Background and Aim: 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 cempedak (Arthocarpus integrifolia) seeds, was selected to induce cellular engulfment of nanoparticles within infected host cells.
Materials and Methods: 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.
Results and Discussion: 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.
Conclusion: 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.

Keywords: surface modification, Box–Behnken design, antibiotic, TLR2 agonists, botanical lectin, electrostatic binding


中文翻译：

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ArtinM 移植磷脂纳米颗粒用于增强抗生素细胞对细胞内感染的摄取

背景和目的：提出了一种以脂质纳米颗粒的表面修饰凝集素形式的抗菌递送，以改善细胞积累。ArtinM 是一种从cempedak ( Arthocarpus integrifolia)种子中分离出来的活性 toll 样受体 2 (TLR2) 激动剂凝集素，被选择用于诱导受感染宿主细胞内纳米颗粒的细胞吞噬。
材料和方法：在静电吸附artinM之前使用乳化技术制备脂质纳米颗粒。Box-Behnken 设计优化了由利福平、大豆磷脂和聚山梨醇酯 80 组成的配方，以产生所需的粒径、包封率和载药量。最佳配方的特征在于形态、体外释放和细胞转运。
结果与讨论：大豆磷脂在控制载药量和包封率方面表现出深远的影响。由于其表面活性，聚山梨醇酯 80 显着降低了粒径；然而，较高的脂质浓度比导致利福平包封减少。artinM 在纳米颗粒表面的吸附是通过在 pH 4 下的静电结合完成的，该过程保持了封装的利福平的稳定性。血凝试验、zeta 电位测量和透射电子显微镜成像显示，高比例的 artinM 吸附在纳米颗粒表面。共聚焦显微镜显示的细胞摄取显示成功地将尼罗红标记的纳米颗粒转运到成纤维细胞中。
结论：带有artinM的纳米颗粒的递送系统成为抗生素靶向治疗由细胞内感染引起的危及生命的慢性疾病的潜在平台技术。

关键词：表面修饰，Box-Behnken 设计，抗生素，TLR2 激动剂，植物凝集素，静电结合