The impact of cyclodextrins(CDs)on wine quality and stability remains largely unknown.This study systematically assessed the protective effect of the post-fermentation addition of CDs on color stability of red wine fr...The impact of cyclodextrins(CDs)on wine quality and stability remains largely unknown.This study systematically assessed the protective effect of the post-fermentation addition of CDs on color stability of red wine from the viewpoints of color characteristics,copigmentation and phenolic profiles.The grey relational analysis(GRA)and principal component analysis(PCA)methods were employed to dissect the key effective determinants related to color quality.The addition of CDs induced a significant hyperchromic effect of 8.19-25.40%,a significant bathochromic effect and an enhancement of the color intensity.Furthermore,the evolution of anthocyanin forms and the content of monomeric anthocyanins revealed that β-CD is a superior favorable cofactor during wine aging,but for long-term aging,2-HP-β-CD and 2-HP-γ-CD are more beneficial in promoting the formation of polymerized anthocyanins and color stability.This work provides an important reference for the use of CDs to enhance the color quality and stability of red wines.展开更多
[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl ...[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was investigated using a single factor method,and a quality evaluation system was established based on the appearance,particle size,PDI,and re-dispersibility of the lyophilized samples.[Results]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was determined by single factor experiments.The pre-freezing period was 16 h at-80℃,the total drying time was 36 h,and the addition of 10%mannitol-sucrose was used as the lyoprotectant.[Conclusions]The product prepared by the lyophilization method exhibits a fluffy and full appearance,with minimal shrinkage and collapse.The volume remains consistent before and after lyophilization,and the re-dispersibility is satisfactory.The re-dissolution process is rapid,and the particle size and polydispersity index(PDI)remain largely unchanged before and after lyophilization.展开更多
In this study, the adsorption effect of β-cyclodextrin modified biochar (BC) on phenanthrene (PHE) in contaminated soil was investigated, aiming to provide an efficient and environmentally friendly remediation strate...In this study, the adsorption effect of β-cyclodextrin modified biochar (BC) on phenanthrene (PHE) in contaminated soil was investigated, aiming to provide an efficient and environmentally friendly remediation strategy for Polycyclic Aromatic Hydrocarbons (PAHs) contaminated soil. Through kinetic and isotherm analysis, β-CDBC-CA showed excellent phenanthrene adsorption performance, and the adsorption effect increased with the increase of time and was affected by temperature. The results show that β-CDBC-CA can not only effectively adsorb phenanthrene in soil, but also serve as a surfactant to help desorption phenanthrene adsorbed by soil organic matter and improve the efficiency of microbial degradation. The experimental data showed that the Elovich model could describe the adsorption behavior of β-CDBC-CA on phenanthrene well, while Langmuir and Freundlich models performed better in fitting parameters, revealing the adsorption mechanism of phenanthrene in contaminated soil by β-cyclodextrin-modified biochar. In addition, temperature has a significant effect on the adsorption capacity of β-CDBC-CA, and its application in soil remediation can be optimized by adjusting temperature. This study not only provides new materials and technical means for soil remediation but also provides important data support for an in-depth understanding of the environmental behavior of PAHs. By citing relevant research results, this study further improves the control and understanding of environmental risks of PAHs, which is of great significance for the protection of ecological environment and human health.展开更多
In this paper, biochar (BC) was used as raw material, activated by deionizing aqueous solution, NaCl solution, CA solution and HCl solution respectively. Epichlorohydrin (EPI) was used as crosslinking agent, and β-cy...In this paper, biochar (BC) was used as raw material, activated by deionizing aqueous solution, NaCl solution, CA solution and HCl solution respectively. Epichlorohydrin (EPI) was used as crosslinking agent, and β-cyclodextrin (β-CD) was used to modify biochar (BC). The prepared modified biochar materials were labeled with β-CDBC, β-CDBC-Na, β-CDBC-CA and β-CDBC-H, respectively. The infrared spectrum, X-ray diffractometer, scanning electron microscope and specific surface area of the four modified materials were tested. The results showed that the C-O stretching vibration peak at 1020 cm<sup>−</sup><sup>1</sup> of the modified materials was slightly offset compared with that of biochar. The characteristic absorption peaks of XRD pattern decrease obviously at 2θ = 26.7˚ and 29.5˚. It can be obviously observed on the electron microscope image that the surface is loaded or formed clathrates, and BET data and graphs also show that the specific surface area of the modified biochar is larger. Therefore, β-cyclodextrin successfully modified biochar and formed clathrates on the surface of biochar or was loaded in the pore structure of biochar, especially β-CDBC-CA achieved better modification effect. Because biochar and β-cyclodextrin raw materials are cheap, easy to prepare and green, and less prone to secondary pollution, it has a good advantage in environmental governance.展开更多
