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Preparation of paraoxonase‐1 liposomes and studies on their in vivo pharmacokinetics in rats
Author(s) -
Han ZhenKun,
Liu ZhenNing,
Yuan Li,
Zhang PengSi,
Zhao Min
Publication year - 2014
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/1440-1681.12275
Subject(s) - pharmacokinetics , paraoxonase , liposome , in vivo , chemistry , phospholipid , enzyme , pharmacology , biochemistry , medicine , biology , membrane , microbiology and biotechnology
Summary A liposome formulation of the enzyme paraoxonase‐1 ( PON 1) was prepared for purposes of prolonging and maintaining its activity in vivo . Following purification of PON 1 from rabbit serum, liposomes containing PON 1 (L‐ PON 1) were prepared using a film‐dispersion method with a soybean phospholipid–cholesterol mixture (5 : 1, w/w). The pharmacokinetic behaviour of conventional injectable PON 1 and L‐ PON 1 was compared following a single intravenous injection in rats. The enzyme activity of PON 1 and its pharmacokinetic parameters were calculated based on a two‐compartment model following conventional injection. The level of PON 1 encapsulation in L‐ PON 1 was 86.20 ± 3.12%. The particle size distribution of L‐ PON 1 was a narrow unimodal form, with an average diameter of 126 nm. The results suggest that compared with conventional injectable PON 1, L‐ PON 1 has an improved half‐life and enhanced enzyme activity in rats. In conclusion, PON 1 can be encapsulated into a lipid bilayer for enhanced stability.