Department of Polymer and Process Engineering, Indian Institute of Technology Roorkee, Roorkee, Uttarakha nd-247667, India.
Nano-biotechnology Laboratory, Centre for Nanotechnology, Indian Institute of Technology Roorkee, Roorkee, Uttarakha nd-247667, India.
Int J Biol Macromol. 2019 May 1;128:204-213. doi: 10.1016/j.ijbiomac.2019.01.101. Epub 2019 Jan 23.
In this study, self-assembled nanoparticles based on amphiphilic xylan-stearic acid (Xyl-SA) conjugates have been developed for the efficient delivery of 5-fluorouracil (5-FU) in cancer therapy. The self-assembled behavior of Xyl-SA conjugates in aqueous medium was investigated using pyrene as fluorescent probe. To enhance the loading efficacy of 5-FU, the lipophilic 5-fluorouracil-stearic acid (5-FUSA) prodrug was synthesized and subsequently encapsulated into the hydrophobic core of Xyl-SA NPs. The obtained Xyl-SA/5-FUSA NPs had an appropriate size (278 nm), high drug loading of 5-FUSA (14.6 wt%) and high physiological stability. The interaction of the Xyl-SA/5-FUSA NPs with blood components was investigated by hemolysis study. The cell cytotoxic studies demonstrated that Xyl-SA/5-FUSA NPs induced higher cytotoxicity than free drugs against the Human colorectal cancer cells (HT-29, HCT-15). These results indicate that Xyl-SA/5-FUSA NPs can serve as a promising drug delivery system for the efficient delivery of 5-FU in cancer therapy.
在这项研究中，开发了基于两亲性木聚糖-硬脂酸（Xyl-SA）缀合物的自组装纳米颗粒，用于癌症治疗中 5-氟尿嘧啶（5-FU）的有效递送。使用芘作为荧光探针研究了 Xyl-SA 缀合物在水介质中的自组装行为。为了提高 5-FU 的载药效率，合成了亲脂性 5-氟尿嘧啶-硬脂酸（5-FUSA）前药，并随后将其包裹在 Xyl-SA NPs 的疏水性核心内。所得的 Xyl-SA/5-FUSA NPs 具有适当的尺寸（278nm）、高的 5-FUSA 载药量（14.6wt%）和高的生理稳定性。通过溶血研究研究了 Xyl-SA/5-FUSA NPs 与血液成分的相互作用。细胞毒性研究表明，与游离药物相比，Xyl-SA/5-FUSA NPs 对人结肠癌细胞（HT-29、HCT-15）诱导的细胞毒性更高。这些结果表明，Xyl-SA/5-FUSA NPs 可以作为一种有前途的药物递送系统，用于癌症治疗中 5-FU 的有效递送。
