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用于口服治疗结核分枝杆菌的套娃型胃耐微球。

Matryoshka-type gastro-resistant microparticles for the oral treatment of Mycobacterium tuberculosis.

机构信息

Department of Chemical Engineering. Aragon Institute of Nanoscience (INA), University of Zaragoza, Campus Río Ebro-Edificio I+D, C/Poeta Mariano Esquillor S/N, Zaragoza 50018, Spain.

Networking Research Center on Bioengineering, Biomaterials & Nanomedicine, CIBER-BBN, Madrid 28029, Spain.

出版信息

Nanomedicine (Lond). 2019 Mar;14(6):707-726. doi: 10.2217/nnm-2018-0258. Epub 2019 Feb 8.

Abstract

AIM

Production of Matryoshka-type gastroresistant microparticles containing antibiotic-loaded poly lactic-co-glycolic acid (PLGA) nanoparticles (NP) against Mycobacterium tuberculosis.

MATERIALS & METHODS: The emulsification and evaporation methods were followed for the synthesis of PLGA-NPs and methacrylic acid-ethyl acrylate-based coatings to protect rifampicin from degradation under simulated gastric conditions.

RESULTS & CONCLUSION: The inner antibiotic-loaded NPs here reported can be released under simulated intestinal conditions whereas their coating protects them from degradation under simulated gastric conditions. The encapsulation does not hinder the antituberculosis action of the encapsulated antibiotic rifampicin. A sustained antibiotic release could be obtained when using the drug-loaded encapsulated NPs. Compared with the administration of the free drug, a more effective elimination of M. tuberculosis was observed when applying the NPs against infected macrophages. The antibiotic-loaded PLGA-NPs were also able to cross an in vitro model of intestinal barrier.

摘要

目的

制备载药聚乳酸-共-羟基乙酸(PLGA)纳米粒的套娃型胃内抗酸型微粒,用于负载抗结核药物利福平。

材料与方法

采用乳化-蒸发法合成 PLGA 纳米粒,并采用甲基丙烯酸-丙烯酸乙酯共聚物进行包衣,以保护利福平在模拟胃液条件下不被降解。

结果与结论

所报道的载药纳米粒在模拟肠液条件下可以释放内部的抗生素,而其包衣可以保护它们在模拟胃液条件下不被降解。包封并不妨碍包封抗生素利福平的抗结核作用。当使用载药包封纳米粒时,可以获得持续的抗生素释放。与使用游离药物相比,当将纳米粒用于感染巨噬细胞时,能够更有效地清除结核分枝杆菌。载药 PLGA 纳米粒也能够穿过体外肠道屏障模型。

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