Enhancement of Bioavailability of Poorly Water Soluble Drug through Liposomal Formulations

Abstract

Hypertension is an important risk factor for the future development of cardiovascular newlinedisease. Telmisartan is an anti-hypertensive drug from BCS class II category which is newlinepoorly water soluble. Hence, solubility is a rate-limiting step for the improvement of newlinebioavailability. Currently, this drug is only present in tablet dosage for the oral route, newlinehaving side effects of poor bioavailability, high first-pass metabolism, poor drug newlinetargeting, therapeutic drug level in the blood. The objective of the present research newlinework was to fabricate, develop and characterize a liposomal formulation of poorly water-soluble drug to enhance the bioavailability. Preliminary Screening of lipids was carried out for liposome development. From the Result it was found that Batch S7 shows highest %EE (80.14±0.02) and Lowest Particle Size (315.6 nm±0.10) newlinecontaining Phospholipon 90H and (1:3) Drug: Lipid Ratio. Hence, Phospholipon 90H, newlineand Drug: Lipid Ratio (1:3) was selected for further liposome formulation development. The effect of different variable on liposome formulation was study using Taguchi L8 standard orthogonal array design. Selected Independent variables studied were the amount of Lipid, amount of Cholesterol, sonication time, Speed of rota evaporator, Hydration volume, Hydration time and temperature. Pareto chart plotted factors against standardize effect shows the pareto chart of the particle size and entrapment efficiency. From the pareto chart it was concluded that Amount of Cholesterol, Amount of Lipid and Sonication time were selected for the further newlineoptimization of Liposomes by BBD Design. Optimized batch was evaluated for particle size and entrapment efficiency. Optimized the Liposomes selected three independent variables were Amount of Lipid, Amount of Cholesterol and Sonication time and dependent variables were particle size and entrapment Efficiency. Preliposomes of telmisartan were prepared by slurry method using rota evaporator.