The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-c...The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-cyclodextrin(Am80-HP-β-CD)was prepared through a freeze-drying method at the mole ratio of 1:1(Am80:HP-β-CD).Fourier transform infrared spectroscopy(FT-IR)and differential scanning calorimetry(DSC)indicated the formation of Am80-HP-β-CD.In vitro dissolution studies showed that the solubility and dissolution percentage of Am80-HP-β-CD was improved substantially compared to Am80.An improved dissolution with approximately 97%drug release in 3 min was observed,in comparison with Am80 with approximately 60% release in 45 min.In vivo studies indicated that the AUC0-∞ has increased 2.79 times and the Cmax 4.37 times after the formation of inclusion complex.The decrease of tmaxindicated the Am80-HP-β-CD inclusion complex can be absorbed into blood faster.In short,the solubility and bio-availability of Am80 has notably increased with the complexation of HP-β-CD.Therefore,using the inclusion technique is a promising method to improve the solubility of insoluble drugs.展开更多
In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolu...In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolution of clenbuterol and propranolol were investigated on these thin-layer chromatography plates using different combinations of solvent systems at ambient temperature. The best simultaneous resolution was achieved in solvent system of acetonitrilen-butanol (50:50, v/v). Rst values of resolution of clenbuterol hydrochloride and propranolol hydrochloride are 3.6 and 4.3, respectively. The spots of different enantiomers are separated clearly. The results showed that hydroxypropyl-β-cyclodextrin bonded silica-gel could be successful in resolution of chiral adrenergic drugs. The study offers a direct, rapid and reliable method for separation of this kind of optically active compounds.展开更多
Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan(CMC-HP-β-CD) were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterize...Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan(CMC-HP-β-CD) were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterized by FT-IR spectroscopy and 1H-NMR spectra. The insulin-loaded nanoparticles were prepared through crosslinking with calcium ions, and the morphology and size of the prepared nanoparticles were characterized by transmission electron microscopy(TEM) and dynamic light scattering(DLS). Cumulative release in vitro study was performed respectively in simulated gastric medium fluid(SGF, p H=1.2), simulated intestinal fluid(SIF, p H=6.8) and simulated colonic fluid(SCF, p H=7.4). The encapsulation efficiency of insulin was up to 87.14 ± 4.32% through high-performance liquid chromatography(HPLC). Statistics indicated that only 15% of the encapsulated insulin was released from the CMC-HP-β-CD nanoparticles in 36 h in SGF, and about 50% of the insulin could be released from the nanoparticles in SIF, whereas more than 80% was released in SCF. In addition, the solution containing insulin nanoparticles could effectively reduce the blood glucose level of diabetic mice. The cytotoxicity test showed that the samples had no cytotoxicity. CMC-HP-β-CD nanoparticles are promising candidates as potential carriers in oral insulin delivery systems.展开更多
The objectives of the study were to investigate the effects of β-cyclodextrin(βCD) and hydroxypropyl-β-cyclodextrin(HPβCD) on the solubility and dissolution rate of norfloxacin prepared using three different metho...The objectives of the study were to investigate the effects of β-cyclodextrin(βCD) and hydroxypropyl-β-cyclodextrin(HPβCD) on the solubility and dissolution rate of norfloxacin prepared using three different methods, at drug to cyclodextrin weight ratios of 1:1, 1:2, 1:4 and 1:8. All the methods increased the solubility and dissolution rate of norfloxacin via inclusion complexation with βCD and HPβCD. Norfloxacin was converted from crystalline to amorphous form through inclusion complexation. Solvent evaporation method was the most effective method in terms of norfloxacin solubilisation, while inclusion complex of HPβCD has higher solubility than βCD complex when prepared using the same procedure.展开更多
