Theranostic liposomes of TPGS coating for targeted co-delivery of docetaxel and quantum dots
Theranostic liposomes of TPGS coating for targeted co-delivery of docetaxel and quantum dots
复制标题
DOI：
10.1016/j.biomaterials.2012.01.036
复制
发表时间：
2012-04-01
期刊：
影响因子：
14
通讯作者：
Feng, Si-Shen
中科院分区：
文献类型：
--
作者：
Muthu, Madaswamy S.;Kulkarni, Sneha A.;Feng, Si-Shen
本工作的目的是开发一种新型的D-α-生育酚聚乙二醇1000琥珀酸单酯(TPGS)包衣的多功能(抗肿瘤)脂质体，其中包含多西紫杉醇和量子点(QD)，用于肿瘤成像和治疗。采用溶剂注射法制备了非靶向和叶酸受体靶向的TPGS包衣治疗用脂质体，并对其粒径、多分散性、Zeta电位、表面化学和药物包封率进行了表征。以叶酸受体高表达的MCF-7乳腺癌细胞为体外模型，评价药物和量子点脂质体的细胞摄取和细胞毒性。非靶向脂质体和靶向脂质体的平均粒径分别为202和210 nm。高分辨率场发射电子显微镜(FETEM)证实了脂质体外围疏水膜中存在量子点。用激光共聚焦扫描显微镜(CLSM)观察多功能脂质体在MCF-7细胞中的定性内化过程。经MCF-7细胞培养24 h后，商品紫杉醇(R)、非靶向和靶向脂质体的IC50值分别为9.54+/-0.76、1.56+/-0.19和0.23+/-0.05微克/毫升。靶向多功能脂质体显示出比非靶向脂质体更好的疗效，因此在改善肿瘤的影像和治疗方面具有巨大的潜力。(C)2012爱思唯尔有限公司。保留所有权利。
The aim of this work was to develop a new type of D-alpha-tocopheryl polyethylene glycol 1000 succinate mono-ester (TPGS) coated multi-functional (theranostic) liposomes, which contain both docetaxel and quantum dots (QDs) for cancer imaging and therapy. Non-targeting and folate receptor targeting TPGS coated theranostic liposomes were prepared by the solvent injection method and characterized for their particle size, polydispersity, zeta potential, surface chemistry and drug encapsulation efficiency. MCF-7 breast cancer cells of folate receptor overexpression were employed as an in vitro model to assess cellular uptake and cytotoxicity of the drug and QDs loaded liposomes. The mean particle size of the non-targeting and the targeting liposomes was found to be 202 and 210 nm, respectively. High resolution field emission transmission electron microscopy (FETEM) confirmed the presence of quantum dots in the peripheral hydrophobic membranes of the liposomes. The qualitative internalization of multifunctional liposomes by MCF-7 cells was visualized by confocal laser scanning microscopy (CLSM). The IC50 value, which is the drug concentration needed to kill 50% cells in a designated time period, was found to be 9.54 +/- 0.76, 1.56 +/- 0.19 and 0.23 +/- 0.05 mu g/ml for the commercial Taxotere (R), non-targeting and targeting liposomes, respectively after 24 h culture with MCF-7 cells. The targeting multi-functional liposomes showed greater efficacy than the non-targeting liposomes and thus great potential to improve the cancer imaging and therapy. (C) 2012 Elsevier Ltd. All rights reserved.