Water-soluble Chitosan Research Articles

Glycol chitosan in situ coating on PLGA nanoparticle curtails extraneous paclitaxel precipitates and imparts protein corona independent hemocompatibility

Poly (lactide-co-glycolide) (PLGA) nanoparticles surface functionalized with water soluble glycol chitosan (GC) and carboxymethyl chitosan (CMC) has been studied for their drug (Paclitaxel and Doxorubicin) loading, yield, cellular uptake, serum protein adsorption and hemocompatibility. It was observed that Paclitaxel (Ptxl) phase out as Extraneous Ptxl Precipitates (EPP) (>25 %) in case of uncoated and CMC coated low molecular weight (LMW) PLGA nanoparticles (PNPs). The EPP formation was significantly reduced to ∼5 % with GC coating as it enhanced LMW PLGA precipitation and yield predominantly spherical polymeric nanoparticles towards better encapsulation of Ptxl and thus uniform intracellular drug distribution. Interestingly, protein corona analysis showed cmcPNPs and gcPNPs to be distinct from each other in associating mainly with serum proteins of molecular weight < 30 kDa and >30 kDa respectively. While CMC functionalization showed >10 % hemolysis, at similar concentration GC coating was found to provide superior hemocompatibility even in the absence of protein corona.

Antibacterial efficacy of chitosan- and poly(hexamethylene biguanide)-immobilized nanofiber membrane

In this study, polyacrylonitrile (PAN) nanofiber membrane was prepared by an electrospinning technique. After alkaline hydrolysis, the ion-exchange nanofiber membrane (P-COOH) was grafted with chitosan molecules to form a chitosan-modified nanofiber membrane (P-COOH-CS). Poly(hexamethylene biguanide) (PHMB) was then covalently immobilized on P-COOH and P-COOH-CS to form P-COOH-PHMB and P-COOH-CS-PHMB, respectively. The nanofiber membranes were subjected to various surface analyses as well as to the evaluations of antibacterial activity against Escherichia coli. The optimal modification conditions for P-COOH-CS-PHMB were attained by water-soluble chitosan at 50 kDa of molecular weight, coupling pH at 7, and 0.05% (w/w) of PHMB. Within 10 min of treatment, the antibacterial rate was close to 100%. Under the similar conditions of antibacterial treatment, the P-COOH-CS-PHMB exhibited a better antibacterial efficacy than the P-COOH-PHMB. When the number of bacterial cells was increased by 2000 folds, both types of nanofiber membranes still maintained the antibacterial rate close to 100%. After five cycles of repeated antibacterial treatment, the antibacterial efficacy of P-COOH-PHMB was 96%, which was higher than that of P-COOH-CS-PHMB (83%). The experimental results revealed that the PHMB-modified nanofiber membranes can be suitably applied in water treatment such as water disinfection and biofouling control.

A competent bidrug loaded water soluble chitosan derivative for the effective inhibition of breast cancer

Drug resistance and damage caused to the normal cells are the drawbacks which have limited the use of the existing effective anticancer drugs. Attainment of a steady and extended release by encapsulating dual drugs into biocompatible and biodegradable vehicles is the key to enable the use of these drugs for effective inhibition of cancer. In this study, carboxymethyl chitosan (CMCS), a proficient water-soluble derivative of chitosan has been synthesized using chemical route and used for the delivery of 5-Fluorouracil and doxorubicin individually as well as in combination. Carboxymethylation occuring at –NH2 and OH sites of chitosan, has been confirmed using FTIR. EDX and Fluorescence studies elucidate the encapsulation of 5-Fluorouracil and doxorubicin into CMCS. The capability of CMCS to release the drugs in a more sustained and prolonged manner is evident from the obtained release profiles. About 14.9 µg/ml is enough to cause 50% cell death by creating oxidative stress and effectuating DNA fragmentation. Amidst the existing reports, the uniqueness of this work lies in using this rare coalition of drugs for the suppression of breast cancer and in reducing the side effects of drugs by encapsulating them into CMCS, which is evidenced by the high hemocompatibilty of the samples.

