A Gelucire 44/14 and labrasol based solid self emulsifying drug delivery system: formulation and evaluation

Abstract

A solid self emulsifying formulation (S-SEF) has been developed with an intention to improve the dissolution characteristics of poorly water soluble lercanidipine hydrochloride (LH). Suitable components for the formulation of liquid self emulsifying drug delivery systems (SEDDS) were selected after screening various vehicles via solubility studies. Formulations were designed with Gelucire® 44/14 as oil, labrasol as surfactant and transcutol-P as co surfactant. The prepared formulations were evaluated for self emulsifying efficiency and ternary phase diagram was used to designate optimum systems in the emulsifying domain. These systems were further investigated for robustness towards different pH conditions, globule size, thermodynamic stability, surface morphology, cloud point and in vitro drug release. The optimized LH loaded formulation possessed a mean globule size of 142.5 ± 5.37 nm and cloud point of 72 ± 2.66 °C. The liquid SEDDS was transformed into free flowing S-SEF by adsorbing on to an inert carrier, Neusilin US2®. The results revealed no difference in globule size and emulsification characteristics between liquid SEDDS and S-SEF. The solid state characterization studies indicated loss of crystallinity for the drug. Significant improvement in dissolution characteristics of LH for prepared S-SEF was observed compared with pure drug.