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二茂铁改性磷脂:一种用于氧化还原触发药物递送囊泡的创新前体,对癌细胞具有选择性。

Ferrocene-Modified Phospholipid: An Innovative Precursor for Redox-Triggered Drug Delivery Vesicles Selective to Cancer Cells.

机构信息

Department of Chemistry, McGill University , 801 Sherbrooke Street West, Montreal, Quebec, Canada H3A OB8.

Laboratoire de Méthodologie et Synthèse de Produits Naturels, Université du Québec à Montréal , C.P. 8888, Succ. Centre-Ville, Montréal, H3C 3P8, Québec, Canada.

出版信息

Langmuir. 2016 May 3;32(17):4169-78. doi: 10.1021/acs.langmuir.6b00511. Epub 2016 Apr 21.

Abstract

Controlled payload release is one of the key elements in the creation of a reliable drug delivery system. We report the discovery of a drug delivery vessel able to transport chemotherapeutic agents to target cancer cells and selectively trigger their release using the electrochemical activity of a ferrocene-modified phospholipid. Supported by in vitro assays, the competitive advantages of this discovery are (i) the simple one step scalability of the synthetic process, (ii) the stable encapsulation of toxic drugs (doxorubicin) during transport, and (iii) the selective redox triggering of the liposomes to harness their cytotoxic payload at the cancer site. Specifically, the redox-modified giant unilamellar vesicle and liposomes were characterized using advanced methods such as scanning electrochemical microscopy (SECM), transmission electron microscopy (TEM), dynamic light scattering (DLS), and fluorescent imaging.

摘要

控制载药释放是可靠药物输送系统构建的关键要素之一。我们报告了一种药物输送载体的发现,该载体能够利用二茂铁修饰磷脂的电化学活性将化疗药物输送到靶癌细胞,并选择性地触发其释放。通过体外实验证实,这一发现具有以下竞争优势:(i)合成过程的简单一步可扩展性;(ii)在运输过程中稳定包载有毒药物(阿霉素);(iii)脂质体的选择性氧化还原触发,以在癌症部位利用其细胞毒性有效载荷。具体而言,使用扫描电化学显微镜(SECM)、透射电子显微镜(TEM)、动态光散射(DLS)和荧光成像等先进方法对氧化还原修饰的巨大单层囊泡和脂质体进行了表征。

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