One-pot synthesis of cellulose-based nonwoven web incorporated with chitosan for hemostat applications

Water-soluble chitosan and wood pulp fiber–based nonwovens were produced using wet-laying technology, and their properties were investigated for the potential application for severe hemorrhage. The pores of the wood pulp nonwovens were completely covered as the concentration of chitosan was increased. A phosphate buffer solution uptake of 997% was attained in the nonwoven loaded with chitosan concentration of 1.5 w/v%. The deposition of blood cells was found to increase with an increase in the water-soluble chitosan concentration. The blood-clotting time was found to be 170 s, making the developed nonwoven to promote blood-clotting mechanism by creating mechanical barrier to reduce the blood loss.

Enhanced microbial safety of channel catfish (Ictalurus punctatus) fillet using recently invented medium molecular weight water-soluble chitosan coating.

Chitosan with higher molecular weight exhibited higher antimicrobial efficacy against foodborne pathogens. However, the poor water solubility of higher or medium molecular weight chitosan limits its applications. To overcome the challenge, our research team searched for simple preparation procedure for fast-dissolving medium molecular weight chitosan in water. Throughout the process, we were able to obtain a higher concentration of medium molecular weight water-soluble (MMWWS) chitosan (400kDa). The MMWWS chitosan showed physicochemical properties that are suitable for edible coating. Antibacterial activities of 400-kDa chitosan coating prepared in acetic acid (1% v/v) or aspartic acid (1% or 3% w/v) were examined. The surface of catfish cubes was inoculated with six foodborne pathogens and then coated with chitosan solutions. The survival of each pathogen was evaluated during shelf life storage. Compared with the control, 3% w/v chitosan coating in aspartic acid solution exhibited the most effective antibacterial activities among other coating treatments, completely inhibiting Vibrio parahaemolyticus on the surface of catfish. The study suggested that chitosan dissolved in aspartic acid has the potential for use as an alternative antimicrobial coating for catfish fillet.

Inhibitory activity of biofunctionalized silver-capped N-methylated water-soluble chitosan thiomer for microbial and biofilm infections

One of the most important self-defense strategies employed by bacteria to resist the action of antibiotics is a biofilm formation upon the infected surface. Thus, there is an urgent need to explore novel candidates that have potent antibacterial and anti-biofilm effects to tackle this challenge. In this endeavor, we have transformed shrimp shell wastes to N-methylated water-soluble chitosan thiomer (MWSCT) which was used as either a chelating agent or bio-reductant and capping agent for Ag(I) ions in the preparation of a Ag(I)MWSCT complex or silver nanocomposite (Ag(0)MWSCT), for targeting antibacterial and anti-biofilm applications. The antibacterial and anti-biofilm performance of the new methylated chitosan thiomer (MWSCT) and its silver architectures (Ag(I)MWSCT, Ag(0)MWSCT) were assessed in vitro against E. coli and S. aureus. These new materials have significant capacities to synergistically inhibit the proliferation of the targeted bacterial cells and biofilm formation, in a structure- and species-dependent manner. Ag(0)MWSCT emerged as the most potent compound in inhibiting the growth of bacterial strains (MICE. coli/ MICS. aureus = 0.05/ 0.34 μg/mL, 1.6-/ 2.5-times lower than that recorded for the clinical drug (ciprofloxacin, Cipro). Also, this nanocomposite showed the highest anti-biofilm effects (only 1.7% E. coli biofilm growth; 11.8% staphylococcal biofilm growth).

Synthesis of Capsule Film from Water-Soluble Chitosan by Adding Sodium Lauryl Sulfate

Mixtures comprising water-soluble chitosan (WSC), agar and different concentrations of sodium lauryl sulphate (SLS) were used to synthesize capsule films. The concentration of agar was fixed at 0.02 %, whereas the concentration (v/v) of SLS varied (0, 0.02, 0.04, 0.06 and 0.08 %). Shrimp shell waste was subjected to demineralization, deproteination and deacetylation to obtain chitosan. The chitosan thus obtained was depolymerized to produce water-soluble chitosan (WSC). Fourier-Transform infrared (FTIR) baseline method was used for calculating the degree of deacetylation of chitosan. FTIR spectra of the obtained capsule film exhibited vibrations of its constituent molecules, namely agar, chitosan and SLS. The elasticity of the film matrix increased with SLS concentrations. In swelling tests conducted using water and 0.1 N HCl, the highest swelling values, 123.74 and 235.87 %, respectively were observed in the capsule film containing 0.08 % SLS in the 10th min. The capsule film containing 0.08 % SLS was degraded (broken) in water and 0.1 N HCl in the 10th and 30th min, respectively. The results indicated that a capsule film containing 0.08% SLS was the most eligible film for commercial use.

