Journal of Bioequivalence & Bioavailability

E-BABE-Formulation and evaluation of optimized microemulsion for improvement of oral bioavailability

6^th World Congress on Bioavailability & Bioequivalence: BA/BE Studies Summit

August 17-19, 2015 Chicago, USA

Mahendra Singh

Posters-Accepted Abstracts: J Bioequiv Availab

Abstract:

The main objective of the study was to develop a microemulsion (ME) formulation of felodipine for the treatment of hypertension.
The oil phase was selected on the basis of drug solubility whereas the surfactant and cosurfactant were screened on the basis of their
oil solubilizing capacity as well as their efficiency to form ME from pseudo-ternary phase diagrams. The optimized microemulsion
formulation consisting of (10mg/ml) felodipine, 15% (w/w) linolenic acid (ω-3 fatty acid) as oil phase, 45% (w/w) Smix (1:1, Tween
80 and isopropyl alcohol). Optimized MEs possessed droplet sizes about 235.0 nm and showed good stability against heating cooling
cycle, freeze thaw cycle and centrifugation test. Microemulsion improved the drug solubility up to 1400-fold than in water. In Fel-
ME, drug content, in vitro drug release at the end of 2 hours and ex-vivo permeation at the end of 6 hours were found 97.35±1.28%,
98.21± 3.14% and 76.81±3.42% respectively. TEM results revealed formation of globules. Cytotoxicity studies revealed limited
toxicity to macrophage-like cells that may allow the formulations to be considered as suitable carriers for Felodipine. The results
of the pharmacokinetic study showed about 2.2-fold increase in concentration of felodipine upon oral administration of Fel-ME
and sustained release profile when compared with pure drug suspension. By analysing the findings of the present investigations
based on drug content, thermodynamic stability study, ex-vivo permeability and pharmacokinetic profile evaluations indicated that
microemulsion consisting felodipine enhance the oral bioavailability of low water soluble felodipine.