Nanocarrier Drug Delivery Systems Research Articles

Synthesis Techniques and Biomedical Applications of Cyclodextrin Metal-Organic Frameworks.

Cyclodextrin Metal-Organic Frameworks (CD MOFs) represent an innovative class of materials with remarkable properties and a broad range of applications. This review provides a comprehensive overview of the synthesis techniques, structural characterization, and diverse applications of CD-MOFs. By combining cyclodextrins (CDs) with metal-organic frameworks (MOFs), CD-MOFs are developed with enhanced functionality. The synthesis methods, including various metal sources, coordination modes, and post-synthesis modifications, are discussed alongside advanced structural characterization techniques like X-ray crystallography and spectroscopic methods. The unique characteristics of CD-MOFs, such as high specific surface area, tunable porosity, and customizable chemical structure, make them exceptional candidates for applications in gas adsorption, drug delivery, catalysis, sensing, and environmental remediation. Notably, CD-MOFs show significant promise as nanocarriers in drug delivery systems, offering improved therapeutic outcomes due to their efficient encapsulation and controlled release capabilities. The review highlights recent advancements and underscores the potential impact of CD-MOFs in driving future innovations across various scientific fields.

Bismuth-based mesoporous nanoball carrying sorafenib for synergistic photothermal and molecularly-targeted therapy in an orthotopic hepatocellular carcinoma xenograft mouse model

Sorafenib (SOR), a multi-kinase inhibitor for advanced hepatocellular carcinoma (HCC), has limited clinical application due to severe side effects and drug resistance. To overcome these challenges, we developed a bismuth-based nanomaterial (BOS) for thermal injury-assisted continuous targeted therapy in HCC. Initially, the mesoporous nanomaterial was loaded with SOR, forming the BOS@SOR nano-carrier system for drug delivery and controlled release. Notably, compared to targeted or photothermal therapy alone, the combination therapy using this nano-carrier system significantly impaired cell proliferation and increased apoptosis. In vivo efficacy evaluations demonstrated that BOS@SOR exhibited excellent biocompatibility, confirmed through hemolysis and biochemical analyses. Additionally, BOS@SOR enhanced contrast in computed tomography, aiding in the precise identification of HCC size and location. The photothermal therapeutic properties of bismuth further contributed to the synergistic anti-tumor activity of BOS@SOR, significantly reducing tumor growth in an orthotopic xenograft HCC model. Taken together, encapsulating SOR within a bismuth-based mesoporous nanomaterial creates a multifunctional and environmentally stable nanocomposite (BOS@SOR), enhancing the therapeutic effect of SOR and presenting an effective strategy for HCC treatment.

Recent Advances in the Use of Vitamin D Organic Nanocarriers for Drug Delivery.

Nanotechnology, now established as a transformative technology, has revolutionized medicine by enabling highly targeted drug delivery. The use of organic nanocarriers in drug delivery systems significantly enhances the bioavailability of vitamins and their analogs, thereby improving cellular delivery and therapeutic effects. Vitamin D, known for its crucial role in bone health, also influences various metabolic functions, such as cellular proliferation, differentiation, and immunomodulation, and is increasingly explored for its anticancer potential. Given its versatile properties and biocompatibility, vitamin D is an attractive candidate for encapsulation within drug delivery systems. This review provides a comprehensive overview of vitamin D synthesis, metabolism, and signaling, as well as its applications in customized drug delivery. Moreover, it examines the design and engineering of organic nanocarriers that incorporate vitamin D and discusses advances in this field, including the synergistic effects achieved through the combination of vitamin D with other therapeutic agents. By highlighting these innovations, this review provides valuable insights into the development of advanced drug delivery systems and their potential to enhance therapeutic outcomes.

Advancements in Cancer Therapeutics: Current Paradigms in Applying Biodegradable Polymer Nanoparticles for Enhanced Management

