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含叶酸功能化环糊精 - 紫杉醇复合物的可注射性乙二醇壳聚糖水凝胶用于乳腺癌治疗

Injectable Glycol Chitosan Hydrogel Containing Folic Acid-Functionalized Cyclodextrin-Paclitaxel Complex for Breast Cancer Therapy.

作者信息

Hyun Hoon, Park Min Ho, Jo Gayoung, Lee Bo Young, Choi Jae Won, Chun Heung Jae, Kim Hyeon Soo, Yang Dae Hyeok

机构信息

Department of Biomedical Sciences, Chonnam National University Medical School, Gwangju 61469, Korea.

Department of Surgery, Chonnam National University Medical School, Gwangju 61469, Korea.

出版信息

Nanomaterials (Basel). 2021 Jan 27;11(2):317. doi: 10.3390/nano11020317.

Abstract

We prepared a drug carrier which consisted of injectable methacrylated glycol chitosan (MGC) hydrogel, and a conjugate of 6-monodeoxy-6-monoamino-β-cyclodextrin⋅hydrochloride (6-NH-β-CD⋅HCl), polyethylene glycol (PEG), and folic acid (FA) for the local delivery and improved cellular uptake of paclitaxel (PTX) (MGC/CDPF-ic-PTX). CDPF refers to a conjugate of 6-NH-β-CD⋅HCl, PEG, and FA. The anti-cancer effect was investigated using a xenograft mouse model. As controls, the animal study on MGC/PTX and MGC/CD-ic-PTX was performed. The swelling ratio of all samples was analyzed for 7 days, and it showed a gradual increase for 3 days and a maintained state afterward. From the release result, the MGC-based samples have an initial burst for 1 day and a sustained release for 7 days. Results of cytotoxicity and animal study showed the biocompatibility and superior anti-cancer effect of MGC/CDPF-ic-PTX against breast cancer. Furthermore, histological results showed the anti-cancer capacity of MGC/CDPF-ic-PTX against breast cancer. These findings suggest that MGC/CDPF-ic-PTX has clinical potential for breast cancer therapy.

摘要

我们制备了一种药物载体,其由可注射的甲基丙烯酸化壳聚糖二醇(MGC)水凝胶以及6-单脱氧-6-单氨基-β-环糊精·盐酸盐(6-NH-β-CD·HCl)、聚乙二醇(PEG)和叶酸(FA)的缀合物组成,用于紫杉醇(PTX)的局部递送并改善其细胞摄取(MGC/CDPF-ic-PTX)。CDPF是指6-NH-β-CD·HCl、PEG和FA的缀合物。使用异种移植小鼠模型研究了其抗癌效果。作为对照,对MGC/PTX和MGC/CD-ic-PTX进行了动物研究。分析了所有样品7天的溶胀率,结果显示其在3天内逐渐增加,之后保持稳定。从释放结果来看,基于MGC的样品有1天的初始突释和7天的缓释。细胞毒性和动物研究结果表明,MGC/CDPF-ic-PTX对乳腺癌具有生物相容性和优异的抗癌效果。此外,组织学结果显示了MGC/CDPF-ic-PTX对乳腺癌的抗癌能力。这些发现表明,MGC/CDPF-ic-PTX在乳腺癌治疗方面具有临床潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e9f/7910883/815fb683f207/nanomaterials-11-00317-g001.jpg

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