Formulation and Evaluation of Solid-Self Nano Emulsifying Drug Delivery System of Darunavir

Abstract

The main aim of this research article is to Formulate and Evaluate the S-SNEDDS of Darunavir. Darunavir is an anti-retroviral protease inhibitor which is in use from long time, but it has poor bioavailability because of poor aqueous solubility and extensive first pass metabolism, when used in the form of conventional dosage form. As it is a BCS Class II drug, which shows low solubility and high permeability. The S-SNEDDS of Darunavir was prepared to improve its oral bioavailability and its release rate was evaluated by in vitro release. The solubility of Darunavir in various oils was to decide and identify the oil phase of formulations. Different oils, surfactants and co-surfactants were screened for their ability to emulsify the selected oil. The pseudo ternary phase diagram was used to know the self -emulsification region of formulation. The optimized S-SNEDDS formulation contain Darunavir (150mg), Caproyl®90(50mg), Labrasol® and Transcutol® mix (45 mg). The data of the FTIR confirms that there is no interaction observed and the drug and excipients was compatible with each other. The developed SNEDDS formulations were examined for nano emulsifying capabilities, and the resulting nano emulsions were investigated for self-emulsification efficiency, dispersibility and in-vitro dissolution. Centrifugation tests, particle size distribution, heating cooling cycle, zeta potential, and freeze thaw cycling were performed on the optimised formulations to establish the stability of the produced SNEDDS formulation. Further produced S-SNEDDS micromeritics studies were done. The formulation was shown to significantly improve drug release, with total drug release occurring within 60 minutes. Darunavir self-emulsifying formulation was thus effectively produced.