Banerjee Kacoli, Banerjee Shubhadeep, Das Subhayan, Mandal Mahitosh
School of Medical Science and Technology, Indian Institute of Technology, Kharagpur 721302, India.
School of Medical Science and Technology, Indian Institute of Technology, Kharagpur 721302, India.
J Colloid Interface Sci. 2015 Sep 1;453:48-59. doi: 10.1016/j.jcis.2015.04.030. Epub 2015 May 2.
Along with discovery of new antibacterial agents, it is important to develop novel drug delivery systems to effectively deliver drugs within bacterial cells for enhanced therapeutic activity. Liposomes have been extensively investigated as pharmaceutical carriers for improvement of therapeutic index of antimicrobial agents. The aim of this present study was to evaluate the antibacterial activity of free and liposomal formulation of apigenin, a plant based isoflavone and elucidate the mode of action. Distearoylphosphatidylcholine liposomes were prepared having nano-range particle size (104.3±1.8 nm), narrow particle distribution (0.204) and high encapsulation efficiency of apigenin (89.9±2.31%). Antibacterial activity of apigenin and efficacy of liposome-mediated apigenin delivery were determined from minimum inhibitory concentration values. Interaction studies using electron microscopy revealed adherence and fusion of liposomal apigenin with the bacteria causing membrane perturbation through reactive oxygen species generation which was evaluated by epi-fluorescence microscopy and fluorescence activated cell sorting. The interaction of apigenin liposomes with bacterial membrane increased intracellular drug concentration and thus, can be employed to deliver apigenin within cells to augment its antibacterial activity. Increased efficacy and hemocompatibility of this formulation paves way for future evaluation of underlying molecular mechanisms and in vivo testing for enhanced therapeutic effects.
随着新型抗菌剂的发现，开发新型药物递送系统以有效地将药物递送至细菌细胞内以增强治疗活性非常重要。脂质体作为改善抗菌剂治疗指数的药物载体已得到广泛研究。本研究的目的是评估芹菜素（一种基于植物的异黄酮）的游离制剂和脂质体制剂的抗菌活性，并阐明其作用方式。制备了具有纳米级粒径（104.3±1.8 nm）、窄粒径分布（0.204）和高芹菜素包封率（89.9±2.31%）的二硬脂酰磷脂酰胆碱脂质体。根据最低抑菌浓度值确定芹菜素的抗菌活性和脂质体介导的芹菜素递送效果。使用电子显微镜进行的相互作用研究表明，脂质体芹菜素与细菌发生粘附和融合，通过活性氧生成导致膜扰动，这通过落射荧光显微镜和荧光激活细胞分选进行评估。芹菜素脂质体与细菌膜的相互作用增加了细胞内药物浓度，因此可用于将芹菜素递送至细胞内以增强其抗菌活性。该制剂提高的疗效和血液相容性为未来评估潜在分子机制和进行体内测试以增强治疗效果铺平了道路。
