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首页> 外文期刊>Molecular pharmaceutics >Cysteine-Functionalized Nanostructured Lipid Carriers for Oral Delivery of Docetaxel: A Permeability and Pharmacokinetic Study
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Cysteine-Functionalized Nanostructured Lipid Carriers for Oral Delivery of Docetaxel: A Permeability and Pharmacokinetic Study

机译：半胱氨酸功能化的纳米结构脂质载体口服多西他赛：渗透性和药代动力学研究。

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Here we report the development and evaluation of cysteine-modified nanostructured lipid carriers (NLCs) for oral delivery of docetaxel (DTX). The NLCs ensure high encapsulation efficiency of docetaxel, while the cysteine bound the NLCs with PEG(2000)-monostearate (PEG(2000)-MSA) as a linker, and allowed a specific interaction with mucin of the intestinal mucus layer and facilitated the intestinal transport of docetaxel. The cysteine-modified NLCs (cNLCs) had a small particle size (<100 nm) and a negative zeta potential (-13.72 +/- 0.07 mV), which was lower than that of the unmodified NLCs (uNLCs) (-6.39 +/- 0.07 mV). This correlates well with the location of the cysteine group on the surface of the NLCs obtained by X-ray photoelectron spectroscopy (XPS). The cNLCs significantly improved the mucoadhesion properties compared with uNLCs. The intestinal absorption of cNLCs in total intestinal segments was greatly improved in comparison with uNLCs and docetaxel solution (DTX-Sol), and the in vivo imaging system captured pictures also showed not only increased intestinal absorption but also improved accumulation in blood. The cNLCs could be absorbed into the enterocytes via both endocytosis and passive transport. The results of the in vivo pharmacokinetic study indicated that the AUC(0-t) of cNLCs (1533.00 ng/mL.h) was markedly increased 12.3-fold, and 1.64-fold compared with docetaxel solution and uNLCs, respectively. Overall, the cysteine modification makes nanostructured lipid carriers more suitable as nanocarriers for oral delivery of docetaxel.
机译：在这里，我们报告口服多西他赛（DTX）的半胱氨酸修饰的纳米结构脂质载体（NLCs）的发展和评估。 NLC确保多西紫杉醇的高包封效率，而半胱氨酸以PEG（2000）-单硬脂酸酯（PEG（2000）-MSA）作为接头将NLC结合，并允许与肠粘液层粘蛋白的特异性相互作用并促进肠道多西他赛的运输。半胱氨酸修饰的NLC（cNLC）具有较小的粒径（<100 nm）和负ζ电势（-13.72 +/- 0.07 mV），低于未修饰的NLC（uNLC）（-6.39 + / -0.07 mV）。这与通过X射线光电子能谱（XPS）获得的NLC表面上半胱氨酸基团的位置密切相关。与uNLC相比，cNLC显着改善了粘膜粘附特性​​。与uNLC和多西他赛溶液（DTX-Sol）相比，cNLC在整个肠段中的肠道吸收得到了极大的改善，并且体内成像系统所拍摄的图像还显示出不仅肠道吸收增加，而且血液中的蓄积也得到了改善。 cNLCs可以通过内吞作用和被动转运途径吸收到肠细胞中。体内药代动力学研究的结果表明，与多西他赛溶液和uNLC相比，cNLC的AUC（0-t）（1533.00 ng / mL.h）分别显着增加了12.3倍和1.64倍。总体而言，半胱氨酸修饰使得纳米结构脂质载体更适合作为多西他赛口服给药的纳米载体。

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