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载紫杉醇的大黄酸偶联物胶束对MCF-7细胞的毒性与细胞摄取研究

王晓颖, 王夏英, 邱梁桢, 欧阳惠枝, 徐伟

王晓颖, 王夏英, 邱梁桢, 欧阳惠枝, 徐伟. 载紫杉醇的大黄酸偶联物胶束对MCF-7细胞的毒性与细胞摄取研究[J]. 中国药科大学学报, 2020, 51(1): 33-37. DOI: 10.11665/j.issn.1000-5048.20200106
引用本文: 王晓颖, 王夏英, 邱梁桢, 欧阳惠枝, 徐伟. 载紫杉醇的大黄酸偶联物胶束对MCF-7细胞的毒性与细胞摄取研究[J]. 中国药科大学学报, 2020, 51(1): 33-37. DOI: 10.11665/j.issn.1000-5048.20200106
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WANG Xiaoying, WANG Xiaying, QIU Liangzhen, OUYANG Huizhi, XU Wei. Cytotoxicity and cellular uptake of paclitaxel-loaded carboxymethyl chitosan-rhein polymeric micelles in MCF-7 cells[J]. Journal of China Pharmaceutical University, 2020, 51(1): 33-37. DOI: 10.11665/j.issn.1000-5048.20200106
Citation: WANG Xiaoying, WANG Xiaying, QIU Liangzhen, OUYANG Huizhi, XU Wei. Cytotoxicity and cellular uptake of paclitaxel-loaded carboxymethyl chitosan-rhein polymeric micelles in MCF-7 cells[J]. Journal of China Pharmaceutical University, 2020, 51(1): 33-37. DOI: 10.11665/j.issn.1000-5048.20200106
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载紫杉醇的大黄酸偶联物胶束对MCF-7细胞的毒性与细胞摄取研究

  • 福建中医药大学药学院

基金项目: 国家自然科学基金资助项目(No.81603301)；福建省卫计委中青年骨干人才培养项目(No.2016-ZQN-69)；中医药公共卫生服务补助专项(财社〔2017〕66号)

Cytotoxicity and cellular uptake of paclitaxel-loaded carboxymethyl chitosan-rhein polymeric micelles in MCF-7 cells

摘要

    摘要
  • 摘要: 通过MTT法评估了羧甲基壳聚糖-大黄酸偶联物(CR偶联物)和载紫杉醇(PTX)的CR偶联物胶束(PTX/CR偶联物胶束)对MCF-7细胞的细胞毒性，结果显示，CR偶联物具有良好的安全性；PTX/CR偶联物胶束24 h内表现出优于Taxol®；的抗肿瘤活性。通过包载环境响应型荧光探针P4，考察了共载P4和PTX的CR偶联物胶束［(P4+PTX)/CR偶联物胶束］在MCF-7细胞中的摄取情况，结果显示，MCF-7细胞对其具有较好的摄取效果，(P4+PTX)/CR偶联物胶束组与其加维拉帕米组摄取量无显著性差异，提示CR偶联物胶束可以保护其所载荧光探针和/或药物不被P-gp外排到细胞外。该研究结果为CR偶联物及PTX/CR偶联物胶束的进一步体内研究奠定了基础。
    Abstract: In this study, in vitro cytotoxicity of carboxymethyl chitosan-rhein conjugate(CR conjugate)and paclitaxel-loaded carboxymethyl chitosan-rhein polymeric micelles(PTX/CR PMs)was evaluated by MTT method in MCF-7 cells. The results showed that CR conjugate displayed good security; PTX/CR PMs in 24 h showed better antitumor activity than Taxol® . Environment-responsive fluorescent probe P4 was used to determine the cellular uptake of PTX/CR PMs in MCF-7 cells. The results also showed that P4 and PTX co-loaded carboxymethyl chitosan-rhein polymeric micelles ［(P4+PTX)/CR PMs］ could be taken up by MCF-7 cells. There was no difference between(P4+PTX)/CR PMs group and(P4+PTX)/CR PMs with verapamil group, suggesting that CR PMs could protect fluorescent probe and/or drugs in their cores avoiding efflux by P-glycoprotein. These results will contribute to in vivo study of CR conjugate and PTX/CR PMs in the future.
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  • [1] Wang XY,Qiu LZ,Li QZ,et al.Synthesis of PEGylated carboxymethyl chitosan-rhein conjugate and preparation of paclitaxel-loaded polymeric micelles[J].J China Pharm Univ(中国药科大学学报),2018,49(5):596-602.
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    [6] Bernabeu E,Gonzalez L,Cagel M,et al.Novel soluplus(+)-TPGS mixed micelles for encapsulation of paclitaxel with enhanced in vitro cytotoxicity on breast and ovarian cancer cell lines[J].Colloids Surf B Biointerfaces,2016,140:403-411.
    [7] Ahmed AA,Wang XY,Lu Z,et al.Modulating microtubule stability enhances the cytotoxic response of cancer cells to Paclitaxel[J].Cancer Res,2011,71(17):5806-5817.
    [8] Hu XW, Zhang J, Yu Z, et al. Environment-responsive aza-BODIPY dyes quenching in water as potential probes to visualize the in vivo fate of lipid-based nanocarriers[J].Nanomed-Nanotechnol Biol Med,2015,11(8):1939-1948.
    [9] Ma YH,He HS,Xia F,et al.In vivo fate of lipid-silybin conjugate nanoparticles:implications on enhanced oral bioavailability[J].Nanomed-Nanotechnol Biol Med,2017,13(8):2643-2654.
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  • 刊出日期:  2020-02-24

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