Description

ABSTRACT

In this study, the emphasis is placed on a strategy for enhancing the drug/carrier interaction for improved drug solubility, drug-loading capacity, self-emulsification and stability.Preliminary solubility of L294 was determined in various oils, surfactants and cosurfactants. A ternary phase diagram was constructed to identify the self-emulsifying region for the selected systems, using series concentrations of Labrafac PG, Labrasol and Transcutol HP. Self-emulsifying properties, particle size, polydispersibility, and zeta potential were studied after dilution of formulations in water.The results demonstrated the development of a self-emulsifying formulation of L294 in liquid form, which upon contact with aqueous media spontaneously forms a clear nanoemulsion having a small droplet size (around 100 nm). The zeta potential of the selected SEDDS formulation was between −11.09 and −20.50 with a viscosity around 40-60 cP. The optimum formulation consisted of a mixture of Labrafac PG, Labrasol and Transcutol HP.The L294 showed extremely low water solubility (0,006 mg.mL^-1), and when formulated in SEDDS, its solubility increased over than 33,000 fold.This study demonstrate that SEDDS can be considered as a very good candidate to optimize the peroral administration of L294.

Keywords: SEDDS, Emulsion Drug Delivery, L294, Oral Dosage Forms, Cardioactive.