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聚乙二醇化喜树碱制备纳米胶束和超分子水凝胶用于农药联合控释

Engineering of Peglayted Camptothecin Into Nanomicelles and Supramolecular Hydrogels for Pesticide Combination Control.

作者信息

Zhang Zhi-Jun, Shang Xiao-Fei, Yang Liu, Shi Yan-Bin, Liu Ying-Qian, Li Jun-Cai, Yang Guan-Zhou, Yang Cheng-Jie

机构信息

School of Pharmacy, Lanzhou University, Lanzhou, China.

Lanzhou Institute of Husbandry and Pharmaceutical Sciences, Chinese Academy of Agricultural Science, Lanzhou, China.

出版信息

Front Chem. 2020 Jan 15;7:922. doi: 10.3389/fchem.2019.00922. eCollection 2019.

Abstract

As a famous quinoline alkaloid, camptothecin (CPT) presented the significant anti-tumor activity, as well as the interesting insecticidal activities, but the low solubility, poor hydrophobicity and cuticular penetration of CPT have been severely limited the field application. In this study, we conjugated the camptothecin with polyethylene glycol, forming amphiphilic copolymer, mPEG-CPT, which could be self-assembled into micelles, or formed a hydrogel with α-CD by super-cross-linking to combine delivery with acetamiprid or nitenpyram. Results showed that the nitenpyram or acetamiprid loaded hydrogels showed dual phase release behavior, while the micelles displayed a synchronous and fast release profile. Moreover, these four nanopesticides showed potent or superior insecticidal activities and a synergetic effect against , and . This finding indicated that micelles and hydrogels could be used as effective carriers for pesticide combination control.

摘要

喜树碱(CPT)作为一种著名的喹啉生物碱,具有显著的抗肿瘤活性以及有趣的杀虫活性,但其低溶解度、疏水性差和角质层渗透性低严重限制了其在田间的应用。在本研究中,我们将喜树碱与聚乙二醇共轭,形成两亲性共聚物mPEG-CPT,其可自组装成胶束,或通过超交联与α-环糊精形成水凝胶,以结合递送啶虫脒或烯啶虫胺。结果表明,负载啶虫脒或烯啶虫胺的水凝胶呈现双相释放行为,而胶束则呈现同步快速释放曲线。此外,这四种纳米农药对[具体害虫名称缺失]显示出强效或优异的杀虫活性以及协同效应。这一发现表明胶束和水凝胶可作为农药组合防治的有效载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c8f2/6974551/ccf7642c0fd3/fchem-07-00922-g0001.jpg

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