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Abstract

Liposomal Daunorubicin : Reduced Cardiotoxicity In The Face Of Unaltered Antitumor Activity In Swiss Mice Bearing Fibrosarcoma

Author(s): S Agrawal, S Tiwari, N Udupa, P Umadevi

Liposomes were prepared by the versatile pH gradient method with an aim to modify drug disposition and increase the therapeutic efficacy of the drug, daunorubicin. The preparation were then characterized with respect to size and its distribution, entrapment efficiency, in vitro drug release profile and its stability under specified conditions of storage. Antitumor efficacy bearing solid tumor namely fibrosarcoma and organ toxicity studies in swiss albino mice were conducted with the liposomes administered by intravenous route at a dose of 5 and 10 mg kg-1 body weight. Liposomes were found to be spherical, multilamellar in nature with mean diameter being 5 pm. The entrapment efficiency of drug was found to be 82.5±1.28%, with the drug being incorporated into the aqueous layer of the vesicles. Prepared liposomes were stable under refrigeration (4) as evident by less drug leakage and released the loaded drug in a controlled fashion. Antitumor studies indicate an insignificant difference (P>0.05) in volume doubling time between the free drug and daunorubicin liposomes at both doses but the animals treated with drug formulation exhibited dramatic decrease in cardiac toxicity. The result revealed that encapsulation of daunorubicin in liposomes are a potential tool for the delivery of drug, as this formulation significantly decreases the inherent cardiac toxicity of daunorubicin.