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In vitro and in vivo aspects of N-acyl-phosphatidylethanolamine-containing liposomes

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Incorporation of the phospholipid, N-acyl-phosphatidylethanolamine (NAPE), has shown to increase the liposomal stability towards plasma components in vitro. Besides increasing the circulation-time, NAPE has been shown to contain fusiogenic properties. Hence, fusion between NAPE-liposomes and target cells may be expected, resulting in a favorable delivery of drug to the target cell. In this study, NAPE has been tested as a potential liposomal component of phosphatidylcholine-liposomes. The liposomes were characterized by size, long-term stability and phase transition temperature (T). In vivo behavior of NAPE-liposomes was determined by the blood-circulation half-life in mice. A characterization of the liposomes revealed that high content of NAPE resulted in liposomes of increased size compared to pure phosphatidylcholine-liposomes. However, the liposomes showed only a slight increase in size during storage for 5 weeks. Determination of T for NAPE-liposomes showed increasing values of T by increasing percentage of NAPE in the liposomal bilayer, due to the higher T of NAPE compared to phosphatidylcholine. Blood-clearance studies showed an initial increase in blood-circulation of liposomes containing high amounts of NAPE. Thus, these results suggest that liposomes containing high percentage of NAPE may be a promising candidate for long-circulating liposomes, possibly in combination with other stabilizing components, e.g. cholesterol.
OriginalsprogEngelsk
TidsskriftInternational Journal of Pharmaceutics
Vol/bind254
Udgave nummer1
Sider (fra-til)49-53
Antal sider5
ISSN0378-5173
DOI
StatusUdgivet - 18 mar. 2003

ID: 45562877