Carbon quantum dots (CDs) are a relatively new class of carbon nanomaterials which have been studied very much in the last fifteen years to improve their already favorable properties.
Most of the dual nano drug delivery systems fail to enter malignant brain tumors due to a lack of proper targeting systems and the size increase of the nanoparticles after drug conjugation. Therefore, a triple conjugated system was developed with carbon dots (C-dots), which have an average particle size of 1.5–1.7 nm. C-dots were conjugated with transferrin (the targeted ligand) and two anti-cancer drugs, epirubicin and temozolomide, to build the triple conjugated system in which the average particle size was increased only up to 3.5 nm. In vitro studies were performed with glioblastoma brain tumor cell lines SJGBM2, CHLA266, CHLA200 (pediatric) and U87 (adult). The efficacy of the triple conjugated system (dual drug conjugation along with transferrin) was compared to those of dual conjugated systems (single drug conjugation along with transferrin), non-transferrin C-dots–drugs, and free drug combinations. Transferrin conjugated samples displayed the lowest cell viability even at a lower concentration. Among the transferrin conjugated samples, the triple conjugated system (C-dots-trans-temo-epi (C-DT)) was more strongly cytotoxic to brain tumor cell lines than dual conjugated systems (C-dots-trans-temo (C-TT) and C-dots-trans-epi (C-ET)). C-DT increased the cytotoxicity to 86% in SJGBM2 at 0.01 μM while C-ET and C-TT reduced it only to 33 and 8%, respectively. Not only did triple conjugated C-DT increase the cytotoxicity, but also the two-drug combination in C-DT displayed a synergistic effect.
Carbon dots (CDs) have been widely studied since their discovery in 2004 as a green substitute of the traditional quantum dots due to their excellent photoluminescence (PL) and high biocompatibility. Meanwhile, polymers have increasingly become an important component for both synthesis and modification of CDs to provide polymeric matrix and enhance their PL property. Furthermore, critical analysis of composites of CDs and polymers has not been available. Herein, in this review, we summarized the use of polymers in the synthesis and functionalization of CDs, and the applications of these CDs in various fields.
The blood–brain barrier (BBB) is a main obstacle for drug delivery targeting the central nervous system (CNS) and treating Alzheimer's disease (AD). In order to enhance the efficiency of drug delivery without harming the BBB integrity, nanoparticle-mediated drug delivery has become a popular therapeutic strategy. Carbon dots (CDs) are one of the most promising and novel nanocarriers. In this study, amphiphilic yellow-emissive CDs (Y-CDs) were synthesized with an ultrasonication-mediated methodology using citric acid and o-phenylenediamine with a size of 3 nm that emit an excitation-independent yellow photoluminescence (PL). The content of primary amine and carboxyl groups on CDs was measured as 6.12 × 10−5 and 8.13 × 10−3 mmol mg−1, respectively, indicating the potential for small-molecule drug loading through bioconjugation. Confocal image analyses revealed that Y-CDs crossed the BBB of 5-day old wild-type zebrafish, most probably by passive diffusion due to the amphiphilicity of Y-CDs. And the amphiphilicity and BBB penetration ability didn't change when Y-CDs were coated with different hydrophilic molecules. Furthermore, Y-CDs were observed to enter cells to inhibit the overexpression of human amyloid precursor protein (APP) and β-amyloid (Aβ) which is a major factor responsible for AD pathology. Therefore, data suggest that Y-CDs have a great potential as nontoxic nanocarriers for drug delivery towards the CNS as well as a promising inhibiting agent of Aβ-related pathology of the AD.