title: Preparation and performance evaluation of emulsomes as a drug delivery system for silybin.
abstract: We developed silybin (SIL) emulsomes and evaluated their physicochemical properties and the in vivo pharmacokinetics of SIL delivered by emulsomes in rats. SIL emulsomes were prepared using the thin film dispersion method. SIL emulsomes were evaluated for their entrapment efficiency, particle size, zeta potential, morphology, in vitro release, and in vivo drug delivery in rats. The entrapment efficiency was above 80 %. The average particle size and zeta potential were 364.1 ± 20 nm and -34 ± 8 mV, respectively. Morphological analysis revealed that the SIL emulsomes were spherical in shape. Compared to an SIL solution, emulsomes produced sustained release of SIL for up to 48 h after an initial burst release in vitro. The pharmacokinetics of SIL emulsomes in rats were evaluated after intravenous injection, and the results were compared with those obtained for the control SIL solution. Following SIL delivery by emulsomes, the area under the curve was 2.2-fold higher and the mean residence time was 2.5-fold higher than the corresponding values recorded using SIL solution. Hence, emulsomes might represent a promising system for improving the bioavailability of lipophilic drugs. Moreover, emulsomes produce sustained drug release, which is advantageous in the clinical setting.
authors.affiliation: Department of Pharmacy, Gansu Provincial Hospital, 204 Donggang West Road, Lanzhou, 730000, China. zhxd0528@163.com.
authors.forename: Xiaodan
authors.initials: X
authors.lastname: Zhou
authors.affiliation: Department of Pharmacy, Nanjing University of Traditional Chinese Medicine, Nanjing, 210046, China. czpcpu@sina.com.cn.
authors.forename: Zhipeng
authors.initials: Z
authors.lastname: Chen
mesh_terms: D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D045703:Emulsifying Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D008081:Liposomes; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D000077385:Silybin; D012838:Silymarin / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000493:pharmacokinetics*
chemical_list: D045703:Emulsifying Agents; D008081:Liposomes; D012838:Silymarin; D000077385:Silybin
keywords: Drug delivery; Emulsomes; Pharmacokinetics; Silybin; Solution; Sustained release