Abstract

ADVANCEMENT OF QUASI-EMULSION SOLVENT DIFFUSION METHOD PROVIDES NOVEL PHYSICOCHEMICAL PROPERTIES: A POTENTIAL TECHNIQUE TO IMPROVE BIOAVAILABILITY AND EFFICIENCY OF TUMOUR INHIBITING MEBENDAZOLE DRUG

Dharmeshkumar M. Modi*, Akshat D. Modi, Rajesh H. Parikh and Jolly R. Parikh

ABSTRACT

Mebendazole (MBZ) is a broad-spectrum anthelmintic drug that has been used for many years to treat parasitic infections. It shows poor flowability due to its needle-like crystals and poorly soluble in water, limiting its bioavailability. In this study, an attempt was made to increase the flowability and solubility of Mebendazole by imparting the spherical shape and converting it into amorphous by novel quasi emulsion solvent diffusion method. A 33 full factorial design was used to see the effects of volume of good solvent, % v/v of bridging liquid in good solvent and volume of poor solvent. The resulting spherical agglomerates were characterized in terms of flowability, compressibility, % Mebendazole dissolved in 60 mins (C60). All batches showed improvements in flowability, compressibility and C60. All three of these variables were optimized to get Mebendazole with desired properties. The treated Mebendazole also showed an increase in particle size and uniformity index. The desirability function approach was used to select the best batch. FTIR study of the best batch showed no chemical changes in treated Mebendazole. The best batch was confirmed by SEM for sphericity and reduced crystallinity was demonstrated by XRD and DSC studies. This method can be used for drugs with properties like Mebendazole.

Keywords: Mebendazole; Spherical agglomerates; Uniformity index; Desirability function; Flowability; Compressibility; Dissolution.