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Int. J. Mol. Sci. 2015, 16(11), 26125-26136; doi:10.3390/ijms161125949

Comparison of Simple Eudragit Microparticles Loaded with Prednisolone and Eudragit-Coated Chitosan-Succinyl-Prednisolone Conjugate Microparticles: Part II. In Vivo Evaluation of Efficacy, Toxicity, and Biodisposition Characteristics

Department of Drug Delivery Research, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan
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Author to whom correspondence should be addressed.
Academic Editors: Shinsuke Ifuku and Hitoshi Sashiwa
Received: 2 September 2015 / Revised: 13 October 2015 / Accepted: 22 October 2015 / Published: 2 November 2015
(This article belongs to the Special Issue Chitins 2015)
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Abstract

We previously prepared and evaluated simple Eudragit S100 microparticles loaded with prednisolone (ES-MP) and Eudragit S100-coated chitosan-succinyl-prednisolone conjugate microparticles (Ch-MP/ES) in vitro. In this work, the effectiveness, toxic side effects (5 mg prednisolone (PD) eq/kg × 3 d, 10 mg PD eq/kg × 3 d), and pharmacokinetic characteristics (5 mg PD eq/kg) were examined using rats with colitis induced through 2,4,6-trinitrobenzenesulfonic acid. ES-MP did not change the efficacy or toxic side effects of PD, and this was attributed to incomplete delivery to the target site and prolonged systemic drug absorption by ES-MP. On the other hand, Ch-MP/ES promoted the efficacy of PD and ameliorated its toxic side effects due to better delivery to the target site, very slow drug release and the strong suppression of drug absorption. Only Ch-MP/ES, which markedly changed drug release characteristics, improved the in vivo features of PD. View Full-Text
Keywords: simple Eudragit S100 microparticle; Eudragit S100-coated chitosan-succinyl-prednisolone conjugate microparticle; efficacy; toxicity; pharmacokinetic characteristics; 2,4,6-trinitrobenzenesulfonic acid-induced simple Eudragit S100 microparticle; Eudragit S100-coated chitosan-succinyl-prednisolone conjugate microparticle; efficacy; toxicity; pharmacokinetic characteristics; 2,4,6-trinitrobenzenesulfonic acid-induced
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Onishi, H.; Kikuchi, H. Comparison of Simple Eudragit Microparticles Loaded with Prednisolone and Eudragit-Coated Chitosan-Succinyl-Prednisolone Conjugate Microparticles: Part II. In Vivo Evaluation of Efficacy, Toxicity, and Biodisposition Characteristics. Int. J. Mol. Sci. 2015, 16, 26125-26136.

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