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

作者：Kim Min Soo; Yeom Dong Woo; Kim Sung Rae; Yoon Ho Yub; Kim Chang Hyun; Son Ho Yong; Kim Jin Han; Lee Sangkil; Choi Young Wook^*

来源：Drug Design, Development and Therapy, 2017, 11: 45-57.

DOI：10.2147/DDDT.S123412

• chitosan
• colon-specific delivery
• acidification
• microflora
• factorial design
• controlled release

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 twolevel 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 CTNasesupplemented simulated colonic fluid), indicating its feasibility as a novel platform for CDD.

• 出版日期2017