Folate-conjugated hybrid SBA-15 particles for targeted anticancer drug delivery

Surface functionalization is one of the key steps toward the utilization of mesoporous materials in drug delivery system. Here, the folic acid (FA) ligands are conjugated onto poly(ethylene imine) (PEI) modified SBA-15 particles (PEI/SBA-15) via amide reaction, which results in the FA/PEI/SBA-15 particles. Doxorubicin hydrochloride (DOX), an anticancer drug, is successfully loaded into these particles. The in vitro cytotoxicity and cellular uptake of the empty FA/PEI/SBA-15 particles and the DOX-loaded ones are evaluated on two kinds of cancer cells (HeLa cells and A549 cells). Specifically, an excellent cellular uptake using the current anticancer drug delivery vehicles (DOX-loaded FA/PEI/SBA-15 particles) mediated by the FA receptor is demonstrated by fluorescence microscope and flow cytometry. The FA/PEI/SBA-15 particles demonstrate a lower cytotoxicity comparing with the PEI/SBA-15 particles, while the DOX-loaded FA/PEI/SBA-15 particles exhibit much greater inhibition to the studied cancer cells. Furthermore, the in vitro release study shows that the targeted FA/PEI/SBA-15 particles have a typical sustained release behavior. This work therefore demonstrates that drug-loaded FA/PEI/SBA-15 particles have great potential application in targeted anticancer drug delivery for cancer therapy.

Graphical abstractDOX-loaded folate-conjugated mesoporous silica particles (DOX-FA/PEI/SBA-15 particles) are prepared and the cellular uptake and in vitro cytotoxicity are evaluated on A549 cells and HeLa cells.Figure optionsDownload full-size imageDownload high-quality image (84 K)Download as PowerPoint slideHighlights► Cellular uptake and cytotoxicity of functionalized silica particles are evaluated. ► Excellent cellular uptake using the current drug delivery vehicles is demonstrated. ► The particles show promising applications in targeted anticancer drug delivery.