the symptoms of diabetes,tissue damage,number of acellular capillaries,and oxidative stress in vivo.Furthermore,in vivo experiments confirmed the results of in vitro experiments.CONCLUSION HYWZF alleviated DR and associated damage by promoting mitophagy via the HIF-1α/BNIP3/NIX axis.
基金supported by Keimyung University Research Grant of 2017
文摘3 D printing is a method of rapid prototyping and manufacturing in which materials are deposited onto one another in layers to produce a three-dimensional object. Although 3 D printing was developed in the 1980 s and the technology has found widespread industrial applications for production from automotive parts to machine tools,its application in pharmaceutical area is still limited. However,the potential of 3 D printing in the pharmaceutical industry is now being recognized. The ability of 3 D printing to produce medications to exact specifications tailored to the needs of individual patients has indicated the possibility of developing personalized medicines. The technology allows dosage forms to be precisely printed in various shapes,sizes and textures that are difficult to produce using traditional techniques. However,there are various challenges associated with the proper application of3 D printing in the pharmaceutical sector which should be overcome to exploit the scope of this technology. In this review,an overview is provided on the various 3 D printing technologies used in fabrication of complex dosage forms along with their feasibility and limitations.
基金supported by grants from the Fundamental Research Funds for the Central Universities, China (2572016DA02)the National Natural Science Foundation of China (31570642)the Science and Technology Innovation and Entrepreneurship Projects of Returned Overseas Personnel in Jilin Province, China (2013-36)
文摘A dry flowable formulation of Clonostachys rosea with fungicidal activity against Sclerotinia sclerotiorum was prepared by spray drying. The formulation was optimized by a four-factor, three-level orthogonal experiment to screen inert ingredients and spray-drying conditions. The optimal dry flowable formulation of C. rosea included 30% C. rosea (ratio of conidia powder and its fermentation broth is 1:3), 3% Morwet EFW, 4% K12, 10% Morwet D425, 9% sodium salt of polynaphthalene sulphonic acid (NNO), 5% croscarmellose sodium, 5% (NH4)2SO4, 0.5% carboxymethyl cellulose sodium (CMC-Na), 1% oxalic acid and palygorskite (carrier) up to 100%. The formulation exhibited good physical characteristics, such as high dispersibility, viability and a long shelf life. Plate antagonism tests and pot trials indicated that the dry flowable formulation was very effective against S. sclerotiorum, with control efficiency of up to 88.30%. This dry flowable formulation of C. rosea is a new potential commercial fungicide for spray drying to control S. sclerotiorum.
基金financially supported by the Universityof Macao Research Grant (MYRG2016-00038-ICMS-QRCM &MYRG2016-00040-ICMS-QRCM)Macao Science and Technology Development Fund (FDCT) (Grant No. 103/2015/A3)the National Natural Science Foundation of China (Grant No. 61562011 )
文摘Oral disintegrating tablets(ODTs) are a novel dosage form that can be dissolved on thetongue within 3 min or less especially for geriatric and pediatric patients. Current ODT for-mulation studies usually rely on the personal experience of pharmaceutical experts andtrial-and-error in the laboratory, which is inefficient and time-consuming. The aim of cur-rent research was to establish the prediction model of ODT formulations with direct com-pression process by artificial neural network(ANN) and deep neural network(DNN) tech-niques. 145 formulation data were extracted from Web of Science. All datasets were dividedinto three parts: training set(105 data), validation set(20) and testing set(20). ANN andDNN were compared for the prediction of the disintegrating time. The accuracy of the ANNmodel have reached 85.60%, 80.00% and 75.00% on the training set, validation set and testingset respectively, whereas that of the DNN model were 85.60%, 85.00% and 80.00%, respec-tively. Compared with the ANN, DNN showed the better prediction for ODT formulations.It is the first time that deep neural network with the improved dataset selection algorithmis applied to formulation prediction on small data. The proposed predictive approach couldevaluate the critical parameters about quality control of formulation, and guide researchand process development. The implementation of this prediction model could effectivelyreduce drug product development timeline and material usage, and proactively facilitatethe development of a robust drug product.
