Preparation and In Vitro Evaluation of a MRI Contrast Agent Based on Aptamer-Modified Gadolinium-Loaded Liposomes for Tumor Targeting

被引:18
|
作者
Zhang, Lan-Xin [1 ,2 ]
Li, Kun-Feng [1 ]
Wang, Huan [1 ,2 ]
Gu, Meng-Jie [1 ,2 ]
Liu, Li-Si [3 ]
Zheng, Zhuo-Zhao [3 ]
Han, Nan-Yin [1 ]
Yang, Zhen-Jun [1 ]
Fan, Tian-Yuan [1 ,2 ]
机构
[1] Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
[2] Peking Univ, Beijing Key Lab Mol Pharmaceut & New Drug Deliver, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
[3] Peking Univ, Dept Radiol, Hosp 3, Beijing 100191, Peoples R China
来源
AAPS PHARMSCITECH | 2017年 / 18卷 / 05期
关键词
aptamer; contrast agent; liposomes; magnetic resonance imaging; target; TENASCIN-C; DELIVERY-SYSTEMS; CANCER-TREATMENT; GBI-10;
D O I
10.1208/s12249-016-0600-5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this study was to prepare aptamer-modified liposomes loaded with gadolinium (Gd) to enhance the effective diagnosis for tumor by MRI. A modified GBI-10 (GBI-10(m)) was used to prepare targeted liposomes (G(m)Ls). Liposomes with GBI-10 aptamer (GLs) and without aptamer (non-targeted liposomes (NLs)) were also prepared as controls. The particle size and zeta potential of G(m)Ls, GLs, and NLs were all assayed. A clinical 3.0 T MR scanner was employed to assess the imaging efficiency and measure the longitudinal relaxivity (r (1)) of the above liposomes. Confocal laser scanning microscopy and flow cytometry were used to analyze and compare the targeting effects of G(m)Ls, GLs, and NLs to MDA-MB-435s cells at 37A degrees C. The particle size of the prepared liposomes was scattered at 100-200 nm, and their values of r (1) were similar to 4 mM(-1) s(-1). The images of confocal laser scanning microscopy showed that G(m)Ls in the cytoplasm were significantly more than GLs and both G(m)Ls and GLs were more than NLs. The fluorescence intensity of G(m)Ls was increased by about two times than that of GLs and three times than that of NLs by flow cytometry. Therefore, the G(m)Ls in this initial study were suggested to be a potential MRI contrast agent at 37A degrees C for diagnosing tumors with the protein of tenascin-C over-expressed.
引用
收藏
页码:1564 / 1571
页数:8
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