Fungal keratitis and endopthalmitis are serious eye diseases.Fluconazole(FL)is indicated for their treatment,but suffers from poor topical ocular availability.This study was intended to improve and prolong its ocular ...Fungal keratitis and endopthalmitis are serious eye diseases.Fluconazole(FL)is indicated for their treatment,but suffers from poor topical ocular availability.This study was intended to improve and prolong its ocular availability.FL niosomal vesicles were prepared using span 60.Also,polymeric nanoparticles were prepared using cationic Eudragit RS100 and Eudragit RL100.The investigated particles had adequate entrapment efficiency(EE%),nanoscale particle size and high zeta potential.Subsequently,formulations were optimized using full factorial design.FL-HP-β-CD complex was encapsulated in selected Eudragit nanoprticles(FL-CD-ERS1)and niosmal vesicles.The niosomes were further coated with cationic and bioadhesive chitosan(FL-CD-Nios-ch).EE%for FL-CD-ERS1 and FL-CD-Niosch formulations were 76.4%and 61.7%;particle sizes were 151.1 and 392 nm;also,they exhibited satisfactory zeta potential+40.1 and+28.5 m V.In situ gels were prepared by poloxamer P407,HPMC and chitosan and evaluated for gelling capacity,rheological behavior and gelling temperature.To increase the precorneal residence time,free drug and selected nano-formulations were incorporated in the selected in situ gel.Release study revealed sustained release within 24 h.Permeation through excised rabbits corneas demonstrated enhanced drug flux and large AUC0-6 h in comparison to plain drug.Corneal permeation of selected formulations labeled with Rhodamine B was visualized by Confocal laser microscopy.Histopathological study and in vivo tolerance test evidenced safety.In vivo susceptibility test using Candida albicans depicted enhanced growth inhibition and sustained effect.In this study the adopted stepwise optimization strategy combined cylodextrin complexation,drug nano-encapsulation and loading within thermosenstive in situ gel.Finally,the developed innovated formulations displayed boosted corneal permeation,enhanced antifungal activity and prolonged action.展开更多
To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt...To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt temperature point. Inclusion complex has a higher stability to UV light and temperature over forythiaside itself. Pharmacological evidence showed that inclusion complex has little effect on pharmacokinetics by chicken intravenous injection. This study is favorable for developing preparations for forsythiaside and its clinical application.展开更多
Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the ...Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the solubility of DOM by inclusion complexation with Hydroxypropyl-β-Cyclodextrin (HP-β-CD) using kneading technique and formulation of fast disintegrating tablets by using Sodium Starch Glycolate as superdisintegrant. Solubility analysis of DOM in different concentrations of HP-β-CD was carried out. Design of experiment (DOE) is done by using MINITAB 15.1 software to find out the variable for dissolution and disintegration time. HP-β-CD and SSG were identified as the variable for disintegration time and dissolution. For optimization of the concentration of HP-β-CD and SSG, two factors at two levels design through central composite design (CCD) were used which gave 13 formulations. All formulations are evaluated for characteristics such as weight variation, hardness, friability, disintegration time and dissolution of drug. Solubility of DOM increases linearly with increase in concentration of HP-β-CD. The optimum concentration of HP-β-CD is found to be in 1:2 molar ratios and SSG of 7%. The In-Vitro dissolution studies of optimized formulation and market sample were carried out in USP type II apparatus at different time intervals of 5, 10, 15 and 30 minutes at 50 rpm in 0.1 N HCl. The dissolution and disintegration time of optimized formulation is found better than market sample.展开更多
Inclusion complexes of nitro-compounds using β-cyclodextrin and hydroxypropyl-β-cyclodextrin as host molecule have been studied by cyclic voltammetric method. The inclusion constants of the corresponding complexes h...Inclusion complexes of nitro-compounds using β-cyclodextrin and hydroxypropyl-β-cyclodextrin as host molecule have been studied by cyclic voltammetric method. The inclusion constants of the corresponding complexes have been determined. Strong inclusion complexation by hydroxypropyl-β-cyclodextrin has been verified展开更多
A cationic cyclodextrin derivative 6-O-(hydroxypropyltrimethylammonia)-β-cyclodextrin (GTA-β-CD) with low degree of substitution was prepared through a convenient method in solid phase. The product could be used...A cationic cyclodextrin derivative 6-O-(hydroxypropyltrimethylammonia)-β-cyclodextrin (GTA-β-CD) with low degree of substitution was prepared through a convenient method in solid phase. The product could be used as a valuable chiral selector in the capillary electrophoresis (CE) separation of some acidic drug enantiomers such as naproxen, ofloxacin, ibuprofen and warfarin.展开更多
[Objectives] To explore the optimal process for preparing hydroxypropyl tetrahydropyrantriol liposomes. [Methods] A refractive index method was used to determine the content of hydroxypropyl tetrahydropyrantriol. Usin...[Objectives] To explore the optimal process for preparing hydroxypropyl tetrahydropyrantriol liposomes. [Methods] A refractive index method was used to determine the content of hydroxypropyl tetrahydropyrantriol. Using particle size distribution and encapsulation rate as evaluation indicators, the effects of hydration time, ratio of organic phase to aqueous phase, granulation method, as well as thin film dispersion and reverse evaporation methods on liposomes preparation were investigated, and the optimal preparation method was selected. Single factor experiments were used to screen the drug phospholipid ratio, ultrasound time, and phospholipid cholesterol ratio, and the preparation process was optimized through orthogonal experiments. [Results] The optimal process of preparing hydroxypropyl tetrahydropyrantriol liposomes was as below: 1 : 10 of drug phospholipid ratio, 6 min of ultrasound time, 4 : 1 of phospholipid cholesterol ratio, (60.94%±7.24%) of entrapment efficiency, (86.44±6.08) nm of particle size, (0.195±0.077) of PDI. [Conclusions] The optimal preparation process of hydroxypropyl tetrahydropyrantriol liposomes selected by orthogonal experiment could effectively improve the encapsulation efficiency of hydroxypropyl tetrahydropyranotriol and reduce particle size. Moreover, the method was stable and reliable.展开更多
