Abstract

In this study, we examined a possible use of a surface-deacetylated chitin nano-fiber (SDCH-NF) and hyaluronic acid (HA) interpolymer complex (IPC) tablet as a potential antioxidative compound in extended-release matrix tablets. The antioxidant properties of untreated chitin (UCH), SDCH-NF, and HA were examined using N-centered radicals derived from 1,1′-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). SDCH-NF and HA had acceptable scavenging abilities and were relatively efficient radical scavengers, but UCH was much less effective. The results suggest that SDCH-NF and HA could serve as scavengers of compounds related to the development of oxidative stress. An SDCH-NF/HA IPC tablet was prepared and evaluated as an extended-release tablet matrix using famotidine (FMT) as a model drug. The release of FMT from the IPC tablet (DCF-NF:HA = 1:1) was slower than that from a SDCH-NF only tablet. Turbidity measurements and X-ray diffraction (XRD) data also indicated that the optimum complexation ratio for IPC between SDCH-NF/HA is 1/1, resulting in a good relationship between turbidity or XRD of the complex and the release ratio of FMT. These results suggest that an SDCH-NF/HA tablet has the potential for use in an extended-release IPC tablet with a high antioxidant activity.

Highlights

  • To achieve a constant in vivo input rate of freely water-soluble drugs, it is very important to select the most appropriate release-retarding excipients

  • Interpolymer complexes (IPCs) between polycationic polymers such as chitosan and polyanionic polymers such as alginate are reported to be useful as sustained-release drug matrices than hydrophilic polymer alone [3,4]

  • We reported in previous papers that chitosan inhibited the peroxidation of human serum albumin (HSA) in both in vitro and in vivo [7,8,9]

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Summary

Introduction

To achieve a constant in vivo input rate of freely water-soluble drugs, it is very important to select the most appropriate release-retarding excipients. Occurring polysaccharides and their derivatives have a bright prospect of constructing IPCs as sustained-release matrices, because of no or minor adverse effects Among these polysaccharides, chitosan is of interest due to its antioxidant activity. Surface-deacetylated chitin nanofibers (SDCH-NF) have received considerable attention, because the cationic amino groups on the fiber surface interact with anionic polymers to form IPCs by electrostatic interactions, endowing the fibers with different physicochemical and biological activities [12,13] They have the potential for use in various fields such as biotechnology, food, cosmetic industries, agriculture, and extreme biomimetics [14,15,16,17]. We evaluated a combination of SDCH-NF and HA with the antioxidant activity as extended-release matrices

Results and Discussion
Reagents
Preparations of SDCH-NF
Turbidity Measurements
Dissolution of Famotidine from Tablets
Statistics
Conclusions
Full Text
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