用一步关联法将壳聚糖包被在脂质纳米颗粒上，以将利福平靶向肺泡巨噬细胞。
Lipid nanoparticles coated with chitosan using a one-step association method to target rifampicin to alveolar macrophages.
机构信息
LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal; Laboratório de tecnologia dos Medicamentos - LTM, Departamento de Ciências Farmacêuticas da Universidade Federal de Pernambuco- UFPE, Portugal.
LAQV, REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.
出版信息
Carbohydr Polym. 2021 Jan 15;252:116978. doi: 10.1016/j.carbpol.2020.116978. Epub 2020 Sep 24.
This work proposes the development and characterization of solid lipid nanoparticles (SLNs) loaded with rifampicin (RIF) aiming to enhance mucoadhesion of the SLNs and consequently internalization by the alveolar macrophages (AMs). The lipid nanoparticles (NPs) were characterized and the results showed that the NPs obtained present a spherical or a starry shape with diameter around 250-500 nm, a monodisperse population, with zeta potential between -31 mV for uncoated SLNs and +33 mV for coated SLNs. The drug EE was approximately 90 % and the loading capacity (LC) 4.5 %. The SLNs coated with chitosan by the association method (aC-SLNs) show an effective mucoadhesive profile, verified by the turdimetry and surface loading method, corroborated with the cellular assays. The presence of chitosan in the aC-SLNs promotes higher mucoadhesive properties to the NPs and permeability in A549, suggesting that the safe aC-SLNs-RIF can be used as a promising drug delivery system for improving tuberculosis treatment.
本工作提出了载有利福平（RIF）的固体脂质纳米粒（SLNs）的开发和表征，旨在增强 SLNs 的黏膜黏附性，进而被肺泡巨噬细胞（AMs）内化。对脂质纳米粒（NPs）进行了表征，结果表明，所得到的 NPs 呈球形或星形，直径约为 250-500nm，具有单分散性，未包覆的 SLNs 的 Zeta 电位在-31mV 左右，包覆的 SLNs 的 Zeta 电位在+33mV 左右。药物 EE 约为 90%，载药量（LC）为 4.5%。通过缔合法用壳聚糖包覆的 SLNs（aC-SLNs）显示出有效的黏膜黏附特性，通过旋转黏度计和表面负载法验证，并与细胞测定结果相符。壳聚糖存在于 aC-SLNs 中可提高 NPs 的黏膜黏附特性和 A549 的通透性，提示安全的 aC-SLNs-RIF 可用作改善结核病治疗的有前途的药物递送系统。
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