School of Chemical Sciences, Central University of Gujarat, Gandhinagar, 382030, India.
Sci Rep. 2021 Apr 15;11(1):8331. doi: 10.1038/s41598-021-86767-1.
Studies related to loading ability and delivery of clinically used first-line anti-tuberculosis drugs (ATDs) such as isoniazid, rifampicin, pyrazinamide and streptomycin on the surface of starch-derived bulk and nanopolyurethanes (SBPUs and SNPUs) as drug delivery systems (DDS) have been focused to minimise or remove the drug-associated adverse effects. The efficiencies of nanopolyurethanes obtained from the differently substituted cyclic aliphatic and aromatic isocyanates have been studied for drug loading and release purposes. Different advanced instrumental techniques analysed the structural and morphological properties, thermal stability and crystallinity of the starch nanopolyurethans. Average particle sizes ranging from 27.35-42.38 nm to 126.89-218.60 nm for starch nanopolyurethans, SNPU3i and SNPU4i, respectively, were determined by high-resolution transmission electron microscopy. Similarly, the loading efficiency of ATDs to the surfaces of SNPUs and SBPUs was observed in the range of 60-97% while ATDs-loaded SNPUs showed a sustainable release profile for all ATDs except for streptomycin. However, most SBPUs provided burst-release for all the above-mentioned ATDs in pH-dependent studies. The anti-tuberculosis assay against the Mycobacterium tuberculosis H37Rv strain revealed that streptomycin-loaded SNPU4i and isoniazid-loaded SNPU7i are approximately 42 and 7 times more active than the native streptomycin and isoniazid, respectively.
已将重点放在研究将异烟肼、利福平、吡嗪酰胺和链霉素等临床一线抗结核药物（ATDs）的负载能力和输送能力与淀粉衍生的块状和纳米聚氨基甲酸酯（SBPUs 和 SNPUs）作为药物输送系统（DDS）结合起来，以尽量减少或消除与药物相关的不良反应。为了药物负载和释放的目的，已经研究了不同取代的环状脂肪族和芳香族异氰酸酯制得的纳米聚氨基甲酸酯的效率。不同的先进仪器技术分析了淀粉纳米聚氨基甲酸酯的结构和形态特性、热稳定性和结晶度。通过高分辨率透射电子显微镜确定淀粉纳米聚氨基甲酸酯 SNPU3i 和 SNPU4i 的平均粒径分别为 27.35-42.38nm 和 126.89-218.60nm。同样，观察到 ATDs 对 SNPUs 和 SBPUs 表面的负载效率在 60-97%之间，而 ATDs 负载的 SNPUs 除了链霉素外，所有 ATDs 都显示出可持续的释放特性。然而，在 pH 依赖性研究中，大多数 SBPUs 为所有上述 ATDs 提供了突释释放。针对结核分枝杆菌 H37Rv 株的抗结核测定表明，负载链霉素的 SNPU4i 和负载异烟肼的 SNPU7i 的活性分别比天然链霉素和异烟肼高约 42 倍和 7 倍。
