pH-responsive prodrug nanoparticles based on xylan-curcumin conjugate for the efficient delivery of curcumin in cancer therapy
pH-responsive prodrug nanoparticles based on xylan-curcumin conjugate for the efficient delivery of curcumin in cancer therapy
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DOI：
10.1016/j.carbpol.2018.02.006
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发表时间：
2018-05-15
影响因子：
11.2
通讯作者：
Negi, Yuvraj Singh
中科院分区：
文献类型：
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作者：
Sauraj;Kumar, S. Uday;Negi, Yuvraj Singh
为了提高姜黄素在癌症治疗中的疗效，本研究开发了一种基于木聚糖-姜黄素（xyl-cur）偶联物的新型ph响应前药纳米颗粒。通过红外光谱（FT-IR）、核磁共振光谱（H-1 NMR）、紫外可见光谱（UV-vis）和荧光光谱（fluorescence spectroscopy）等方法证实了羟基-cur缀合物（前药）的合成。在平均粒径为253 nm， zeta电位为-18.76 mV的水介质中，将羟基-cur前体药物自组装成纳米颗粒（羟基-cur前体药物NPs）。羟基乙酸前药NPs对ph高度敏感，大部分药物在较低ph下释放。通过溶血实验检测了羟基乙酸前药NPs与血液成分的相互作用。羟基-苯酚前药NPs对人结肠癌细胞（HT-29, HCT-15）的细胞毒活性表明，前药NPs比姜黄素具有更强的细胞毒作用。因此，这些结果表明，在癌症治疗中，yl-cur前药NPs可能是改善姜黄素细胞内递送的有希望的候选者。
In the present study, novel pH-responsive prodrug nanoparticles based on xylan-curcumin (xyl-cur) conjugate were developed to enhance the therapeutic efficacy of curcumin in cancer therapy. The synthesis of xyl-cur conjugate (prodrug) was confirmed by FT-IR, H-1 NMR, UV-vis and fluorescence spectroscopy. The xyl-cur prodrug was subsequently self-assembled in to nanoparticles (xyl-cur prodrug NPs) in an aqueous medium with the average particle size 253 nm and the zeta potential of -18.76 mV. The xyl-cur prodrug NPs were highly pH-sensitive in nature and most of the drug was released at lower pH. The interaction of the xyl-cur prodrug NPs with blood components was tested by hemolysis study. The cytotoxic activity of the xyl-cur prodrug NPs against human colon cancer cells (HT-29, HCT-15) demonstrated that the prodrug NPs exhibits greater cytotoxic effect than curcumin. Therefore, these results reveal that xyl-cur prodrug NPs could be a promising candidate for improving the intracellular delivery of curcumin in cancer therapy.