۱- Introduction

۲- Material and methods

۳- Results and discussion

۴- Conclusions

References

Abstract

Mesoporous silica nanoparticles with folic acid (MSN−COOH-Tet-HBP-FA) are able to mediate targeting and have a pH stimulation response character, and therefore have been successfully synthesized as vectors for antitumor drug delivery. The model drug is tetrandrine (Tet). The chemical structure and properties of these NPs were characterized through systematic characterization analyses. Their drug loading capacity was significantly improved through carboxy modification (26.86 % in max), and they exhibited pH-dependent drug release profiles(“zero pre-release” within 20 h in a normal physiological environment). In vitro cytotoxicity and cell uptake of the as-synthesized NPs in Hela and A549 cells were also evaluated, and exhibited high cytotoxicity and cell-targeted uptake capacity. It was concluded that MSN−COOH-Tet-HBP-FA could be used as a promising drug delivery system for cancer therapy.

Introduction

Cancer is currently considered to be a leading factor that threatens human lives, and chemotherapy remains one of the most common methods used for cancer treatment. However, traditional drugs are nonspecific and cannot discriminate cancer cells and normal cells, which not only limits the accumulation of drugs in tumor cells, but also leads to systemic toxicity and adverse side effects. In order to improve the efficacy of chemotherapy, many studies have been devoted to the development of tumor-targeted nanocarriers, which can be used to control the delivery of antitumor drugs. Using the enhanced permeation and retention (EPR) effects, researchers have developed multiple nanocarrier platforms, including liposomes, polymer nanoparticles, nano-micelles, and dendrimers, which are used to delivery anticancer drugs into tumor tissues. However, the EPR effect is not efficient enough to eradicate the side effects of cytotoxic drugs and to exert the anticancer therapy selectively in cancer cells. In order to enhance the targeting and tumoral uptake ability, the external surface of nanocarrier is often modified with various ligands, which can significantly enhance the interaction between the cancer cells and the nanocarriers[. Targeted agents typically include antibodies (such as monoclonal antibodies), peptides (such as Arg-Gly-Asp (RGD)), and small molecule compounds (such as folic acid).