School of Pharmacy, Bandung Institute of Technology, Bandung, Indonesia.
Faculty of Pharmacy, Pancasila University, Jakarta, Indonesia.
Int J Nanomedicine. 2020 Nov 10;15:8829-8843. doi: 10.2147/IJN.S275449. eCollection 2020.
An antimicrobial delivery in the form of surface-modified lectin of lipid nanoparticles was proposed to improve cellular accumulation. ArtinM, an active toll-like receptor 2 (TLR2) agonist lectin isolated from ( seeds, was selected to induce cellular engulfment of nanoparticles within infected host cells.
Lipid nanoparticles were prepared using the emulsification technique before electrostatic adsorption of artinM. The formula comprising of rifampicin, soy phospholipid, and polysorbate 80 was optimized by Box-Behnken design to produce the desired particle size, entrapment efficiency, and drug loading. The optimum formula was characterized for morphology, in vitro release, and cellular transport.
Soy phospholipid showed a profound effect on controlling drug loading and entrapment efficiency. Owing to its surface activity, polysorbate 80 contributed significantly to reduce particle size; however, a higher ratio to lipid concentration resulted in a decrease of rifampicin encapsulation. The adsorption of artinM on the surface of nanoparticles was accomplished by electrostatic binding at pH 4, where this process maintained the stability of encapsulated rifampicin. A high proportion of artinM adsorbed on the surface of the nanoparticles shown by haemagglutination assay, zeta potential measurement, and transmission electron microscopy imaging. Cellular uptake revealed by confocal microscopy showed the success in transporting Nile-red labelled nanoparticles across fibroblast cells.
The delivery system of nanoparticles bearing artinM becomes a potential platform technology for antibiotic targeting in the treatment of life-threatening chronic diseases caused by intracellular infections.
提出了一种表面修饰的脂质纳米粒结合凝集素的抗菌药物递释系统，以提高细胞摄取。ArtinM 是一种从 （种子）中分离出的活性 Toll 样受体 2（TLR2）激动剂凝集素，可诱导受感染宿主细胞内的纳米颗粒被细胞吞噬。
采用乳化技术制备脂质纳米粒，然后静电吸附 ArtinM。采用 Box-Behnken 设计优化包含利福平、大豆磷脂和聚山梨酯 80 的配方，以获得所需的粒径、包封效率和载药量。对最佳配方进行形态学、体外释放和细胞转运研究。
大豆磷脂对控制载药量和包封效率有显著影响。由于其表面活性，聚山梨酯 80 显著降低了粒径；然而，当与脂质浓度的比值较高时，利福平的包封率会降低。在 pH 4 下，通过静电结合将 ArtinM 吸附在纳米粒表面，在此过程中保持了包封利福平的稳定性。通过血凝试验、Zeta 电位测量和透射电子显微镜成像显示，纳米粒表面吸附了大量的 ArtinM。共聚焦显微镜显示的细胞摄取表明，成功地将 Nile-red 标记的纳米粒转运穿过成纤维细胞。
载有 ArtinM 的纳米粒递释系统有望成为治疗由细胞内感染引起的危及生命的慢性疾病的抗生素靶向给药的平台技术。
