Anticarcinogenic activity of blue fluorescent hexagonal boron nitride quantum dots: as an effective enhancer for DNA cleavage activity of anticancer drug doxorubicin (2025)

New Unsymmetrical Bisacridine Derivatives Noncovalently Attached to Quaternary Quantum Dots Improve Cancer Therapy by Enhancing Cytotoxicity toward Cancer Cells and Protecting Normal Cells

ACS Applied Materials & Interfaces, 2020

The use of nanoparticles for the controlled drug delivery to cells has emerged as a good alternative to traditional systemic delivery. Quantum dots (QDs) offer potentially invaluable societal benefits such as drug targeting and in vivo biomedical imaging. In contrast, QDs may also pose risks to human health and the environment under certain conditions. Here, we demonstrated that a unique combination of nanocrystals core components (Ag-In-Zn-S) would eliminate the toxicity problem and increase their biomedical applications. The alloyed quaternary nanocrystals Ag-In-Zn-S (QD green , Ag 1.0 In 1.2 Zn 5.6 S 9.4 ; QD red , Ag 1.0 In 1.0 Zn 1.0 S 3.5) were used to transport new unsymmetrical bisacridine derivatives (UAs, C-2028 and C-2045) into lung H460 and colon HCT116 cancer cells for improving the cytotoxic and antitumor action of these compounds. UAs were coupled with QD through physical adsorption. The obtained results clearly indicate that the synthesized nanoconjugates exhibited higher cytotoxic activity than unbound compounds, especially toward lung H460 cancer cells. Importantly, unsymmetrical bisacridines noncovalently attached to QD strongly protect normal cells from the drug action. It is worth pointing out that QD green or QD red without UAs did not influence the growth of cancer and normal cells, which is consistent with in vivo results. In noncellular systems, at pH 5.5 and 4.0, which relates to the conditions of endosomes and lysosomes, the UAs were released from QD-UAs nanoconjugates. An increase of total lysosomes content was observed in H460 cells treated with QDs-UAs which can affect the release of the UAs from the conjugates. Moreover, confocal laser scanning microscopy analyses revealed that QD-UAs nanoconjugates enter H460 cells more efficiently than to HCT116 and normal cells, which may be the reason for their higher cytotoxicity against lung cancer. Summarizing, the noncovalent attachment of UAs to QDs increases the therapeutic efficiency of UAs by improving cytotoxicity toward lung H460 cancer cells and having protecting effects on normal cells.

A Facile Approach for Doxorubicine Delivery in Cancer Cells by Responsive and Fluorescent Core/Shell Quantum Dots

Bioconjugate Chem, 2018

Biocompatible thermoresponsive copolymers based on 2-(2- methoxyethoxy) ethyl methacrylate (MEO2MA) and oligo (ethylene glycol) methacrylate (OEGMA) were grown from the surface of ZnO quantum dots (QDs) by surface initiated atom transfer radical polymerization with activators regenerated by electron transfer (SI-ARGET ATRP) in order to design smart and fluorescent core/shell nanosystems to be used toward cancer cells. Tunable lower critical solution temperature (LCST) values were obtained and studied in water and in culture medium. The complete efficiency of the process was demonstrated by the combination of spectroscopic and microscopic studies. The colloidal behavior of the ZnO/ copolymer core/shell QDs in water and in physiological media with temperature was assessed. Finally, the cytotoxicity toward human colon cancer HT29 cells of the core/shell QDs was tested. The results showed that the polymer-capped QDs exhibited almost no toxicity at concentrations up to 12.5 μg.mL−1, while when loaded with doxorubicin hydrochloride (DOX), a higher cytotoxicity and a decreased HT29 cancer cell viability in a short time were observed.

Oxidative Synthesis of Highly Fluorescent Boron/Nitrogen Co-Doped Carbon Nanodots Enabling Detection of Photosensitizer and Carcinogenic Dye

Current research efforts have demonstrated the facile hydrothermal oxidative synthetic route to develop highly fluorescent boron/nitrogen co-doped carbon nanodots (CNDs). During this process, N-(4-hydroxyphenyl)glycine served as a source of N doping and a carbon precursor as well, while boric acid H 3 BO 3 is used as an oxidizing agent in the N 2 environment. Surface passivation through ultrasonic treatment of CNDs was performed to induce modifications by using various surface passivating agents. Polyethyleneimine (PEI) remarkably enhanced the fluorescence performance and monodispersity of polymerized carbon nanodots (P-CNDs) in aqueous phase with an enhanced quantum yield of 23.71%, along with an increase in size from ∼3 nm to ∼200 nm. For characterization of CNDs and P-CNDs, UV, infrared, photoluminescence, transmission electron microscopy, x-ray photo-electron spectra, and atomic force microscopy techniques were utilized. Application potentials of synthesized P-CNDs were developed via introduction of protoporphyrin (PPD, a photosensitizer) which has great doping affinity with polymer PEI to switch-off the fluorescence of P-CNDs, leading to the production of dye-doped nanoprobes. Fluorescence resonance energy transfer (FRET) was also observed during dye-doping, and PPD was detected with a limit of detection (LOD, 3σ) of 15 pM. The fluorescence recovery of this switched-off nanoprobe was made possible by using Sudan red III (carcinogenic dye), which was oxidized by PPD doped in P-CNDs. Sudan red III was detected in the concentration range of 9.9 pM−0.37 nM. Meanwhile, it was also confirmed that the dye-doped nanoprobe is highly selective and exceptionally sensitive to detect this carcinogenic agent in commercial products with a LOD (3σ) of 90 fM.

