期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 91, 期 8, 页码 1795-1802出版社
JOHN WILEY & SONS INC
DOI: 10.1002/jps.10172
关键词
pH-sensitive liposomes; poly(N-isopropylacrylamide); sterically stabilized liposomes
The aim of this study was to characterize a pH-sensitive liposome formulation bearing a terminally alkylated N-isopropylacrylamide (NIPAM) copolymer with regard to its pH responsiveness, surface properties, and pharmacokinetics. The interacting forces between two lipid bilayers bearing the anchored NIPAM copolymer were measured with a surface force apparatus. The pH-triggered content release was evaluated in buffer before and after incubation in human serum. The pharmacokinetics was determined in rats following the intravenous injection of Ga-67-loaded liposomes with or without the polymer coating. The force measurements between lipid bilayers showed that NIPAM copolymers provide a steric barrier that was dependent on pH. The pH-sensitive liposomes maintained their pH sensitivity after incubation in serum. In vivo, the polymer-coated liposomes exhibited a prolonged circulation time in rats, with an area under the blood concentration-time curve that is 1.6-fold higher than the control formulation. This study showed that liposomes can be rendered pH sensitive by anchoring a terminally alkylated NIPAM copolymer at their surface. At neutral pH, the polymer provides a steric barrier that increases the liposome circulation time in vivo. (C) 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association.
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