The fluorescence quenching of inclusion complex of neutral red (NR) and hydroxypropyl-β-cyclodextrin (HP-β-CD) carried by chlorobenzene was investigated. The fluorescence intensity of NR increased due to the for...The fluorescence quenching of inclusion complex of neutral red (NR) and hydroxypropyl-β-cyclodextrin (HP-β-CD) carried by chlorobenzene was investigated. The fluorescence intensity of NR increased due to the formed inclusion complex of HP-β-CD and NR. But the fluorescence intensity of NR-HP-β-CD diminished when chlorobenzene was added, and there was a linear relationship between the fluorescence quenching value of the system (△IF = IF, NR-HP-β-CD - IF, CB-NB-NR-HP-β-CD) and the concentration of chlorobenzene. Based on this, a novel fluorescence quenching method for the determination of chlorobenzene with NR as a fluorescence probe has been developed. Under the optimal conditions, the linear range of calibration curve for the determination of chlorobenzene was 5.0 × 10^-8 - 8.0 × 10^-6 mol/L and the detection limit was 1.0 × 10^-8 mol/L. It has been applied to determination ofchlorobenzene in synthetic waste water samples with satisfactory results.展开更多
2-acetoxy-benzencarboxylic acid is one of the most famous salicylate drugs today, a pharmaceutically active compound known as aspirin. It is poorly soluble in water which results in decreased bioavailability of the dr...2-acetoxy-benzencarboxylic acid is one of the most famous salicylate drugs today, a pharmaceutically active compound known as aspirin. It is poorly soluble in water which results in decreased bioavailability of the drug in the organism. The increase in water solubility of insoluble or poorly soluble drugs is therefore of great importance, which is the aim of this study. Inclusion of the drug in the molecule with a higher water solubility significantly increases its solubility and biological availability. Natural and hydrophilic derivatives of natural cyclodextrins are in the spotlight for their role as solubilizing excipients. Studies indicate that the use of β-cyclodextrin inclusion complexes with acetylsalicylic acid formed, increases the solubility of the drug in water. Many advantages of drug-complexation with cyclodextrins have been reported in scientific literature which includes increased solubility, enhanced bioavailability, improved stability, masking of bad test or odour, reduced side effect. Orally administered aspirin requires high and frequent dosing because it undergoes extensive pre systematic metabolism. Also chronic oral aspirin use is associated with serious gastrointestinal side-effects. Complexation with CD alleviates the side effects to some extent. The bioavailability and solubility of aspirin has to be increased to overcome the side-effects of aspirin related to stomach and gastro intestinal tract. The phase solubility study was performed according to the method of Higuchi and Connors by adding the 2-acetoxi-benzencarboxylic acid in excess to different concentrations of different beta cyclodextrins solutions. Phase solubility study records shown that the stability constant and complex stoichiometry of 2-acetoxi-benzencarboxylic acid-CD complexes gives linearly improve with the concentration of CD. Complexes were analyzed by UV-VIS spectroscopy and were characterized by infrared spectroscopy.展开更多
基金supported by the Regional Collaborative Innovation Project in Xinjiang Autonomous Region of China(2022E02011)the National Key R&D Program of China(2019YFD1002500)the Key Project of Research and Development Plan in Ningxia Hui Autonomous Region of China(2018BBF02001)。
文摘The impact of cyclodextrins(CDs)on wine quality and stability remains largely unknown.This study systematically assessed the protective effect of the post-fermentation addition of CDs on color stability of red wine from the viewpoints of color characteristics,copigmentation and phenolic profiles.The grey relational analysis(GRA)and principal component analysis(PCA)methods were employed to dissect the key effective determinants related to color quality.The addition of CDs induced a significant hyperchromic effect of 8.19-25.40%,a significant bathochromic effect and an enhancement of the color intensity.Furthermore,the evolution of anthocyanin forms and the content of monomeric anthocyanins revealed that β-CD is a superior favorable cofactor during wine aging,but for long-term aging,2-HP-β-CD and 2-HP-γ-CD are more beneficial in promoting the formation of polymerized anthocyanins and color stability.This work provides an important reference for the use of CDs to enhance the color quality and stability of red wines.
