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• Yasufuku, T
• Anraku, M
• Kondo, Y
• Hata, T
• Hirose, J
• Kobayashi, N
• Tomida, H
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• Yasufuku, T
• Anraku, M
• Kondo, Y
• Hata, T
• Hirose, J
• Kobayashi, N
• Tomida, H
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• Yasufuku, T
• Anraku, M
• Kondo, Y
• Hata, T
• Hirose, J
• Kobayashi, N
• Tomida, H

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Pharmaceutics 2010, 2(2), 245-257; doi:10.3390/pharmaceutics2020245

Article

Useful Extend-release Chitosan Tablets with High Antioxidant Activity

Taira Yasufuku ^1,† , Makoto Anraku ^1,† , Yuko Kondo ¹ , Toshiyuki Hata ¹ , Junzo Hirose ¹ , Nobuyuki Kobayashi ²  and Hisao Tomida ^1,*

¹ Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, 1 Sanzo, Gakuen-cho, Fukuyama 729-0292, Japan ² Dainichiseika Color & Chemicals Mfg. Co., Ltd., 7-6, Nihonbashi Bakuro-cho 1-chome, Chuo-ku, Tokyo, 103-8383, Japan ^† These authors contributed equally to this work.

* Author to whom correspondence should be addressed.

Received: 6 May 2010; in revised form: 21 May 2010 / Accepted: 26 May 2010 / Published: 27 May 2010

Download PDF Full-Text [801 KB, uploaded 27 May 2010 09:57 CEST]

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.

Keywords: chitosan; antioxidant; molecular weight; matrix tablet; extend-release; radicals

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