Dataset Information

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:Many active pharmaceutical ingredients (API) possess poor aqueous solubility and thus lead to poor bioavailability upon oral administration and topical application. Nanocrystals have a well-established, universal formulation approach to overcome poor solubility. Various nanocrystal-based products have entered the market for oral application. However, their use in dermal formulations is relatively novel. Previous studies confirmed that nanocrystals are a superior formulation principle to improve the dermal penetration of poorly soluble API. Other studies showed that nanocrystals can also be used to target the hair follicles where they create a drug depot, enabling long acting drug therapy with only one application. Very recent studies show that also the vehicle in which the nanocrystals are incorporated can have a tremendous influence on the pathway of the API and the nanocrystals. In order to elucidate the influence of the excipient in more detail, a systematic study was conducted to investigate the influence of excipients on the penetration efficacy of the formulated API and the pathway of nanocrystals upon dermal application. Results showed that already small quantities of excipients can strongly affect the passive dermal penetration of curcumin and the hair follicle targeting of curcumin nanocrystals. The addition of 2% ethanol promoted hair follicle targeting of nanocrystals and hampered passive diffusion into the stratum corneum of the API, whereas the addition of glycerol hampered hair follicle targeting and promoted passive diffusion. Propylene glycol was found to promote both pathways. In fact, the study proved that formulating nanocrystals to improve the bioefficacy of poorly soluble API upon dermal application is highly effective. However, this is only true, if the correct excipient is selected for the formulation of the vehicle. The study also showed that excipients can be used to allow for a targeted dermal drug delivery, which enables to control if API should be delivered via passive diffusion and/or as drug reservoir by depositing API in the hair follicles.

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.

Similar Datasets

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