Accelerated Aqueous Solubility and Antibacterial Activity of Cefuroxime Axetil Using Microcrystalline Cellulose as Carrier

This investigation was undertaken to enhance the\r\nsolubility and consequent antibacterial activity of cefuroxime axetil (CA), a β-lactamase-stable broad spectrum second\r\ngeneration cephalosporin through solid dispersion (SD) technique. For this\r\npurpose, CA loaded SDs (CSDs) were prepared by solvent evaporation method using\r\ndifferent concentrations of microcrystalline cellulose (MCC) as carrier. The\r\nCSDs were characterized by in-vitro dissolution study, thermal analysis (DSC), crystallinity (PXRD), interactions\r\n(FTIR) and morphology (SEM). Among the formulations, CSD-2 showed the highest\r\ndissolution rate which was 2.59-fold higher than pure CA with a drug-carrier\r\n(CA: MCC) ratio of 1:3. Enhanced dissolution rate was attributed to conversion\r\nof drug from crystalline to amorphous state during preparation of SDs, which\r\nwas validated by DSC, PXRD, FTIR and SEM analyses. Antibacterial activity of\r\nCSD-2 against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) showed 1.94- and 6.75-fold higher relative zone of inhibition\r\n(RZOI), respectively than pure CA. CSD-2 has been found to be the most\r\neffective optimized formulation in terms of both enhanced dissolution rate and\r\nantibacterial activity. Thus, it can be an effective alternative to\r\nconventional dosage forms of CA. However, further investigations are needed to\r\nvalidate its pharmacokinetic properties, in-vivo antibacterial efficacy and safety before recommending as a novel formulation