Nanoparticle-Mediated Dual Targeting: An Approach for Enhanced Baicalin Delivery to the Liver.

In this study, water-soluble chitosan lactate (CL) was reacted with lactobionic acid (LA), a disaccharide with remarkable affinity to hepatic asialoglycoprotein (ASGP) receptors, to form dual liver-targeting LA-modified-CL polymer for site-specific drug delivery to the liver. The synthesized polymer was used to encapsulate baicalin (BA), a promising bioactive flavonoid with pH-dependent solubility, into ultrahigh drug-loaded nanoparticles (NPs) via the ionic gelation method. The successful chemical conjugation of LA with CL was tested and the formulated drug-loaded LA-modified-CL-NPs were assessed in terms of particle size (PS), encapsulation efficiency (EE) and zeta potential (ZP) using full factorial design. The in vivo biodistribution and pharmacokinetics of the designed NPs were assessed using 99mTc-radiolabeled BA following oral administration to mice and results were compared to 99mTc-BA-loaded-LA-free-NPs and 99mTc-BA solution as controls. Results showed that the chemical modification of CL with LA was successfully achieved and the method of preparation of the optimized NPs was very efficient in encapsulating BA into nearly spherical particles with an extremely high EE exceeding 90%. The optimized BA-loaded-LA-modified-CL-NPs showed an average PS of 490 nm, EE of 93.7% and ZP of 48.1 mV. Oral administration of 99mTc-BA-loaded-LA-modified-CL-NPs showed a remarkable increase in BA delivery to the liver over 99mTc-BA-loaded-LA-free-CL-NPs and 99mTc-BA oral solution. The mean area under the curve (AUC0–24) estimates from liver data were determined to be 11-fold and 26-fold higher from 99mTc-BA-loaded-LA-modified-CL-NPs relative to 99mTc-BA-loaded-LA-free-CL-NPs and 99mTc-BA solution respectively. In conclusion, the outcome of this study highlights the great potential of using LA-modified-CL-NPs for the ultrahigh encapsulation of therapeutic molecules with pH-dependent/poor water-solubility and for targeting the liver.

Novel heterocyclic chitosan derivatives and their derived nanoparticles: Catalytic and antibacterial properties

The metal-assisted nitrone-nitrile cycloaddition reaction is apply to empower chitosan chemistry. The ultrasonic irradiation has proven to efficiently accelerate the cycloaddition affording new heterocyclic (1,2,4-oxadiazoline) chitosan derivatives and avoiding ultrasonic degradation of the chitosan macromolecules. By varying the nitrone nature, both water- and toluene-soluble chitosan derivatives were successfully synthesized. Relying on the ionic gelation approach nanoparticles of heterocyclic chitosan derivatives were prepared. Water-soluble chitosan derivative demonstrated a high antibacterial activity coupled with low toxicity. The toxicity of the synthesized heterocyclic chitosan derivatives and their based nanoparticles are comparable with those of the starting chitosan, while their antibacterial activity is superior. Toluene-soluble derivatives are shown to be efficient homogeneous catalysts towards monoglyceride synthesis via the epoxide ring opening. They efficiently catalyze selective conversion of fatty acids and glycidol into corresponding monoglycerides allowing one to simplify significantly the procedure for separating the reaction product from the catalyst for its recovery and reusage.