Abstract: The development of novel colloidal formulations that can regulate the pharmacological and biological properties of medications has been made possible by the developments of nanotechnology. Biodegradable nanoparticles were exploited as drug delivery methods because of their high bioavailability, improved encapsulation, controlled release, and less toxic characteristics. Over the past few decades, a variety of synthetic polymers have been investigated for application in nanomedicine, particularly in drug delivery systems. Drug delivery polymers need to be environmentally friendly, biodegradable, and biocompatible. As they have the ability to provide targeted delivery to a specified site, polymeric nanoparticles have the potential to increase the effectiveness of cancer therapies significantly. It is possible to modify the physical and chemical characteristics of polymers to provide delivery across the many biological barriers needed to reach different cell subsets. The use of biodegradable polymers as nanocarriers is particularly appealing since these materials can be developed to show triggered functionality at certain locations or activated by an external source in addition to degrading under physiological circumstances. Biodegradable polymers can be developed as easy drug-delivery systems that specifically target the tumour microenvironment. This is because these nanomedicines can directly target cancer cells, as well as blood vessels that supply the nutrition and oxygen required for tumour growth and immune cells that support anti-cancer immunotherapy. With the advancements in nanotechnology-based drug delivery systems for pharmaceutical applications, it is exciting to examine and highlight the significance of polymeric nanocarrier systems for drug delivery in chemotherapy.

Effects of phospholipid type and particle size on lipid nanoparticle distribution in vivo and in pancreatic islets

Lipid nanoparticles (LNPs) have recently been used as nanocarriers in drug delivery systems for nucleic acid drugs. Their practical applications are currently primarily limited to the liver and specific organs. However, altering the type and composition ratio of phospholipids improves their distribution in organs other than the liver, such as the spleen and lungs. This study aimed to elucidate the effects of LNP components and particle size on in vivo distribution through systemic circulation to pancreatic islets to achieve better targeting of islets, which are a fundamental therapeutic target for diabetes. Fluorescence-labeled LNPs were prepared using three phospholipids: 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), with particle sizes of 30–160 nm (diameter) using a microfluidic device. Baffled-structured iLiNP devices with adjusted flow-rate ratios and total flow rates were used. After the intravenous administration of LNPs to C57BL/6 J mice, the distribution of each LNP type to the major organs, including the pancreas and pancreatic islets, was compared using ex vivo fluorescence imaging and observation of pancreatic tissue sections. DSPC-LNPs- and DOPE-LNPs showed the highest distribution in the spleen and liver, respectively. In contrast, the DOPC-LNPs showed the highest distribution in the pancreas and the lowest distribution in the liver and spleen. In addition, smaller particles showed better distribution throughout the pancreas. The most significant LNP distribution in the islets was observed for DOPC-LNPs with a particle size of 160 nm. Furthermore, larger LNPs tended to be distributed in the islets, whereas smaller LNPs tended to be distributed in the exocrine glands. DOPC-LNPs were distributed in the islets at all cholesterol concentrations, with a high distribution observed at >40% cholesterol and > 3% PEG and the distribution was higher at 24 h than at 4 h. Thus, LNP composition and particle size significantly affected islet distribution characteristics, indicating that DOPC-LNPs may be a drug delivery system for effectively targeting the pancreas and islets.

Simple strategy of the use of pharmaceutically functionalized ionic liquids in a new generation of polymer nanocarriers for the combined delivery of ionic p-aminosalicylate and ampicillin

Single and dual bioactive linear poly(ionic liquid)s (PIL) were synthesized for use as nanocarriers in drug delivery systems (DDS). These PILs were obtained through the (co)polymerization of the choline-based monomeric ionic liquids (MIL) with pharmaceutical anions possessing antibacterial properties, specifically [2-(methacryloyloxy)ethyl]trimethyl-ammonium with ampicillin and p-aminosalicylate (TMAMA/AMP and TMAMA/PAS). The copolymers exhibited varying chain lengths defined by a degree of polymerization (DPn = 122–370), and differing contents of ionic fraction and drugs (TMAMA 61–92 %, AMP 61–93 % and PAS 16–21 %). These parameters were adjustable by the monomer conversion (33–92 %) and the initial ratio of comonomers. In aqueous solution, the polymer particles reached nanosizes, i.e. 190–328 nm for AMP systems and 200–235 nm for AMP/PAS systems. In the release process, the pharmaceutical anions were released through exchange by phosphate anions in PBS at pH 7.4 at 37 °C. Depending on the copolymer composition the release of AMP was attained in 72–100 % (11.1–19.5 µg/mL) within 26 h by the single drug systems, while the dual drug systems released 61–100 % of AMP (14.8–24.7 µg/mL) and 82–100 % of PAS (3.1–4.8 µg/mL) within 72 h. The effectiveness in the drug delivery of the designed TMAMA polymers seems to be promising for future applications in antibiotic therapy and the combined therapy.

