Preparation of Vorapaxar loaded with Vitamin E TPGS and PVA emulsified PLGA nanoparticles In vitro studies

Vitamin E TPGS has been approved by FDA as a safe adjuvant and commonly utilized in drug delivery systems. It has many advantages for its medical employment in drug delivery like high biocompatibility, improvement of drug permeation enhancement of drug solubility and selective. Methods: Vorapaxar-loaded PLGA nanoparticles were prepared by a step nanoprecipitation technique. In vitro drug encapsulation, efficiency (EE) and relative drug loading (DL) of nanoparticles were examined by UV-Vis spectrophotometry. Our study evaluated the effect of the organic phase with different concentrations and different forms of the aqueous phase on particle size and Encapsulation Efficiency (E E), Polydispersity index and (PDI). Loading efficiency (LD). Our data showed that acetone alone as well as mixed with dimethyl sulfoxide (DMSO) and 0.03% TPGS results particle sizes with small diameters as well as with suitable ID and EE reach to 110nm, 9.89 %, and 95.9% respectively. On the other hand particles sizes were recorded to increase in diameter after using some organic compounds as well as a high concentration of TPGS (0.1, 0.3%), in organic phase dichloromethane (DCM) alone or mixed with chloroform or DMSO. PVA 1% in concentration showed an increase in particle size in the organic phase of the solvent used even through acetone lowerd EE to 83.3 and LD to 9.05. Actually, our result with FTIR showed the disappearance of (OH) group in PLGA at (3515) region that indicating the potent conjugation between PLGA and vitamin E -TPGSV as well as the formation of a hydrogen bond between Vorapaxar and PLGA. The hemato-compatibility of Vorapaxar-NPs in multi concentration ranges (0.022- 0.44mg/ml) showed modest hemolytic activity in the formulations. In vitro antioxidant activity of Vorapaxar when compared with ascorbic acid. Conclusion: TPGS at (0.03%) when used with an organic phase acetone or/ and DMSO lead optimal nanosizes as well as perfect stability accompanied by has antioxidant activity and negligable haemolysis activity on rats blood cells, that permit to candidate as new drug for atherosclerosis Patient in future.