Folate-Receptor-Targeted Gold Nanoparticles Bearing a DNA-Binding Anthraquinone

In recent years, anthraquinones have been widening their therapeutic opportunities given their numerous health benefits. The search for adequate delivery platforms to improve their pharmacokinetics leads us to propose herein folate-capped gold nanoparticles with an anthraquinone derivative attached onto their surface. Through a straightforward, two-step procedure, we obtained stable nanoparticles that can deliver anthraquinones selectively to cells overexpressing folate receptors. The new conjugates were highly toxic against two tumour cell lines, lung carcinoma A549 and cervical carcinoma HeLa, and showed significant in vitro targeting effects for FR+ HeLa cells. We anticipate that the convenience of this synthetic procedure could enable the future development of folate-targeted conjugates bearing highly active anthraquinone-derived drugs.