Red blood cell derived nanocarrier drug delivery system: a promising strategy for tumor therapy (3/2024)

Red blood cell derived nanocarrier drug delivery system: a promising strategy for tumor therapy (3/2024)

Exploring Disulfiram's Anticancer Potential: PLGA Nano-Carriers for Prolonged Drug Delivery and Potential Improved Therapeutic Efficacy.

Disulfiram (DS) has been shown to have potent anti-cancer activity; however, it is also characterised by its low water solubility and rapid metabolism in vivo. Biodegradable polylactic-co-glycolic acid (PLGA) polymers have been frequently employed in the manufacturing of PLGA nano-carrier drug delivery systems. Thus, to develop DS-loaded PLGA nanoparticles (NPs) capable of overcoming DS's limitations, two methodologies were used to formulate the NPs: direct nanoprecipitation (DNP) and single emulsion/solvent evaporation (SE), followed by particle size reduction. The DNP method was demonstrated to produce NPs of superior characteristics in terms of size (151.3 nm), PDI (0.083), charge (-37.9 mV), and loading efficiency (65.3%). Consequently, NPs consisting of PLGA and encapsulated DS coated with mPEG2k-PLGA at adjustable ratios were prepared using the DNP method. Formulations were then characterised, and their stability in horse serum was assessed. Results revealed the PEGylated DS-loaded PLGA nano-carriers to be more efficient; hence, in-vitro studies testing these formulations were subsequently performed using two distinct breast cancer cell lines, showing great potential to significantly enhance cancer therapy.

Targeted Delivery Strategies for Multiple Myeloma and Their Adverse Drug Reactions.

Currently, multiple myeloma (MM) is a prevalent hematopoietic system malignancy, known for its insidious onset and unfavorable prognosis. Recently developed chemotherapy drugs for MM have exhibited promising therapeutic outcomes. Nevertheless, to overcome the shortcomings of traditional clinical drug treatment, such as off-target effects, multiple drug resistance, and systemic toxicity, targeted drug delivery systems are optimizing the conventional pharmaceuticals for precise delivery to designated sites at controlled rates, striving for maximal efficacy and safety, presenting a promising approach for MM treatment. This review will delve into the outstanding performance of antibody-drug conjugates, peptide-drug conjugates, aptamer-drug conjugates, and nanocarrier drug delivery systems in preclinical studies or clinical trials for MM and monitor their adverse reactions during treatment.

Red blood cell derived nanocarrier drug delivery system: A promising strategy for tumor therapy

AbstractNano drug delivery systems have been widely used in tumor therapy. Researchers have been devoted to exploring novel nano‐carriers to prolong circulation time biocompatibility and tumor targeting efficiency in vivo. Erythrocyte membranes as bionic nano‐drug delivery systems have attracted more attention recently. There are abundant red blood cells (RBCs) in circulation, which are natural carriers for nanomaterial delivery. There are mainly two strategies to use RBCs as nanomaterial carriers: RBC‐hitchhiking and bionic nanomaterial coated with erythrocyte membrane loading with drugs. Although nano‐carrier based on RBCs have yielded some progress, the mechanism of mutual effect between nanoparticles and RBCs is still unclear. Here, we review the effects of nanoparticles on RBCs (morphology and function, etc) and application of RBCs membrane as nano‐drug delivery carriers in tumor therapy.

Stimuli-responsive drug release of polyacrylic acid-coated silica–titania hollow nanoparticles

Inorganic hollow nanoparticles have received a great deal of attention as nanocarriers for drug delivery system, but it is still challenging to control the drug release time and achieve high drug delivery efficiency. In this study, we intend to build a controllable smart drug delivery system that delivers drugs to a desired location for a desired time using a stimulus-responsive material. Polyacrylic acid (PAA), a pH-responsive material, is coated on the silica–titania hollow nanoparticles (HNPs) to acquire stimulus-responsive material for controlled drug release.

Advances in 2,3-Dimethylmaleic Anhydride (DMMA)-Modified Nanocarriers in Drug Delivery Systems.

