Department of Materials and Textile Engineering, College of Engineering, Razi University, Kermanshah, Iran.
Department of Chemical and Petrochemical Engineering, Sharif University of Technology, Tehran, Iran.
Int J Pharm. 2019 Oct 5;569:118580. doi: 10.1016/j.ijpharm.2019.118580. Epub 2019 Jul 30.
In this study, optimized cephalexin-loaded niosomal formulations based on span 60 and tween 60 were prepared as a promising drug carrier system. The niosomal formulations were characterized using a series of techniques such as scanning electron microscopy, Fourier transformed infrared spectroscopy, dynamic light scattering, and zeta potential measurement. The size and drug encapsulation efficiency are determined by the type and composition of surfactant. The developed niosomal formulations showed great storage stability up to 30 days with low change in size and drug entrapment during the storage, making them potential candidates for real applications. Moreover, the prepared niosomes showed negligible cytotoxicity for HepG2 cells, measured by MTT assay. The antibacterial properties of cephalexin-loaded niosome were investigated using S. aureus and E. coli as gram-positive and gram-negative bacteria, respectively. The results showed that the encapsulation of antibiotic drug in niosomal formulation could enhance the antibacterial efficiency of the drug, where the minimum inhibitory concentration was droped from 8 µg/mL (cephalexin) to 4 µg/mL (cephalexin-loaded niosome) and from 4 µg/mL (cephalexin) to 1 µg/mL (cephalexin-loaded niosome) against E. coli and S. aureus, respectively. The findings of our study show that the improvement of cephalexin bioavailability and prolonged drug release profile could be obtained by niosomal formulation as a favorable antibiotic drug delivery system.
在这项研究中,基于司盘 60 和吐温 60 制备了优化的头孢氨苄载药脂质体作为有前途的药物载体系统。采用扫描电子显微镜、傅里叶变换红外光谱、动态光散射和zeta 电位测量等一系列技术对脂质体进行了表征。载药脂质体的粒径和包封率取决于表面活性剂的类型和组成。研究表明,所开发的脂质体在 30 天的储存期内具有良好的储存稳定性,粒径和药物包封率的变化很小,使其成为实际应用的潜在候选物。此外,通过 MTT 测定法,制备的脂质体对 HepG2 细胞表现出可忽略不计的细胞毒性。采用金黄色葡萄球菌和大肠杆菌分别作为革兰氏阳性菌和革兰氏阴性菌,研究了载头孢氨苄脂质体的抗菌性能。结果表明,将抗生素药物包封在脂质体中可以提高药物的抗菌效率,最低抑菌浓度从 8μg/mL(头孢氨苄)降至 4μg/mL(载头孢氨苄脂质体)和 4μg/mL(头孢氨苄)降至 1μg/mL(载头孢氨苄脂质体)对大肠杆菌和金黄色葡萄球菌分别。本研究结果表明,通过脂质体作为有利的抗生素药物递送系统,可以提高头孢氨苄的生物利用度并延长药物释放曲线。