title: Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation.
abstract: 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-OCH3-PPD). Optimized SMEDDS formulations for 25-OCH3-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-OCH3-PPD suspension and SMEDDS were evaluated and compared in rats. The plasma concentrations of 25-OCH3-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-OCH3-PPD via the oral route.
authors.affiliation: Department of Pharmacy, The First Affiliated Hospital of China Medical University, People's Republic of China.
authors.forename: Shuang
authors.initials: S
authors.lastname: Cai
authors.affiliation: Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
authors.forename: Cai-Hong
authors.initials: CH
authors.lastname: Shi
authors.affiliation: Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
authors.forename: Xiangrong
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
authors.forename: Xiaojiao
authors.initials: X
authors.lastname: Tang
authors.affiliation: Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
authors.forename: Hao
authors.initials: H
authors.lastname: Suo
authors.affiliation: Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
authors.forename: Li
authors.initials: L
authors.lastname: Yang
authors.affiliation: Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
authors.forename: Yuqing
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004355:Drug Stability; D004655:Emulsions; D005260:Female; D036145:Ginsenosides / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D050997:Nanomedicine; D051381:Rats; D017208:Rats, Wistar; D012502:Sapogenins / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D012995:Solubility; D013501:Surface-Active Agents
chemical_list: C529607:25-hydroxyprotopanaxadiol; D004655:Emulsions; D036145:Ginsenosides; D012502:Sapogenins; D013501:Surface-Active Agents
keywords: 12β; 20-triol (25-OCH3-PPD); 25-OH-PPD; 25-methoxydammarane-3β; bioavailability; pharmacokinetics; self-microemulsifying drug delivery system