Department of Bio-Health Convergence, Kangwon National University, Chuncheon, 200-701, Republic of Korea.
Carbohydr Polym. 2021 Jun 15;262:117907. doi: 10.1016/j.carbpol.2021.117907. Epub 2021 Mar 5.
This study developed the pH, and over-expressed nucleolin receptor responsive nano-drug delivery system (nDDS) composed by bio-synthesized gold nanoparticles (Au NPs), chitosan (CS) with aptamer (Apt) to deliver the 5-fluorouracil (5FU) and doxorubicin (Dox) for the improved glioblastoma treatment. The characterization results demonstrated that Apt-Dox-CS-Au-5FU NPs were monodispersed in nature with an average hydrodynamic particle size of 196.2 ± 2.89 nm and zeta potential of 16.26 ± 0.51 mV. The drug release, drug encapsulation efficiency (DEE), and loading efficiency (DLE) were measured by HPLC. The pH-responsive dual drug release was instigated the higher glioblastoma cell death instead of the single drug release through G/G phase cell cycle arrest. In addition, the internalization of Apt-Dox-CS-Au-5FU NPs in cell organelles was affirmed by bio-TEM analysis. Overall, this work revealed the newly designed drug-loaded smart nDDS improved the glioblastoma treatments.
本研究开发了由生物合成的金纳米粒子（Au NPs）、壳聚糖（CS）与适体（Apt）组成的 pH 值和过表达核仁素受体响应的纳米药物递送系统（nDDS），用于递送 5-氟尿嘧啶（5FU）和阿霉素（Dox），以改善脑胶质瘤的治疗效果。表征结果表明，Apt-Dox-CS-Au-5FU NPs 具有单分散性，平均水动力粒径为 196.2 ± 2.89nm，zeta 电位为 16.26 ± 0.51mV。通过 HPLC 测量药物释放、药物包封效率（DEE）和载药效率（DLE）。通过 G/G 期细胞周期阻滞引发 pH 响应的双重药物释放，从而导致更高的脑胶质瘤细胞死亡，而不是单一药物释放。此外，通过生物-TEM 分析证实了 Apt-Dox-CS-Au-5FU NPs 在细胞细胞器中的内化。总的来说，这项工作揭示了新设计的载药智能 nDDS 改善了脑胶质瘤的治疗效果。
