Preparation of the aperpitant-loaded self-nanoemulsion for intestinal permeability studies

Abstract

Aperpitant is an Nk1 inhibitor used in the prevention and treatment of chemotherapy-induced nausea and vomiting and is a class BCS II drug. This drug is almost insoluble in water and has low bioavailability.Aim: The aim of this study was to compare the intestinal permeability of aprepitant-loaded self-nanoemulsifying drug delivery system compared with the free drug. The self-nanoemulsifying drug delivery system is a lipid-based drug delivery system that consists of natural or synthetic oils, surfactant and co-solvent, and after oral administration upon contact with gastrointestinal fluids, the aforementioned formulation begins to emulsify spontaneously and form a micro or nanoemulsion. In addition to increasing drug solubility, self-nanoemulsifying drug delivery systems also increase the intestinal permeability of different types of drugs.Methods: In this study, self-nanoemulsifying drug delivery system was prepared by experimental design using oleic acid (oil), Tween 80 (surfactant) and transcutol P (co-solvent) as the formulation excipients. SPIP method was used to measure intestinal permeability. Intestinal perfusion method in small laboratory animals, especially rats, in a best way imitates absorption in the body in animals. Unlike the in-vitro methods, in this method, the absorption barriers on the way of the drug until it reaches the hepatic blood flow are the same as the conditions inside the body, which increases its reliability. In this method, after cannulation of rat intestinal jejunum, the drug entered the intestine at a constant speed and by comparing the corrected concentration of the output to the input concentration of the drug, the intestinal permeability (Peff) was calculated.Results: The intestinal permeability of free aprepitant and aprepitant-loaded self-nanoemulsifying drug delivery system were obtained as (74.46 ± 26.45)× 10 -4 and (175.71 ± 46.36) × 10 -4 cm/min, respectively. Conclusion: The intestinal permeability of aprepitant is significantly increased follow using the self-nanoemulsifying drug delivery system.