Self-microemulsifying drug-delivery system for improved oral bioavailability of 20-25-methoxyl-dammarane- β, 12β, 20-triol: preparation and evaluation

• Published in: International journal of nanomedicine Vol. 9; p. 913
• Main Authors: Cai, Shuang, Shi, Cai-Hong, Zhang, Xiangrong, Tang, Xiaojiao, Suo, Hao, Yang, Li, Zao, Yuqing
• Format: Journal Article
• Language: English
• Published: Dove Medical Press Limited 01.01.2014
• Subjects: Comparative analysis; Drug delivery systems; Drugs; Nanoparticles; Pharmacokinetics; Physiological aspects; Vehicles; China
• ISSN: 1178-2013; 1178-2013
• DOI: 10.2147/IJN.S56894

The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-soluble compound 20(S)-25-methoxydammarane-3β;12β;20-triol (25-OC[H.sub.3]-PPD). Optimized SMEDDS formulations for 25-OC[H.sub.3]-PPD contained Cremophor® EL (50%) as the surfactant, glycerin (20%) as the cosurfactant, and Labrafil® M1944 (30%) as the oil. The SMEDDS were characterized by morphological observation and mean droplet size. The pharmacokinetics and bioavailability of the 25-OC[H.sub.3]-PPD suspension and SMEDDS were evaluated and compared in rats. The plasma concentrations of 25-OC[H.sub.3]-PPD and its main metabolite, 25-OH-PPD, were determined by ultra performance liquid chromatography-tandem mass spectrometry. The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension. Improved solubility and lymphatic transport may contribute to this enhanced bioavailability. Our studies highlight the promise of SMEDDS for the delivery of 25-OC[H.sub.3]-PPD via the oral route. Keywords: 25-methoxydammarane-3β;12β;20-triol (25-OC[H.sub.3]-PPD), 25-OH-PPD, self-microemulsifying drug delivery system, bioavailability, pharmacokinetics