Release Model of Water-soluble Chitosan Nanoparticles for Protein Delivery

[Objective] The experiment aimed to explore release rule of water-soluble chitosan (WSC) in vitro. [Method]The bovine serum albumin(BSA) was taken as a model protein drug and some existing release models such as Kinetics model, Gompertz model, Weibull model, Higuchi model and Logistic model were used to fit the BSA release profile from WSC carriers. [Result] Except Higuchi model and Logistic model, other models could fit BSA release profile better. [Conclusion] Gompertz two-order kinetics model could fit the release of WSC nano-particles better and model parameters had practical physical meaning.

Synthesis of Water-Soluble Chitosan From Squid Pens Waste for Capsule Shell Materials

Water-Soluble Chitosan(WSC)has been sucessfuly synthesized from squid pens waste.The synthesis of chitosan from chitin was carried out by optimization of deacetylation temperature and time.Chitin was obtained from squid pens waste by demineralization and deproteinization process.HCl 7%was used for demineralization and NaOH 10%at 60℃ was applied for deproteinization process.Deacetylation reaction was carried out at varied temperatures i.e.,60℃,70℃,80℃,90℃ and 100℃ in NaOH 50%solution for 10 hours.Deacetylation reaction time were varied for 2 hours,4 hours,6 hours,8 hours,and 10 hours.The crude chitosan obtained then reacted with H2O230%to depolymerize.The synthesis product obtained then characterized by FTIR.The result of squid chitin yield was 33.9%.The optimum temperature and time of chitosan deacetylation process were 90℃ for 8 hours as indicated by the value of deacetylation degree(DD)that equal to 83.94%at optimum temperature and 82.22%at optimum reaction time.The percentage of WSC yield at optimum temperature(90℃)and optimum time(8 hours)were 27.59%and 23.16%,respectively.WSC solubility test was done in water and HCl 0,1N.The solubility of 2.8325 mg/mL and 0.8125 mg/mL were obtained in acid medium and water medium,respectively.

Preparation and characterization of complexes of RE^(3+) with furfural modified water-soluble chitosan

Degraded chitosan, with highly water-solubility, was obtained by the oxidation of chitosan with H2O2, and then reacted with furrural. The final product coordinated with the rare earth ions （RE^3＋ = Sm^3＋, Eu^3＋）, which led to the formation of the complexes. The prepared complexes were characterized with Infrared Spectroscopy （IR）, Ultra Violet （UV）, fluorescence, X-Ray Diffraction （XRD）, and Thermogravimetric-Differential Scanning Calorimetry （TG-DSC） measurements.

Elastosonographic Changes in Patients with Peyronie's Disease, before and after Treatment with a Compound Based on <i>Ecklonia bicyclis</i>, <i>Tribulus terrestris</i>, and Water-Soluble Chitosan

Several diagnostic techniques have been proposed during the time for the diagnostic evaluation of Induratio Penis Plastica (IPP), due to poor sensitivity and specificity of standard B-Mode Ultrasonography. Shear-Wave elastosonography (SWE) is a relative new ultrasound technique, already used for several organs, which allows evaluating the rigidity of the tissues. Furthermore, we used a compound consisting of Ecklonia bicyclis, Tribulus terrestris, and Biovis (water-soluble Chitosan) with antifibrotic and antioxidant properties and analyzed the elastosonographic variations following the assumption of the compound. From March 2016 to April 2017, 40 patients were recruited with a mean age of 62. All patients underwent elastosonographic measurements at the start of treatment. Subsequently each patient took 1 tablet of the compound of Ecklonia bicyclis, Tribulus terrestris, and Biovis (water-soluble Chitosan) for 6 months. All patients underwent elastosonographic investigation at the end of treatment. The elastosonographic measurement prior treatment, showed that the average of the three measurements (proximal, medial and distal), was 37.05 KPa ± 7.76 SD and 38.8 KPa ± 10.11 SD for the left and right cavernous body, respectively. The examination at the end of the six months of treatment, with the compound showed that the average values of fibrosity were 31.07 KPa ± 7.5 SD and 30.86 KPa ± 11.4 SD for the left and right cavernous body respectively, demonstrating a decrease in fibrosity that was statistically significant (P < 0.01). Our data demonstrate that taking the compound for six months reduces the stiffness of the corpora cavernosa.

