Functional nanoparticles of tea polyphenols for doxorubicin delivery in cancer treatment.

Abstract

Nanoparticulate pharmaceutical drug delivery systems (NDDSs) are widely used to enhance the effectiveness and to decrease the side effects of chemotherapeutic drugs. Owing to the complex multistep synthesis process, expensive or not safe constituents, clinical applications of NDDSs have severely been constrained. Green tea polyphenols (TPs) are well recognized for their beneficial health effects, including anticancer activity. Herein, we reported the sole use of tea polyphenols to fabricate TP nanoparticles for chemo-drug delivery in cancer treatment. The TP nanoparticles (TP-NPs) with diameters of 100-130 nm, exhibited a high doxorubicin hydrochloride (DOX·HCl) loading capability. The DOX loaded TP-NPs (DOX@TP-NPs) were glutathione (GSH)- and pH-responsive for the release of DOX. In vitro cell experiments showed higher cancer cell inhibition rates of DOX@TP-NPs compared to the free drug on both HT-29 cells and HeLa cells, possibly due to induced accumulation of reactive oxygen species and decreasing mitochondrial membrane potential. Animal studies further confirmed that efficient accumulation and retention of DOX in the tumor site were achieved with the DOX@TP-NP formulation, resulting in enhanced anticancer efficacy with negligible systemic toxicity. The simply-prepared TP nanoparticles as functional nanocarriers for therapeutic agents are promising in cancer treatment.