Abstract

PREPARATION, CHARACTERIZATION AND EVALUATION OF HEPATOPROTECTIVE ACTIVITY OF AN INTRAVENOUS LIPOSOMAL FORMULATION OF BIS-DEMETHOXY CURCUMIN ANALOGUE (BDMCA)

The aim of study was to prepare small unilamellar vesicles (SUVs) incorporating BDMCA that can injected by intravenous route and further, evaluate hepatoprotective activity of the formulation. SUV liposomes were prepared using thin film hydration followed by sonication method. Soya lecithin was used as lipid and stearyl amine was used as cationic charge inducer. In the preparation of liposomes, process and formulation parameters were standardized. After preparation SUVs were characterized for physicochemical properties, particle size, zetapotential, percent drug entrapment, in vitro drug release and the drug-polymer interaction. The sustenance of drug release into the plasma after intravenous BDMCA SUV administration was determined. Hepatoprotective activity was evaluated in CCl4 treated rats. The liposomal formulations were successfully prepared using thin film hydration followed by sonication method. The desired encapsulation was achieved by increase in the area of the lipid film formed. The size of SUVs obtained was 327 nm. FTIR results indicate there was no interaction between lipid and drug. In vitro release data showed that the release was sustained for 10 days in vitro and could be described as diffusion-controlled. The liposomal formulations were able to sustain the release of drug in vivo also. Liposomal formulations showed better hepatoprotective activity to the drug compared to its solution form.


Author(s): JITHAN AUKUNURU, SREEKANTH JOGINAPALLY, NARESH GADDAM, MADHU BURRA, CHANDRASEKHAR R.BONEPALLY, PRABHAKAR K

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