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硫酸软骨素修饰的阿霉素纳米晶的酶/pH 触发型抗癌药物递送。

Enzyme/pH-triggered anticancer drug delivery of chondroitin sulfate modified doxorubicin nanocrystal.

机构信息

Department of Pharmaceutics, School of Pharmacy, Qingdao University, Qingdao, China.

Department of Clinical Laboratory, Hospital of the People's Liberation Army Navy, Qingdao, China.

出版信息

Artif Cells Nanomed Biotechnol. 2020 Dec;48(1):1114-1124. doi: 10.1080/21691401.2020.1813741.

DOI:10.1080/21691401.2020.1813741
PMID:32880192
Abstract

In this paper, we developed a novel strategy of preparing doxorubicin (DOX) nanocrystal (NC) exerting spherical particles with a diameter of 102 nm, which experienced following coating of chondroitin sulphate derivative (CSOA) shell electrostatic and hydrophobic interactions. Such multifunctional outerwear resulted in drug nanocapsules with high drug loading content up to 70% and high colloidal stability under physiological conditions. It exhibited accelerated drug release behaviour when dispersing in hyaluronidase (HAase) containing medium or incubated with cancer cells. CSOA/NCs were effectively taken up by cancer cells CD44 receptor-mediated endocytosis, but were rarely internalised into normal fibroblasts. With the comparison of typical drug-loaded micelles system (DOX/PEG-PCL), CSOA/NCs showed greater inhibition to cancer cells due to the targeted and sensitive drug delivery.

摘要

在本文中,我们开发了一种将阿霉素(DOX)纳米晶体(NC)制备成具有 102nm 直径的球形颗粒的新策略,该策略经历了随后的硫酸软骨素衍生物(CSOA)壳的静电和疏水相互作用的包裹。这种多功能外套导致药物纳米胶囊具有高达 70%的高载药量和在生理条件下的高胶体稳定性。当在含有透明质酸酶(HAase)的介质中分散或与癌细胞孵育时,它表现出加速的药物释放行为。CSOA/NCs 被癌细胞通过 CD44 受体介导的内吞作用有效摄取,但很少被正常成纤维细胞内化。与典型的载药胶束系统(DOX/PEG-PCL)相比,CSOA/NCs 由于靶向和敏感的药物递送,对癌细胞表现出更大的抑制作用。

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