基金Youth Science Foundation Project of Sichuan Provincial Department of Science and Technology(2022NSFSC1437)Special Project of Scientific and Technological Research of Sichuan Provincial Administration of Traditional Chinese Medicine(2021MS121)Fundamental Research Funds for the Central Universities of Southwest Minzu University(ZYN2022040).
文摘[Objectives]To enhance the skin permeability of hydroxypropyl tetrahydropyrantriol and provide a reference for the subsequent prevention or treatment of skin aging.[Methods]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was investigated using a single factor method,and a quality evaluation system was established based on the appearance,particle size,PDI,and re-dispersibility of the lyophilized samples.[Results]The lyophilization process of hydroxypropyl tetrahydropyrantriol liposomes was determined by single factor experiments.The pre-freezing period was 16 h at-80℃,the total drying time was 36 h,and the addition of 10%mannitol-sucrose was used as the lyoprotectant.[Conclusions]The product prepared by the lyophilization method exhibits a fluffy and full appearance,with minimal shrinkage and collapse.The volume remains consistent before and after lyophilization,and the re-dispersibility is satisfactory.The re-dissolution process is rapid,and the particle size and polydispersity index(PDI)remain largely unchanged before and after lyophilization.
文摘In this study, the adsorption effect of β-cyclodextrin modified biochar (BC) on phenanthrene (PHE) in contaminated soil was investigated, aiming to provide an efficient and environmentally friendly remediation strategy for Polycyclic Aromatic Hydrocarbons (PAHs) contaminated soil. Through kinetic and isotherm analysis, β-CDBC-CA showed excellent phenanthrene adsorption performance, and the adsorption effect increased with the increase of time and was affected by temperature. The results show that β-CDBC-CA can not only effectively adsorb phenanthrene in soil, but also serve as a surfactant to help desorption phenanthrene adsorbed by soil organic matter and improve the efficiency of microbial degradation. The experimental data showed that the Elovich model could describe the adsorption behavior of β-CDBC-CA on phenanthrene well, while Langmuir and Freundlich models performed better in fitting parameters, revealing the adsorption mechanism of phenanthrene in contaminated soil by β-cyclodextrin-modified biochar. In addition, temperature has a significant effect on the adsorption capacity of β-CDBC-CA, and its application in soil remediation can be optimized by adjusting temperature. This study not only provides new materials and technical means for soil remediation but also provides important data support for an in-depth understanding of the environmental behavior of PAHs. By citing relevant research results, this study further improves the control and understanding of environmental risks of PAHs, which is of great significance for the protection of ecological environment and human health.
文摘In this paper, biochar (BC) was used as raw material, activated by deionizing aqueous solution, NaCl solution, CA solution and HCl solution respectively. Epichlorohydrin (EPI) was used as crosslinking agent, and β-cyclodextrin (β-CD) was used to modify biochar (BC). The prepared modified biochar materials were labeled with β-CDBC, β-CDBC-Na, β-CDBC-CA and β-CDBC-H, respectively. The infrared spectrum, X-ray diffractometer, scanning electron microscope and specific surface area of the four modified materials were tested. The results showed that the C-O stretching vibration peak at 1020 cm<sup>−</sup><sup>1</sup> of the modified materials was slightly offset compared with that of biochar. The characteristic absorption peaks of XRD pattern decrease obviously at 2θ = 26.7˚ and 29.5˚. It can be obviously observed on the electron microscope image that the surface is loaded or formed clathrates, and BET data and graphs also show that the specific surface area of the modified biochar is larger. Therefore, β-cyclodextrin successfully modified biochar and formed clathrates on the surface of biochar or was loaded in the pore structure of biochar, especially β-CDBC-CA achieved better modification effect. Because biochar and β-cyclodextrin raw materials are cheap, easy to prepare and green, and less prone to secondary pollution, it has a good advantage in environmental governance.
