Malignant brain tumors significantly cause morbidity and mortality in adults and children. Among the brain tumors, the highest prognosis glioma brain tumor is glioblastoma (GBM). The fatality of the GBM is gradually increasing due to the inability of surgical removal of the entire tumor, the poor blood-brain barrier (BBB) penetration of the active drugs at therapeutic levels, and the development of multidrug resistance (MDR). The Enhanced Permeability and Retention (EPR) effect enhances the accumulation of nanoparticles in the tumor tissues, which promotes the localization of nanoparticle drug delivery systems on the tumor by reducing drug side effects and enhancing the drug bio-availability and the tolerance. However, most of the nanoparticle drug delivery systems fail to treat GBM due to the lack of target specificity. Therefore, the goal of this study is to deliver two DNA annihilating chemotherapeutic drugs to the nucleus of the GBM tumors while promoting the receptor-mediated endocytosis with the help of IL-13Ra2 receptor, which is only overexpressed in GBM tumors. Long-chain peptide 1 (lnPep1) and short-chain peptide 1 (shPep1) was conjugated to nanoparticle carbon dots via an amide linkage, to facilitate the receptor and the nucleus binding respectively. The two chemotherapeutic drugs of temozolomide and epirubicin were conjugated to the peptide-loaded carbon dots. The <i>in vitro</i> synergistic cytotoxicity effect of epirubicin and temozolomide was 86%, as analyzed in our previous study. The in vitro cytotoxicity studies and the nucleus targeting images were acquired with GBM tumors of SJGBM2, CHLA266, CHLA200, and U87.

Peptide conjugated multipurpose carbon dots as nano-cargoes for glioblastoma brain tumors

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.