Department of Pharmacology & Toxicology, College of Medicine, University of the Philippines, 3rd Floor Salcedo Bldg., 547 Pedro Gil St, Ermita, Manila, 1000, Philippines.
Department of Medicine, Philippine General Hospital, Taft Ave, Ermita, Manila, 1000, Philippines.
Ther Deliv. 2022 Aug;13(8):391-402. doi: 10.4155/tde-2022-0034. Epub 2022 Nov 21.
This study seeks to optimize niosomal formulations of azithromycin (AZ) and evaluate their activities against methicillin-resistant (MRSA). The thin-film hydration was used to prepare niosomes containing various molar ratios of span 60, cholesterol, dicetylphosphate and AZ. Formulation 5, with 5:1:1:1 molar ratio, was optimized based on entrapment efficiency. Solid state analyses and accelerated stability were carried out. The antibacterial properties against MRSA was determined by agar well diffusion method. Physico-chemical characterization of formulation 5 confirmed successful encapsulation of AZ with slightly improved stability at 30°C for 6 months. Niosomal AZ at 0.1% is as effective as vancomycin in inhibiting the growth of MRSA. The antibacterial activities of AZ against MRSA is enhanced when encapsulated within niosomes.
本研究旨在优化阿奇霉素(AZ)的脂质体配方,并评估其对耐甲氧西林金黄色葡萄球菌(MRSA)的活性。采用薄膜水化法制备含有不同摩尔比的司盘 60、胆固醇、双十六烷基磷酸酯和 AZ 的脂质体。基于包封效率,对摩尔比为 5:1:1:1 的配方 5 进行了优化。进行了固态分析和加速稳定性测试。通过琼脂孔扩散法测定了制剂 5 对 MRSA 的抗菌特性。制剂 5 的理化特性证实了 AZ 的成功包封,在 30°C 下稳定性略有提高,可稳定 6 个月。脂质体 AZ 浓度为 0.1%时,与万古霉素抑制 MRSA 生长的效果相当。将 AZ 包封在脂质体中可增强其对 MRSA 的抗菌活性。