J. Meler, B. Grimling, M. Szcześniak, B. Karolewicz, Paweł Biernat
{"title":"ATORVASTATIN ADSORPTION STUDIES ON CHITOSANS IN AN in vitro PHARMACEUTICAL MODEL","authors":"J. Meler, B. Grimling, M. Szcześniak, B. Karolewicz, Paweł Biernat","doi":"10.15259/PCACD.23.014","DOIUrl":"https://doi.org/10.15259/PCACD.23.014","url":null,"abstract":"During the pharmacological therapy of specific diseases, drugs are used which, with other preparations or foods, can create connections, in many cases changing or even blocking their action. On the other hand, the use of unsuitable polymers as excipients may result in drug-polymer incompatibilities. Interactions consisting mainly of the occurrence of the adsorption phenomenon and on the formation of complex bonds that reduce the effect of the drugs are of particular importance.\u0000The aim of the study was to investigate whether the active substance atorvastatin is incompatible with dietary supplements containing chitosan.\u0000The phenomenon of the adsorption of the drug was examined using a static model of a pharmaceutical gastrointestinal tract, in the concentration range generally ingested in a single dose. Measurement results of the amount of bound drug were used to determine the average percentage of adsorbed drug dose. The results of the study prove that the anticholinesterase drug is adsorbed on chitosan in the pH ranges used, and that the binding capacity depends on the chitosan variety, which indirectly affects the reaction of the environment. It was observed that the average size of sorption depending on the chitosan variety ranged from 38% to 86%. The fact that the lowest value of adsorption was at pH 6.4 can be explained by the chemical properties of chitosan, which shows a charge only at pH >6.7. Under such conditions, the phenomenon of electrostatic adsorption may occur in relation to the healing substances of weak acids.\u0000At a pH above 7.6, corresponding to the intestinal fluid-filled intestine, the mean sorption for the highest dose of chitosan was from 38–86%. The increase in the adsorbed amount of anticholinesterase drugs on the polymer along with the increase in pH from 7.6 to 8.0 can be explained by the chitosan swelling properties, which increase with an increase in the pH.\u0000As a result, the specific surface area of the polymer and its sorption capacity increase. Based on the above considerations, it can be concluded that there is an antagonistic interaction between the drug and the polymer studied, which involves the adsorption of a drug from this group on the polymer (chitosan) and a decrease in its bioavailability.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48424591","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Konovalova, B. Shagdarova, A. Zubareva, A. Generalov, M. Grechikhina, E. Svirshchevskaya
{"title":"DEVELOPMENT OF MUCOADHESIVE CHITOSAN-BASED DRUG DELIVERY SYSTEM","authors":"M. Konovalova, B. Shagdarova, A. Zubareva, A. Generalov, M. Grechikhina, E. Svirshchevskaya","doi":"10.15259/PCACD.23.10","DOIUrl":"https://doi.org/10.15259/PCACD.23.10","url":null,"abstract":"Chitosan is a highly versatile biopolymer characterised by low toxicity, biocompatibility, and slow but complete biodegradation in the human body, possessing multiple reactive groups. One of the most well-known properties of positively charged chitosan derivatives is their ability to bind mucous membranes. The aim of this work was the analysis of mucoadhesion of unmodified 20 kDa chitosan and its hydrophobic (HC) and hydrophobic quaternised (QHC) derivatives in vitro and ex vivo. Unmodified chitosan formed large aggregates in vitro in keratinocyte and colon cell cultures and ex vivo in murine small intestine and muscle explants. At the same time, HC and especially QHC bound cells in vitro and ex vivo in a fine dotted manner, as evidenced by confocal microscopy. Such a pattern of hydrophobic derivatives distribution provides the possibility to develop mucoadhesive drug delivery systems with increased local drug release and improved chitosan biodegradation.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45865339","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
U. Filipkowska, T. Jóźwiak, Paula Bugajska, M. Kuczajowska-Zadrożna
