Bioavailability study of Posaconazole in rats after oral Poloxamer P188 Nano-micelles and oral Posaconazole pure drug

Abstract

Posaconazole (POCZ) is a triazole antifungal with poor solubility and low bioavailability, so this work is aimed to compare between bioavailability parameters of pure POCZ and the prepared lyophilized POCZ nano-micelles. In this study, twelve Wistar rats were used with a weight of 200±20g and divided into twice groups (each group with six animals). The dose of 10mg/kg of pure POCZ and POCZ nano-micelles was administered to rats by oral gavage after reconstitution with water. The determination of POCZ in the plasma of rats is done by using (HPLC) after the construction of a spiked calibration curve with plasma and internal standard itraconazole. The bioavailability parameters for pure POCZ and POCZ nano-micelles were determined. The results show that C max , T max , AUC 0-72, and AUC 0-∞ were 230±4ng/ml, 8±0.5hr, 8622±127 ng.h/ml,10050±110 ng.h/ml and 2107±7ng, 2±0.2hr, 27261. 2±233ng.h/ml, 30364±205 respectively for pure POCZ suspension and POCZ nano-micelles. The obtained results from this work are that the time T max required for maximum concentration C max was statistically different from pure POCZ and POCZ nano-micelles ( p< 0.05). The POCZ nano-micelles show relative bioavailability 3.02 times than pure Posaconazole. In conclusion, the prepared POCZ nano-micelles enhance the oral absorption and bioavailability of the drug.