Department of Pharmacy, Chemical Engineering, Qingdao University of Science and Technology, Qingdao, 266042, China.
Institute of Physics, Nankai University, Tianjin, 300071, China.
J Nanosci Nanotechnol. 2020 Sep 1;20(9):5295-5304. doi: 10.1166/jnn.2020.17882.
A drug co-delivery system composed of selenium nanoparticles (SeNPs) has attracted increasing interest due to its ability to increase the anticancer efficacy against multidrug-resistant cancer cells. In this study, a cancer-targeted drug co-delivery system combining fluorescein-loaded liposomes and SeNPs was designed and evaluated. The system was developed by coating SeNPs and fluorescein-loaded liposomes with folic acid-chitosan conjugates (FA-CS-SeNPs-Lips). Folic acid-chitosan conjugates (FA-CS) were synthesized by coupling folic acid (FA) with chitosan (CS), and the structure was confirmed by performing Fourier transform spectroscopy (FT-IR) and nuclear magnetic resonance (H-NMR) spectroscopy. Dynamic light scattering (DLS) measurements and transmission electron microscopy (TEM) were used to evaluate the particle size, Zeta potential, and morphology. The cytotoxicity of SeNPs coated with FA-CS conjugates (FA-CS-SeNPs) toward A549 cells and HeLa cells was examined using the MTT assay. The cancer-targeting ability and drug release behaviors were evaluated by measuring the cellular uptake of fluorescein and dialysis, respectively. The FA-CS-SeNPs were uniform, spherical particles with a ~50 nm diameter and high positive Zeta potential (+57.7 mV). Based on the results of the MTT assay, FA-CS-SeNPs displayed a more significant increase in the anticancer efficacy in HeLa cells than CS-SeNPs. FA-CS-SeNPs-Lips not only slowly released fluorescein but also specifically targeted HeLa cells through selective binding between folate and folate receptors to increase the cellular uptake of fluorescein.
一种由硒纳米颗粒（SeNPs）组成的药物共递送系统由于能够提高对多药耐药癌细胞的抗癌疗效而引起了越来越多的关注。在这项研究中，设计并评估了一种结合荧光素负载脂质体和 SeNPs 的癌症靶向药物共递送系统。该系统通过将 SeNPs 和荧光素负载脂质体用叶酸-壳聚糖缀合物（FA-CS-SeNPs-Lips）进行包覆而开发。叶酸-壳聚糖缀合物（FA-CS）通过将叶酸（FA）与壳聚糖（CS）偶联合成，并通过傅里叶变换光谱（FT-IR）和核磁共振（H-NMR）光谱进行结构确认。动态光散射（DLS）测量和透射电子显微镜（TEM）用于评估粒径、Zeta 电位和形态。使用 MTT 测定法检查 FA-CS 缀合物（FA-CS-SeNPs）包覆的 SeNPs 对 A549 细胞和 HeLa 细胞的细胞毒性。通过分别测量荧光素的细胞摄取和透析来评估癌症靶向能力和药物释放行为。FA-CS-SeNPs 是均匀的、球形颗粒，粒径约为 50nm，Zeta 电位为正（+57.7mV）。根据 MTT 测定的结果，FA-CS-SeNPs 在 HeLa 细胞中显示出比 CS-SeNPs 更高的抗癌疗效增加。FA-CS-SeNPs-Lips 不仅缓慢释放荧光素，而且还通过叶酸与叶酸受体之间的选择性结合特异性靶向 HeLa 细胞，以增加荧光素的细胞摄取。
