NOVEL LIPOSOME COCKTAIL FORMULATIONS CONTAINING DOXORUBICIN AND THE POTENT MULTIDRUG RESISTANCE INHIBITOR AMIODARONE

摘要

A novel liposome encapsulated amiodarone - doxorubicin cocktail formulation is provided that is expected to enhance the therapeutic index of liposomal doxorubicin by amiodarone mediated multidrug resistance defeat. Also provided is a liposome encapsulated amiodarone in liposomes bearing guanidinylated lipids which can enhance cellular binding through molecular recognition. Liposomes having these properties are comprised of phosphatidylcholine, cholesterol, guanidinylated lipids Octadecylguanidine hydrochloride (ODG) or N- [3- (octadecylamino) propyl] guanidine hydrochloride (ODPG), amiodarone and doxorubicin encapsulated in their aqueous cores. These liposomes are unilamellar and have and approximative size of 100 nanometers and are expected to be stable in whole mammal blood, upon the introduction of polyethylene glycol (PEG) or other counterpart groups.