文摘Nutritional evaluation of complementary food formulations from maize, soybean and peanut fortified with Moringa oleifera leaf powder was carried out. Maize, soybean and peanut were blended in a ratio of 60:30:10 to produce a complementary food, which was then fortified. While the unfortified food product (sample A) served as control, the other three formulations were fortified with 5%, 10% and 15% Moringa leaf powder to give three samples (B, C and D respectively) of fortified food. Nutritional composition determination and feeding trials were then carried out, using two weeks old male albino rats to determine the performance of the food formulations. While the crude protein, crude fibre, and ash contents of the diets increased significantly (p with fortification, with values ranging from 16.04% to 17.59%, 2.25% to 4.42% and 1.40% to 2.50% respectively, crude fat and carbohydrate decreased significantly (p < 0.05), with concomitant decrease in energy, with values ranging from 23.48% to 20.80%, 49.32% to 47.63% and 472.76% to 448.08 kcal/100g respectively in samples A to D. PER values significantly (p < 0.05) improved up to 10% substitution, from 1.77 in unfortified (sample A) to 1.90 in 10% fortified (sample C), but declined at 15% substitution (sample D) to 1.69. Similarly, NPR values increased from 0.71 to 0.76 and 0.68. However, all the PER values including that of Nestle Cerelac (2.04) were lower than, though within the same range, with the value of 2.10 recommended by the Protein Advisory Group (PAG) for complementary foods. Sample C (10% Moringa flour blend) gave the best performance after rat feeding trials.
基金This work was supported by the National Natural Science Foundation of China(No.81130059).
文摘Liposome is one of the most successful drug delivery systems applying nanotechnology topotentiate the therapeutic efficacy and reduce toxicities of conventional medicines. Sincethe first doxorubicin-loaded liposome reached the market, numerous researches have beencarried out to develop new liposomal formulations over the past decade and have givenbirth to a series of commercial products. Therapeutic agents, most of which are anti-cancerdrugs, are encapsulated in the aqueous core or lipid bilayers of liposomes to improve theirdelivery to the targeted tissue. There are several liposomal formulations, such as EndoTAG-1 (paclitaxel-loaded cationic liposomes), Lipoplatin (cisplatin-loaded long circulating liposomes) and Stimuvax (a cancer vaccine), showing promising therapeutic value in clinicalstudies. Besides, new designs including environmentally sensitive liposomes, liposomaldrug combinations and liposomal vaccines are now tested in clinical trials.
文摘Androgens have an intense consequence on the human scalp and body hair.Scalp hair sprouts fundamentally in awol of androgens whereas the body hair hike is vulnerable to the activity of androgens.Androgenetic alopecia(AGA)invoked as males emulate Alopecia due to the cause of the dynamic reduction of scalp hair.Androgens are medium of terminus growth of hair although the body.Local and system androgens convert the extensive terminal follicles into lesser vellus like structure.The out start of this type of alopecia is intensely irregular and the reason behind this existence of enough circulating steroidal hormones androgens and due to genetic predisposition.Effective treatments are available in the market as well as under clinical and preclinical testing.Many herbal formulations are also available but not FDA approved.Different conventional and NDDS formulations are already available in the market.To avoid various systemic side effects of both Finasteride and Minoxidil,topical formulations and natural products(nutrients,minerals,vitamins)now a days are being widely used to treat Androgenic alopecia.CAM(complementary and alternative medicine)provides the option to elect favorable,low-risk,adjuvant and alternative therapies.Herein,we offer a widespread review of topical marketed formulations,natural products,and CAM treatment options for AGA.
基金Supported by the National Natural Science Foundation of China(11702119,11502071)the Natural Science Foundation of Jiangsu Province(BK20170565)
文摘The Birkhoffian mechanics is more general than the Hamilton mechanics,but only some dynamical systems can be realized as a Birkhoffian formulation.This paper proposes a novel Birkhoffian formulation for the classical Bessel equation.Based on the first method of Santilli,the Birkhoffian formulation of Bessel equation is established under the assumption that the Birkhoffian describes the total physical energy of the corresponding conservative systems.Zero and n-th order classical Bessel equations are studied to verify the effectiveness of the proposed formulation.
