Search Results (106)

Background: The design of multifunctional carbon based nanosystems exhibiting light-triggered hyperthermia, emission, low cytotoxicity, and drug delivery capability is of significant interest in the area of nanomaterials. In this study, we present red-emitting and photothermal carbon nanodots (Cdots-βCD/PTC) obtained by the encapsulation of hydrophobic pentacene (PTC) within Carbon nanodots (Cdots) synthesized from beta-cyclodextrin (βCD). Methods: The prepared nanostructures were investigated in terms of morphology, size, and optical properties, by absorption and emission optical spectroscopy, atomic force microscopy, dynamics light scattering, Z-potential, nuclear magnetic resonance, and infra-red spectroscopy. Molecular modelling simulation was used to investigate the geometry and the stabilization energy of the Cdots-βCD/PTC inclusion complex. Results: The as prepared Cdots-βCD/PTC demonstrated good water dispersibility, green-emission (ϕ_PL = 1.7%), and photothermal conversion (η = 17.4%) upon red-light excitation (680 nm). Furthermore, Cdots-βCD/PTC low cytotoxicity in the range 0.008 μg–0.8 μg and good interaction with albumin protein (K_SV = 2.78 ± 0.28 mL mg⁻¹) were demonstrated. Molecular simulation analysis revealed the formation of the inclusion complex with an energy of −5.32 kcal mol⁻¹, where PTC is orthogonally oriented in the βCD cavity. Conclusions: The results presented in this work highlight the potential of Cdots-βCD/PTC as a novel versatile nanosystem for biomedical applications, such as bioimaging and site-specific photothermal treatment of cancer cells. Full article

BODIPY (Boron-Dipyrromethene) dyes have emerged as versatile fluorescent probes in cellular imaging and therapeutic applications owing to their unique chemical properties, including high fluorescence quantum yield, strong extinction coefficients, and remarkable photostability. This review synthesizes the recent advancements in BODIPY dyes, focusing on their deployment in biological imaging and therapy. The exceptional ability of BODIPY dyes to selectively stain cellular structures enables precise visualization of lipids, proteins, and nucleic acids within live and tumor cells, thereby facilitating enhanced understanding of biochemical processes. Moreover, BODIPY derivatives are increasingly utilized in Photodynamic therapy (PDT) and Photothermal therapies (PTT) for targeting cancer cells, where their capability to generate cytotoxic reactive oxygen species upon light activation offers a promising approach to tumor treatment. Recently, BODIPY derivatives have been used for Boron Neutron Capture Therapy (BNCT) for various tumors, and it is a growing research field. Advancements in nanotechnology have allowed the fabrication of BODIPY dye-based nanomedicines, either alone or with the use of metallic nanoparticles as a matrix offering the development of a new class of bioimaging and theragnostic agents. This review also discusses innovative BODIPY-based formulations and strategies that amplify therapeutic efficacy while minimizing adverse effects, underscoring the potential of these dyes as integral components in next-generation diagnostic and therapeutic modalities. By summarizing current research and future perspectives, this review highlights the critical importance of BODIPY dyes in advancing the fields of cellular imaging and treatment methodologies. Full article

Due to their structural features, macrocyclic compounds such as calixarenes, conjugated with a variety of fluorophores have led to the development of fluorescent probes for numerous applications. This review covers the recent advances (from 2009 to date) made in calixarene-based fluorescent sensors and their biological applications. In addition to the fluorescence mechanisms used to signal the analyte binding, this article focuses mainly on the detection of biological relevant ions, on the selective sensing of biomolecules, such as amino acids, enzymes, drugs and other organic compounds, and on intracellular imaging. Calixarene-containing fluorescent nanoparticles and nanoaggregates for imaging and drug delivery are also described. Finally, this review presents some conclusions and future perspectives in this field. Full article

