PREPARATION AND CHARACTERIZATION OF SELF EMULSIFYING SOLID DISPERSIONS OF MEBENDAZOLE TO IMPROVE SOLUBILITY

Abstract

Background: In drug development process, poor aqueous solubility is one of the challenging factors. To design an oral dosage form, poor bioavailability is the major challenge. Objectives: The aim of this study was to improve the solubility of mebendazole (MBZ) by formulating solid dispersion (SDS) and self-emulsifying solid dispersions (SESDS). Mebendazole is an BCS class II drug having low solubility and can ultimately lead to poor absorption and low bioavailability. Methodology:  Physical mixture and kneading method were employed to enhance the solubility of MBZ and prepare SDS and SESDS using poloxamer-188 as the hydrophilic carrier. Soybean oil, sodium lauryl sulfate (SLS) and Transcutol-P were used as oil, surfactant, and cosurfactant, respectively. Eight formulations were designed to formulate SDS by varying the ratios of MBZ and Poloxamer-188 (1:1, 1:2, 1:3 and 1:4). All formulations were evaluated for solubility studies, and a formulation that showed maximum enhanced solubility was selected to prepare SESDS of mebendazole. All of the prepared formulations were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, and scanning electron microscopy to check chemical interactions, crystallinity, thermal stability, drug entrapment and morphological changes, respectively. Results: The results show that SDS and SESDS improved solubility compared to that of a pure drug. However, SESDS prepared using kneading methods showed the highest drug solubility (6.61 folds) as compared to pure drug. Conclusion: The study concluded that solubility of MBZ improved due to increased wettability, hydrophilicity of carrier and reduced crystallinity.