基金supported by the Technology Fund of Zhangzhou City in China,No.Z2010086
文摘Corticosteroids are widely used for the treatment of acute central nervous system injury. However, their bioactivity is limited by their short half-life. Sustained release of glucocorticoids can prolong their efficacy and inhibit scar formation at the site of nerve injury. In the present study, we wrapped the anastomotic ends of the rat sciatic nerve with a methylprednisolone sustained-release membrane. Compared with methylprednisone alone or methylprednisone microspheres, the methylprednisolone microsphere sustained-release membrane reduced tissue adhesion and inhibited scar tissue formation at the site of anastomosis. It also increased sciatic nerve function index and the thickness of the myelin sheath. Our findings show that the methylprednisolone microsphere sustained-release membrane effectively inhibits scar formation at the site of anastomosis of the peripheral nerve, thereby promoting nerve regeneration.
基金Supported by Ventrus Biosciences,Inc.,New York,NY,United States
文摘AIM:To investigate the quality of topical 2%diltiazem formulations extemporaneously compounded by retail pharmacies openly offering drug-compounding services.METHODS:A participating healthcare professional wrote 12 prescriptions for compounded 2%diltiazem cream,with 2 refills allowed per prescription.The 12sets of prescriptions were filled,at intervals of 1-2 wk between refills,at 12 different independent retail pharmacies that openly offer drug-compounding services in a major metropolitan region.The 36 resultant preparations,provided as jars or tubes,were shipped,as soon as each was filled,at ambient temperature to the study core laboratory for high-performance liquid chromatography(HPLC)analysis,within 10 d of receipt.For the HPLC analysis,8 different samples of the topical diltiazem,each approximately 1 g in weight,were taken from prespecified locations within each container.To initiate the HPLC analysis,each sample was transferredto a 100 mL volumetric flask,to which methanol was added.The HPLC analysis was conducted in accordance with the laboratory-validated method for diltiazem in cream,ointment,and gel formulations.The main outcome measures were potency(percentage of label claim)and content uniformity of the compounded topical 2%diltiazem formulations.RESULTS:Of the 36 prescriptions filled,30 were packaged in jars and 6 were packaged as tubes.The prescriptions were specifically for cream formulations,but6 of the 12 pharmacies compounded 2%diltiazem as an ointment;for another pharmacy,which had inadequate labeling,the dosage form was unknown.The United States Pharmacopoeia(USP)standard for potency is 90%-115%of label claim.Of the 36 preparations,5(13.89%)were suprapotent and 13(36.11%)were subpotent.The suprapotent prescriptions ranged in potency from 117.2%to 128.5%of label claim,and the subpotent prescriptions ranged in potency from34.8%to 89.8%of label claim.Fourteen(38.9%)preparations lacked content uniformity according to the USP standard of 90%-110%potency and<6%relative standard deviation.Of the 30 formulations packaged in jars,12(40%)lacked content uniformity,while of the6 formulations packaged in tubes,2(33.3%)lacked content uniformity.Nine of the 12 pharmacies(75%)failed USP potency or content-uniformity specifications for at least 1 of the 3 prescription fills.For 5 of the 12pharmacies(41.7%),the mean potency across all three prescription fills was<90%of label claim.CONCLUSION:Patients prescribed topical 2%diltiazem for treatment of anal fissure frequently receive compounded formulations that are misbranded with respect to potency and that lack content uniformity.
文摘Caffeine is present in products marketed for weight loss, with the purpose of increasing thermogenesis and lipid metabolism. The dosage declared by the product manufacturer, or even its presence, is not always correctly described on the label. This work aimed to investigate the undeclared synthetic caffeine in weight loss formulations by a high-performance liquid chromatography with diode array detection(HPLC-DAD) method. From one hundred products purchased through Brazilian e-commerce, seventeen contained caffeine, either naturally or synthetically added to formulation. The caffeine-containing samples were confirmed by an ultra-high performance liquid chromatography-tandem mass spectrometry(UHPLC-MS/MS) method, and adulteration was clearly proven in five products. The content highest caffeine contained 448.8 mg per dose. Other irregularities were also found; nevertheless, the most serious was the addition of synthetic drugs without asking the consumers. Additional drugs expose the consumer to more possible side-effects as well as deleterious drug interactions. Intentional adulteration with any unlabeled substance is typically motivated by a desire to increase or alter the claimed effect of the marketed product to gain a commercial advantage.