The Fabrication of Water-Soluble Chitosan Capsule Shell Modified by Alginate and Gembili Starch(Dioscorea esculenta L)

Capsule shells have been successfully fabricated from water-soluble chitosan(WSC)with the addition of alginate and Gembili starch.WSC was synthesized from crab shell chitosan by depolymerization reaction.The capsule shells were made with the composition of WSC:Alginate,2:1,3:1 and 4:1(w/w)with and without the addition of Gembili starch.Gembili starch was added with a ratio of Alginate:Starch,1:1(w/w).The capsule shell properties were evaluated according to Indonesian Pharmacopoeia standard.The solubility test showed that the capsule shells were comply with the standard.The highest degrees of swelling in water and HCl 0.1 N solution were 491.93%and 410.51%,respectively.The highest degradation percentages in water and HCl 0.1 N solution were 57.80%and 21.44%,respectively.The observation of physical appearance indicated that the capsule shell with WSC:Alginate:Starch in ratio of 3:1:1 has appearance close to commercial capsule shell.

Water-soluble chitosan promotes remediation of Pb-contaminated soil by Hylotelephium spectabile

Water-soluble chitosan(WSC)has been studied for its ability to mobilize soil Pb and promote the phytoremediation by Hylotelephium spectabile in Pb-contaminated fields.We aimed to clarify the internal mechanism by which wSC impacts phytoremediation by examining plant growth and Pb accumulation performance of H.spectabile as well as the Pb form,functional groups,and mineral phases of Pb-contaminated soil.WSC effectively decreased soil pH and activated Pb migration in rhizosphere soils,with a considerable increase in water-soluble and acid-extractable Pb by 29%-102%and 9%-65%,respectively,and a clear decreasing trend in reducible and oxidizable Pb.Fourier-transform infrared spectroscopy revealed a significant increase in amino and hydroxyl groups in the soil generated by WSC.The coordination of Pb with amino and hydroxyl groups may play an important role in the formation of Pb complexes and activation of Pb in soil.In field trials,the application of WSC significantly increased Pb accumulation in H.spectabile by 125.44%,reaching 92 g/hm^(2).Moreover,the organic matter and nitrogen in the soils were increased by WSc,which improved the growth conditions of H.spectabile.No obvious growth inhibition was observed in either the pot or field trials.Therefore,WSC is a promising chelating agent for mobilizing Pb in soil.Additionally,WSC can be potentially used to boost H.spectabil-mediated phytoremediation of Pb-contaminatedfarmland.

Structure, properties and application to water-soluble coatings of complex antimicrobial agent Ag-carboxymethyl chitosan-thiabendazole

The structure, properties and application to water-soluble coatings of a new complex antimicrobial agent Ag-carboxylmethyl citosan-thiabendazole （Ag-CMCTS-TBZ） prepared from different materiel ratios were reported. The silver ions were preferably coordinated with the free-NH2 groups and the -OH groups of secondary alcohol and carboxyl in CMCTS. TBZ preferably bonded to carboxyl group in CMCTS by electrostatic force and hydrogen bonding. Increase in silver ions content in the complex agent improved to some limited extent the antibacterial activity, but enhanced coloring and cost of the complex agent. Increase in TBZ content resulted in increase of antifungal activity, but decrease of water solubility of the complex agent. The antimicrobial MICs of the complex agent to Esherichia coil, Staphylococcus aureus, Candida albicans, Aspergillus niger, Mucor sp. were 20 -80, 15 -60, 20 - 55, 40 - 250, and 400 - 1700 mg/kg, respectively. Addition of 0.1% of this complex agent to acrylic emulsion paint made the paint without substantial change in color, luster, viscosity, odor or pH value, but with an excellent and chronically persisting broad-spectra antimicrobial activity.