Cancer represents a significant threat to human health. The cells and tissues within the microenvironment of solid tumors exhibit complex and abnormal properties in comparison to healthy tissues. The efficacy of nanomedicines is inhibited by the presence of substantial and complex physical barriers in the tumor tissue. The latest generation of intelligent drug delivery systems, particularly nanomedicines capable of charge reversal, have shown promise in addressing this issue. These systems can transform their charge from negative to positive upon reaching the tumor site, thereby enhancing tumor penetration via transcytosis and promoting cell internalization by interacting with the negatively charged cell membranes. The modification of nanocarriers with 2,3-dimethylmaleic anhydride (DMMA) and its derivatives, which are responsive to weak acid stimulation, represents a significant advance in the field of charge-reversal nanomedicines. This review provides a comprehensive examination of the recent insights into DMMA-modified nanocarriers in drug delivery systems, with a particular focus on their potential in targeted therapeutics. It also discusses the synthesis of DMMA derivatives and their role in charge reversal, shell detachment, size shift, and ligand reactivation mechanisms, offering the prospect of a tailored, next-generation therapeutic approach to overcome the diverse challenges associated with cancer therapy.

Synthesis and Characterization of SiO2/nGO/Fe3O4/SeQDs Nanoparticles as Potential Nanocarriers in Drug Delivery Systems.

Herein, we constructed the branch-shaped SiO2/nano GO (nGO)/Fe3O4/selenium quantum dots (QDs) (SeQDs) nanoparticles (SGF/SeQDs) embodying magnetism, fluorescence, and microwave stimulus response properties to enhance the performance of releasing drugs. The SGF/SeQDs composite was characterized by technologies including powder X-ray diffraction, transmission electron microscopy, infrared spectroscopy, etc. In the nanoparticles, the branch-shaped SiO2 provides a large specific surface area, nGO as the dielectric loss-style material promotes microwave-absorbing performance, and the Fe3O4 serves as a magnetic targeting agent and microwave absorber. Integrating nGO and Fe3O4 could further strengthen the microwave absorption of the entire composite; selenium features both fluorescence and anticancer effects. The synthesized nanoparticles as carriers exhibited a branch-like mesoporous sphere of ∼260 nm, a specific surface area of 258.57 m2 g-1, a saturation magnetization of 24.59 emu g-1, and good microwave thermal conversion performance that the temperature was elevated from 25 to 70 °C under microwave irradiation. These physical characteristics, including large pore volume (5.30 nm), high specific surface area, and fibrous morphology, are in favor of loading drugs. Meanwhile, the cumulative etoposide (VP16) loading rate of the nanoparticles reached to 21 wt % after 360 min. The noncovalent interaction between the VP16 and SGF/SeQDs was mainly the hydrogen-bonding effect during the loading process. Furthermore, the drug release rates at 180 min were up to 81.46, 61.92, and 56.84 wt % at pH 4, 5, and 7, respectively. At 25, 37, and 50 °C, the rates of drug release reach 25.40, 56.84, and 65.32 wt %, respectively. After microwave stimulation at pH 7, the rate of releasing drug increased distinctly from 56.84 to 71.74 wt % compared to that of nonmicrowave irradiation. Cytotoxicity tests manifested that the carrier had good biocompatibility. Therefore, the nanoparticles are looking forward to paving one platform for further applications in biomedicine and drug delivery systems.

Applications of Nanotechnology-mediated Herbal Nanosystems for Ophthalmic Drug.

In recent years, herbal nanomedicines have gained tremendous popularity for novel drug discovery. Nanotechnology has provided several advances in the healthcare sector, emerging several novel nanocarriers that potentiate the bioavailability and therapeutic efficacy of the herbal drug. The recent advances in nanotechnology with accelerated strategies of ophthalmic nanosystems have paved a new path for overcoming the limitations associated with ocular drug delivery systems, such as low bioavailability, poor absorption, stability, and precorneal drug loss. Ophthalmic drug delivery is challenging due to anatomical and physiological barriers. Due to the presence of these barriers, the herbal drug entry into the eyes can be affected when administered by following multiple routes, i.e., topical, injectables, or systemic. However, the advancement of nanotechnology with intelligent systems enables the herbal active constituent to successfully entrap within the system, which is usually difficult to reach employing conventional herbal formulations. Herbal-loaded nanocarrier drug delivery systems demonstrated enhanced herbal drug permeation and prolonged herbal drug delivery. In this current manuscript, an extensive search is conducted for original research papers using databases Viz., PubMed, Google Scholar, Science Direct, Web of Science, etc. Further painstaking efforts are made to compile and update the novel herbal nanocarriers such as liposomes, polymeric nanoparticles, solid lipid nanoparticles, nanostructure lipid carriers, micelles, niosomes, nanoemulsions, dendrimers, etc., which are mostly used for ophthalmic drug delivery system. This article presents a comprehensive survey of diverse applications used for the preventative measures and treatment therapy of varied eye disorders. Further, this article highlights the recent findings that the innovators are exclusively working on ophthalmic nanosystems for herbal drug delivery systems. The nanocarriers are promising drug delivery systems that enable an effective and supreme therapeutic potential circumventing the limitations associated with conventional ocular drug delivery systems. The nanotechnology-based approach is useful to encapsulate the herbal bioactive and prevent them from degradation and therefore providing them for controlled and sustained release with enhanced herbal drug permeation. Extensive research is still being carried out in the field of herbal nanotechnology to design an ophthalmic nanosystem with improved biopharmaceutical properties.

