Liposomal palmitoyl-L-asparaginase: characterization and biological activity.
A new derivative of L-asparaginase, palmitoyl-L-asparaginase (palmitoyl-L-ASNase), has been incorporated in liposomes. For this purpose we modified the dehydration-rehydration method and optimized the liposomal composition. The pharmacokinetics, toxicity, and in vivo antitumor activity against P1534 lymphoma of different liposomal palmitoyl-L-ASNase formulations were studied. Liposomal encapsulation of palmitoyl-L-ASNase as compared with free palmitoyl-L-ASNase resulted in a prolongation of the blood half-life (from 2.88 h to longer than 23.7 h), abrogation of acute toxicity, and preservation of in vivo antitumor activity.
Jorge
J C
JC
Departamento de Biotecnologia/INETI, Estrada das Palmeiras, Portugal.
Perez-Soler
R
R
Morais
J G
JG
Cruz
M E
ME
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001215:Asparaginase / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D008081:Liposomes; D008223:Lymphoma / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D009368:Neoplasm Transplantation; D010168:Palmitates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D008081:Liposomes; D010168:Palmitates; C087753:palmitoyl-L-asparaginase; D001215:Asparaginase