Electrostatic spraying for fine-tuning particle dimensions to enhance oral bioavailability of poorly water-soluble drugs

While spray-drying has been widely utilized to improve the bioavailability of poorly water-soluble drugs,the outcomes often exhibit suboptimal particle size distribution and large particle sizes,limiting their effectiveness.In this study,we introduce electrostatic spraying as an advanced technology tailored for poorly water-soluble drugs,enabling the fabrication of nanoparticles with fine and uniform particle size distribution.Regorafenib(1 g),as a model drug,copovidone(5 g),and sodium dodecyl sulfate(0.1 g)were dissolved in 200 ml ethanol and subjected to conventional-spray-dryer and electrostatic spray dryer.The electrostatic spray-dried nanoparticles(ESDN)showed smaller particle sizes with better uniformity compared to conventional spray-dried nanoparticles(CSDN).ESDN demonstrated significantly enhanced solubility and rapid release in water.In vitro studies revealed that ESDN induced apoptosis in HCT-116 cells to a greater extent,exhibiting superior cytotoxicity compared to CSDN.Furthermore,ESDN substantially improved oral bioavailability and antitumor efficacy compared to CSDN.These findings suggest that ESD shows potential in developing enhanced drug delivery systems for poorly water-soluble drugs,effectively addressing the limitations associated with CSD methods.

Effect of formulation variables on in vitro release of a water-soluble drug from chitosanesodium alginate matrix tablets

The objective of this study is to investigate the feasibility of using chitosanesodium alginate(CSeSA)based matrix tablets for extended-release of highly water-soluble drugs by changing formulation variables.Using trimetazidine hydrochloride(TH)as a water-soluble model drug,influence of dissolution medium,the amount of CSeSA,the CS:SA ratio,the type of SA,the type and amount of diluents,on in vitro drug release from CSeSA based matrix tablets were studied.Drug release kinetics and release mechanisms were elucidated.In vitro release experiments were conducted in simulated gastric fluid(SGF)followed by simulated intestinal fluid(SIF).Drug release rate decreased with the increase of CSeSA amount.CS:SA ratio had only slight effect on drug release and no influence of SA type on drug release was found.On the other hand,a large amount of water-soluble diluents could modify drug release profiles.It was found that drug release kinetics showed the best fit to Higuchi equation with Fickian diffusion as the main release mechanism.In conclusion,this study demonstrated that it is possible to design extended-release tablets of watersoluble drugs using CSeSA as the matrix by optimizing formulation components,and provide better understanding about drug release from CSeSA matrix tablets.

Water-soluble chitosan nanoparticles as a novel carrier system for protein delivery

High MW chitosan (CS) solutions have already been proposed as vehicles for protein delivery. The aim of the present work is to investigate the potential utility of water-soluble chitosan (WSC) as vehicles to load and deliver proteins. WSC nanoparticles (WSC NP) with various formations were prepared based on ionic gelation of WSC with pentasodium tripolyphosphate (TPP) anions. Bovine serum albumin (BSA) was used as a model protein drug incorporated into the WSC nanoparticles. Blank and BSA-loaded WSC nanoparticles were examined and determined to have a spherical shape with diameters between 35―190 nm, and zeta potential between 35―42 mV. FTIR confirmed that the tripolyphosphoric groups of TPP linked to the ammonium groups of WSC in the nanoparticles. Some factors affecting delivery properties of BSA have been investigated. Altering the concentration of BSA from 0.05 to 1 mg/mL enhanced the loading capacity of BSA but decreased loading efficiency simultaneously. Also, with the introduction of poly ethylene glycol (PEG), BSA release accelerated. Nanoparticle preparation from WSC with various deacetylation degrees (DDs) from 72.6% to 90% and MWs ranging from 3.5 to 15.8 kDa promoted loading efficiency and decreased the release rate. These results indicate that WSC nanoparticles are promising carriers for protein delivery.

A study of the properties of hydrophobically associating water-soluble polymers used in drilling fluids

Hydrophobically associating water-soluble polymers (HPAP) have been synthesized from acrylamide(AM), acrylate (AA), 2-acrylamido-2-methyl propane sulfonic acid (AMPS) and hydrophobic monomer (AP) in aqueous solution by radical polymerization. New polymer drilling fluids are made up of HPAP, which is used as viscosifiers and encapsulation agents. Properties of this system are reported in this paper. Results indicate that this system has a high value of yield point to plastic viscosity (YP/PV≥0.7), high viscosity at a low-shear rate (LSRV≥30000mPa·s), excellent shear thinning behavior, good solid-carrying behavior, resistance to shear, good thermal stability (as high as 140℃) and salt resistance. The system has excellent behavior in high-density solution of NaCl and in calcium and magnesium rich saline solutions. Hence, HPAP also can be used in saltwater polymer drilling fluids.

