Investigation of the strategies for targeting of the afterglow nanoparticles to tumor cells

• AG NPs were conjugated with biomolecules to investigate cancer cells targeting.
• Cellular uptake and targeting of AG NPs enhanced by conjugation to biomolecules.
• It was also shown that the cellular uptake is receptor dependent.
• R11 peptide is preferable as it has high specificity for prostate cancer targeting.
• For breast cancer targeting, the RGD peptide used here is highly recommended.

Afterglow nanoparticles have been widely investigated as new agents for cancer imaging and as a light source for photodynamic activation for cancer treatment. For both applications, the targeting of the afterglow nanoparticles to tumor cells is an important and challenging issue. Here we report the strategies for targeting Sr3MgSi2O8:Eu2+,Dy3+ afterglow nanoparticles to tumor cells by conjugating with variety of targeting molecules such as folic acid, RGD peptide, and R-11 peptide. For folic acid targeting, experimental observations were conducted on PC-3 cells (folate receptor negative), MCF-7 (folate receptor positive), and KB cells (folate receptor positive) to compare the cellular uptake and confirm targeted delivery. For the cyclic RGDfK peptide, experiments were carried out on the integrin αvβ3 positive MDA-MB-231 breast cancer cell line and the integrin αvβ3 negative MCF-7 breast cancer cell lines in order to compare the cellular uptakes. As for R11-SH peptide, cellular uptake of the afterglow nanoparticles was observed on LNCaP and PC3 prostate cancer cell lines. All the observations showed that the cellular uptakes of the nanoparticles were enhanced by conjugation to variety of targeting molecules which are specific for breast and prostate cancer cells.