Formulation and Evaluation of Vesicular Systems for Enhanced Transdermal Drug Delivery

Abstract

Tropisetron is one of the 5-HT3 receptor antagonists, reported to be effective in the prophylaxis of acute chemotherapy-induced nausea and vomiting (CINV). Tropisetron as the hydrochloride salt (TRO) is available in the pharmaceutical market, under the trade name Navoban® produced by Novartis Pharmaceuticals Ltd, in the form of hard gelatin capsules containing drug dose equivalent to 5 mg of the base as well as ampoules (2 or 5 mL) containing doses equivalent respectively to 2 or 5 mg of the base. Due to first-pass metabolism in the liver, the absolute bioavailability of TRO is about 60%. However, it suffers from phenotypic variability in hepatic metabolism due to genetic polymorphism of the cytochrome P450 enzyme, thus generating population of either poor or extensive TRO metabolizers. Headache and constipation with abdominal pain are the main adverse effects associated with recurrent TRO administration.