载维生素 B12 的丝胶蛋白胶束用于靶向过表达 CD320 的胃癌和逆转耐药性。
Vitamin B12-conjugated sericin micelles for targeting CD320-overexpressed gastric cancer and reversing drug resistance.
机构信息
Department of General Surgery, Nanfang Hospital, Southern Medical University, Guangzhou 510515, PR China.
PCFM Lab & GDHPPC Lab, School of Materials Science & Engineering, Sun Yat-sen University, Guangzhou 510275, PR China.
出版信息
Nanomedicine (Lond). 2019 Feb;14(3):353-370. doi: 10.2217/nnm-2018-0321. Epub 2018 Oct 17.
AIM
Our previous research has introduced sericin micelles to reverse drug resistance. However, these micelles could not selectively bind to gastric cancer (GC) cells. We developed vitamin B12 (VB12) conjugated sericin micelles for targeted GC therapy.
MATERIALS & METHODS: We used VB12, sericin, synthetic poly(γ-benzyl-L-glutamate) (PBLG) and paclitaxel (PTX) to develop VB12-conjugated and PTX-loaded micelles (VB12-sericin-PBLG-PTX). Then we explored their physicochemical properties, cellular uptake and antitumor mechanism.
RESULTS
VB12-sericin-PBLG-PTX micelles were proved to be of appropriate particle size, have good dispersion and are bio-safe. Following transcobalamin II (CD320)-receptor-mediated endocytosis, these swallowed micelles with GC-targeting and enhanced cellular uptake abilities, alter mitochondrial transmembrane potential/apoptosis pathway and reverse drug resistance.
CONCLUSION
VB12-sericin-PBLG-PTX micelles are promising materials for GC-targeted clinical applications.
目的
我们之前的研究已经将丝胶纳米胶束用于逆转药物耐药性。然而，这些胶束不能选择性地与胃癌（GC）细胞结合。我们开发了维生素 B12（VB12）缀合丝胶纳米胶束用于靶向 GC 治疗。
材料与方法
我们使用 VB12、丝胶、合成聚（γ-苄基-L-谷氨酸）（PBLG）和紫杉醇（PTX）来开发 VB12 缀合和 PTX 负载的纳米胶束（VB12-丝胶-PBLG-PTX）。然后，我们探索了它们的物理化学性质、细胞摄取和抗肿瘤机制。
结果
VB12-丝胶-PBLG-PTX 纳米胶束被证明具有适当的粒径，具有良好的分散性和生物安全性。在转钴胺素 II（CD320）受体介导的内吞作用下，这些具有 GC 靶向和增强细胞摄取能力的纳米胶束，改变线粒体跨膜电位/凋亡途径并逆转药物耐药性。
结论
VB12-丝胶-PBLG-PTX 纳米胶束是用于 GC 靶向临床应用的有前途的材料。
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