Polymer Laboratory, School of Chemistry, College of Science, University of Tehran, PO Box 14155 6455, Tehran, Iran.
Biological and Chemical Engineering, Aarhus University, Aarhus, Denmark.
J Biomed Mater Res A. 2020 Nov 1;108(11):2291-2304. doi: 10.1002/jbm.a.36986. Epub 2020 Jun 9.
Active targeted nanotechnology-based drug delivery systems have gained significant favor because they have the ability to decrease side effects, improve drug bioavailability, and the potency of anticancer treatment. In this study, functional amphiphilic Janus nanoparticles (JNPs), consisting of hydrophilic and hydrophobic biocompatible polymers as two distinct sides, have been prepared via a robust and simple synthesis method. The surface-active hydrophilic side of this Janus platform is functionalized with an aptamer against epithelial cell adhesion molecule (EpCAM) to deliver Doxorubicin (DOX) for the treatment of metastasis colorectal adenocarcinoma HT29 cells. The Janus morphology of the nanoparticles and their cell penetration behavior are shown in microscopic evaluations. By evaluating the prepared DOX-loaded aptamer-modified JNPs by cell-toxicity assay and confocal microscopy, it was determined that the utilization of an internalization strategy to enhance cell uptake would increase the anticancer effect of the Janus nanocarrier and improve the capacity to deliver the chemotherapeutical drug site-specifically.
主动靶向纳米技术药物传递系统因其能够降低副作用、提高药物生物利用度和抗癌治疗效果而受到广泛关注。在本研究中，通过一种稳健且简单的合成方法制备了由亲水性和疏水性生物相容性聚合物作为两个截然不同的侧面组成的功能性两亲性 Janus 纳米粒子（JNPs）。Janus 平台的表面活性亲水侧通过与针对上皮细胞黏附分子（EpCAM）的适体功能化，用于递送多柔比星（DOX）以治疗转移性结直肠腺癌 HT29 细胞。通过微观评估显示了纳米粒子的 Janus 形态及其细胞穿透行为。通过细胞毒性测定和共聚焦显微镜评估载 DOX 的适体修饰 JNPs 的制备，确定利用内化策略增强细胞摄取将提高 Janus 纳米载体的抗癌效果，并提高化学治疗药物的靶向递药能力。
