TRASTUZUMAB-DENDRIMER-FLUORINE DRUG DELIVERY SYSTEM

被引:2
|
作者
Bartusik-Aebisher, Dorota [1 ]
机构
[1] Univ Rzeszow, Med Coll, Dept Biochem & Gen Chem, Rzeszow, Poland
来源
ACTA POLONIAE PHARMACEUTICA | 2020年 / 77卷 / 02期
关键词
Trastuzumab; drug delivery system; Her-2; receptor; fluorine; PAMAM-G5; BREAST-CANCER CELLS; RECEPTOR; ANTIBODY;
D O I
10.32383/appdr/118740
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Breast cancer is the most frequently occurring cancer in women worldwide with more than one million new cases diagnosed each year. The objective of this study was to develop a Trastuzumab-dendrimer-fluorine drug delivery system by covalent attachment of Trastuzumab to a fluorinated PAMAM-G5 dendrimer. The Trastuzumab-dendrimer-fluorine drug delivery system was used to treat MCF-7 with Her-2 overexpression. The use of PAMAM-G5, which bears 128 primary amine surface groups, enables covalent attachment of both antibody and fluorinated functional groups for enhancement of cellular uptake. Thus, Trastuzumab was covalently attached to fluorinated PAMAM-G5 dendrimers and used as a vehicle for drug delivery to three dimensional (3D) cultured cells. The efficiency of Trastuzumab-dendrimer-fluorine drug delivery system binding to Her-2 receptors was measured by cell viability. The Trastuzumab-dendrimer-fluorine drug delivery system was found to have a higher efficiency in the treatment of Her-2 overexpressing MCF-7 cells than Trastuzumab alone. The incorporation of 'I' by addition of heptatluorobutyric acid anhydride (HFAA) to PAMAM-G5 increased lipophilicity and hydrophobicity of the drug delivery system.
引用
收藏
页码:331 / 341
页数:11
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