A pharmaceutical study of doxorubicin-loaded PEGylated nanoparticles for magnetic drug targeting
A pharmaceutical study of doxorubicin-loaded PEGylated nanoparticles for magnetic drug targeting
复制标题
DOI：
10.1016/j.ijpharm.2011.06.010
复制
发表时间：
2012-02-14
影响因子：
5.8
通讯作者：
Chourpa, I.
中科院分区：
文献类型：
--
作者：
Gautier, J.;Munnier, E.;Chourpa, I.
改善癌症化疗的新策略之一是基于新的药物递送系统，如聚乙二醇包覆的超顺磁性氧化铁纳米颗粒（PEG-SPION，此后称为PS）。在这项研究中，PS装载有阿霉素（DOX）抗癌药物，使用预形成的DOX-Fe 2+复合物在肿瘤组织和癌细胞的较低pH下可逆。负载DOX的PS（DLPS，3%w/w DOX/氧化铁）在生理pH下呈现约60 nm的流体动力学尺寸和接近零的ζ电位，这两个参数有利于增加生物介质中的胶体稳定性和减少免疫系统的消除。在生理pH 7.4下，60%的负载药物在类似于2 h内从DLPS中逐渐释放。通过药物荧光的共聚焦光谱成像（CSI）跟踪DOX的细胞内释放和分布。DLPS对MCF-7乳腺癌细胞的体外细胞毒性与DOX溶液相当。DOX到SPION表面的可逆缔合和聚合物涂层对药物装载/释放的作用进行了讨论，这两者对于设计用于化疗的新型隐形磁性纳米载体至关重要。(C)2011 Elsevier B. V.保留所有权利。
One of the new strategies to improve cancer chemotherapy is based on new drug delivery systems, like the polyethylene glycol-coated superparamagnetic iron oxide nanoparticles (PEG-SPION, thereafter called PS). In this study, PS are loaded with doxorubicin (DOX) anticancer drug, using a pre-formed DOX-Fe2+ complex reversible at lower pH of tumour tissues and cancer cells. The DOX loaded PS (DLPS, 3% w/w DOX/iron oxide) present a hydrodynamic size around 60 nm and a zeta potential near zero at physiological pH, both parameters being favourable for increased colloidal stability in biological media and decreased elimination by the immune system. At physiological pH of 7.4, 60% of the loaded drug is gradually released from the DLPS in similar to 2h. The intracellular release and distribution of DOX is followed by means of confocal spectral imaging (CSI) of the drug fluorescence. The in vitro cytotoxicity of the DLPS on MCF-7 breast cancer cells is equivalent to that of a DOX solution. The reversible association of DOX to the SPION surface and the role of polymer coating on the drug loading/release are discussed, both being critical for the design of novel stealth magnetic nanovectors for chemotherapy. (C) 2011 Elsevier B.V. All rights reserved.