DESIGN, DEVELOPMENT AND FORMULATION OF ECONAZOLE NITRATE CO-CRYSTAL LOADED GEL TO CURE TOPICAL ANTIFUNGAL DISEASEAbstract
In the past years many drug discoveries were investigated to be poorly soluble in aqueous medium. These poorly aqueous soluble drugs include Econazole Nitrate (ECZN) having high permeability. ECZN is an effective, potent anti-fungal drug used to cure large range of fungus. Oral administration of ECZN causes gastrointestinal irritation. To overcome or avoid the “first pass metabolism” and to optimise the drug concentration at the infected site of action topical gel was formulated, topical gels have better tendency to convey the drug via skin as compared to ointment, because gels are non-greasy and comfortable for application. To improve the solubility of ECZN in aqueous medium, Co-crystal technique was established to be a boon to the pharmaceutical industry. Crystalline structure of co-crystals consists of ECZN and Co-former either amino-acid or carboxylic-acid in equimolar ratio and penetration-enhancer was used. Liquid based grinding method used for fabrication of co-crystals. Formulated Co-crystal was incorporated in Carbomer-934 based topical gel. Characteristic peak was determined by Fourier transform infrared spectroscopy, the large number of particle size was found in the scale of 600- 1000 nm. Endothermic point was determined by thermal analysis (Differential scanning calorimetry) and Powder x-ray diffraction; microscopy of co-crystal was obtained by scanning electron microscopy. The formulated optimized co-crystal gel showed good potential of hydrogen, Viscosity, Zone of inhibition, drug content. ECZN co-crystal showed good in-vitro dissolution. Selected formulation of ECZN co-crystal loaded topical gel showed good ex-vivo permeability on topical skin and antifungal activity against C. albicans.
Mohammad Wais, Priyanka S. Gala * and Anagha Raut
Department of Pharmaceutics, H. K. College of Pharmacy, Oshiwara, Jogeshwari [W], Mumbai, Maharashtra, India.
21 January 2023
05 October 2023
06 October 2023
01 November 2023