DefinePK

Abstract

Background and Objective: The emergence of HIV/AIDS and its therapy has revolutionized antiretroviral therapy. Nevertheless, antiretroviral therapy in pediatric HIV infection still faces challenges. Pediatric antiretroviral therapy faces inaccurate dosing and thus reduced efficacy and/or safety. Materials and Methods: Therefore, in the present research, a nanoemulsion formulation of efavirenz was developed to overcome such issues. The nanoemulsion was prepared using a high-pressure homogenization technique using Box-Behnken experimental design with three factors namely surfactant level, homogenization cycle and pressure at three levels. Results: Electron microscopy results confirmed the globule size in the range of 30-40 nm. Non-everted gut sac method showed a 2.24 (p<0.05) fold increase in the drug permeability when compared to suspension in 2 hrs. Pharmacokinetic studies confirmed an assuring in vivo absorption pattern as compared to the suspension of efavirenz (p<0.05). In plasma, a 2.2-fold increment in the value of AUC0→∞ was found for nanoemulsion when compared with aqueous suspension. Conclusion: The results confirmed that this formulation of efavirenz can serve as an effective dose adjustable formulation with improved bioavailability for HIV therapy especially in pediatric population.