通过精氨酸多功能黏附性 SNEDDS(利福平 SNEDDS)抗击结核分枝杆菌。

IF 4.4 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Macromolecular bioscience Pub Date : 2024-09-25 DOI:10.1002/mabi.202400288
Sana Saeed, Muhammad Farooq, Rabia Arshad, Sherjeel Adnan, Hammad Ahmad, Zeeshan Masood, Abdul Malik, Ayesha Saeed, Tanveer A Tabish
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引用次数: 0

摘要

该研究旨在开发硫醇化聚钚基自乳化给药系统(SNEDDS),通过细胞内靶向给药增强药物载量、粘附性、粘液渗透性、位点特异性、针对细胞内结核分枝杆菌(M. tb)的稳定给药,减少细菌负担和产生。根据溶解能力和假三元图区域,选择油酸油、PEG 200 和吐温 80 作为油、助表面活性剂和表面活性剂。在含配体精氨酸的 SNEDDS 上涂覆硫醇化聚合物(Arg-Th-F407 SNEDDDS),可通过巨噬细胞的细胞内靶向作用减少细菌的负担和产生。通过扫描电子显微镜(SEM)、EDAX 分析、衍射激光散射(DLS)、傅立叶变换红外光谱(FTIR)和热分析(DSC 和 TGA)对配方进行了评估。硫醇化聚合物 SNEDDS(Th-F407 SNEDDS)和 Arg-Th-F407 SNEDDS 的流体力学直径分别为 148.4 纳米和 188.5 纳米,PDI 分别为 0.4 和 0.3。Arg-Th-F407 SNEDDS 的体外药物释放研究表明,在受控条件下,72 小时内 80% 的药物持续释放。与传统的利福平(RIF)相比,Arg-Th-F407 SNEDDDS 即使在低剂量下也能杀死巨噬细胞中的 M.tb 菌株,而且具有良好的生物相容性、无细胞毒性和血液相容性。因此,RIF 的 Arg-Th-F407 SNEDDDS 被证明是靶向治疗巨噬细胞内 M.tb 菌株的理想药物。
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Responding to Hitch in Fighting Mycobacterium Tuberculosis Through Arginine Multi Functionalized Mucoadhesive SNEDDS of Rifampicin.

The study aimed to develop thiolated pluronic-based self-emulsifying drug delivery system (SNEDDS) targeted delivery of Rifampicin coated by arginine for enhanced drug loading, mucoadhesion, muco penetration, site-specific delivery, stabilized delivery against intracellular mycobacterium tuberculosis (M. tb), decreased bacterial burden and production by intracellular targeting. Oleic oil, PEG 200 and Tween 80 are selected as oil, co-surfactant and surfactant based on solubilizing capacity and pseudo ternary diagram region. Coating of thiolated polymer on SNEDDS with ligand arginine (Arg-Th-F407 SNEDDDS) decreased bacterial burden and production by intracellular targeting in macrophages. Formulation are evaluated through scanning electron microscope (SEM), EDAX analysis, diffraction laser scattering (DLS), Fourier transform infrared (FTIR) spectroscopy, and thermal analysis (DSC & TGA). Hydrodynamic diameter of thiolated polymeric SNEDDS (Th-F407 SNEDDS) and Arg-Th-F407 SNEDDS is observed to be 148.4 and 188.5 nm with low PDI of 0.4 and 0.3, respectively. Invitro drug release study from Arg-Th-F407 SNEDDS indicates 80% sustained release in 72 h under controlled conditions. Arg-Th-F407 SNEDDDS shows excellent capability of killing M.tb strains in macrophages even at low dose as compared to traditional rifampicin (RIF) and is found biocompatible, non-cytotoxic, and hemocompatible. Therefore, Arg-Th-F407 SNEDDDS of RIF proved ideal for targeting and treating M.tb strains within macrophages.

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来源期刊
Macromolecular bioscience
Macromolecular bioscience 生物-材料科学:生物材料
CiteScore
7.90
自引率
2.20%
发文量
211
审稿时长
1.5 months
期刊介绍: Macromolecular Bioscience is a leading journal at the intersection of polymer and materials sciences with life science and medicine. With an Impact Factor of 2.895 (2018 Journal Impact Factor, Journal Citation Reports (Clarivate Analytics, 2019)), it is currently ranked among the top biomaterials and polymer journals. Macromolecular Bioscience offers an attractive mixture of high-quality Reviews, Feature Articles, Communications, and Full Papers. With average reviewing times below 30 days, publication times of 2.5 months and listing in all major indices, including Medline, Macromolecular Bioscience is the journal of choice for your best contributions at the intersection of polymer and life sciences.
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