DEVELOPMENT AND CHARACTERIZATION OF A SELF-EMULSIFYING DRUG DELIVERY SYSTEM (SMEDDS) OF RILPIVIRINE HCL

Abstract

The present study was aimed towards to formulate and characterize self-emulsifying drug delivery system containing Rilpivirine HCl (RIL). Exhaustive Solubility study of the model drug, RIL was performed in different edible and GRAS listed oils to select oil component. Similarly, a supportive mixture of surfactants and Co-surfactants (Smix) of was selected. Pseudo-ternary diagram was plotted to judge micro emulsification existence area. The d-optimal design was employed to optimize SMEDDS composition using the amount of oil, surfactant, and Co-surfactant as independent variables and globule size and emulsification time as dependent variables. Developed SMEDDS formulations tested for self-micro emulsifying properties and the resultant formulation loaded with RIL measured for clarity, phase separation, % transmittance, globule size, and zeta potential. TEM study was performed to check the morphology of developed microemulsion globules. In vitro drug release study was undertaken and comparison was done with market formulation (Edurant®). Out of different trials, Capryol (Oil), Labrasol (Surfactant) and Transcutol-P (Co surfactant) were selected SMEDDS components. Highest microemulsion region was found in 1:1 Smix ratio. Significant impact of selected independent variables was found on responses, which was confirmed by regression equations (Y1 and Y2) and contour plots (2D). Significant improvement in the dissolution of RIL was observed by SMEDDS as compared to pure drug and marketed formulation. Short term stability study revealed stable characteristics of developed SMEDDS.