Preparation and characterization of a dual-receptor mesoporous silica nanoparticle-hyaluronic acid-RGD peptide targeting drug delivery system

A dual-receptor targeting delivery system based on mesoporous silica nanoparticles modified with hyaluronic acid and RGD peptide (MSNs/NH2-HA-RGD) was developed in the present study, and characterized by TEM, SAXRD, nitrogen adsorption-desorption analysis, DLS, FT-IR, C-13 NMR and UV-vis. The results showed that MSNs/NH2-HA-RGD had an ideal monodispersibility, uniform particle size (172.5 +/- 10 nm) and well-defined mesoporous structure. Moreover, cellular uptake results showed that MSNs/NH2-HA-RGD had an ideal dual-receptor mediated endocytosis pathway and could be significantly internalized into ovarian cancer cells. Chlorambucil (CHL), an anticancer drug, was chosen as a model drug to investigate drug loading, in vitro drug release behaviors and cytotoxicity. The results showed that CHL-loaded MSNs/NH2-HA-RGD exhibited a high drug loading capacity of about 10.1% and pH-sensitive drug controlled release behaviors. The cytotoxicity test showed that CHL-loaded MSNs/NH2-HA-RGD had a stronger cytotoxicity for ovarian cancer cells than one receptor or no receptor modified MSNs. It is expected that MSNs/NH2-HA-RGD may be a prospective candidate for targeted delivery of anticancer drugs to cancer foci.