Preparation of paraoxonase-1 liposomes and studies on their in vivo pharmacokinetics in rats

被引：15

作者：

Han, Zhen-Kun ^{[1
]}

Liu, Zhen-Ning ^{[1
]}

Yuan, Li ^{[1
]}

Zhang, Peng-Si ^{[1
]}

Zhao, Min ^{[1
]}

机构：

[1] China Med Univ, Shengjing Hosp, Emergency Dept, Shenyang 110004, Peoples R China

来源：

CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY | 2014年 / 41卷 / 10期

基金：

中国国家自然科学基金;

关键词：

encapsulation efficiency; long-circulating liposomes; organophosphate poisoning; paraoxonase-1; pharmacokinetics; SERUM PARAOXONASE; PON1; TOXICITY; POLYMORPHISMS; PROTECTS; MICE;

D O I：

10.1111/1440-1681.12275

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

A liposome formulation of the enzyme paraoxonase-1 (PON1) was prepared for purposes of prolonging and maintaining its activity in vivo. Following purification of PON1 from rabbit serum, liposomes containing PON1 (L-PON1) were prepared using a film-dispersion method with a soybean phospholipid-cholesterol mixture (5:1, w/w). The pharmacokinetic behaviour of conventional injectable PON1 and L-PON1 was compared following a single intravenous injection in rats. The enzyme activity of PON1 and its pharmacokinetic parameters were calculated based on a two-compartment model following conventional injection. The level of PON1 encapsulation in L-PON1 was 86.20 +/- 3.12%. The particle size distribution of L-PON1 was a narrow unimodal form, with an average diameter of 126nm. The results suggest that compared with conventional injectable PON1, L-PON1 has an improved half-life and enhanced enzyme activity in rats. In conclusion, PON1 can be encapsulated into a lipid bilayer for enhanced stability.

引用

页码：825 / 829

页数：5

共 24 条

[1]

The 'evolvability' of promiscuous protein functions [J].