TY - JOUR
T1 - In vitro and in vivo aspects of N-acyl-phosphatidylethanolamine-containing liposomes
AU - Vermehren, C.
AU - Clausen-Beck, B.
AU - Frøkjær, S.
AU - Hansen, Harald S.
PY - 2003/3/18
Y1 - 2003/3/18
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0037453171&partnerID=8YFLogxK
U2 - 10.1016/S0378-5173(02)00681-6
DO - 10.1016/S0378-5173(02)00681-6
M3 - Journal article
AN - SCOPUS:0037453171
SN - 0378-5173
VL - 254
SP - 49
EP - 53
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1
ER -