Silver nanoparticles (NPs) have become highly promising agents in the field of biomedical science, offering wide therapeutic potential due to their unique physicochemical properties. The unique characteristics of silver NPs, such as their higher surface-area-to-volume ratio, make them ideal for a variety of biological applications. They are easily processed thanks to their large surface area, strong surface plasmon resonance (SPR), stable nature, and multifunctionality. With an emphasis on the mechanisms of action, efficacy, and prospective advantages of silver NPs, this review attempts to give a thorough overview of the numerous biological applications of these particles. The utilization of silver NPs in diagnostics, such as bioimaging and biosensing, as well as their functions in therapeutic interventions such as antimicrobial therapies, cancer therapy, diabetes treatment, bone repair, and wound healing, are investigated. The underlying processes by which silver NPs exercise their effects, such as oxidative stress induction, apoptosis, and microbial cell membrane rupture, are explored. Furthermore, toxicological concerns and regulatory issues are discussed, as well as the present difficulties and restrictions related to the application of silver NPs in medicine. Full article

The design and development of fluorescent materials for detecting cancer-related enzymes are crucial for cancer diagnosis and treatment. Herein, we present a substituted rhodamine derivative for the chromogenic and fluorogenic detection of the cancer-relevant enzyme γ-glutamyltranspeptidase (GGT). Initially, the probe is non-chromic and non-emissive due to its spirolactam form, which hinders extensive electronic delocalization over broader pathway. However, selective enzymatic cleavage of the side-coupled group triggers spirolactam ring opening, resulting in electronic flow across the rhodamine skeleton, and reduces the band gap for low-energy electronic transitions. This transformation turns the reaction mixture from colorless to intense pink, with prominent UV and fluorescence bands. The sensor’s selectivity was tested against various human enzymes, including urease, alkaline phosphatase, acetylcholinesterase, tyrosinase, and cyclooxygenase, and showed no response. Absorption and fluorescence titration analyses of the probe upon incremental addition of GGT into the probe solution revealed a consistent increase in both absorption and emission spectra, along with intensified pink coloration. The cellular toxicity of the receptor was evaluated using the MTT assay, and bioimaging analysis was performed on BHK-21 cells, which produced bright red fluorescence, demonstrating the probe’s excellent cell penetration and digestion capabilities for intracellular analytical detection. Molecular docking results supported the fact that probe-4 made stable interactions with the GGT active site residues. Full article

Backgroung: The rising complexity and associated side effects of cancer treatments highlight the need for safer and more effective therapeutic agents. Carbon-based nanomaterials such as CDs have been gaining prominence for their unique characteristics, opening avenues for diverse applications such as fluorescence imaging, drug and gene transport, controlled drug delivery, medical diagnosis, and biosensing. Despite promising advancements in research, it remains imperative to scrutinize the properties and potential cytotoxicity of newly developed CDs, ensuring their viability for these applications. Methods: We synthesized four N-doped CDs through a hydrothermal method. Cell viability assays were conducted on A549 and UM-UC-5 cancer cells at a range of concentrations and incubation times, both individually and with the chemotherapeutic agent 5-fluorouracil (5-FU). Results: The obtained results suggest that the newly developed CDs exhibit suitability for applications such as bioimaging, as no significant impact on cell viability was observed for CDs alone. Full article

The combination of photodynamic therapy (PDT) and pneumatotherapy is emerging as one of the most effective strategies for increasing cancer treatment efficacy while minimizing side effects. Photodynamic forces affect nitric oxide (NO) levels as activated photosensitizers produce NO, and NO levels in the tumor and microenvironment directly impact tumor cell responsiveness to PDT. In this paper, 3-benzenesulfonyl-4-(1-hydroxy ether)-1,2,5-oxadiazole-2-oxide NO donor–silicon phthalocyanine coupling (SiPc–NO) was designed and prepared into self-assembled nanoparticles (SiPc–NO@NPs) by precipitation method. By further introducing arginyl-glycyl-aspartic acid (RGD) on the surface of nanoparticles, NO-photosensitizer delivery systems (SiPc–NO@RGD NPs) with photo-responsive and tumor-targeting properties were finally prepared and preliminarily evaluated in terms of their formulation properties, NO release, and photosensitizing effects. Furthermore, high reactive oxygen species (ROS) generation efficiency and high PDT efficiency in two breast cancer cell lines (human MCF-7 and mouse 4T1) under irradiation were also demonstrated. The novel SiPc–NO@RGD NPs show great potential for application in NO delivery and two-photon bioimaging-guided photodynamic tumor therapy. Full article