文摘The goal of this study was to improve the solubility and oral bioavailability of tamibarotene by complexing it with hydroxypropyl-β-cyclodextrin(HP-β-CD).The inclusion complex of tamibarotene with hydroxypropyl-β-cyclodextrin(Am80-HP-β-CD)was prepared through a freeze-drying method at the mole ratio of 1:1(Am80:HP-β-CD).Fourier transform infrared spectroscopy(FT-IR)and differential scanning calorimetry(DSC)indicated the formation of Am80-HP-β-CD.In vitro dissolution studies showed that the solubility and dissolution percentage of Am80-HP-β-CD was improved substantially compared to Am80.An improved dissolution with approximately 97%drug release in 3 min was observed,in comparison with Am80 with approximately 60% release in 45 min.In vivo studies indicated that the AUC0-∞ has increased 2.79 times and the Cmax 4.37 times after the formation of inclusion complex.The decrease of tmaxindicated the Am80-HP-β-CD inclusion complex can be absorbed into blood faster.In short,the solubility and bio-availability of Am80 has notably increased with the complexation of HP-β-CD.Therefore,using the inclusion technique is a promising method to improve the solubility of insoluble drugs.
基金the National Natural Science Foundation of China(No.20376085,No.20576142)for its financial support.
文摘In order to set up a simple and effective method for resolution of optical isomers, hydroxypropyl-β-cyclodextrin was bonded to silica-gel, which can be used for preparation of thin-layer chromatography plates. Resolution of clenbuterol and propranolol were investigated on these thin-layer chromatography plates using different combinations of solvent systems at ambient temperature. The best simultaneous resolution was achieved in solvent system of acetonitrilen-butanol (50:50, v/v). Rst values of resolution of clenbuterol hydrochloride and propranolol hydrochloride are 3.6 and 4.3, respectively. The spots of different enantiomers are separated clearly. The results showed that hydroxypropyl-β-cyclodextrin bonded silica-gel could be successful in resolution of chiral adrenergic drugs. The study offers a direct, rapid and reliable method for separation of this kind of optically active compounds.
基金Funded by the National Nature Science Foundation of China(No.51273156)the Open Foundation of Hubei key laboratory of Purification and Application of Plant Anti-cancer Active Ingredients(No.HLPAI2014005)
文摘Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan(CMC-HP-β-CD) were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterized by FT-IR spectroscopy and 1H-NMR spectra. The insulin-loaded nanoparticles were prepared through crosslinking with calcium ions, and the morphology and size of the prepared nanoparticles were characterized by transmission electron microscopy(TEM) and dynamic light scattering(DLS). Cumulative release in vitro study was performed respectively in simulated gastric medium fluid(SGF, p H=1.2), simulated intestinal fluid(SIF, p H=6.8) and simulated colonic fluid(SCF, p H=7.4). The encapsulation efficiency of insulin was up to 87.14 ± 4.32% through high-performance liquid chromatography(HPLC). Statistics indicated that only 15% of the encapsulated insulin was released from the CMC-HP-β-CD nanoparticles in 36 h in SGF, and about 50% of the insulin could be released from the nanoparticles in SIF, whereas more than 80% was released in SCF. In addition, the solution containing insulin nanoparticles could effectively reduce the blood glucose level of diabetic mice. The cytotoxicity test showed that the samples had no cytotoxicity. CMC-HP-β-CD nanoparticles are promising candidates as potential carriers in oral insulin delivery systems.
文摘The objectives of the study were to investigate the effects of β-cyclodextrin(βCD) and hydroxypropyl-β-cyclodextrin(HPβCD) on the solubility and dissolution rate of norfloxacin prepared using three different methods, at drug to cyclodextrin weight ratios of 1:1, 1:2, 1:4 and 1:8. All the methods increased the solubility and dissolution rate of norfloxacin via inclusion complexation with βCD and HPβCD. Norfloxacin was converted from crystalline to amorphous form through inclusion complexation. Solvent evaporation method was the most effective method in terms of norfloxacin solubilisation, while inclusion complex of HPβCD has higher solubility than βCD complex when prepared using the same procedure.
