用于喜树碱和阿霉素联合协同抗癌活性的低分子量聚合物-药物缀合物
Low-molecular-weight polymer-drug conjugates for synergistic anticancer activity of camptothecin and doxorubicin combinations.
作者信息
Camacho Kathryn M, Menegatti Stefano, Mitragotri Samir
机构信息
Department of Chemical Engineering, Center for Bioengineering, University of California at Santa Barbara, Santa Barbara, CA 93106, USA.
Department of Chemical & Biomolecular Engineering, Department of Biomedical Engineering, Biomanufacturing Training and Education Center (BTEC), North Carolina State University, Raleigh, NC 27695, USA.
出版信息
Nanomedicine (Lond). 2016 May;11(9):1139-51. doi: 10.2217/nnm.16.33. Epub 2016 Apr 15.
BACKGROUND
High-molecular-weight (MW) polymers (>50,000 Da) can be conjugated to chemotherapy drugs in order to improve their tumor accumulation, while low MW polymers ≤10,000 Da are often overlooked due to faster plasma clearance. Small polymers, however, may facilitate deeper tumor penetration.
MATERIALS & METHODS: Here, we investigate the anticancer efficacy of 10 kDa hyaluronic acid or poly(vinyl alcohol) conjugated to synergistic combinations of camptothecin and doxorubicin, with emphasis on chemical linker impacts.
RESULTS
Our results emphasize drug hydrolyzability for synergy preservation, and also demonstrate superior cancer cell inhibition with low MW polymer-drug conjugates.
CONCLUSION
This study shows the high therapeutic potential of low MW polymer-drug conjugates for polychemotherapy delivery, and provides further insight into the development of polymer-drug therapeutics.
背景
高分子量（MW）聚合物（>50,000道尔顿）可与化疗药物偶联，以提高其在肿瘤中的蓄积，而分子量≤10,000道尔顿的低分子量聚合物由于血浆清除速度较快，常被忽视。然而，小聚合物可能有助于更深地渗透肿瘤。
材料与方法
在此，我们研究了与喜树碱和阿霉素协同组合偶联的10 kDa透明质酸或聚乙烯醇的抗癌效果，重点关注化学连接体的影响。
结果
我们的结果强调了药物水解性对协同作用的保持，并证明低分子量聚合物-药物偶联物对癌细胞的抑制作用更强。
结论
本研究表明低分子量聚合物-药物偶联物在多化疗给药方面具有很高的治疗潜力，并为聚合物-药物疗法的发展提供了进一步的见解。
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