Effect of Different Environmental Conditions on Algicidal Effect of Water-soluble Extracts of Chinese Chive

[Objective] The paper was to study the algicidal effect of water-soluble extracts of Chinese chive under different environmental conditions, so as to provide reference for further study and development of new algicidal substances. [Method] The effects of water-soluble extracts of Chinese chive on the growth of Microcystis aeruginosa under different pH, light and aeration conditions were compared and studied. [Result] The growth inhibition rate of water-soluble extracts of Chinese chive on M. aeruginosa was greater than 90% under different pH conditions. With the growth of M. aeruginosa, the culture liquid with different initial pH was finally tended to 9-9.5. The growth inhibition rate of water-soluble extracts of Chinese chive on algae cell increased with the prolongation of culture time within the light intensity range of 1 000-4 000 lx. The inhibition effect of water-soluble extracts of Chinese chive on M. aeruginosa under low light intensity（1 000 lx）was better than that under high light intensity, the best light intensity for growth was not conducive to the exertion of allelopathic effect. Meanwhile, aeration condition was more conducive to the inhibition effect of water-soluble extracts of Chinese chive on the growth of M. aeruginosa. [Conclusion] pH, light and aeration conditions all affected the inhibition effect of water-soluble extracts of Chinese chive treated by high temperature on M. aeruginosa. Understanding the effect of these environmental factors on algicidal effect of allelochemicals could provide reference for further study and development of new algicidal substances.

Effect of thatch on water-soluble phosphorus of pasture soil fertilized with broiler litter

The presence of a thatch layer in established pastures could reduce the contact between broiler litter and soil, thus increasing the potential for surface runoff contamination with litter P. We conducted a laboratory study to evaluate the effect of a thatch layer on the dynamics of water-soluble P in undisturbed cores taken from a pasture. Cores with and without a thatch layer received a surface application of broiler litter (5 thm-2) and were incubated at 25 oC for 56 d. The result showed that on the soil surface the contents of water soluble-P (39 kghm-2) of the cores with the thatch layer was higher than that (20 kghm-2) of the cores without the thatch layer. Therefore on well-established pastures fertilized with broiler litter, the presence of a thatch layer might lead to high concentrations of water-soluble P on the soil surface.

Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs

Nanocrystals,a carrier-free colloidal delivery system in nano-sized range,is an interesting approach for poorly soluble drugs.Nanocrystals provide special features including enhancement of saturation solubility,dissolution velocity and adhesiveness to surface/cell membranes.Several strategies are applied for nanocrystals production including precipitation,milling,high pressure homogenization and combination methods such as Nano-Edge^(TM),SmartCrystal and Precipitation-lyophilization-homogenization(PLH)technology.For oral administration,many publications reported useful advantages of nanocrystals to improve in vivo performances i.e.pharmacokinetics,pharmacodynamics,safety and targeted delivery which were discussed in this review.Additionally,transformation of nanocrystals to final formulations and future trends of nanocrystals were also described.

Application of ion chromatography to the determination of water-soluble inorganic and organic ions in atmospheric aerosols

A simple, sensitive and convenient ion chromatography(IC) method was established for the simultaneous determination of twelve water-soluble inorganic anions(F -, Cl -, NO - 2, NO - 3, SO 2- 3, SO 2- 4, PO 3- 4), and fifteen water-soluble organic ions(formate, acetate, MSA, oxalate, malonate, succinate, phthalates, etc.) in atmospheric aerosols. The linear concentrations ranged from 0.005 μg/m 3 to 500 μg/m 3(r = 0.999—0.9999). The relative standard deviation(RSD) were 0.43%—2.00% and the detection limits were from 2.7 ng/m 3 to 88 ng/m 3. The proposed method was successfully applied to the simultaneous determination of those inorganic ions and organic ions in PM 2.5 of Beijing.

