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Chitosan-modified cholesterol-free liposomes for improving the oral bioavailability of progesterone B Biointerfaces

Author:
Wang, Mei, Liu, Meng, Xie, Tingting, Zhang, Bing-Feng, Gao, Xiao-Li
Source:
Colloids and surfaces 2017 v.159 pp. 580-585
ISSN:
0927-7765
Subject:
bioavailability, cholesterol, colloids, drugs, gastrointestinal system, mice, oral administration, progesterone
Abstract:
Based on the structurally similar properties of progesterone and cholesterol, chitosan-coated cholesterol-free liposomes (CS-Lipo/Prog) were formulated. CS-Lipo/Prog are spherical and uniform in size (662.1±19.3nm) with positive potential (28.19±1.97mV). The average drug entrapment efficiency (EE) is approximately 80%. The in vitro release profile of CS-Lipo/Prog shows sustained release. The in vitro stability evaluation demonstrated that CS-Lipo/Prog can efficiently shield Prog from degradation in the gastrointestinal tract. CS-Lipo/Prog showed a longer MRT and higher AUC0-infinite after oral administration to mice than in the control group (progesterone-free). The relative bioavailability of CS-Lipo/Prog was higher than that of progesterone soft capsules (QINING®) and Lipo/Prog. Collectively, these findings suggest that cholesterol-free chitosan-coated liposomes are a promising alternative for improving the oral bioavailability of progesterone.
Agid:
5828896