Novel Approach for Enhancement of Oral Bioavailability of Bcs Class II Drugs

Abstract

Enzalutamide and Dabigatran Etexilate is BCS class II drugs and have low solubility and newlinewhich leading to low bioavailability. In present study, it was successfully formulated hard gelatin capsules of Enzalutamide and Dabigatran Etexilate with conventional process using two solubiliser i.e captex and labrasol in optimized ratio and desired dissolution can achieved. There were increases the dissolution with an increase in the ratio of solubilizer with combinations of Labrasol and captex. Developed compositions had improved dissolution rate which increase the bioavailability. The present invention also provides a solution comprising newlinepolymer and a surfactant comprising a mixture of fatty and sterol in a water miscible solvent, which upon dilution with an aqueous vehicle gives nanodispersion of Enzalutamide. The Present compositions of Dabigatran Etexilate shows higher dissolution rate with 15 minutes as compare to marketed formulations. Stability study indicated there was no such change in the formulation after 6 months. So, it indicates formulation is stable. In vitro dissolution studies revealed a significant improvement in the dissolution behavior of both innovative formulations. Following oral administration in rats, innovative compositions of both drugs provided a marked increase in bioavailability compared with that of the marketed capsules. In addition, in-vitro dissolution efficiency was well correlated to in-vivo pharmacokinetic parameters (Cmax, and AUC). Overall, the present investigation illustrated that both novel formulations providing promising formulation of BCS class II drugs with improved oral absorption and bioavailability.