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目的:肿瘤的多药耐药现象会显著降低肿瘤细胞内药物浓度,本研究通过制备抗肿瘤多药耐药的靶向给药系统来逆转肿瘤的耐药性以提升细胞对药物的敏感性,从而降低该现象对癌症治疗的阻碍。方法:本文使用乳化溶剂挥发法制备以含姜黄素两亲性嵌段共聚物载体、以紫杉醇和磁性粒为核心的抗肿瘤多药耐药纳米粒,使用透射电镜和动态粒径散射仪等对纳米粒进行表征和磁响应性测试后,使用MTT法测定纳米粒对肿瘤耐药细胞MCF-7/ADR的抑制率以探究给药系统的耐药逆转性能。结果:制备的抗肿瘤多耐药纳米粒粒径为105 nm左右,磁响应性良好。所制得载紫杉醇纳米粒包封率为74.74%,载药率为12.40%。纳米粒可以通过磁场和生物素受体介导作用促进肿瘤细胞对粒子的内化,以增加抗癌药物的蓄积。与游离紫杉醇相比,逆转细胞耐药指数达8.5。结论:纳米系统在维持自身稳定性同时,能够凭借协同作用和靶向作用较大程度提升药物对耐药肿瘤细胞的杀伤效果。
OBJECTIVE: Multidrug resistance of tumor can significantly reduce the concentration of drug in tumor cells. In this study, drug-resistance of tumor was reversed by preparing targeted anti-tumor multidrug drug delivery system to enhance cell sensitivity to drugs, Thus reducing the barrier to cancer treatment. Methods: The antitumor multidrug-resistant nanoparticles with curcumin amphiphilic block copolymer carrier, paclitaxel and magnetic particles as the core were prepared by the emulsion solvent evaporation method. Transmission electron microscopy and dynamic particle size analyzer After the nanoparticles were characterized and magnetically responsive, the inhibition rate of the nanoparticles on the drug-resistant cell MCF-7 / ADR was measured by MTT assay to explore the drug resistance reversal performance of the drug delivery system. Results: The prepared antitumor multidrug-resistant nanoparticles had a particle size of about 105 nm and good magnetic response. Paclitaxel nanoparticles prepared encapsulation efficiency was 74.74%, drug loading rate was 12.40%. Nanoparticles can promote the internalization of particles by tumor cells via magnetic field and biotin receptor-mediated interactions to increase the accumulation of anti-cancer drugs. Compared with free paclitaxel, reversal of cell resistance index reached 8.5. Conclusion: While maintaining its own stability, nanosystems can greatly enhance the killing effect of drug on drug-resistant tumor cells by virtue of synergism and targeting.