Useful Extend-release Chitosan Tablets with High Antioxidant Activity.

Taira Yasufuku,Hisao Tomida,Nobuyuki Kobayashi,Toshiyuki Hata,Makoto Anraku,Yuko Kondo,Junzo Hirose

doi:10.3390/pharmaceutics2020245

Taira Yasufuku, Hisao Tomida + Show 5 more

Open Access

https://doi.org/10.3390/pharmaceutics2020245

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Journal: Pharmaceutics	Publication Date: May 27, 2010
Citations: 38	License type: CC BY 3.0

Affiliation: Fukuyama University, Dainichiseika (Japan)

Abstract

The antioxidant properties of different low molecular weight (LMW) chitosans (CS1; 22 kDa, CS2; 38 kDa, CS3; 52 kDa, CS4; 81 kDa) were examined for possible use in extended-release tablets. The criteria used were the ability of the chitosans to reduce Cu2+, and hydroxyl and superoxide radicals and N-centered radicals derived from 1,1'-diphenyl-2-picrylhydrazyl, via the use of ESR spectrometry. CS2 showed the highest scavenging activity. CS1 and CS3, however, were much less effective and CS4 was not a viable antioxidant. The results suggest that CS2 could be useful in combating the development of oxidative stress. A series of chitosan tablets were prepared using a spray drying method and evaluated as an extended-release matrix tablet using theophylline (TPH) as a model drug. The release of TPH from the different MW chitosan tablets increased with increasing MW of the chitosan used. CS2, CS3 and CS4 showed a reasonable release activity, but CS1 showed the shortest release activity. Moreover, the CS2-TPH tablet showed the highest scavenging activity of the three chitosan tablets (CS2-CS4) using 2,2’-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) radicals. These results suggest that a CS2-TPH tablet could be potentially useful in an extended-release matrix tablet with a high antioxidant activity.

Highlights

When a drug is freely soluble in water, the judicious selection of release-retarding excipients is necessary to achieve a constant in vivo input rate
We reported that the scavenging of hydroxyl radicals by low molecular weight (LMW) chitosan inhibits the peroxidation of human serum albumin (HSA) [11]
We showed that the administration of LMW chitosan to human volunteers prevented the oxidation of HSA in vivo (Anraku et al, 2009) [14]

Summary

Introduction

When a drug is freely soluble in water, the judicious selection of release-retarding excipients is necessary to achieve a constant in vivo input rate. Chitosan is a naturally occurring cationic copolymer comprised of glucosamine, and can be produced by the deacetylation of chitin, which is the second most abundant polysaccharide after cellulose in the world. It is widely used in a variety of pharmaceutical formulations as sustained release carrier systems such as beads, gels, films, sponges and microspheres, because of many unique properties, which include low toxicity, biocompatibility, biodegradability and mucoadhesive properties [4,5,6,7,8]. We reported that the scavenging of hydroxyl radicals by low molecular weight (LMW) chitosan inhibits the peroxidation of human serum albumin (HSA) [11]

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