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Indexed by:期刊论文

Date of Publication:2018-10-15

Journal:JOURNAL OF MOLECULAR LIQUIDS

Included Journals:SCIE

Volume:268

Page Number:77-86

ISSN No.:0167-7322

Key Words:MRI; Gd-DTPA-dialkylamine; Drug delivery; Vesicles; Self-assembly

Abstract: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.