Optimization and evaluation of Oridonin-loaded Soluplus^®-Pluronic P105 mixed micelles for oral administration

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• 作者：Zhongcheng Ke^a ; ^b ; ^c ; Zhenghai Zhang^c ; Hao Wu^c ; Xiaobin Jia^a ; ^c ; ^{jxiaobin2005@hotmail.com} ; Youjie Wang^d ; ^{shutcmyo@163.com}
• 关键词：Oridonin ; Soluplus® ; Pluronic® ; P105 ; Micelles ; Bioavailability
• 刊名：International Journal of Pharmaceutics
• 出版年：2017
• 出版时间：25 February 2017
• 年：2017
• 卷：518
• 期：1-2
• 页码：193-202
• 全文大小：2011 K
• 卷排序：518

文摘

In this study, a new type of mixed micelles was developed using Soluplus® (SOL) and Pluronic® P105 (P105) for the encapsulation of Oridonin (ORN). Oridonin-loaded micelles (ORN-M) were simply prepared using solvent evaporation and characterized for particle size, particle morphology, encapsulation efficiency, and drug loading. In addition, the in vitro drug release behavior of ORN-M was assessed using the widely applied dialysis bag technique. The pharmacokinetic property of ORN was explored in rats after oral administration of ORN-M. Optimized ORN-M were of a small size (137.2 ± 1.65 nm) and spherical shape when the ratio of SOL:P105 was 3:1, with entrapment efficiency 90.48 ± 1.85% and drug loading 15.08 ± 0.38%. Oral absorption capacity of ORN was greatly enhanced with a relative bioavailability of 210.55% in comparison to that of in-house suspensions, which suggests that ORN-M shows significantly improved bioavailability and drug absorption characteristics. Overall, the optimized SOL-P105 dual mixed micelles show great potential for use as oral drug carriers for cancer treatment.