Structural Optimization of Carboxy-Terminal Phenylalanine-Modified Dendrimers for T-Cell Association and Model Drug Loading.

Dendrimers are potent nanocarriers in drug delivery systems because their structure can be precisely controlled. We previously reported that polyamidoamine (PAMAM) dendrimers that were modified with 1,2-cyclohexanedicarboxylic acid (CHex) and phenylalanine (Phe), PAMAM-CHex-Phe, exhibited an effective association with various immune cells, including T-cells. In this study, we synthesized various carboxy-terminal Phe-modified dendrimers with different linkers using phthalic acid and linear dicarboxylic acids to determine the association of these dendrimers with Jurkat cells, a T-cell model. PAMAM-n-hexyl-Phe demonstrated the highest association with Jurkat T-cells. In addition, dendri-graft polylysine (DGL) with CHex and Phe, DGL-CHex-Phe, was synthesized, and its association with Jurkat cells was investigated. The association of DGL-CHex-Phe with T-cells was higher than that of PAMAM-CHex-Phe. However, it was insoluble in water and thus it is unsuitable as a drug carrier. Model drugs, such as protoporphyrin IX and paclitaxel, were loaded onto these dendrimers, and the most model drug molecules could be loaded into PAMAM-CHex-Phe. PTX-loaded PAMAM-CHex-Phe exhibited cytotoxicity against Jurkat cells at a similar level to free PTX. These results suggest that PAMAM-CHex-Phe exhibited both efficient T-cell association and drug loading properties.

The Emerging Roles of Nanocarrier Drug Delivery System in Treatment of Intervertebral Disc Degeneration-Current Knowledge, Hot Spots, Challenges and Future Perspectives.

Low back pain (LBP) is a common condition that has substantial consequences on individuals and society, both socially and economically. The primary contributor to LBP is often identified as intervertebral disc degeneration (IVDD), which worsens and leads to significant spinal problems. The conventional treatment approach for IVDD involves physiotherapy, drug therapy for pain management, and, in severe cases, surgery. However, none of these treatments address the underlying cause of the condition, meaning that they cannot fundamentally reverse IVDD or restore the mechanical function of the spine. Nanotechnology and regenerative medicine have made significant advancements in the field of healthcare, particularly in the area of nanodrug delivery systems (NDDSs). These approaches have demonstrated significant potential in enhancing the efficacy of IVDD treatments by providing benefits such as high biocompatibility, biodegradability, precise drug delivery to targeted areas, prolonged drug release, and improved therapeutic results. The advancements in different NDDSs designed for delivering various genes, cells, proteins and therapeutic drugs have opened up new opportunities for effectively addressing IVDD. This comprehensive review provides a consolidated overview of the recent advancements in the use of NDDSs for the treatment of IVDD. It emphasizes the potential of these systems in overcoming the challenges associated with this condition. Meanwhile, the insights and ideas presented in this review aim to contribute to the advancement of precise IVDD treatment using NDDSs.

An Overview of Polymeric Nanoplatforms to Deliver Veterinary Antimicrobials.

There is an urgent need to find new solutions for the global dilemma of increasing antibiotic resistance in humans and animals. Modifying the performance of existing antibiotics using the nanocarrier drug delivery system (DDS) is a good option considering economic costs, labor costs, and time investment compared to the development of new antibiotics. Numerous studies on nanomedicine carriers that can be used for humans are available in the literature, but relatively few studies have been reported specifically for veterinary pharmaceutical products. Polymer-based nano-DDS are becoming a research hotspot in the pharmaceutical industry owing to their advantages, such as stability and modifiability. This review presents current research progress on polymer-based nanodelivery systems for veterinary antimicrobial drugs, focusing on the role of polymeric materials in enhancing drug performance. The use of polymer-based nanoformulations improves treatment compliance in livestock and companion animals, thereby reducing the workload of managers. Although promising advances have been made, many obstacles remain to be addressed before nanoformulations can be used in a clinical setting. Some crucial issues currently facing this field, including toxicity, quality control, and mass production, are discussed in this review. With the continuous optimization of nanotechnology, polymer-based DDS has shown its potential in reducing antibiotic resistance to veterinary medicines.

