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纳米胶束, 是由疏水性内核及亲水性外壳自组装形成的纳米粒子, 利用其在肿瘤部位增强的渗透和滞留效应(EPR效应), 已成功用作靶向药物输送载体。本研究将近红外荧光染料Cy7-NHS与NH2-PEG-b-PCL连接合成了Cy7-PEG-PCL,并将其组装修饰在胶束结构中, 作为紫杉醇药物的递送载体。研究结果显示, 当药物/载体比例确定为1/4, 由聚乙二醇-聚己内酯共聚物自组装形成的胶束粒径为30 nm左右, zeta电位为 -3 mV, 包封率可达95%以上。体外细胞毒实验表明,载紫杉醇胶束对人乳腺癌MCF-7细胞增殖的抑制能力与Taxol 制剂相似。活体成像实验结果显示Cy7标记的聚合物胶束在静脉注射后可以有效地被动靶向到肿瘤部位。另外, 以异位接种MCF-7细胞荷瘤裸鼠为模型的体内药效学实验中,载紫杉醇聚合物胶束显示出与Taxol 制剂相似的抗肿瘤活性。综上所述, 在肿瘤靶向成像和治疗方面, 本研究所构建的胶束载药系统显示出良好的潜力。
Nanophase micelles, a self-assembled nanoparticle composed of a hydrophobic core and a hydrophilic shell, have been successfully used as targeted drug delivery vehicles due to their enhanced infiltration and retention effects (EPR effect) at tumor sites. In this study, Cy7-PEG-PCL was synthesized by linking the near-infrared fluorescent dye Cy7-NHS with NH2-PEG-b-PCL and its assembly was modified in the micellar structure to serve as a delivery carrier for paclitaxel. The results showed that when the drug / carrier ratio was determined to be 1/4, the size of micelles formed by the self-assembly of PEG-polycaprolactone copolymer was about 30 nm and the zeta potential was -3 mV. The entrapment efficiency Up to 95%. In vitro cytotoxicity experiments showed that Paclitaxel micelles inhibit the proliferation of human breast cancer MCF-7 cells similar to Taxol preparations. The results of in vivo imaging showed that Cy7-labeled polymer micelles could be efficiently and passively targeted to the tumor site after intravenous injection. In addition, paclitaxel polymer micelles exhibited similar antitumor activity to Taxol preparations in in vivo pharmacodynamic models of ectopic MCF-7-bearing nude mice. In summary, the micellar drug delivery system constructed in this study shows good potential in tumor targeted imaging and therapy.