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基于聚碳酸酯的共聚物胶束作为抗癌鬼臼毒素或杜松提取物的可生物降解载体

Polycarbonate-Based Copolymer Micelles as Biodegradable Carriers of Anticancer Podophyllotoxin or Juniper Extracts.

作者信息

Kalinova Radostina G, Dimitrov Ivaylo V, Ivanova Diana I, Ilieva Yana E, Tashev Alexander N, Zaharieva Maya M, Angelov George, Najdenski Hristo M

机构信息

Institute of Polymers, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.

Institute of Chemical Engineering, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.

出版信息

J Funct Biomater. 2024 Feb 21;15(3):53. doi: 10.3390/jfb15030053.

Abstract

Podophyllotoxin (PPT) is used in the industrial production of efficient anticancer, antiviral and other drugs. or are natural sources of PPT, but at present they are considered as endangered species. Their PPT content is variable, depending on the growing conditions. Searching for new sources of PPT, some representatives of the genus were found to exhibit efficient PPT biosynthesis. However, PPT is highly toxic and poorly soluble in water compound, which limits its clinical applications. In this connection, amphiphilic polymer micelles are considered to be suitable PPT carriers, aimed at increase in water solubility and decrease in toxicity. The present research deals with the evaluation of MPEG-polycarbonate block copolymer micelles loaded with PPT or juniper extracts. The active component-loaded polymer nanocarriers were characterized by dynamic and electrophoretic light scattering, as well as by transmission electron microscopy. The active component loading efficiency and loading capacity were also determined. Highly efficient antiproliferative activity of the loaded micelles was determined in a panel of cancer cell lines. The obtained amphiphilic nanocarriers, loaded with PPT-containing bioactive components, have application in future in vivo preclinical trials of their pharmacokinetics and pharmacodynamics as potential therapeutical agents in the prospective nanomedicine.

摘要

鬼臼毒素(PPT)用于高效抗癌、抗病毒及其他药物的工业生产。[植物名称1]和[植物名称2]是PPT的天然来源,但目前它们被视为濒危物种。其PPT含量因生长条件而异。在寻找PPT新来源的过程中,发现[植物属名称]的一些代表植物具有高效的PPT生物合成能力。然而,PPT毒性极高且在水中的溶解性很差,这限制了其临床应用。就此而言,两亲性聚合物胶束被认为是合适的PPT载体,旨在提高其水溶性并降低毒性。本研究涉及对负载PPT或杜松提取物的聚乙二醇单甲醚 - 聚碳酸酯嵌段共聚物胶束的评估。通过动态光散射、电泳光散射以及透射电子显微镜对负载活性成分的聚合物纳米载体进行了表征。还测定了活性成分的负载效率和负载量。在一组癌细胞系中测定了负载胶束的高效抗增殖活性。所获得的负载含PPT生物活性成分的两亲性纳米载体,未来可应用于其药代动力学和药效学的体内临床前试验,作为潜在的治疗剂用于未来的纳米医学。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2af5/10971044/d662e32073fe/jfb-15-00053-g001.jpg

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