On-line Measurement of Water-Soluble Ions in Ambient Particles

Combining the system of rapid collection of ambient particles and ion chromatography, the system of rapid collection of fine particles and ion chromatography （RCFP-IC） was established to automatically analyze on-line the concentrations of water-soluble ions in ambient particles. Here, the general scheme of RCFP-IC is described and its basic performance is tested. The detection limit of RCFP-IC for SO4^2-, NO3^-, NO2^-, Cl^- and F- is below 0.3μg m^-3. The collection efficiency of RCFP-IC increases rapidly with increasing sized particles. For particles larger than 300 nm, the collection efficiency approaches 100%. The precision of RCFP-IC is more than 90% over 28 repetitions. The response of RCFP-IC is very sensitive and no obvious cross-pollution is found during measurement. A comparison of RCFP-IC with an integrated filter measurement indicates that the measurement of RCFP-IC is comparable in both laboratory experiments and field observations. The results of the field experiment prove that RCFP-IC is an effective on-line monitoring system and is helpful in source apportionment and pollution episode monitoring.

Adverse effects of metal exposure on chemotaxis towards water-soluble attractants regulated mainly by ASE sensory neuron in nematode Caenorhabditis elegans

Chemotaxis to water-soluble attractants is mainly controlled by ASE sensory neuron whose specification is regulated by che-1 in Caenorhabditis elegans. Our data suggested that exposure to high concentrations of metals, such as Pb, Cu, Ag, and Cr, would result in severe defects of chemotaxis to water-soluble attractants of NaCl, cAMP, and biotin. Moreover, the morphology of ASE neuron structures as observed by relative fluorescent intensities and relative size of fluorescent puncta of cell bodies, relative lengths of sensory endings in ASE neurons, and the expression patterns of che-1 were obviously altered in metal exposed animals when they meanwhile exhibited obvious chemotaxis defects to water-soluble attractants. In addition, the dendrite morphology could be noticeably changed in animals exposed to 150 μmol/L of Pb, Cu, and Ag. Furthermore, we observed significant decreases of chemotaxis to water-soluble attractants in Pb exposed che-1 mutant at concentrations more than 2.5 μmol/L, and in Cu, Ag, and Cr exposed che-1 mutant at concentrations more than 50 μmol/L. Therefore, impairment of the ASE neuron structures and functions may largely contribute to the appearance of chemotaxis defects to water-soluble attractants in metal exposed nematodes.

Preparation of Ultrafine Water-soluble Polymers Nanofiber Mats via Electrospinning

A series of water-soluble polymers such as poly（ethylene oxide）（PEO）, polyacrylamide（PAM） and poly（vinyl pyrrilidone）（PVP） was successfully prepared via the electrospinning of their aqueous solutions without the use of a surfactant. The effects of solution properties on the electrospinning of PEO, PAM and PVP solutions were investigated. The viscosity of the solution, charge density carried by the jet, and the surface tension of the solution are the key factors that influence the morphology and diameter size of the fibers. The viscosity of the solution was measured on a modular compact rheometer. The morphology and the diameter size distribution of the fibers were observed under an environmental scanning electron microscope（ESEM）. The results show that the diameters of the nanofibers electro spun from the solutions of these water soluble polymers were uniform and less than 300 nm.

Effect of kaolin on tensile strength and humidity resistance of a water-soluble potassium carbonate sand core

Water soluble cores(WSCs) have been widely applied in manufacture of complex metal components with hollow configurations or internal channels. However, the WSCs without any additons have low tensile strength and low humidity resistance. The purpose of this study is to prepare a water-soluble potassium carbonate sand core with addition of kaolin by the hot-temping method. The effects of kaolin on tensile strength, humidity resistance, fracture mechanism, as well as the gas evolution and collapsibility of WSCs were investigated. Results show that both the crystal morphology and the fracture mechanism of the inorganic salt are changed under the participation of kaolin, contributing to the increase of the tensile strength and the humidity resistance of the core. With the addition of 3wt.% kaolin, the tensile strength could be increased by a factor of 2, reached 1.50 MPa and the hygroscopic rate could be decreased by 14%, achieved 0.559%(after stored for 8 h), respectively. As the addition amount of kaolin increases from 0wt.% to 3wt.%, the main fracture mechanism changes from a adhesive to a cohesive fracture mechanism. The water-soluble potassium carbonate core obtained has the low gas evolution and excellent collapsibility, which makes it suitable for casting low melting metal with complex cavities and crooked channels.

Study on Dyeing Performance of Cationic Water-soluble Sulphur Black on Silk

A novel polyquaternaryammonium cationic sulphur black dye was synthesized and its dyeing behavior on silk was studied. The dye exhibited excellent dyeing fixation of up to 98.2 %, as well as excellent dyeing fastness on silk.