FORMULATION AND CHARACTERIZATION OF DOXORUBICIN HYDROCHLORIDE LIPOSOMES BY DOUBLE EMULSION METHOD

Abstract

Doxorubicin hydrochloride is one of the most commonly used cytotoxic anthracycline antibiotics used in cancer chemotherapy and has been shown to have activity against a wide variety of neoplasms. Conventional compositions of doxorubicin hydrochloride are available as freeze-dried product (or) as a solution of doxorubicin hydrochloride in water. Both these products have been associated with a number of toxicities when administered intravenously. Several approaches have taken in an effort to increase the circulation time of liposomes by coating the liposomal surface with a hydrophilic polymer such as polyethylene glycol, but have new toxic effects appeared like skin toxicity generally known as “Hand-Foot Syndrome”^. In the present study Doxorubicin Liposomes were formulated by “Double emulsion method to form Multivescicular liposomes”. The influence of various formulation and process parameters using different ratios of inner aqueous phase: oil phase: outer aqueous phase, homogenization speed, homogenization time on encapsulation efficiency, % free drug, particle size, zeta potential, surface morphology and release were investigated. Less than 10 % free drug was achieved with double emulsion method. The Scanning Electron Microscopy image showed the spherical shape having 33 ± 5 µm particle sizes. The in-vitro drug release for optimized formulation was found to be controlled release of drug over a period of 7 days.