Investigations on surface modified dendrimers: enzymatic hydrolysis and uptake into MCF-7 breast cancer cells.
A series of G(0) and G(1) generation 1,3,5-tris(3-aminopropyl)benzene dendrimers surface modified with the amino acids phenylalanine (Phe), methionine (Met), aspartic acid (Asp), and diaminopropionic acid (Dap) was investigated with regard to their stability against enzymatic hydrolysis with the model enzymes papain, chymotrypsin, trypsin, and pepsin. Additionally, the cytosol of MCF-7 cells was used to get an insight into the possible degradation in intracellular medium. The cytosol, chymotrypsin, and papain had similar activities on the tested dendrimers and efficiently cleaved methionine and phenylalanine from the surface of the dendrimers. The cellular uptake of the dendrimers into the MCF-7 cells depended on the surface modification (Phe>Met unmodified>>Dap=Asp) and the generations (G(0)>G(1)).
Kapp
Timo
T
Institute of Pharmacy Free University of Berlin, Königin Luise Strasse 2+4, 14195 Berlin, Germany.
Francke
Peter
P
Gust
Ronald
R
D001943:Breast Neoplasms / Q000378:metabolism; D045744:Cell Line, Tumor; D003600:Cytosol / Q000378:metabolism; D050091:Dendrimers / Q000737:chemistry* / Q000378:metabolism; D016503:Drug Delivery Systems; D019075:Electrophoresis, Capillary; D005260:Female; D006801:Humans; D006868:Hydrolysis; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
D050091:Dendrimers