Nanoparticles for the Treatment of Bone Metastasis in Breast Cancer: Recent Advances and Challenges.

Although the frequency of bone metastases from breast cancer has increased, effective treatment is lacking, prompting the development of nanomedicine, which involves the use of nanotechnology for disease diagnosis and treatment. Nanocarrier drug delivery systems offer several advantages over traditional drug delivery methods, such as higher reliability and biological activity, improved penetration and retention, and precise targeting and delivery. Various nanoparticles that can selectively target tumor cells without causing harm to healthy cells or organs have been synthesized. Recent advances in nanotechnology have enabled the diagnosis and prevention of metastatic diseases as well as the ability to deliver complex molecular "cargo" particles to metastatic regions. Nanoparticles can modulate systemic biodistribution and enable the targeted accumulation of therapeutic agents. Several delivery strategies are used to treat bone metastases, including untargeted delivery, bone-targeted delivery, and cancer cell-targeted delivery. Combining targeted agents with nanoparticles enhances the selective delivery of payloads to breast cancer bone metastatic lesions, providing multiple delivery advantages for treatment. In this review, we describe recent advances in nanoparticle development for treating breast cancer bone metastases.

Targeting the Endocannabinoid System Present in the Glioblastoma Tumour Microenvironment as a Potential Anti-Cancer Strategy.

The highly aggressive and invasive glioblastoma (GBM) tumour is the most malignant lesion among adult-type diffuse gliomas, representing the most common primary brain tumour in the neuro-oncology practice of adults. With a poor overall prognosis and strong resistance to treatment, this nervous system tumour requires new innovative treatment. GBM is a polymorphic tumour consisting of an array of stromal cells and various malignant cells contributing to tumour initiation, progression, and treatment response. Cannabinoids possess anti-cancer potencies against glioma cell lines and in animal models. To improve existing treatment, cannabinoids as functionalised ligands on nanocarriers were investigated as potential anti-cancer agents. The GBM tumour microenvironment is a multifaceted system consisting of resident or recruited immune cells, extracellular matrix components, tissue-resident cells, and soluble factors. The immune microenvironment accounts for a substantial volume of GBM tumours. The barriers to the treatment of glioblastoma with cannabinoids, such as crossing the blood-brain barrier and psychoactive and off-target side effects, can be alleviated with the use of nanocarrier drug delivery systems and functionalised ligands for improved specificity and targeting of pharmacological receptors and anti-cancer signalling pathways. This review has shown the presence of endocannabinoid receptors in the tumour microenvironment, which can be used as a potential unique target for specific drug delivery. Existing cannabinoid agents, studied previously, show anti-cancer potencies via signalling pathways associated with the hallmarks of cancer. The results of the review can be used to provide guidance in the design of future drug therapy for glioblastoma tumours.

CARBON DOTS: Bioimaging and Anticancer Drug Delivery.

Cancer, responsible for approximately 10 million lives annually, urgently requires innovative treatments, as well as solutions to mitigate the limitations of traditional chemotherapy, such as long-term adverse side effects and multidrug resistance. This review focuses on Carbon Dots (CDs), an emergent class of nanoparticles (NPs) with remarkable physicochemical and biological properties, and their burgeoning applications in bioimaging and as nanocarriers in drug delivery systems for cancer treatment. The review initiates with an overview of NPs as nanocarriers, followed by an in-depth look into the biological barriers that could affect their distribution, from barriers to administration, to intracellular trafficking. It further explores CDs' synthesis, including both bottom-up and top-down approaches, and their notable biocompatibility, supported by a selection of in vitro, in vivo, and ex vivo studies. Special attention is given to CDs' role in bioimaging, highlighting their optical properties. The discussion extends to their emerging significance as drug carriers, particularly in the delivery of doxorubicin and other anticancer agents, underscoring recent advancements and challenges in this field. Finally, we showcase examples of other promising bioapplications of CDs, emergent owing to the NPs flexible design. As research on CDs evolves, we envisage key challenges, as well as the potential of CD-based systems in bioimaging and cancer therapy.