Comparative Bioavailability of Cefuroxime Axetil from Tablets and Self-Microemulsifying Drug Delivery Systems in Rats

Abstract

Cefuroxime axetil has poor bioavailability due to low solubility. This can be surmounted by preparing the drug by self-microemulsifying drug delivery system (SMEDDS). In this study the bioavailability of cefuroxime axetil from SMEDDS and tablets was evaluated in Wistar rats. The optimized SMEDDS formulation was prepared using Labrasol®, Gelucire® 44/14 and Lutrol®E400. The formulation was evaluated for micro-emulsification properties and percent in-vitro dissolution. The HPLC method was developed and optimized to estimate the drug content in the plasma. The method was clearly separating the cefuroxime A and B polymorphs and LOD and LOQ values are satisfactory. Rats were randomized in to two groups - one group of animals were administered with SMEDDS and another with tablet formulation. At frequent intervals the blood samples were withdrawn and analysed for drug content. The pharmacokinetic parameters were calculated using PK Solve software. The calculated bioavailability and tmax from SMEDDS was 1687.06 μg/ mL.min and 50 min, respectively, whereas for tablet it was 1219.803 μg/mL.min and 62 minutes, respectively. The bioavailability of SMEDDS formulation was 1.5 times more than the marketed formulation, indicating a significant improvement in oral bioavailability. In conclusion, this study confirms that the SMEDDS formulation is a viable strategy for enhancing the oral bioavailability of cefuroxime axetil