title: Preparation of paraoxonase-1 liposomes and studies on their in vivo pharmacokinetics in rats.
abstract: 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 126 nm. 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.
authors.affiliation: Department of Emergency, Shengjing Hospital of China Medical University, Shenyang, China.
authors.forename: Zhen-Kun
authors.initials: ZK
authors.lastname: Han
authors.forename: Zhen-Ning
authors.initials: ZN
authors.lastname: Liu
authors.forename: Li
authors.initials: L
authors.lastname: Yuan
authors.forename: Peng-Si
authors.initials: PS
authors.lastname: Zhang
authors.forename: Min
authors.initials: M
authors.lastname: Zhao
mesh_terms: D000818:Animals; D043303:Aryldialkylphosphatase / Q000378:metabolism*; D004337:Drug Carriers / Q000378:metabolism; D004355:Drug Stability; D006207:Half-Life; D007275:Injections, Intravenous; D008051:Lipid Bilayers / Q000378:metabolism; D008081:Liposomes / Q000378:metabolism*; D008297:Male; D010316:Particle Size; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar
chemical_list: D004337:Drug Carriers; D008051:Lipid Bilayers; D008081:Liposomes; D043303:Aryldialkylphosphatase
keywords: encapsulation efficiency; long-circulating liposomes; organophosphate poisoning; paraoxonase-1; pharmacokinetics