Design and Development of Solid Self-Microemulsifying Drug Delivery of Gefitinib

Solid self-microemulsifying drug delivery system (SMEDDS) of Gefitinib was aimed at overcoming the problems of poor solubility and bioavailability.

The formulation strategy included selection of oil phase based on saturated solubility studies and surfactant and co-surfactant screening on the basis of their emulsification ability. Ternary phase diagrams were constructed to identify the self-emulsifying region using a dilution method. The prepared formulations of SMEDDS were evaluated for their drug content, loading efficiency, morphology, globule size determination.

The formulation containing gefitinib (25 mg), oleic acid (20% w/w), tween 80 (30% w/w), propylene glycol (10% w/w) and water (40% w/w) was concluded to be optimized. The optimized SMEDDS and solid-SMEDDS exhibited 84.4% in vitro drug release up to 60 min, which was significantly higher than that of the pure drug. Solid-SMEDDS may be considered as a better solid dosage form as solidified formulations are more ideal than liquid ones in terms of its stability.

These results suggest the potential use of SMEDDS and solid-SMEDDS to improve the dissolution and hence oral bioavailability of poorly water-soluble drugs like Gefitinib through oral route.