{"title":"THE INFLUENCE OF CHITIN AMINATION ON THE EFFECTIVENESS OF RB5 AND RY84 DYE SORPTION","authors":"U. Filipkowska, T. Jóźwiak, Paula Bugajska, M. Kuczajowska-Zadrożna","doi":"10.15259/PCACD.23.006","DOIUrl":"https://doi.org/10.15259/PCACD.23.006","url":null,"abstract":"This article presents the influence of chitin amination on the effectiveness of RB5 and RY84 dye sorption. For chitin and chitin modified by amination, the optimal pH of sorption and the maximum sorption capacity were determined in relation to two reactive dyes: Reactive Black 5 (RB5) and Reactive Yellow 84 (RY84), differing in the active group and molecular weight. Three sorption models were used to describe the experimental data: Langmuir, Langmuir 2 and Freundlich. The highest sorption capacity was obtained for aminated chitin for both tested dyes: 386.53 mg/g for RB5 and 261.56 mg/g for RY84. In the case of sorption on unmodified chitin, the sorption capacities were lower: up to 235.65 mg/g.d.m. for RB5 and 208.88 mg/g.d.m. for RY84. The modification of chitin by amination has a beneficial effect on the amount of dye adsorbed in the process. The adsorptive capacity increased by 1.6-times in the case of RB5 and 1.25-times in case of RY84.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45880958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
T. Jóźwiak, U. Filipkowska, Paula Bugajska, M. Kuczajowska-Zadrożna, A. Mielcarek
{"title":"THE INFLUENCE OF THE DEACETYLATION DEGREE OF CHITOSAN IN THE FORM OF FLAKES ON THE EFFECTIVENESS OF NITRATES V SORPTION FROM AQUEOUS SOLUTIONS","authors":"T. Jóźwiak, U. Filipkowska, Paula Bugajska, M. Kuczajowska-Zadrożna, A. Mielcarek","doi":"10.15259/PCACD.23.008","DOIUrl":"https://doi.org/10.15259/PCACD.23.008","url":null,"abstract":"The influence of the degree of deacetylation of chitosan from the range of DD = 75–90% on the effectiveness of sorption of nitrates from aqueous solutions was investigated. The scope of the research included: determining the effect of pH on the effectiveness of N-NO3 binding on chitosan sorbents and determining the sorption capacity of chitosan sorbents with different degrees of deacetylation after 5, 15, 30 and 60 minutes.\u0000The effectiveness of sorption of nitrates on chitosan sorbents increased in the series DD=75% < DD=85% < DD=90%. Regardless of the degree of deacetylation, the sorption effectiveness of nitrates on chitosan was the highest at pH 4. The amount of nitrate-related sorbents was the highest after 30 min of sorption. A process time which was too long resulted in desorption of nitrates. The maximum sorption capacity for chitosan with the degree of deacetylation DD = 75, 85 and 90% was 0.59 mg N-NO3/g, 0.60 mg N-NO3/g and 0.87 mg N-NO3/g, respectively.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44261775","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"WETTING PROPERTIES OF CHITOSAN-MODIFIED AND PLASMA-TREATED PEEK SURFACES","authors":"K. Przykaza, M. Jurak, A. Wiącek","doi":"10.15259/PCACD.23.016","DOIUrl":"https://doi.org/10.15259/PCACD.23.016","url":null,"abstract":"In this paper, the wettability of chitosan/phospholipid (1,2-dipalmitoyl-sn-glycero-3-phosphocholine – DPPC), chitosan/lipid (cholesterol – Chol) and chitosan/protein (cyclosporine A – CsA) films on air plasma activated polyetheretherketone (PEEK) plates was studied. The layers were prepared using the solution spreading technique and their surface wetting properties were determined based on the measurements of the advancing and receding contact angles of water, formamide and diiodomethane. Moreover, based on the contact angle hysteresis model of Chibowski, values of total surface free energy were estimated. Significant changes in PEEK polarity were observed after plasma activation and modifications with Ch/DPPC, Ch/Chol and Ch/CsA layers. These molecules modulate the chitosan film surface by changing the type and magnitude of interactions, which is revealed in the values of surface free energy. These results may be important for the development and implementation of highly biocompatible bone substitution polymers coated with chitosan film with anti-fungal and anti-bactericidal properties. Those systems based on chitosan may also carry and release biologically active substances which could be relevant in the new generation of drug delivery systems.