Encapsulation of a potential anticancer drug within multifunctional poly(amidoamine) dendrimers for targeted inhibition of cancer cells

摘要

Poly(amidoamine) (PAMAM) dendrimer-based multifunctional drug delivery carrier has been designed and synthesized by modifying the periphery primary amine groups of generation 5 (G5) PAMAM dendrimer with fluorescein isothiocyanate (FI, an imaging agent) and folic acid (FA, a targeting agent), followed by acetylation of the remaining amine groups (G5.NHAc-FI-FA). 2-Methoxyoestradiol (2-ME), a potential anticancer drug, was encapsulated within the synthesized multifunctional dendrimers. In vitro cytotoxicity results showed that G5.NHAc-FI-FA/2-ME complexes displayed similar therapeutic activity to that of pure drug. More importantly, G5.NHAc-FI-FA/2-ME complexes were able to specifically inhibit the growth of cancer cells overexpressing folic acid receptors. It indicates that multifunctional dendrimer nanodevices are promising drug carriers for targeted cancer therapy.