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载一线抗结核药物的淀粉纳米晶用于抗击 H37Rv 结核分枝杆菌菌株的威胁。

First-line anti-tubercutilosis drugs-loaded starch nanocrystals for combating the threat of M. tuberculosis H37Rv strain.

机构信息

School of Chemical Sciences, Central University of Gujarat, Gandhinagar, 382030, India.

School of Chemical Sciences, Central University of Gujarat, Gandhinagar, 382030, India.

出版信息

Carbohydr Res. 2020 Sep;495:108070. doi: 10.1016/j.carres.2020.108070. Epub 2020 Jun 27.

Abstract

Nanoparticles-based drug delivery is at the forefront in the field of pharmaceutical and medicinal research to eradicate or alleviate the associated impediments, such as prolonged treatment time, high doses, toxicity and resistance problem of anti-tuberculosis drugs for the treatment of age-old tuberculosis disease. Herein, the first-line anti-tuberculosis drugs were loaded into the biodegradable starch nanocrystals and native starch to improve the therapeutic profile addressing the existing issues related to conventional drugs. The loading performance of anti-tuberculosis drugs with starch nanocrystals and native starch was found in the range of 65-95%. According to the release study, the native starch was not appropriate, however, the starch nanocrystals demonstrated sustained release drug delivery for isoniazid and pyrazinamide ranging from 50 to 93% for 24 h; the burst release for streptomycin was reported at pH 2 in 6.5 h while only 14% rifampicin was released at pH 8 buffer. An anti-mycobacterium analysis of strain H37Rv showed that minimum inhibition concentration of starch nanocrystals loaded with isoniazid and pyrazinamide (0.033 μg/mL and 1.25 μg/mL, respectively) were more effective than the parent isoniazid (0.2 μg/mL) and pyrazinamide (25.0 μg/mL) at pH 5.5.

摘要

基于纳米粒子的药物输送是药物和医学研究领域的前沿技术,旨在消除或减轻相关障碍,如延长治疗时间、高剂量、抗结核药物的毒性和耐药性问题,以治疗古老的结核病。在此,将一线抗结核药物载入可生物降解的淀粉纳米晶和天然淀粉中,以改善治疗效果,解决与传统药物相关的现有问题。研究发现,淀粉纳米晶和天然淀粉对抗结核药物的载药性能在 65-95%范围内。根据释放研究,天然淀粉并不合适,但淀粉纳米晶对异烟肼和吡嗪酰胺的药物释放表现出持续释放的特点,在 24 小时内释放 50-93%;链霉素在 pH 2 时在 6.5 小时内快速释放,而 rifampicin 仅在 pH 8 缓冲液中释放 14%。对 H37Rv 菌株的抗分枝杆菌分析表明,载有异烟肼和吡嗪酰胺的淀粉纳米晶的最低抑菌浓度(分别为 0.033μg/mL 和 1.25μg/mL)比原药异烟肼(0.2μg/mL)和吡嗪酰胺(25.0μg/mL)在 pH 5.5 时更有效。

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