A novel ph–enzyme-dependent melamine colon-specific delivery system

Abstract: The aim of the present study was to design a new pH–enzyme double-dependent mesalamine colon-specific delivery system. The drug release behaviors in vitro and pharmacokinetics and biodistribution in vivo were further evaluated. The mean particle diameters of mesalamine-coated microparticles were 312.2 μm. In vitro, a small amount of mesalamine was released in HCl at a pH of 1.2 and PBS medium at a pH of 7.4 for 5 hours, and 71% of the entrapped mesalamine was further released during the subsequent 20 hours of incubation. A greater area under the plasma concentration–time curve (AUC) was obtained for the coated microparticles (1.9-fold) compared to the suspensions group, which indicated that the encapsulated mesalamine had mostly been absorbed in rats over the period of 12 hours. The AUC0–t of the coated microparticles in colon was 2.63-fold higher compared to the suspensions (P,0.05). Hence, mesalamine-coated microparticles are considered to maintain the drug concentration within target ranges for a long period of time.

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A novel ph–enzyme-dependent mesalamine colon-speci c delivery system
Drug Design, Development and Therapy 2016:10 2021–2028
correspondence: Qin cao
Department of gastroenterology, Putuo hospital, shanghai University of Traditional chinese Medicine, 164 lanxi road, Putuo District, shanghai 200062, People’s republic of china
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