Antibody-Functionalized Porous Silicon Nanoparticles for Vectorization of Hydrophobic Drugs

We describe the preparation of biodegradable porous silicon nanoparticles (pSiNP) functionalized with cancer cell targeting antibodies and loaded with the hydrophobic anti-cancer drug camptothecin. Orientated immobilization of the antibody on the pSiNP is achieved using novel semicarbazide based bioconjugate chemistry. To demonstrate the generality of this targeting approach, the three antibodies MLR2, mAb528 and Rituximab are used, which target neuroblastoma, glioblastoma and B lymphoma cells, respectively. Successful targeting is demonstrated by means of flow cytometry and immunocytochemistry both with cell lines and primary cells. Cell viability assays after incubation with pSiNPs show selective killing of cells expressing the receptor corresponding to the antibody attached on the pSiNP. Mesoporous silicon nanoparticles that are able to specifically target and deliver hydrophobic anti-cancer drugs to cancer cells are developed. Porous silicon nanoparticles are functionalized with antibodies in a controlled way, in order to efficiently target cancer cells expressing the corresponding receptor. High targeting and killing efficiency is demonstrated in vitro on three types on cancer cells: neuroblastoma, glioblastoma and lymphoma cells.