Formulation and Evaluation of Self-Emulsifying Drug Delivery System Of Methotrexate

ABSTRACT

The objective of this study was to prepare the self-emulsifying drug delivery system of methotrexate for oral use. Preparation composed of soybean oil as oil phase, Span 80 as surfactants, isopropyl alcohol as co-surfactant, 0.1 N NaOH as the aqueous phase. Methotrexate is given orally in treatment of cancer and rheumatoid arthritis. The Anti-neoplastic drug MTX is having less aqueous solubility (50-60 %) and bioavailability of 60-70 %. Hence the present study is aimed to formulate and evaluate solid self-nano emulsifying drug delivery system with the aim of increasing the solubility and bioavailability which will decrease the dosing frequency in turn increase patient compliance. Liquid SNEDDS was prepared by adding drug to oil, surfactant and co-surfactant and heated up to at 60 ºC under continuous stirring until a clear solution is formed. All the formulations were optimized to get the best solubility results for MTX. Solid SNEDDS was prepared by mixing liquid SNEDDS with MCC in 1:1 proportion. The formulations were evaluated for angle of repose, bulk density, zeta potential, IR spectroscopy, in vitro dissolution, average particle size, size distribution and stability studies. The average particle size of the liquid SNEDDS was 60.4 nm and solid SNEDDS was 60.4nm. The surface charge was confirmed by the measurement of the zeta potential for the liquid SNEDDS and it was found to be -22.4 mV and that of the solid SNEDDS was -22.4 mV. The PDI value remained approximately around 0.565 indicated that all the nano particles were uniformly dispersed in the emulsion.

Keywords: Methotrexate, soyabean oil, span 80, solid self nano emulsifying drug delivery system, Antineoplastic, Pseudoternary phase