Novel Super Saturated Self- Emulsifying System for Oral Delivery of Griseofulvin Design, Preparation and ex-vivo Intestinal Permeability

Abstract

The Objective of the study was to prepare and design a stable formulation for self-emulsifying drug delivery system in order to enhance the solubility and oral absorption of a poorly-soluble drug, called griseofulvin. The prepared self-emulsifying systems were evaluated regarding their refractory index, particle size, emulsifying strength, drug release, and rat intestine permeability. The results showed that a mixture of oleic acid (as a fatty acid) with Labrafil-Tween 20 (as a surfactant), Labrafac PG (as a co-surfactant), and Poloxamer and hydroxypropyl methylcellulose (as a polymer) led to prepare stable emulsions with a refractive index higher than acidic medium and water. The particle size of the formulations was obtained between 310 to 834 nm. The particle size of samples was influenced by S/C ratios, so that the mean particle size decreases with an increasing in the S/C ratios. The percentage of drug release after 24 hours for formulations was 22.38 to 46.95. The correlation between the percentages of drug released after 24 hours with S/Oil and S/C ratios was significant. In Ex-vivo intestinal permeability, there was a significant and direct correlation between Q4 and surfactant/oil ratio. The selected formulations showed drug permeability through the rat intestine 3- folds more, compared with the control.