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Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery

Authors Kim MS, Yeom DW, Kim SR, Yoon HY, Kim CH, Son HY, Kim JH, Lee S, Choi YW

Received 28 September 2016

Accepted for publication 26 November 2016

Published 21 December 2016 Volume 2017:11 Pages 45—57

DOI https://doi.org/10.2147/DDDT.S123412

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Akshita Wason

Peer reviewer comments 2

Editor who approved publication: Dr Anastasios Lymperopoulos


Min Soo Kim,1,* Dong Woo Yeom,1,* Sung Rae Kim,1 Ho Yub Yoon,1 Chang Hyun Kim,1 Ho Yong Son,1 Jin Han Kim,1 Sangkil Lee,2 Young Wook Choi1

1College of Pharmacy, Chung-Ang University, Seoul, 2College of Pharmacy, Keimyung University, Daegu, South Korea

*These authors contributed equally to this work

Abstract: A double layer-coated colon-specific drug delivery system (DL-CDDS) was developed, which consisted of chitosan (CTN) based polymeric subcoating of the core tablet containing citric acid for microclimate acidification, followed by an enteric coating. The polymeric composition ratio of Eudragit E100 and ethyl cellulose and amount of subcoating were optimized using a two-level factorial design method. Drug-release characteristics in terms of dissolution efficiency and controlled-release duration were evaluated in various dissolution media, such as simulated colonic fluid in the presence or absence of CTNase. Microflora activation and a stepwise mechanism for drug release were postulated. Consequently, the optimized DL-CDDS showed drug release in a controlled manner by inhibiting drug release in the stomach and intestine, but releasing the drug gradually in the colon (approximately 40% at 10 hours and 92% at 24 hours in CTNase-supplemented simulated colonic fluid), indicating its feasibility as a novel platform for CDD.

Keywords: chitosan, colon-specific delivery, acidification, microflora, factorial design, controlled release

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