Functional drug carriers formed by RGD-modified β-CD-HPG for the delivery of docetaxel for targeted inhibition of nasopharyngeal carcinoma cells.

Functional drug carriers formed by RGD-modified β-CD-HPG for the delivery of docetaxel for targeted inhibition of nasopharyngeal carcinoma cells.
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DOI:
10.1039/d2ra02301f
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发表时间:
2022-06-14
期刊:
影响因子:
3.9
通讯作者:
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中科院分区:
化学3区
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本研究将靶向分子精氨酸-甘氨酸-天冬氨酸(RGD)接枝到高支化聚甘油(HPG)修饰的β-环糊精(β-CD-HPG)上,制备了靶向抑制鼻咽癌(NPC)细胞的给药体系。通过激光共聚焦扫描显微镜和流式细胞术证实,所获得的β-CD-HPG-RGD具有相对小的尺寸和低表面电荷,能有效递送docetaxel (Doc),并对人鼻鼻癌HNE-1细胞具有靶向作用。体外释药分析显示了β-CD-HPG-RGD/Doc纳米药物的控释动力学。β-CD-HPG-RGD/Doc能有效抑制HNE-1细胞的增殖,促进细胞凋亡。并对其体外和体内生物相容性进行了评价。结果表明,β-CD-HPG-RGD/Doc纳米药物在鼻咽癌靶向治疗中具有潜在的应用前景。合成了一种基于hpg修饰β-CD的RGD靶向药物载体。该载体具有良好的生物相容性和靶向性。得到的NPs能有效抑制肿瘤细胞的增殖。
In this study, a drug delivery system was prepared by grafting the targeting molecule arginine-glycine-aspartic acid (RGD) onto hyperbranched polyglycerol (HPG)-modified β-cyclodextrin (β-CD-HPG) for the targeted inhibition of nasopharyngeal carcinoma (NPC) cells. The obtained β-CD-HPG-RGD with a relatively small size and low surface charge delivered docetaxel (Doc) effectively and displayed a targeting effect to human NPC HNE-1 cells, as confirmed by confocal laser scanning microscopy and flow cytometry. The in vitro drug release analysis exhibited the controlled drug release kinetics of the β-CD-HPG-RGD/Doc nanomedicine. β-CD-HPG-RGD/Doc effectively inhibited the proliferation of HNE-1 cells and promoted apoptosis. Moreover, its biocompatibility in vitro and in vivo was assessed. The results indicate that the β-CD-HPG-RGD/Doc nanomedicine has potential application in NPC targeting therapy. A new RGD targeting drug carrier based on HPG-modified β-CD has been synthesized. This carrier showed excellent biocompatibility and targeting ability. The obtained NPs could effectively inhibit the proliferation of tumor cells.
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