Multi-functionalized graphene oxide based anticancer drug-carrier with dual-targeting function and pH-sensitivity

TLDR

The study develops a dual‑targeting, pH‑responsive graphene oxide drug‑carrier to improve targeted anticancer delivery and enable controlled release. The carrier was fabricated by chemically precipitating Fe₃O₄ onto GO, functionalizing with folic acid via APS linkage, loading doxorubicin through π–π stacking, and its uptake was assessed using fluorescent labeling. The multifunctional GO achieved a loading capacity of 0.387 mg mg⁻¹, released doxorubicin in a pH‑dependent manner, and demonstrated promising targeted delivery and controlled release in tumor cells.

Abstract

A dual-targeting drug delivery and pH-sensitive controlled release system based on multi-functionalized graphene oxide (GO) was established in order to enhance the effect of targeted drug delivery and realize intelligently controlled release. A superparamagnetic GO–Fe3O4 nanohybrid was firstly prepared via a simple and effective chemical precipitation method. Then folic acid, a targeting agent toward some tumor cells, was conjugated onto Fe3O4 nanoparticlesvia the chemical linkage with amino groups of the 3-aminopropyl triethoxysilane (APS) modified superparamagnetic GO–Fe3O4 nanohybrid, to give the multi-functionalized GO. Doxorubicin hydrochloride (Dox) as an anti-tumor drug model was loaded onto the surface of this multi-functionalized GO via π–π stacking. The drug loading capacity of this multi-functionalized GO is as high as 0.387 mg mg−1 and the drug release depends strongly on pH values. Cell uptake studies were carried out using fluorescein isothiocyanate labeled or Dox loaded multi-functionalized GO to evaluate their targeted delivery property and toxicity to tumor cells. The results show that this multi-functionalized GO has potential applications for targeted delivery and the controlled release of anticancer drugs.