Upconversion nanoparticles (UCNPs) are well-reported for bioimaging. However, their applications are limited by low luminescence intensity. To enhance the intensity, often the UCNPs are coated with macromolecules or excited with high laser power, which is detrimental to their long-term biological applications. Herein, we report a novel approach to prepare co-doped CaF₂:Yb³⁺ (20%), Er³⁺ with varying concentrations of Er (2%, 2.5%, 3%, and 5%) at ambient temperature with minimal surfactant and high-pressure homogenization. Strong luminescence and effective red emission of the UCNPs were seen even at low power and without functionalization. X-ray diffraction (XRD) of UCNPs revealed the formation of highly crystalline, single-phase cubic fluorite-type nanostructures, and transmission electron microscopy (TEM) showed co-doped UCNPs are of $~$12 nm. The successful doping of Yb and Er was evident from TEM–energy dispersive X-ray analysis (TEM-EDAX) and X-ray photoelectron spectroscopy (XPS) studies. Photoluminescence studies of UCNPs revealed the effect of phonon coupling between host lattice (CaF₂), sensitizer (Yb³⁺), and activator (Er³⁺). They exhibited tunable upconversion luminescence (UCL) under irradiation of near-infrared (NIR) light (980 nm) at low laser powers (0.28–0.7 W). The UCL properties increased until 3% doping of Er³⁺ ions, after which quenching of UCL was observed with higher Er³⁺ ion concentration, probably due to non-radiative energy transfer and cross-relaxation between Yb³⁺-Er³⁺ and Er³⁺-Er³⁺ ions. The decay studies aligned with the above observation and showed the dependence of UCL on Er³⁺ concentration. Further, the UCNPs exhibited strong red emission under irradiation of 980 nm light and retained their red luminescence upon internalization into cancer cell lines, as evident from confocal microscopic imaging. The present study demonstrated an effective approach to designing UCNPs with tunable luminescence properties and their capability for cellular imaging under low laser power. Full article

Numerous human adenovirus (AdV) types are endowed with arginine–glycine–aspartic acid (RGD) sequences that enable them to recognize vitronectin-binding (αv) integrins. These RGD-binding cell receptors mediate AdV entry into host cells, a crucial early step in virus infection. Integrin interactions with adenoviruses not only initiate receptor-mediated endocytosis but also facilitate AdV capsid disassembly, a prerequisite for membrane penetration by AdV protein VI. This review discusses fundamental aspects of AdV–host interactions mediated by integrins. Recent efforts to re-engineer AdV vectors and non-viral nanoparticles to target αv integrins for bioimaging and the eradication of cancer cells will also be discussed. Full article

(1) Background: Despite the encouraging indications regarding the suitability (biocompatibility) of iron carbide nanoparticles (ICNPs) in various biomedical applications, the published evidence of their biosafety is dispersed and relatively sparse. The present review synthesizes the existing nanotoxicological data from in vitro studies relevant to the diagnosis and treatment of cancer. (2) Methods: A systematic review was performed in electronic databases (PubMed, Scopus, and Wiley Online Library) on December 2023, searching for toxicity assessments of ICNPs of different sizes, coatings, and surface modifications investigated in immortalized human and murine cell lines. The risk of bias in the studies was assessed using the ToxRTool for in vitro studies. (3) Results: Among the selected studies (n = 22), cell viability emerged as the most frequently assessed cellular-level toxicity endpoint. The results of the meta-analysis showed that cell models treated with ICNPs had a reduced cell viability (SMD = −2.531; 95% CI: −2.959 to −2.109) compared to untreated samples. A subgroup analysis was performed due to the high magnitude of heterogeneity (I² = 77.1%), revealing that ICNP concentration and conjugated ligands are the factors that largely influence toxicity (p < 0.001). (4) Conclusions: A dose-dependent cytotoxicity of ICNP exposure was observed, regardless of the health status of the cell, tested organism, and NP size. Inconsistent reporting of ICNP physicochemical properties was noted, which hinders comparability among the studies. A comprehensive exploration of the available in vivo studies is required in future research to assess the safety of ICNPs’ use in bioimaging and cancer treatment. Full article

