ABSTRACT

Curcumin is a major constituent of turmeric, a plant product used extensively in Ayurveda. Curcumin has poor bioavailability because of extensive systemic metabolism and poor oral absorption. In order to improve the bioavailability of Curcumin we developed small unilamellar vesicules (SUVs) encapsulating the active by thin film hydration followed by probe sonication method. SUV liposomal formulations selected can also lead to highest concentration in the liver cells because of phagocytosis and endocytosis of this formulation in these cells. Four formulations (CL1, CL2, CL3, CL4) were prepared by taking different drug to lipid ratio. The prepared formulations were evaluated for particles size, surface potential, entrapment efficiency, in vitro release, drug excipient compatibility. Particle size of all formulations was in the range of 110-240 nm and the entrapment efficiencies were in the range of 44-70 %. From the four formulations CL3 was selected as best formulation by considering the size, entrapment efficiency and release profiles. Pharmacokinetic parameters of the CL3 formulations were evaluated in rat. CL3 formulation was evaluated for hepatoprotective activity in CCl4 induced liver toxicity model and drug levels in different tissues were determined. Formulation CL3 showed better in vivo performance compared to curcumin iv and oral solutions. Tissue levels especially in liver were more with formulation CL3 was more compared to curcumin iv and oral solutions.