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45864063","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"FUNCTIONAL THREE-COMPONENT POLYMERIC BIOCOMPOSITES FOR THE TREATMENT OF BEDSORES","authors":"M. Wiśniewska-Wrona, M. E. Fray","doi":"10.15259/PCACD.23.019","DOIUrl":"https://doi.org/10.15259/PCACD.23.019","url":null,"abstract":"Presented here are the results of investigations into the preparation of three-component dressing materials from various biopolymers in the form of a single-layer film which is suitable as a carrier for pain-relieving (lidocaine) and bacteriostatic (sulphanilamid) therapeutic agents. Physical-chemical, biological and usable properties of the prepared materials were tested and assessed. The amount of added active substance was adopted based on the dose recommended by the Polish Pharmacopeia for external medicinal preparations.\u0000Antibacterial activity against gram (-) Escherichia coli and gram (+) Staphylococcus aureus was assessed in some of the biocomposites by quantitative methods. The cytotoxic action in direct contact with the mouse fibroblast NCTC clone 929 was also estimated.\u0000Thermal analysis (DSC), infrared spectrophotometry (FTIR) and nuclear magnetic resonance spectroscopy were employed to investigate the impact of the variable contents of chitosan, alginate, carboxymethyl cellulose (CMC), and the active substance upon the chemical- and phase-structure of the prepared three-component polymeric biocomposites.\u0000It was found that the quantitative composition of the biocomposites and the additive of active substances lidocaine and sulphanilamide exert a vital impact upon their physical-mechanical and usable properties (imbibition, absorption). Investigations into the release of the medicinal substance from the investigated biocomposites to an acceptor fluid led to the conclusion that the kinetics of the process may be described by a complex first order rate equation with two exponential functions.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46210924","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
A. Pestov, A. V. Mekhaev, Y. Privar, N. Prokuda, E. Modin, S. Bratskaya
{"title":"SCREENING OF THE CATALYTIC ACTIVITY OF Pd0 AND Pd2+- SUPPORTED ON CHITOSAN BEADS AND CRYOGELS","authors":"A. Pestov, A. V. Mekhaev, Y. Privar, N. Prokuda, E. Modin, S. Bratskaya","doi":"10.15259/PCACD.23.015","DOIUrl":"https://doi.org/10.15259/PCACD.23.015","url":null,"abstract":"Here, we report the results of screening of the catalytic activity of Pd-containing chitosan beads and cryogels in the cross-coupling reaction, hydrogenation of alkenes, nitro-, and carbonyl compounds and the hydrodechlorination of chlorophenols. Pd0-containing chitosan beads and cryogels show moderate catalytic activity in the reduction of alkenes and nitroaromatics. The conversion of nitroaromatics decreases for substrates with electron-withdrawing substituents, while the conversion of alkenes increases with the activation of carbon-carbon double bonds. For several substrates, a significant difference in kinetics and conversion degrees was observed for Pd nanoparticles supported on chitosan beads and cryogels. It was found that conversion in the hydrodechlorination reaction depends on substrate structure, being higher for substrates containing substituents with a positive mesomeric effect. Pd2+-chitosan catalysts showed high catalytic activity in cross-coupling (Heck reaction) offering the following advantages over known catalytic systems: lower reaction temperature, the selective functionalisation of C-I bonds, and the possibility to perform reactions with iodobenzene without base addition.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46407606","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Renata Czechowska-Biskup, R. Wach, J. Rosiak, P. Ulański
