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两亲性萘普生-聚乙二醇核壳纳米组装体的合成、表征及作为药物传递系统的评价。

Core/shell nanoassembly of amphiphilic naproxen-polyethylene glycol: synthesis, characterisation and evaluation as drug delivery system.

机构信息

Nucleic Acids Research Laboratory, CSIR-Institute of Genomics and Integrative Biology, Mall Road, Delhi 110007, India.

出版信息

IET Nanobiotechnol. 2018 Sep;12(6):814-821. doi: 10.1049/iet-nbt.2017.0219.

Abstract

Small molecule-based amphiphiles self-assemble into nanostructures (micelles) in aqueous medium which are currently being explored as novel drug delivery systems. Here, naproxen-polyethylene glycol (N-PEG), a small molecule-derived amphiphile, has been synthesised, characterised and evaluated as hydrophobic drug carrier. H, C Nuclear magnetic resonance (NMR), mass spectrometry (MS) and Fourier-transform infrared spectroscopy (FTIR) confirmed the formation of N-PEG and dynamic light scattering (DLS) revealed the formation of nano-sized structures of ∼228 nm. Transmission electron microscope (TEM) analysis showed aggregation behaviour of the structures with average size of ∼230 nm. Biodegradability aspect of the micellar-structured N-PEG was demonstrated by lipase-mediated degradation studies using DLS and TEM. High encapsulation efficiency followed by release in a sustained manner of a well-known anticancer drug, doxorubicin, demonstrated the feasibility of the new drug delivery system. These results advocate the promising potential of N-PEG micelles as efficient drug delivery system for specific delivery to cancerous cells in vitro and in vivo.

摘要

基于小分子的两亲分子在水介质中自组装成纳米结构(胶束),目前正被探索作为新型药物传递系统。在这里,合成了一种小分子衍生的两亲分子萘普生-聚乙二醇(N-PEG),并对其进行了表征和评估,作为疏水性药物载体。氢、碳核磁共振(NMR)、质谱(MS)和傅里叶变换红外光谱(FTIR)证实了 N-PEG 的形成,动态光散射(DLS)显示形成了约 228nm 的纳米级结构。透射电子显微镜(TEM)分析显示结构具有约 230nm 的平均尺寸的聚集行为。通过使用 DLS 和 TEM 的脂肪酶介导的降解研究,证明了胶束结构的 N-PEG 具有生物降解性。高包封效率以及以持续方式释放一种众所周知的抗癌药物阿霉素,证明了这种新药物传递系统的可行性。这些结果表明,N-PEG 胶束作为一种有效的药物传递系统,具有向体外和体内癌细胞进行特异性传递的巨大潜力。

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