Researches on the Internal Molecular Weight Uniformity of Chitosan Biomaterials

Uniform molecular weight (Mw) chitosan (CS) is highly demanded in medical biomaterial industry. This present article described heterogeneous degradation of CS in aqueous HCl/ethanol solution, in which progress uniform Mw CS was successfully prepared. The Mw distribution of CS was measured by gel permeation chromatography (GPC) analysis. Moreover, the structure and properties of degraded CS were characterized by Fourier transform infrared spectroscopy (FT-IR), nuclear magnetic resonance spectroscopy ( 1 H NMR), X-ray diffraction (XRD) and thermogravimetric (TG) analysis. In addition, the biocompatibility of degraded CS was also assessed by hemolysis rate (HR) measurement. The Mw of CS dramatically decreased from 246 KDa to 76 kDa at the initial 30 min, and stabilized at 18 kDa after 24 h. GPC analysis results showed that the degraded CS molecular become homogenization. FT-IR and 1H NMR analysis confirmed the basic structure of CS molecular backbone was not destroyed during this progress. Besides, the water solubility of CS was not significantly influenced by this reaction. Moreover, the XRD analysis revealed that crystallinity of degraded CS increased from 70.32% to 99.25% with time. The TG analysis showed improved thermal stability of degraded CS. HR measurement demonstrated the degraded CS possessed excellent biocompatibility. This simple and efficient heterogeneous degradation would open up a new route to produce uniform Mw CS.

Graft modification of carboxymethyl chitosan with styrene and its biological applications

BackgroundCarboxymethyl chitosan (CMCh) is a water-soluble chitosan derivative and it has been widely used in biomedical applications due to its unique properties. Modification of CMCh by graft copolymerization with different monomers is done in order to enhance its applications.ResultsGraft copolymerization of styrene (S) onto CMCh using ammonium persulfate (APS) as initiator was successfully done with optimization of grafting parameters. The new materials were prepared in nano size. The antibacterial activities against Streptococcus pneumonia (RCMB 010010), Staphylococcus aureus (RCMB 010028) as Gram-positive and Escherichia coli (RCMB 010052) as Gram-negative bacteria and antifungal activity against Aspergillus fumigates (RCMB 02568), Candida albicans (RCMB 05036), Syncephalastrum racemosum (RCMB 05922), and Geotricum candidum (RCMB 05097) were examined using the diffusion agar technique. Also, the cytotoxicity effect against mammalian cell lines (MCF-7cells (human breast cancer) and HTC-116 (colon carcinoma)) was evaluated.ConclusionsThe obtained data proved that grafted carboxymethyl chitosan with styrene (CMCh-g-S) shows better antimicrobial activities, while parent carboxymethyl chitosan showed higher activity than new grafted materials. Also the nano scaled grafted CMCh showed higher activities than grafted carboxymetyl chitosan in macro scale.

Comparison of acid and water-soluble chitosan doped fibrous cellulose hemostat wet laid nonwoven web for hemorrhage application

Fibrous hemostat was produced using wet laying technique comprising of acid and water soluble chitosan with fibrous cellulose. The hemostatic efficiency and their structural properties were evaluated using blood clotting time, whole blood adhesion and analytical characterization techniques. The maximum concentration of chitosan utilised for the production of nonwoven was 1.5 w/v % upon which increased the viscosity of the solution. The absorption of phosphate buffer solution was found to be 1117% for acid soluble chitosan based nonwoven whereas for water soluble chitosan based nonwoven was 997%. Increased red blood cells and platelets were found to be higher in acid soluble chitosan compared to water soluble chitosan based cellulose nonwoven. The blood clotting time for acid soluble chitosan nonwoven was found to be 166 s and water soluble chitosan nonwoven was 170 s. The developed hemostat have potential application in reducing blood loss and also inducing the blood coagulation pathway which was confirmed by the adhesion of platelets on to the surface of nonwoven web.

Nghiên cứu chiết rút và khảo sát tính kháng khuẩn của chitosan tan trong nước từ vỏ tôm thẻ chân trắng (Litopenaeus vannamei)

The aim of research was to produce water-soluble chitosan and inhibit bacterial growth from the white leg shrimp shell (Litopenaeus vannamei) through deacetylation of chitin in NaOH solution to obtain the crude chitosan. Next, crude chitosan was treated in acetic acid solution at various concentrations and different times to convert it into the water-soluble chitosan. The result showed that chitin was treated in NaOH at the concentration of 50% for 36 hours to collect chitosan with degree of deacetylation (93.1%), viscosity (20 mPas) and high recovery yield (46.8%). The crude chitosan was soaked in acetic acid 2% in the presence of H2O2 4% for 4 hours to collect the water-soluble chitosan. The solubility of water-soluble chitosan reached to 88.6% and FTIR spectrum showed that the functional groups were almost similar to crude chitosan. The antibacterial activity of water-soluble chitosan was lower than the crude chitosan with the concentration inhibited Escherichia coli, Staphylococcus aureus, Salmonella typhimurium of water-soluble chitosan was 8% while the concentration of crude chitosan was 2%. However, the water-soluble chitosan could be enhanced the application in food processing field.