{"title":"PROCEDURE FOR DETERMINATION OF THE MOLECULAR WEIGHT OF CHITOSAN BY VISCOMETRY","authors":"Renata Czechowska-Biskup, R. Wach, J. Rosiak, P. Ulański","doi":"10.15259/PCACD.23.004","DOIUrl":"https://doi.org/10.15259/PCACD.23.004","url":null,"abstract":"The aim of this publication is to facilitate the estimation of chitosan molecular weight (MW) in laboratories with no access to sophisticated analytical instruments, by applying the easily accessible and economical capillary viscometry. The procedure of viscosity-average molecular weight (Mv) determination is described in details. The examples provided encompass testing of the experimental procedure for determination of the Mv of chitosan with a low-molecular weight of 7.7 kDa and 88 kDa, after verification with a high-molecular weight polymer (477 kDa). The experimental work demonstrated the importance of the initial concentration of low-MW chitosan for the accurate determination of intrinsic viscosity and, as a consequence, the viscosity-average molecular weight.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46812248","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Paula Bugajska, U. Filipkowska, T. Jóźwiak, M. Kuczajowska-Zadrożna
{"title":"THE INFLUENCE OF CHITOSAN FLAKE DEACETYLATION DEGREE ON ORTHOPHOSPHATE SORPTION EFFICIENCY FROM AQUEOUS SOLUTIONS","authors":"Paula Bugajska, U. Filipkowska, T. Jóźwiak, M. Kuczajowska-Zadrożna","doi":"10.15259/PCACD.23.003","DOIUrl":"https://doi.org/10.15259/PCACD.23.003","url":null,"abstract":"The article presents the effectiveness of orthophosphate sorption from aqueous solutions depending on the deacetylation degree of chitosan flakes.\u0000The first stage of the research was to determine the pH value at which the sorption process was the most effective (from the pH range 2–11). In the second stage, research was carried out to determine the maximum sorption capacities of chitosan with deacetylation degrees of 75%, 85% and 90% in relation to PO43-. The highest effectiveness of orthophosphate removal on chitosan, regardless of its deacetylation degree, was obtained at pH 4. At pH 2 and 3, the chitosan flakes dissolved. This study showed that the sorption effectiveness of phosphorus compounds depends on the deacetylation degree of chitosan. Along with the increase in deacetylation degree, the sorption capacity of chitosan also increases in relation to orthophosphates. It is related to the higher number of amino groups in the structure of chitosan, which are responsible for the sorption of pollutants in the form of anions. The maximum sorption capacity of chitosan-DD = 75% in relation to biogen was 5.13 mg/g, chitosan-DD = 85% was 5.65 mg/g, and chitosan-DD = 90% was 5.91 mg/g.\u0000After 60 minutes, the desorption process had begun and was most likely caused by an increase in the pH of the solution. Due to chitosan's ability to neutralise the sample and the associated risk of desorption, the time of sorbent contact with sewage cannot be longer than 60 minutes.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49586492","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
N. Drozd, Yu.S. Logvinova, B. Shagdarova, A. Il’ina, V. Varlamov
{"title":"THE INHIBITION OF HUMAN PLATELET AGGREGATION BY A LOW-MOLECULAR WEIGHT CHITOSAN","authors":"N. Drozd, Yu.S. Logvinova, B. Shagdarova, A. Il’ina, V. Varlamov","doi":"10.15259/PCACD.23.005","DOIUrl":"https://doi.org/10.15259/PCACD.23.005","url":null,"abstract":"Chitosan derivatives were obtained by chemical (MW of 6 kDa, DD 99% - Ch6/99; MW13 kDa, DD 98% - Ch13/98) and enzymatic (MW of 5 kDa, DD 85% - Ch5/85; MW of 10 kDa, DD 85% - Ch10/85) depolymeri-sation of chitosan with a MW of 334 and 1000 kDa. Chitosan derivatives (almost identical MW pairs and different DD) possessed insignificant an-ticoagulant activity, did not promote human platelet aggregation and re-duced ADP or collagen-induced platelet aggregation. The studied sam-ples at a concentration of 2 mg/ml reduced the aggregation of platelets more than twice induced in 2x10-6M and 1x10-5M concentrations; at weak activation in 2x10-6M, the Ch10/85 sample was the most effective. The Ch6/99 and Ch13/98 samples were 20 times more effective at the inhibi-tion of collagen-induced platelet aggregation than the Ch10/85 sample. The latter can be explained by the greater value of positive charge (DD) and polydispersity (Mw/Mn) of chitosan samples obtained by chemical de-polymerisation.","PeriodicalId":44461,"journal":{"name":"Progress on Chemistry and Application of Chitin and its Derivatives","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2018-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42803349","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}