Multivesicular liposomes containing 1-beta-D-arabinofuranosylcytosine for slow-release intrathecal therapy.
Optimal anticancer treatment with cell cycle-specific antimetabolites requires maintenance of a cytotoxic drug level for a prolonged period of time. We explored the use of multivesicular liposomes as a slow-release depot of 1-beta-D-arabinofuranosylcytosine for intrathecal administration. The intrathecal half-life of the liposome-encapsulated drug was 148 h, in contrast to the half-life of 2.7 h for the unencapsulated free drug, in a Sprague-Dawley rat model. The prolonged maintenance of a therapeutic drug level may increase efficacy, and the elimination of the very high peak level may decrease toxicity.
D000818:Animals; D003561:Cytarabine / Q000008:administration & dosage* / Q000378:metabolism / Q000633:toxicity; D003692:Delayed-Action Preparations; D004353:Drug Evaluation, Preclinical; D006207:Half-Life; D007278:Injections, Spinal; D007700:Kinetics; D008081:Liposomes / Q000008:administration & dosage*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
D003692:Delayed-Action Preparations; D008081:Liposomes; D003561:Cytarabine