Improvement stability of phycocyanin from Spirulina platensis encapsulated by water soluble chitosan nanoparticles

Spirulina platensis is a microalga containing protein and other nutrients, also pigments which has several advantages in food and pharmaceuticals. Phycocyanin is a blue pigment from Spirulina sp. composed by α and β polypeptide with phycocyanobilin. Phycocyanin can be extracted by ultra-sonication method. However, this pigment can be easily degraded because of its instability caused by pH, temperature, and light. One of methods for maintaining the stability is encapsulation by coating material. Water soluble chitosan (WSC) is known as a low-molecular weight and low toxic coating material dissolve in water. The purposes of this study were to determine phycocyanin extraction with different time and evaluate the stability of phycocyanin in WSC nanoparticles. Phycocyanin-WSC nanoparticles were prepared with three different ratio of WSC to phycocyanin i.e 1:1, 1:0.75, 1:0.5 (w/w). Extraction phycocyanin using ultrasonicator for 15 min showed the highest concentration (1.28 mg/mL) and yield (2.56%). The smallest size and narrow polydispersities of phycocyanin-WSC nanoparticles was achieved with ratio of WSC to phycocyanin of 1:0.75 (w/w). Encapsulation of phycocyanin in WSC nanoparticle enhanced the stability at 50°C for 90 min. Encapsulation can be used for any supplement application.

Effect of acetic acid hydrolysis on the characteristics of water soluble chitosan

Chitosan is a derivative product of chitin deacetylation and has many functions in food industry. However, it has limitation on application caused by low solubility in water. In order to increase the solubility in water, the hydrolysis using acetic acid was performed to reduce the molecular weight. The concentration of acetic acid, temperature of hydrolysis and hydrolysis time related to the solubility were investigated. Hydrolysis using 5% acetic acid was able to produce water soluble chitosan (WSC) with a molecular weight of 198.64 kDa and 46.10% solubility in water. WSC that was obtained at 60 oC for 90 min of hydrolysis process in 5% acetic acid had characteristics of viscosity, molecular weight, solubility in water and deacetylation degree were 0.85 cP, 166.34 kDa, 53.66% and 92.92%, respectively.

An evaluation of antimicrobial potential of irreversible hydrocolloid impression material incorporated with chitosan.

Aim:To evaluate the antimicrobial potential of irreversible hydrocolloid impression material manipulated using chitosan impregnated solution at various time intervals.Setting and Design:Evaluative invivo study design.Materials and Methods:Maxillary impressions made for 20 dentulous volunteers using irreversible hydrocolloid impression material manipulated using distilled water as control and using 1% chitosan impregnated solution as test group using stock metal trays with one-week interval. Bacterial samples were collected using dry sterile cotton swab in the mid-palatal region at the time intervals of 0, 10, 20 minutes. Bacterial swabs were inoculated on nutrient agar media and incubated at 37° C for 24 hours. Bacterial colonies were counted with the aid of colony counter.Statistical Analysis Used:The resultant data was subjected to statistical analysis using repeated measures ANOVA and independent t test.Results:Adding water soluble chitosan to irreversible hydrocolloid impression material resulted in superior antimicrobial activity. With the passage of time there was a significant decrease in the microbial colony count upto 10min (p=0.016). However, the rate of decrease of microbial colony count was statistically insignificant between the samples collected at 10 and 20 min.Conclusion:Incorporation of water soluble chitosan to irreversible hydrocolloid impression material showed significant antimicrobial activity in 10 minutes.

