Targeting cancer cells with biotin–dendrimer conjugates

Abstract: Star-burst dendrimers represent a superior carrier platform for targeted drug delivery. Partially acetylated generation 5 (G5) polyamidoamine (PAMAM) dendrimer was conjugated with the targeting moiety (biotin) and the imaging moiety (fluoresceinisothiocyanate, FITC), and the resulting dendrimer–biotin conjugate was characterized by 1H NMR, UV–vis spectrum. As revealed by flow cytometry and confocal microscopy, the bifunctional conjugate (dendrimer–biotin–FITC) exhibited much higher cellular uptake into HeLa cells than the conjugate without biotin. The uptake was energy-dependent, dose-dependent, and could be effectively blocked by dendrimer-conjugated biotin. Our results indicated that the biocompatible biotin–dendrimer conjugate might be a promising nano-platform for cancer therapy and cancer diagnosis. [Copyright &y& Elsevier]