Development of darunavir proliposome powder for oral delivery by using box-bhenken design.

The aim of present study is to develop Darunavir pro-liposome powder for oral delivery. Darunavir-loaded oral pro-liposome powder (OPP) was prepared by a solvent evaporation technique with varying independent variables at three different levels. Based on different levels pro-liposome powder formulation was optimized by using Box-Behnken design. The formulations were analyzed for its size distribution, entrapment efficiency and surface morphology. Optimized pro-liposome batch A was evaluated for physical parameter, morphological parameters, entrapment efficiency, followed by in vitro, ex- vivo and in-vivo studies. Oral pro-liposome powder showed good micromeritic properties with angle of repose was less than 30°, Carr's index and Hausner's ratio were also less than 21 and 1.25, respectively. The mean size of the vesicles was in the range of 180 to 290 nm. The assay and entrapment efficiency of pro-liposome powder formulations were 79.00 ± 0.2% and 93.46 ± 0.2% respectively. In vitro release of Darunavir pro-liposome powder was 78.17 ± 0.1% after 24 hrs which shows good release from the vesicle of pro-liposome . Ex vivo permeation study shows 58.11% enhancement which shows good permeation. The optimize batch A of pro-liposome powder indicated 50% enhancement in the relative bioavailability as compared to the Darunavir suspension. The results showed that pro-liposome powder containing Darunavir can efficiently deliver in to the blood stream. This drug delivery system has been designed as a novel platform for potential oral delivery of drugs having poor water solubility and high first-pass metabolism.