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

被引：41

作者：

Wang, Mei ^{[1
]}

Liu, Meng ^{[3
]}

Xie, Tingting ^{[4
]}

Zhang, Bing-Feng ^{[2
]}

Gao, Xiao-Li ^{[1
]}

机构：

[1] Xinjiang Med Univ, Dept Pharmaceut, Coll Pharm, Urumqi, Peoples R China

[2] Yichun Univ, Coll Chem & Bioengn, Yichun, Peoples R China

[3] Xinjiang Med Univ, Affiliated Tumor Hosp, Urumqi, Peoples R China

[4] Peoples Liberat Army Gen Hosp, Dept Pharmaceut Care, Beijing, Peoples R China

来源：

COLLOIDS AND SURFACES B-BIOINTERFACES | 2017年 / 159卷

基金：

中国国家自然科学基金;

关键词：

Progesterone; Oral bioavailability; Chitosan; Cholesterol-free liposomes; INSULIN-LOADED LIPOSOMES; DRUG-DELIVERY; BILE-SALTS; CANCER; SYSTEM;

D O I：

10.1016/j.colsurfb.2017.08.028

中图分类号：

Q6 [生物物理学];

学科分类号：

071011 ;

摘要：

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 +/- 19.3 nm) with positive potential (28.19 +/- 1.97 mV). 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 AUC(0-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 (R)) and Lipo/Prog. Collectively, these findings suggest that cholesterol-free chitosan-coated liposomes are a promising alternative for improving the oral bioavailability of progesterone. (C) 2017 Elsevier B.V. All rights reserved.

引用

页码：580 / 585

页数：6

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