Fluorescent graphitic carbon nitride (g-C₃N₄) doped with various heteroatoms, such as B, P, and S, named ^Bg-C₃N₄, ^Pg-C₃N₄, and ^Sg-C₃N₄, were synthesized with variable band-gap values as diagnostic materials. Furthermore, they were embedded within hyaluronic acid (HA) microgels as g-C₃N₄@HA microgel composites. The g-C₃N₄@HA microgels had a 0.5–20 μm size range that is suitable for intravenous administration. Bare g-C₃N₄ showed excellent fluorescence ability with 360 nm excitation wavelength and 410–460 emission wavelengths for possible cell imaging application of g-C₃N₄@HA microgel composites as diagnostic agents. The g-C₃N₄@HA-based microgels were non-hemolytic, and no clotting effects on blood cells or cell toxicity on fibroblasts were observed at 1000 μg/mL concentration. In addition, approximately 70% cell viability for SKMEL-30 melanoma cells was seen with ^Sg-C₃N₄ and its HA microgel composites. The prepared g-C₃N₄@HA and ^Sg-C₃N₄@HA microgels were used in cell imaging because of their excellent penetration capability for healthy fibroblasts. Furthermore, g-C₃N₄-based materials did not interact with malignant cells, but their HA microgel composites had significant penetration capability linked to the binding function of HA with the cancerous cells. Flow cytometry analysis revealed that g-C₃N₄ and g-C₃N₄@HA microgel composites did not interfere with the viability of healthy fibroblast cells and provided fluorescence imaging without any staining while significantly decreasing the viability of cancerous cells. Overall, heteroatom-doped g-C₃N₄@HA microgel composites, especially ^Sg-C₃N₄@HA microgels, can be safely used as multifunctional theragnostic agents for both diagnostic as well as target and treatment purposes in cancer therapy because of their fluorescent nature. Full article

The excellent physicochemical properties of two-dimensional transition-metal dichalcogenides (2D TMDCs) such as WS₂ and WSe₂ provide potential benefits for biomedical applications, such as drug delivery, photothermal therapy, and bioimaging. WS₂ and WSe₂ have recently been used as chemosensitizers; however, the detailed molecular basis underlying WS₂- and WSe₂-induced sensitization remains elusive. Our recent findings showed that 2D TMDCs with different thicknesses and different element compositions induced autophagy in normal human bronchial epithelial cells and mouse alveolar macrophages at sublethal concentrations. Here, we explored the mechanism by which WS₂ and WSe₂ act as sensitizers to increase lung cancer cell susceptibility to chemotherapeutic agents. The results showed that WS₂ and WSe₂ enhanced autophagy flux in A549 lung cancer cells at sublethal concentrations without causing significant cell death. Through the autophagy-specific RT² Profiler PCR Array, we identified the genes significantly affected by WS₂ and WSe₂ treatment. Furthermore, the key genes that play central roles in regulating autophagy were identified by constructing a molecular interaction network. A mechanism investigation uncovered that WS₂ and WSe₂ activated autophagy-related signaling pathways by interacting with different cell surface proteins or cytoplasmic proteins. By utilizing this mechanism, the efficacy of the chemotherapeutic agent doxorubicin was enhanced by WS₂ and WSe₂ pre-treatment in A549 lung cancer cells. This study revealed a feature of WS₂ and WSe₂ in cancer therapy, in which they eliminate the resistance of A549 lung cancer cells against doxorubicin, at least partially, by inducing autophagy. Full article

