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Trastuzumab-dendrimer-fluorine drug delivery system

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Bartusik-Aebisher D.

Acta Poloniae Pharmaceutica - Drug Research

2020

vol. 77

issue 2

331-341

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 19F by addition of heptafluorobutyric acid anhydride (HFAA) to PAMAM-G5 increased lipophilicity and hydrophobicity of drug delivery system.

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1 Acta Poloniae Pharmaceutica - Drug Research

1 2020

1 Bartusik-Aebisher D.

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Trastuzumab-dendrimer-fluorine drug delivery system