In vitro and in vivo aspects of N-acyl-phosphatidylethanolamine-containing liposomes
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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.
Originalsprog | Engelsk |
---|---|
Tidsskrift | International Journal of Pharmaceutics |
Vol/bind | 254 |
Udgave nummer | 1 |
Sider (fra-til) | 49-53 |
Antal sider | 5 |
ISSN | 0378-5173 |
DOI | |
Status | Udgivet - 18 mar. 2003 |
ID: 45562877