Self-microemulsifying Drug Delivery System for Solubility and Bioavailability Enhancement of Eprosartan Mesylate: Preparation, In-vitro, and In-vivo Evaluation

Abstract

Background: Liquid self-micro emulsifying drug delivery system (SMEDDS) formulation of Eprosartanmesylate has been studied by applications of Surfactant like Kolliphor HS 15, Oil Phase like Labrafil M 1944 CS and cosurfactantTranscutol HP following screening by several vehicles. Objective: The aim is to prepare Liquid self microemulsifying drug delivery system for solubility enhancement of water insoluble drug Eprosartanmesylate. Method: The micro-emulsion unit, achieved through the phase diagram and augmented with the central- composite design (CCD) surface response process, was adjusted into SMEDDS by lyophilization using sucrose as a cryoprotective agent. Particle size, self-emulsification time, polydispersion index (PDI), zeta potential, differential scanning calorimeter (DSC) screening, in-vitro drug release, and in-vivo pharmacokinetics were the essential features of the formulations. The subsequent DSC experimentation indicated that the drug has been integrated into S-SMEDDS. EprosartanMesylateloaded SMEDDS formulation showed greater In-Vitro and In-Vivo drug release than conventional solid doses form. Results: SMEDDS has reported effectiveness in reducing the impact of EprosartanMesylate pH thereby improving its release efficiency. The HPLC method was successfully implemented to assess EprosartanMesylate concentration in Wister rat plasma after oral administration of commercial tablet EM, SMEDDS, and EprosartanMesylate. The pharmacokinetics parameters for rats were Cmax 1064.91 ± 225 and 1856.22 ± 749 ngmL-1, Tmax 1.9 ± 0.3 hr, and 1.2 ± 0.4 hr and AUC0~t were 5314.36 ± 322.61 and 7760.09 ± 249 ng/ml hr for marketed tablets and prepared S-SMEDDS, respectively. When determined by AUC0~1, the relative bioavailability of EprosartanMesylate S-SMEDDC was 152.09 ± 14.33%. Conclusion: Present study reports the formulation of self-microemulsifying drug delivery system for enhancing the solubility and bioavaibility of a poorly water soluble EprosartanMesylate in an appropriate solid dosage form.