IEEE Trans Nanobioscience. 2017 Dec;16(8):764-772. doi: 10.1109/TNB.2017.2757958. Epub 2017 Sep 29.
Self-assembled nanoformulations have been finding various applications in biomedical sciences. Here, we have designed and synthesized a small molecule-based amphiphilic conjugate of azobenzene, Azo-PEG-OMe, which self-assembles into nanostructures in an aqueous environment. The formation of nanostructures was evidenced by light scattering and electron microscopic analyses, which revealed the size of the so formed nanostructures ~199 and ~42 nm, respectively. Responsiveness of these nanostructures to various stimuli was demonstrated by enzyme and UV-Vis light exposure, pH and chemical reductant, sodium dithionite. Morphological alterations in the nanostructures on exposure to these stimuli were recorded and subsequently, these nanostructures were demonstrated as efficient carrier of drugs by entrapping an antiprotozoan drug, ornidazole, with ~82% entrapment efficiency. Under influence of different stimuli (light, pH, and enzyme), the drug release behavior displayed good response to each stimulus implying that the projected nanostructures could be used as efficient drug delivery system. Response to azoreductase enzyme further established that the formulation can be used for site specific drug delivery particularly useful for colonic drug delivery.
自组装纳米制剂在生物医学科学中有着广泛的应用。在这里,我们设计并合成了一种基于偶氮苯的两亲性小分子缀合物 Azo-PEG-OMe,它在水相环境中自组装成纳米结构。光散射和电子显微镜分析证明了纳米结构的形成,结果表明所形成的纳米结构的尺寸分别约为 199nm 和 42nm。通过酶和紫外光照射、pH 值和化学还原剂(连二亚硫酸钠)对这些纳米结构的响应性进行了证明。记录了这些纳米结构在暴露于这些刺激时的形态变化,随后通过包封抗原生动物药物奥硝唑(~82%的包封效率)证明了这些纳米结构是有效的药物载体。在不同刺激(光、pH 值和酶)的影响下,药物释放行为对每种刺激都有很好的响应,这意味着所提出的纳米结构可用于高效药物传递系统。对偶氮还原酶的响应进一步证实,该制剂可用于特定部位的药物输送,特别是对结肠药物输送有用。