Содержание деценовых кислот в препаратах трутневого расплода и комбинированных препаратах на его основе

The drone brood contains a large number of substances with antioxidant activity. These substances require stabilization and strict adherence to storage conditions. Among these substances are unique decenoic acids, the content of which is an indicator of the quality of drone brood and products based on it. The ability of drone brood to reduce the manifestations of oxidative stress is shown. There are dietary supplements for food and drugs based on drone brood, which are used for a wide range of diseases. Together with drone brood, chitosan-containing products, propolis, royal jelly can be used. They enrich the composition with their own biologically active substances and affect the preservation of the biologically active substances of the drone brood. Promising are the products containing, in addition to the drone brood, a chitin-chitosan-melanin complex from bees, propolis, royal jelly. The chitin-chitosan-melanin complex in the amount of 5% in the composition of the adsorbent practically does not affect the preservation of decenic acids, while in the amount of 2% and 10% it somewhat worsens. The acid-soluble and water-soluble chitosan of marine crustaceans significantly worsens the preservation of decenoic acids in the product. Drone brood with royal jelly demonstrates a rather high content of decenoic acids. When propolis is introduced into the composition of the product, the content of decenoic acids increases according to the content of propolis.

Possibility of Producing Semisolid Dosage Forms Based on Aqueous Solutions of Chitosan Succinamide in the Presence of Modification Additives

The rheological behavior of the water-soluble chitosan derivative chitosan succinamide in a solvent—modifying additive system (ethanol, ethylene glycol, glycerin, sorbitol) was studied to find the conditions for the formation of highly viscous gels suitable for creating semisolid dosage forms. It was found that in the presence of modifying additives of polyhydric alcohols (glycerol and sorbitol), the complex viscosity of chitosan succinamide solutions increases and earlier formation occurs of the spatial network of macromolecules, whose strength makes it possible to form yield stress systems. It was shown that in the range of chitosan succinamide concentrations in a solution of 7.0–10.0 wt %, the use of polyhydric alcohols glycerol and sorbitol with a concentration of 1.5–4.0 M allows producing systems suitable for use as a polymer base for semisolid dosage forms with rheological characteristics, corresponding to the optimum consistency of hydrophilic ointments in the temperature range from 20–40°C, that is, under conditions that reflect the storage and direct use of semisolid dosage forms.

Synthesis of Chitosan-&lt;i&gt;graft&lt;/i&gt;-Poly(vinyl ether) as a Thermoresponsive Water-Soluble Chitosan

Synthesis of Chitosan-&lt;i&gt;graft&lt;/i&gt;-Poly(vinyl ether) as a Thermoresponsive Water-Soluble Chitosan

Activity of chitosan antifungal denture adhesive against common Candida species and Candida albicans adherence on denture base acrylic resin

Statement of problemCandida adherence to the denture base is an important cause of denture stomatitis. In addition, infections with drug-resistant Candida have become more prevalent, especially among elderly and immunocompromised patients. Thus, alternative safe antifungal agents for oral applications are needed. PurposeThe purpose of this in vitro study was to investigate the activity of chitosan, a natural biopolymer, against common oral Candida species and its efficacy in inhibiting C albicans adherence to denture-base acrylic resin. Material and methodsThe minimum fungicidal concentrations (MFCs) of 5 types of chitosan against 6 species of Candida and 10 C albicans clinical isolates were determined by broth and agar dilution, respectively. N-succinyl chitosan (NSC), low- and high-molecular-weight water-soluble chitosan (LMWC and HMWC), and oligomer and polymer shrimp-chitosan were examined. NSC and HMWC, as pure gel and as a mixture with carboxymethylcellulose (CMC), were applied to acrylic resin disks, incubated with C albicans for 24 hours, and washed, and adherent cells were collected for colony count. The effects of HMWC on human gingival fibroblasts after 1 and 24 hours of treatment were measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The retention force of HMWC gel was measured by using a universal testing machine. The Kruskal-Wallis and Mann-Whitney U tests were used to compare the antiadherence activity (α=.05). ResultsHMWC had the highest antifungal activity against most Candida species tested and C albicans clinical isolates. HMWC gel completely inhibited C albicans adherence to denture base acrylic resin (P<.001). CMC denture adhesive significantly increased C albicans adherence (P<.001), but adding 2×MFC HMWC into CMC reduced the adherence, although this was not statistically significant (P=.06). HMWC at 1×MFC and 2×MFC showed no toxic effect on gingival fibroblast viability and proliferation. Moreover, the retention force provided by HMWC gel was sufficient for use as a denture adhesive (>5000 Pa). ConclusionsHigh-molecular-weight, water-soluble chitosan is a biocompatible biopolymer that could inhibit C albicans adherence and that showed properties suitable for development into an antifungal denture adhesive.