文摘A very simple, non-destructive, inexpensive and green strategy was applied for the simultaneous determination of ibu-profen (IBP) and paracetamol (PC) using transmission Fourier Transform Infrared (FTIR) spectroscopy in tablet formulations for routine quality control laboratories. For the determination of the active pharmaceutical ingredients (API), KBr pellets containing known amount of standards and samples were used for acquisition of the FTIR spectra. The partial least squares (PLS) calibration model was developed using the spectral region from 1781 - 1683 cm-1 for IBP and 1630 - 1530 cm-1 for PC. The excellent coefficients of determination (R2), 0.9999 and 0.9998 were achieved for IBP and PC, respectively. The accuracy of calibration model was also verified through root mean square error of cross validation (RMSECV) which was found to be 0.064. This work clearly shows the capability of transmission FTIR spectroscopy for assessment of exact quantity of API to control the quality of finished products as well as during processing in pharmaceutical industries without involvement of any solvent.
基金(Lab of Drug Metabolism and Pharmacokinetics,Sun Yat-sen University,Guangzhou,China)for the help and technical assistance.
文摘Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate(HEMA)and Methyl methacrylate(MMA)cross-linked copolymer(P(HEMA-co-MMA))was prepared to examine the potential use for preventing posterior capsule opacification(PCO).The preparations were prepared by polymerizing the mixture of HEMA,MMA,cross-linking agent(EGDMA),initiator(AIBN)and docetaxel.The influence factors and mechanism of drug release were studied in the experiments.FT-IR,X-RD and SEM methods were used to characterize the polymer(P(HEMA-co-MMA))and docetaxel-loaded sustained-release preparations.Biocompatibility of P(HEMA-co-MMA)and in-vitro effect of docetaxel-loaded sustained-release preparations were also evaluated.The results showed that docetaxel could release sustainedly from these preparations prepared by cross-linking polymerization.And the release rate could be accelerated by increasing the MMA ratio or EGDMA ratio of the polymer.Release mechanism of docetaxel fitted the Higuchi model well.The results of IR and X-RD showed that only a hydrogen bond was formed between docetaxel and P(HEMA-co-MMA).Docetaxel dispersed in P(HEMA-co-MMA)in amorphous form.The elution test showed that P(HEMA-co-MMA)had good biocompatibility and the in-vitro pharmacodynamics study proved that docetaxel could release stably from the preparations and inhibit HLECs’proliferation.The docetaxel-loaded sustained-release preparations proved to be a promising therapy for preventing PCO.These results also lay a theoretical and experimental foundation for the future.
文摘By the modified three-field Hu-Washizu principle, this paper establishes a theoretical founda- tion and general convenient formulations to generate convergent stable generalized hybrid/mixed cle- ment (GH/ME) model which is invariant with respect to coordinate, insensitive to geometric distortion and suitable for improved stress computation. In the two proposed formulations, the stress equilibrium and orthogonality constraints are imposed through incompatible displacement and internal strain modes respectively. The proposed model by the general formulations in this paper is characterized by including as- sumed stress/strain, assumed stress, variable-node, singular, compatible and incompatible GH/ME models. When using regular meshes or the constant values of the isoparametric Jacobian Det in the assumed strain in- terpolation, the incompatible GH/ME model degenerates to the hybrid/mixed element model. Both general and concrete guidelines for the optimal selection of element shape functions are suggested. By means of the GH/ME theory in this paper, a family of new GH/ME can be and have been easily constructed. The software can also be developed conveniently because all the standard subroutines for the corresponding isoparametric displacement elements can be utilized directly.
文摘Matrix metalloproteinases (MMPs) are known to be involved in a number of pathological processes including cancer, atherosclerosis, arthritis and neurodegenerative disease among others. The drive to develop MMP inhibitors as therapeutics has been put forward for years by pharmaceutical companies as well as academicians. In an attempt to screen for MMP inhibitors from Traditional Chinese Medicines (TCMs) , a number of Chinese formulations used to treat inflammatory diseases such as nephritis and hepatitis have been studied. Strong inhibitory effects of three Chinese formulations toward the activity of MMP-16 have been discovered. These results suggest that these anti-inflammatory medicines contain some unknown MMP inhibitory compound(s) and provide reasonable molecular mechanisms for their theraoeutic effects.