Development and In vivo Evaluation of Pitavastatin Self-emulsifying Drug Delivery Systems

Abstract

The current research was intended at formulation and in vivo evaluation of pitavastatin self-nano emulsifying drug delivery system (PTN SNEDDS) for enhanced drug dissolution and bioavailability. Solubility studies carried out to construct pseudoternary phase diagram employing the blends of oil (capmulPG8), surfactant (acrysol K140), and cosurfactant (transcutol P). The PNT SNEDDS was prepared and optimized by adopting response surface methodology employing a 33 Box-Behnken design. The SNEDDS formulations characterized for % drug content, % entrapment efficiency, in-vitro release studies, particle size, zeta potential, Fourier Transform Infrared Spectroscopy (FTIR), and scanning electron microscopy (SEM) studies. The bioavailability studies were carried out in Wistar rats. The study indicated that PTN12 comprising of 40% capmul PG8, 40% acrysol K140, and 30% transcutol P displayed minimum droplet size (24.8nm), optimal zeta potential (-10.4 mV), and maximum drug release (98.75%). The SEM data revealed that droplet size is in the nanometer range. The pharmacokinetic studies conducted in rats indicated that Cmax of optimized PTN SNEDDS (2.25±0.02ng/mL) was higher than pure PTN suspension (0.75±0.03ng/mL) and optimized SNEDDS exhibited superior oral bioavailability about 4 times of AUC, along with higher plasma concentration than pure drug. The above results indicated that the application of SNEDDS formulation technique for PTN increases solubility and dissolution