Timely diagnosis and appropriate antitumoral treatments remain of utmost importance, since cancer remains a leading cause of death worldwide. Within this context, nanotechnology offers specific benefits in terms of cancer therapy by reducing its adverse effects and guiding drugs to selectively target cancer cells. In this comprehensive review, we have summarized the most relevant novel outcomes in the range of 2010–2023, covering the design and application of nanosystems for cancer therapy. We have established the general requirements for nanoparticles to be used in drug delivery and strategies for their uptake in tumor microenvironment and vasculature, including the reticuloendothelial system uptake and surface functionalization with protein corona. After a brief review of the classes of nanovectors, we have covered different classes of nanoparticles used in cancer therapies. First, the advances in the encapsulation of drugs (such as paclitaxel and fisetin) into nanoliposomes and nanoemulsions are described, as well as their relevance in current clinical trials. Then, polymeric nanoparticles are presented, namely the ones comprising poly lactic-co-glycolic acid, polyethylene glycol (and PEG dilemma) and dendrimers. The relevance of quantum dots in bioimaging is also covered, namely the systems with zinc sulfide and indium phosphide. Afterwards, we have reviewed gold nanoparticles (spheres and anisotropic) and their application in plasmon-induced photothermal therapy. The clinical relevance of iron oxide nanoparticles, such as magnetite and maghemite, has been analyzed in different fields, namely for magnetic resonance imaging, immunotherapy, hyperthermia, and drug delivery. Lastly, we have covered the recent advances in the systems using carbon nanomaterials, namely graphene oxide, carbon nanotubes, fullerenes, and carbon dots. Finally, we have compared the strategies of passive and active targeting of nanoparticles and their relevance in cancer theranostics. This review aims to be a (nano)mark on the ongoing journey towards realizing the remarkable potential of different nanoparticles in the realm of cancer therapeutics. Full article

With their distinctive core–shell design, core–shell nanocrystals have drawn interest in catalysis, medicinal research, and nanotechnology. These nanocrystals have a variety of characteristics and possible uses. The application of core–shell nanocrystals offers significant potential in increasing diagnostic and therapeutic approaches for cancer research in apoptosis and in vitro cancer cell imaging. In the present study, we investigated the fluorescence behavior of hydrophilic CdSe (core-only) and CdSe@CdS (core–shell) nanocrystals (NCs) and their potential in cancer cell imaging. The addition of a CdS coating to CdSe NCs increased the fluorescence intensity tenfold. The successful fabrication of core–shell CdSe@CdS nanocrystals was proven by a larger particle size (evaluated via DLS and TEM) and their XRD pattern and surface morphology compared to CdSe (core-only) NCs. When these NCs were used for bioimaging in MCF-7 and HEK-293 cell lines, they demonstrated excellent cellular uptake due to higher fluorescence intensity within cancerous cells than normal cells. Comparative cytotoxicity studies revealed that CdSe NCs were more toxic to all three cell lines (HEK-293, MCF-7, and HeLa) than CdSe@CdS core–shell structures. Furthermore, a decrease in mitochondrial membrane potential and intracellular ROS production supported NCs inducing oxidative stress, which led to apoptosis via the mitochondria-mediated pathway. Increased cytochrome c levels, regulation of pro-apoptotic gene expression (e.g., p53, Bax), and down-regulation of Bcl-2 all suggested cellular apoptosis occurred via the intrinsic pathway. Significantly, at an equivalent dose of core–shell NCs, core-only NCs induced more oxidative stress, resulting in increased apoptosis. These findings shed light on the role of a CdS surface coating in reducing free radical release, decreasing cytotoxicity, and improving fluorescence, advancing the field of cell imaging. Full article

Self-assembled DNA nanospheres, as versatile and ideal vehicles, have offered new opportunities to create intelligent delivery systems for precise bioimaging and cancer therapy, due to their good biostability and cell permeability, large loading capacity, and programmable self–assembly behaviors. DNA nanospheres can be synthesized by the self–assembly of Y–shaped DNA monomers, ultra–long single-stranded DNA (ssDNA), and even metal–DNA coordination. Interestingly, they are size–controllable by varying some parameters including concentration, reaction time, and mixing ratio. This review summarizes the design of DNA nanospheres and their extensive biomedical applications. First, the characteristics of DNA are briefly introduced, and different DNA nanostructures are mentioned. Then, the design of DNA nanospheres is emphasized and classified into three main categories, including Y–shaped DNA unit self-assembly by Watson–Crick base pairing, liquid crystallization and the dense packaging of ultra–long DNA strands generated via rolling circle amplification (RCA), and metal–DNA coordination–driven hybrids. Meanwhile, the advantages and disadvantages of different self–assembled DNA nanospheres are discussed, respectively. Next, the biomedical applications of DNA nanospheres are mainly focused on. Especially, DNA nanospheres serve as promising nanocarriers to deliver functional nucleic acids and drugs for biosensing, bioimaging, and therapeutics. Finally, the current challenges and perspectives for self-assembled DNA nanospheres in the future are provided. Full article