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

• 作者: Akito Hata Ashim Kumar Hiromu Kondo Md. Abdus Salam Md. Rafiqul Islam Khan Mir Imam Ibne Wahed Moushumi Tabassoom Salam Ranjan Kumar Barman
• 来源期刊: 药理与制药(英文)
• 学科: 化学
• 关键词: Cefuroxime Axetil DISPERSION SOLUBILITY Antibacterial Activity
• 年，卷（期）: 2020,（8）
• 页码范围: 159-173
• 页数: 15页
• 分类号: O64

摘要

This investigation was undertaken to enhance the solubility and consequent antibacterial activity of cefuroxime axetil (CA), a </span><i><span style="font-family:Verdana;">β</span></i><span style="font-family:Verdana;">-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 </span><i><span style="font-family:Verdana;">in-vitro</span></i><span style="font-family:Verdana;"> 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 </span><i><span style="font-family:Verdana;">Staphylococcus aureus</span></i><span style="font-family:Verdana;"> (ATCC 25923) and </span><i><span style="font-family:Verdana;">Escherichia coli</span></i><span style="font-family:Verdana;"> (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, </span><i><span style="font-family:Verdana;">in-vivo </span></i><span style="font-family:Verdana;">antibacterial efficacy and safety before recommending as a novel formulation