Among the large variety of subcellular organelles, the nucleus is a major target for macromolecules and nanoparticles, with potential diagnostic and therapeutic applications, because the genetic information of the cell and its transcription machinery reside there. Novel therapeutic strategies (for example, gene therapy), enabled by safe and efficient delivery of drug molecules and nanoparticles into the nucleus, are heralded by many as the ultimate treatment for severe and intractable diseases. However, most nanomaterials and macromolecules are incapable of reaching the cell nucleus on their own, because of biological barriers carefully honed by evolution: the cellular membrane and the nuclear envelope. In this presentation, we have demonstrated an approach of fabrication of biocompatible gold nanoparticle-based vehicles which can enter into cancer cell nucleus via optimization of conjugation of  both PEG 5000 and two different peptides (RGD and nuclear localization signal (NLS) peptide) to gold nanoparticles by independently adjusting amounts of PEG and two different peptides bound onto surface of gold nanoparticles so as to maximize their nuclear targeting performance and biocompatibility regarding the cell line of interest. Both optical microscopy and transmission electron microscopy (TEM) are used to confirm the targeted nuclear delivery of such peptide-conjugated biocompatible gold nanoparticles by showing their presence in the cancer cell nucleus.

Optimization of peptide conjugation onto partially PEGylated gold nanoparticles for their delivery into cancer cell nuclei

246th National Meeting (2013)

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