生物素受体在各种癌细胞类型中过表达,在肿瘤发展中至关重要,新陈代谢,和转移。如果化学治疗剂特异性地靶向癌细胞上的生物素受体,则它们可能更有效并且具有更少的副作用。具有纳米级尺寸的聚合物胶束(PM)经由过程EPR效应在肿瘤组织附近积聚。我们利用溶剂交换技术来处理聚合物生物素-PEG-SeSe-PBLA胶束。这经历了自组装以产生具有81.54±0.23nm的流体动力学直径的均匀分散的PM。所得PM通过1HNMR表征,13CNMR,FTIR,和拉曼光谱。PM表现出高效力的阿霉素封装(EE)和负载含量(DLC),值为5.93wt%和74.32%,分别。DOX@生物素-PEG-SeSe-PBLA胶束显示出最佳的DOX释放,在10mM谷胱甘肽和0.1%H2O2中分别约为89%和74%,在72小时内,在模拟的癌症氧化还原池中。令人着迷的是,空白生物素-PEG-SeSe-PBLA胶束不影响HaCaT或HeLa细胞系;大约85%的细胞具有代谢活性。相反,浓度为5μg/ml,DOX@生物素-PEG-SeSe-PBLA特异性抑制大约76%的HeLa细胞和11%的HaCaT细胞的增殖。荧光显微镜结果表明,生物素修饰的胶束更成功地被HeLa细胞内化,过度表达生物素受体,比体外非靶向胶束。总之,与二硒化物连接的生物素-PEGSeSe-PBLA形成了智能PM,可以精确地提供针对癌细胞的DOX,并且在生理上具有持久性。
Biotin receptors are overexpressed in various cancer cell types, essential in tumor development, metabolism, and metastasis. Chemotherapeutic agents may be more effective and have fewer adverse effects if they specifically target the biotin receptors on cancer cells. Polymeric micelles (PMs) with nanoscale size via the EPR effect to accumulate near tumor tissue. We utilized the solvent exchange technique to crate polymeric
Biotin-PEG-SeSe-PBLA micelles. This underwent self-assembly to create uniformly dispersed PMs with a hydrodynamic diameter of 81.54 ± 0.23 nm. The resulting PMs characterized by 1HNMR, 13CNMR, FTIR, and Raman spectroscopy. PMs exhibited a high efficacy of Doxorubicin encapsulation (EE) and loading content (DLC), with values of 5.93 wt% and 74.32 %, respectively. DOX@
Biotin-PEG-SeSe-PBLA micelles showed optimal DOX release, around 89 % and 74 % in 10 mM glutathione and 0.1 % H2O2, respectively, within 72 hours, in the simulated cancer redox pool. Fascinatingly, the blank Biotin-PEG-SeSe-PBLA micelles did not affect the HaCaT or HeLa cell lines; approximately 85 % of the cells were metabolically active. Contrarily, at a 5 μg/ml concentration, DOX@Biotin-PEG-SeSe-PBLA specifically inhibited the proliferation of roughly 76 % of HeLa cells and 11 % of HaCaT cells. The fluorescence microscopy results demonstrated that biotin-decorated micelles were more successfully internalized by HeLa cells, which overexpress the
biotin receptor, than by non-targeted micelles in vitro. In summary, the diselenide-linked
Biotin-PEGSeSe-PBLA formed smart PMs that could offer DOX specific to cancer cells with precision and are physiologically durable.