基金the National Research Centre,Cairo,Egypt for all the facilities and supports。
文摘Fungal keratitis and endopthalmitis are serious eye diseases.Fluconazole(FL)is indicated for their treatment,but suffers from poor topical ocular availability.This study was intended to improve and prolong its ocular availability.FL niosomal vesicles were prepared using span 60.Also,polymeric nanoparticles were prepared using cationic Eudragit RS100 and Eudragit RL100.The investigated particles had adequate entrapment efficiency(EE%),nanoscale particle size and high zeta potential.Subsequently,formulations were optimized using full factorial design.FL-HP-β-CD complex was encapsulated in selected Eudragit nanoprticles(FL-CD-ERS1)and niosmal vesicles.The niosomes were further coated with cationic and bioadhesive chitosan(FL-CD-Nios-ch).EE%for FL-CD-ERS1 and FL-CD-Niosch formulations were 76.4%and 61.7%;particle sizes were 151.1 and 392 nm;also,they exhibited satisfactory zeta potential+40.1 and+28.5 m V.In situ gels were prepared by poloxamer P407,HPMC and chitosan and evaluated for gelling capacity,rheological behavior and gelling temperature.To increase the precorneal residence time,free drug and selected nano-formulations were incorporated in the selected in situ gel.Release study revealed sustained release within 24 h.Permeation through excised rabbits corneas demonstrated enhanced drug flux and large AUC0-6 h in comparison to plain drug.Corneal permeation of selected formulations labeled with Rhodamine B was visualized by Confocal laser microscopy.Histopathological study and in vivo tolerance test evidenced safety.In vivo susceptibility test using Candida albicans depicted enhanced growth inhibition and sustained effect.In this study the adopted stepwise optimization strategy combined cylodextrin complexation,drug nano-encapsulation and loading within thermosenstive in situ gel.Finally,the developed innovated formulations displayed boosted corneal permeation,enhanced antifungal activity and prolonged action.
基金Supported by National Science&Technology Pillar Program during the TwelfthFive-year Plan Period(2011BAD34B01)National Natural Science Foundation of China(31372485,31172362)the opening fund from Beijing Key Laboratory of TCVM(BUA-TCVM-200904)
文摘To overcome the chemical instability of forsythiaside,the forsythiaside-hydroxypropyl-β-cyclodextrin inclusion complex was prepared by triturating. The inclusion complex was found having a varied UV spectrum and melt temperature point. Inclusion complex has a higher stability to UV light and temperature over forythiaside itself. Pharmacological evidence showed that inclusion complex has little effect on pharmacokinetics by chicken intravenous injection. This study is favorable for developing preparations for forsythiaside and its clinical application.
文摘Domperidone Maleate (DOM), an antiemetic drug, has been used in treatment of adults and children. It has low aqueous solubility and hence low bioavailability. In present study, an attempt has been made to enhance the solubility of DOM by inclusion complexation with Hydroxypropyl-β-Cyclodextrin (HP-β-CD) using kneading technique and formulation of fast disintegrating tablets by using Sodium Starch Glycolate as superdisintegrant. Solubility analysis of DOM in different concentrations of HP-β-CD was carried out. Design of experiment (DOE) is done by using MINITAB 15.1 software to find out the variable for dissolution and disintegration time. HP-β-CD and SSG were identified as the variable for disintegration time and dissolution. For optimization of the concentration of HP-β-CD and SSG, two factors at two levels design through central composite design (CCD) were used which gave 13 formulations. All formulations are evaluated for characteristics such as weight variation, hardness, friability, disintegration time and dissolution of drug. Solubility of DOM increases linearly with increase in concentration of HP-β-CD. The optimum concentration of HP-β-CD is found to be in 1:2 molar ratios and SSG of 7%. The In-Vitro dissolution studies of optimized formulation and market sample were carried out in USP type II apparatus at different time intervals of 5, 10, 15 and 30 minutes at 50 rpm in 0.1 N HCl. The dissolution and disintegration time of optimized formulation is found better than market sample.
文摘Inclusion complexes of nitro-compounds using β-cyclodextrin and hydroxypropyl-β-cyclodextrin as host molecule have been studied by cyclic voltammetric method. The inclusion constants of the corresponding complexes have been determined. Strong inclusion complexation by hydroxypropyl-β-cyclodextrin has been verified
文摘A cationic cyclodextrin derivative 6-O-(hydroxypropyltrimethylammonia)-β-cyclodextrin (GTA-β-CD) with low degree of substitution was prepared through a convenient method in solid phase. The product could be used as a valuable chiral selector in the capillary electrophoresis (CE) separation of some acidic drug enantiomers such as naproxen, ofloxacin, ibuprofen and warfarin.
