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已发表论文

pH 敏感的聚 (丙交酯-共-乙交酯) 纳米颗粒复合微胶囊用于胰岛素的口服给药

 

Authors Sun S, Liang N, Yamamoto H, Kawashima Y, Cui F, Yan P

Published Date May 2015 Volume 2015:10 Pages 3489—3498

DOI http://dx.doi.org/10.2147/IJN.S81715

Received 28 January 2015, Accepted 20 March 2015, Published 11 May 2015

Abstract: This study proposes a new concept of pH-sensitive poly(lactide-co-glycolide) (PLGA) nanoparticle composite microcapsules for oral delivery of insulin. Firstly, insulin–sodium oleate complex was prepared by the hydrophobic ion pairing method and then encapsulated into PLGA nanoparticles by the emulsion solvent diffusion method. In order to reduce the burst release of insulin from PLGA nanoparticles and deliver insulin to specific gastrointestinal regions, hence to enhance bioavailability of insulin, the PLGA nanoparticles were further encapsulated into Eudragit® FS 30D to prepare PLGA nanoparticle composite microcapsules by organic spray-drying method. The preparation was evaluated in vitro and in vivo, and the absorption mechanism was discussed. The in vitro drug release studies revealed that the drug release was pH dependent, and the in vivo results demonstrated that the formulation of PLGA nanoparticle composite microcapsules was an effective candidate for oral insulin delivery.
Keywords: sodium oleate, complex, PLGA nanoparticles, Eudragit® FS 30D





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