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Self-stabilized chitosan and its complexes with carboxymethyl starch as excipients in drug delivery.

ABSTRACT: This study focuses on the behavior of chitosan (CHI) and its polyelectrolyte complexes with carboxymethyl starch (CMS) used as monolithic matrices with acetaminophen as drug tracer. Two different chitosan grades were tested alone or associated in various ratios with CMS as excipients for tablets obtained by direct compression. The degree of deacetylation (DDA) of CHI, estimated from ¹H NMR and FTIR data, was correlated with X-ray diffraction and scanning electron microscopy (SEM) to evaluate structural organization of the monolithic matrices. In vitro drug dissolution assays showed major differences in CHI kinetic profiles between tablets exposed to acidic medium for 2h (to mimick gastric passage) prior to dissolution in simulated intestinal fluid (SIF), and those administered directly to SIF. Prior exposure to acidic SGF conducted to longer dissolution profiles (release completed after 16?h) and preservation of tablet shape, whereas tablets directly incubated in SIF were rapidly disintegrated. The improved properties of chitosan matrices exposed to SGF may be related to an outer compact coating layer (visible in SEM). The effect of self-stabilization of chitosan in acidic medium was compared to that due to formation of polyelectrolyte complexes (PEC) in co-processed polymeric systems (CHI:CMS). The self-formed membrane following exposure to gastric acidity appears to help maintaining tablet integrity and allows higher drug loading, recommending CHI and its complexes with CMS as excipients for drug delivery.

SUBMITTER: Leonida M

PROVIDER: S-EPMC6026327 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature

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Self-stabilized chitosan and its complexes with carboxymethyl starch as excipients in drug delivery.

Leonida Mihaela M Ispas-Szabo Pompilia P Mateescu Mircea Alexandru MA

Bioactive materials 20180508 3

This study focuses on the behavior of chitosan (CHI) and its polyelectrolyte complexes with carboxymethyl starch (CMS) used as monolithic matrices with acetaminophen as drug tracer. Two different chitosan grades were tested alone or associated in various ratios with CMS as excipients for tablets obtained by direct compression. The degree of deacetylation (DDA) of CHI, estimated from 1H NMR and FTIR data, was correlated with X-ray diffraction and scanning electron microsc ...[more]

PMID: 29988516

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Project description:Polymeric micelles combining the advantages of biocompatible poly- and oligosaccharides with classical micellar amphiphilic systems represent a promising class of drug carriers. In this work, micelles based on chitosan (or cyclodextrin) and oleic acid with various modification degrees were synthesized-the most optimal grafting degree is 15-30% in terms of CMC. According to NTA data, micelles have a hydrodynamic diameter of the main fraction of 60-100 nm. The inclusion of the antibacterial agents: moxifloxacin or rifampicin in micelles was studied by FTIR spectroscopy and fluorescence spectroscopy using a pyrene label (using monomer-excimer approach). When aromatic molecules are incorporated into micelles, the absorption bands of C-H bonds of the fatty tails of micelles shift towards smaller wavenumbers, indicating a stabilization of the micelles structure, and the microenvironment of the drug molecule changes according to the low frequencies shift and intensity changes in oscillation frequencies of 1450 cm-1 corresponding to aromatic fragment. Loading of moxifloxacin and rifampicin into micelles leads to a change in the fluorescent properties: a shift of the maximum of fluorescence emission to the long-wavelength region and an increase in the fluorescence anisotropy due to a drastic increase in the hydrodynamic volume of the fluorophore-containing rotating fragment. Using the pyrene label, the critical micelle concentrations were determined: from 4 to 30 nM depending on the polymer composition. Micellar systems enhance the effect of the antibiotic by increasing the penetration into bacterial cells and storing the drug in a protective coat. As a part of the supramolecular structure, the antibiotic remains active for more than four days, while in free form, the activity decreases after two days. In pharmacokinetic experiments, in vivo moxifloxacin in micellar systems show 1.7 times more efficiency compared to free form; moreover, two times higher maximal concentration in the blood is achieved. The advantage of polymer micellar systems in comparison with simple cyclodextrins and chitosan, which do not so significantly contribute to the antibacterial and pharmacokinetic parameters, was shown. Thus, polymeric micelles are one of the key approaches to improving the effectiveness of antibacterial drugs and solving the problems of resistant bacterial infections and multidrug resistance.

Dataset Information

Self-stabilized chitosan and its complexes with carboxymethyl starch as excipients in drug delivery.

Publications

Self-stabilized chitosan and its complexes with carboxymethyl starch as excipients in drug delivery.

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