Cefuroxime Axetil Loaded Dispersed Formulation for Enhanced Drug Release and Antibacterial Activity

Abstract:

Aim: Aqueous solubility of drugs is a determining factor for bioavailability in systemic circulation and confronts in the unbeaten formulation of therapeutic agents. Cefuroxime axetil (CA) is a broad-spectrum β-lactamase cephalosporin that pertains to class II drugs under Biopharmaceutical Classification System (BCS) with poor aqueous solubility and high absorption permeability after oral administration. The objective of this current work was to achieve the enhanced solubility in water and subsequent antibacterial activity of CA loaded coarse dispersion (CCD) formulations. Materials and Methods: CCDs were prepared by anti-solvent precipitation method by blending CA with a carrier, Microcrystalline cellulose (MCC) at different ratios. In-vitro dissolution test using paddle method and antibacterial study against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) were carried out for both pure CA and CCDs for performance comparison. Results: Among the formulations, CCD-3 exhibited maximized dissolution rate by 1.67-fold higher than that of pure CA with the drug-carrier (CA: MCC) ratio of 1:3. Antibacterial activity of CCD-3 against S. aureus and E. coli was also found by 1.75-fold and 5.25-fold higher relative zone of inhibition (RZOI), respectively than that of pure drug. Conclusion: As an optimized formulation, CCD-3 is a promising to be a fruitful substitute to conventional dosage forms of CA for the modified dissolution rate and antibacterial potency. However, before its recommendation as a novel formulation validation study to point its pharmacokinetics, competence with in-vivo antibacterial property and safety is needed.

Keywords: Cefroxime axetil, Coarse dispersion, Solubility, Dissolution, Antibacterial activity.