Applications of Quantum dots in Cancer Treatment

Today in the field of medical science, cancer has become the most discussed and most concerned subject. Due to the increasing death rate all over the world researches nowadays are mostly based on finding some cures for cancer and also understanding the causes of cancers. Quantum dots are the nano-sized crystals used for imaging and therapy of cancers because of their striking characteristic of high photobleaching resistance. Quantum dots (Qds) proved to be more successful various cancer imaging followed by therapies. Multicolor Qds could be used to detect multiple markers at a time. These crystallized nanosensors with more enhancements and more efforts could be made an accurate source for cancer treatment, in the form of drug carriers and photobleaching protection agents. They are also capable of certain toxic effects that are yet to be understood to overcome. Once proved to be more successful they would also be made available for medical treatments at affordable costs.

In Vivo Assessment of the Effect of Hexagonal Boron Nitride Nanoparticles on Biochemical, Histopathological, Oxidant and Antioxidant Status

Journal of Cluster Science, 2020

The aim of our study is to investigate the dose-dependent biological system effect of hexagonal boron nitride (hBN) nanoparticles, which is directly produced nanoscale, in vivo. Wistar albino rats (n = 80) weighing 200-250 g were divided into eight groups (n = 10). The acute effects of hBN NPs (i.v) on the rats were investigated by measuring the biochemical, hematological parameters and oxidant-antioxidant status. The results show that no significant change was observed in the hematological and biochemical parameters when the control group and other low dose groups were compared, except for the 1600 and 3200 lg/kg b.w. dose groups. Histological detection indicated that 1600 and 3200 lg/kg hBN NPs treatment could induce significant damage in the liver, kidney, heart, spleen and pancreas. With the findings obtained, it can be seen that hBN NPs cannot be evaluated independently of particle morphology, and that the hBN NPs used in this study may be suitable for biomedical applications where low doses between 50 and 800 lg/kg are not toxic.

Graphene quantum dots: Synthesis, characterization, cell viability, genotoxicity for biomedical applications

Saudi Pharmaceutical Journal

We report the synthesis and applications of a novel N-doped graphene quantum dots (GQDs) using hydrothermal reaction between citric acid and p-aminophenol. The synthesized N-doped GQDs have been characterized physico-chemically and evaluated its antioxidant, antimicrobial, DNA binding and cleavage activities. siRNA loading studies were performed and their effects on cells were evaluated. Obtained results indicate that monodisperse solution of N-doped GQDs has been obtained with particles size ca. $10.9 ± 1.3 nm. UV-Vis spectroscopy studies of the interactions between the N-doped GQDs and calf thymus DNA (CT-DNA) showed that the compound interact with CT-DNA via both intercalative and electrostatic binding. The DNA cleavage study showed that the N-doped GQDs cleaved DNA without any external agents. The antioxidant activity of N-doped GQDS was very active when compared to BHT. As the concentration of the compound increased, the antioxidant activity also increased. Cell viability assay demonstrated that the Ndoped GQDs showed cell viability (70%) when the concentration reached 200 lg/mL for A549 and also MDA-MB-231, 150 lg/mL for NIH-3T3 cell lines at 24 h incubation. Ndoped GQDs were coated with Eudragit RS 100 and EphA2-siRNA was loaded. As a result of the studies on these formulations, it was concluded that there may be significant effects on A549 cells. The microscopy results revealed that N-doped GQDs was quickly internalized into the cell. Our novel N-doped-GQDs with siRNA are candidate for in situ tumor suppression via DNA and mRNA breakage.

Fluorescent quantum dots: An insight on synthesis and potential biological application as drug carrier in cancer

Biochemistry and Biophysics Reports, 2021

Quantum dots (QDs) are nanocrystals of semiconducting material possessing quantum mechanical characteristics with capability to get conjugated with drug moieties. The particle size of QDs varies from 2 to 10 nm and can radiate a wide range of colours depending upon their size. Their wide and diverse usage of QDs across the world is due to their adaptable properties like large quantum yield, photostability, and adjustable emission spectrum. QDs are nanomaterials with inherent electrical characteristics that can be used as drug carrier vehicle and as a diagnostic in the field of nanomedicine. Scientists from various fields are aggressively working for the development of single platform that can sense, can produce a microscopic image and even be used to deliver a therapeutic agent. QDs are the fluorescent nano dots with which the possibilities of the drug delivery to a targeted site and its biomedical imaging can be explored. This review is mainly focused on the different process of synthesis of QDs, their application especially in the areas of malignancies and as a theranostic tool. The attempt is to consolidate the data available for the use of QDs in the biomedical applications.

