TITLE:
Accelerated Aqueous Solubility and Antibacterial Activity of Cefuroxime Axetil Using Microcrystalline Cellulose as Carrier
AUTHORS:
Moushumi Tabassoom Salam, Ashim Kumar, Akito Hata, Hiromu Kondo, Md. Abdus Salam, Mir Imam Ibne Wahed, Md. Rafiqul Islam Khan, Ranjan Kumar Barman
KEYWORDS:
Cefuroxime Axetil, Dispersion, Solubility, Antibacterial Activity
JOURNAL NAME:
Pharmacology & Pharmacy,
Vol.11 No.8,
August
12,
2020
ABSTRACT: 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