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

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