In vitro investigation of the effects of boron nitride nanotubes and curcumin on DNA damage

Backround Stem cells provide an opportunity to analyse the effects of xenobiotic on cell viability, differentiation and cell functions. Evaluation of the possible cytotoxic and DNA damaging effects on bone marrow CD34 + stem cells is important for their ability to differentiate into blood cells, and also for bone marrow diseases therapy. Boron nitride nanotubes and curcumin are potential nanoformulation agents that can be used together in the treatment of cancer or bone marrow diseases. Therefore, it is important to evaluate their possible effects on different cell lines. Objectives In this study, it was aimed to evaluate the cytotoxic and DNA damaging effects of boron nitride nanotubes which are commonly used in pyroelectric, piezoelectric and optical applications, but there is not enough information about its biocompatibility. Also, it was intended to research the effects of curcumin being used frequently in treatment processes for antioxidant properties. Methods The possible cytotoxic and DNA damaging effects of boron nitride nanotubes and curcumin on CD34 + cells, HeLa and V79 cells were evaluated by MTT assay and Comet assay, respectively. Results and conclusion Boron nitride nanotubes and curcumin had cytotoxic effects and cause DNA damage on CD34 + cells, HeLa and V79 cells at several concentrations, probably because of increased ROS level. However, there were not concentrationdependent effect and there were controversial toxicity results of the studied cell lines. Its mechanism needs to be enlightened by further analysis for potential targeted drug development.

Fluorinated Boron Nitride Quantum Dots: A New 0D Material for Energy Conversion and Detection of Cellular Metabolism

Particle & Particle Systems Characterization, 2018

thermal, and magnetic properties are perceived. [3-5] When these 2D materials are further confined to atomic scale quantum dots (QDs), size less than the Bohr radius of charge carriers, the confinement in space raises their energy and the electronic states become discrete, exhibiting properties strikingly different from the bulk material. [6] QDs have higher surface to volume ratio than bulk material, making them highly sensitive to surface defects and adsorbates and opening a plethora of applications such as molecular sensing, drug loading, and catalysis. [7-9] The high surface area and large number of dangling bonds for anchoring surface adsorbates enable high-sensitivity molecular detection. [10-12] For graphene QDs in particular, the larger bandgap compared to the bulk leads to phonon-assisted slow relaxation of charge carriers enabling their separation, thus making them a desirable material for photocatalytic applications. [13] Next of kin to graphene, hexagonal boron nitride (h-BN) is acclaimed for its chemical and thermal stability and deep Quantum dots encompass a broad spectrum of optical, catalytic, and electrochemical properties bringing in novel applications in catalysis, imaging, displays, and optoelectronics. Herein, the unanticipated broad-spectrum light absorption and high fluorescence quantum yield in fluorinated boron nitride (FBN) quantum dots are discussed. A heterostructure of FBN quantum dots with a wide-bandgap semiconductor, titania nanotube arrays, exhibits high photocatalytic activity as evidenced by high external quantum efficiency extending from ultraviolet to green region of the solar spectrum (≈24% at 400 nm). The high activity is confirmed using photoelectrochemical hydrogen evolution experiments. Further, it is demonstrated that high fluorescence quantum yield could be tapped for the detection of glycolytic activity in cancer cells compared to normal cells. This finding could shift the paradigm of molecular detection using quantum dots. The 0D structure and the gap states introduced through fluorination are believed to be responsible for these unprecedented characteristics of boron nitride. Quantum Dots The inception of 2D materials marked by graphene brought several ambitious ideas into reality, primarily due to their unique properties provided by the absence of the third dimension for the lattice. [1,2] In the pool of different 2D materials having similar structure, a wide range of electronic, optical,

Quantum Dots: A New Hope for the Pharmaceutical Field

Journal of Drug Delivery and Therapeutics

Quantum dots (QDs) are nanoparticles that have been developed for a number of biological and biomedical applications, such as drug delivery and simultaneous imaging of several cells. As a result of their unique physicochemical features, QDs have shown remarkable potential in receptor-based targeting. Functionalized QDs (f-QDs) are nano-sized smart systems that can deliver a wide spectrum of bioactive. Surface modified fluorescent carbon QDs has received interest as a targeting ligand for achieving cellular targeting with increased specificity. Several surface-designed and conjugated fluorescent carbon QDs are currently being investigated for cancer treatment, and the results are awaited with bated breath. This review emphasizes different synthesis methods, their characterizations, and different applications of QDs in cancer therapies. Keywords: Quantum dots, Synthesis, Medical applications.