基金Supported by Innovation and Entrepreneurship Training Program Project of Southwest Minzu University(S202210656134)Project of Sichuan Department of Science and Technology(2022NSFSC1437)Project of Sichuan Administration of Traditional Chinese Medicine(2021MS121).
文摘[Objectives] To explore the optimal process for preparing hydroxypropyl tetrahydropyrantriol liposomes. [Methods] A refractive index method was used to determine the content of hydroxypropyl tetrahydropyrantriol. Using particle size distribution and encapsulation rate as evaluation indicators, the effects of hydration time, ratio of organic phase to aqueous phase, granulation method, as well as thin film dispersion and reverse evaporation methods on liposomes preparation were investigated, and the optimal preparation method was selected. Single factor experiments were used to screen the drug phospholipid ratio, ultrasound time, and phospholipid cholesterol ratio, and the preparation process was optimized through orthogonal experiments. [Results] The optimal process of preparing hydroxypropyl tetrahydropyrantriol liposomes was as below: 1 : 10 of drug phospholipid ratio, 6 min of ultrasound time, 4 : 1 of phospholipid cholesterol ratio, (60.94%±7.24%) of entrapment efficiency, (86.44±6.08) nm of particle size, (0.195±0.077) of PDI. [Conclusions] The optimal preparation process of hydroxypropyl tetrahydropyrantriol liposomes selected by orthogonal experiment could effectively improve the encapsulation efficiency of hydroxypropyl tetrahydropyranotriol and reduce particle size. Moreover, the method was stable and reliable.
基金This project was supported by the National Basic Research Program of China (No. 2007CB936602) and the Natural Science Foundation of Shandong Province in China (No. Y2008B20).
文摘The fluorescence quenching of inclusion complex of neutral red (NR) and hydroxypropyl-β-cyclodextrin (HP-β-CD) carried by chlorobenzene was investigated. The fluorescence intensity of NR increased due to the formed inclusion complex of HP-β-CD and NR. But the fluorescence intensity of NR-HP-β-CD diminished when chlorobenzene was added, and there was a linear relationship between the fluorescence quenching value of the system (△IF = IF, NR-HP-β-CD - IF, CB-NB-NR-HP-β-CD) and the concentration of chlorobenzene. Based on this, a novel fluorescence quenching method for the determination of chlorobenzene with NR as a fluorescence probe has been developed. Under the optimal conditions, the linear range of calibration curve for the determination of chlorobenzene was 5.0 × 10^-8 - 8.0 × 10^-6 mol/L and the detection limit was 1.0 × 10^-8 mol/L. It has been applied to determination ofchlorobenzene in synthetic waste water samples with satisfactory results.
文摘2-acetoxy-benzencarboxylic acid is one of the most famous salicylate drugs today, a pharmaceutically active compound known as aspirin. It is poorly soluble in water which results in decreased bioavailability of the drug in the organism. The increase in water solubility of insoluble or poorly soluble drugs is therefore of great importance, which is the aim of this study. Inclusion of the drug in the molecule with a higher water solubility significantly increases its solubility and biological availability. Natural and hydrophilic derivatives of natural cyclodextrins are in the spotlight for their role as solubilizing excipients. Studies indicate that the use of β-cyclodextrin inclusion complexes with acetylsalicylic acid formed, increases the solubility of the drug in water. Many advantages of drug-complexation with cyclodextrins have been reported in scientific literature which includes increased solubility, enhanced bioavailability, improved stability, masking of bad test or odour, reduced side effect. Orally administered aspirin requires high and frequent dosing because it undergoes extensive pre systematic metabolism. Also chronic oral aspirin use is associated with serious gastrointestinal side-effects. Complexation with CD alleviates the side effects to some extent. The bioavailability and solubility of aspirin has to be increased to overcome the side-effects of aspirin related to stomach and gastro intestinal tract. The phase solubility study was performed according to the method of Higuchi and Connors by adding the 2-acetoxi-benzencarboxylic acid in excess to different concentrations of different beta cyclodextrins solutions. Phase solubility study records shown that the stability constant and complex stoichiometry of 2-acetoxi-benzencarboxylic acid-CD complexes gives linearly improve with the concentration of CD. Complexes were analyzed by UV-VIS spectroscopy and were characterized by infrared spectroscopy.