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论文类型：期刊论文
发表时间：2018-10-15
发表刊物：JOURNAL OF MOLECULAR LIQUIDS
收录刊物：SCIE
卷号：268
页面范围：77-86
ISSN号：0167-7322
关键字：MRI; Gd-DTPA-dialkylamine; Drug delivery; Vesicles; Self-assembly
摘要：Magnetic resonance imaging contrast agents (MRI CAs) are used to enhance the quality of MRI diagnosis. However, clinical CAs cannot meet the demand of early diagnosis of the disease. Herein, a series of novel amphiphilic Gd-DTPA-dialkylamines with different hydrophobic carbon chains (Gd-DTPA-Nn-n) were designed to self assemble into stable vesicles artful applicable to MRI. MS, H-1 NMR and FT-IR were employed to confirm the structures. Not only the vesicles of Gd-DTPA-Nn-n showed excellent surface activity and stability, but also Gd-DTPA-N16-16 presented lower cytotoxicity to MCF-7 and HL-7702 cells. Moreover, doxorubicin (DOX) was loaded into the hydrophilic cavity of vesicles with a high drug loading efficiency of over 67%. Interestingly, in vitro releasing could be controlled by adjusting pH. The DOX-loaded Gd-DTPA-N16-16 vesicles showed best anti-tumor effects against MCF-7 cells because of the facilitated release of DOX into the cytoplasm. The relaxivity of Gd-DTPA-N16-16 vesicles was four times better than the clinical CA Magnevist in vitro, meanwhile, Gd-DTPA-N6-16 could significantly enhance MRI imaging effect in the liver and kidneys of mice compared with Gd-DTPA. Therefore, the innovative amphiphilic molecular demonstrated a promising drug loaded vesicle for MRI CAs to achieve theranostic applications (i.e. combining therapeutic and diagnostic abilities in a single vector). (C) 2018 Elsevier B.V. All rights reserved.