Search Results (160)

Imatinib (IMT) is a small-molecule tyrosine kinase inhibitor that primarily targets platelet-derived growth factor receptor-β and related kinases. Beyond its established efficacy in chronic myeloid leukemia, IMT has also demonstrated therapeutic benefits in gastrointestinal stromal tumors, dermatofibrosarcoma, acute lymphoblastic leukemia, and as a second-line treatment for aggressive systemic mastocytosis or as an anti-Mycobacterium agent. From a physicochemical perspective, IMT exhibits poor aqueous solubility but high membrane permeability, classifying it as a Biopharmaceutics Classification System Class II compound. Pharmacokinetically, IMT shows variable oral absorption and a prolonged terminal half-life, resulting in dose-dependent systemic exposure. Despite relatively high oral bioavailability, its clinical use requires large doses to achieve therapeutic efficacy, underscoring the need for advanced drug delivery strategies. Nano- and microscale delivery systems offer promising approaches to enhance tumor-specific accumulation through the enhanced permeability and retention effect while mitigating resistance mechanisms. However, achieving high drug loading introduces formulation challenges, such as controlling particle size distribution, polydispersity, and scalability. Moreover, designing carriers capable of controlled release without premature leakage remains crucial for maintaining systemic bioavailability and therapeutic performance. Emerging delivery platforms—including polymeric, lipid-based, carbon-derived, and stimuli-responsive nanocarriers—have shown significant potential in overcoming these limitations. Such systems can enhance IMT’s bioavailability, improve selective tumor targeting, and minimize systemic toxicity, thereby advancing its translational potential. This review aims to highlight the different biomedical applications of IMT and off-label uses, and to discuss current advances in drug delivery to optimize its clinical efficacy and safety profile. Full article

According to the World Health Organization, Alzheimer’s disease and other forms of dementia were the seventh leading cause of death in 2021. The prevalence of these disorders is predictable to increase with life expectancy, and their control is hampered by several factors, including late diagnosis due to the lack of specific biomarkers and the absence of disease-modifying treatments, as currently available therapies can only lighten some of the symptoms. Nanotechnology could be the key to overcoming some of the limitations associated with neurodegenerative diseases, as nanomaterials have excellent properties compared to their bulk counterparts and can be used as drug delivery systems, diagnostic tools and platforms for tissue regeneration. Chitosan is a biopolymer with numerous properties that impart it with great potential for biomedical applications, in particular its ability to cross the blood–brain barrier and its versatility in nanoscale design. In this context, the aim of this review is to provide an in-depth analysis of the latest developments and future opportunities for chitosan (nano)formulations for the treatment and management of neurodegenerative diseases. Full article

Background/Objectives: The melt-spinning process has seen limited application in the pharmaceutical industry. However, nano- and microfibrous structures show significant potential for novel drug delivery systems, due to their high specific surface area. To facilitate broader adoption in pharmaceutical technology, critical parameters influencing fiber quality and yield must be investigated. In this study, we aimed to develop an isomalt-based microfibrous carrier system for active pharmaceutical ingredients. Methods: The effects of different isomalt compositions—specifically, varying ratios of GPS (6-O-α-d-glucopyranosyl-d-sorbitol) and GPM (1-O-α-d-glucopyranosyl-d-mannitol)—as well as key process parameters, were systematically investigated to optimize fiber formation. The prepared fibers underwent different treatments. Morphological changes were monitored with a microscope, and microstructural changes were studied using a differential scanning calorimeter and X-ray diffractometer. The macroscopic behavior of the fibers was evaluated by image analysis under monitored conditions. Results: Statistical analysis was used to determine the optimal setting to produce isomalt-based fibers. We found that storage over ethanol vapor has a positive effect on the stability of the fibers. We successfully prepared ibuprofen sodium-containing fibers that remained stable after alcohol treatment and enabled drug release within 15 s. Conclusions: It was found that the applied GPS:GPM isomalt ratio significantly influenced fiber formation and that storage over ethanol positively influenced the processability and stability of the fibrous structure. An isomalt-based microfibrous system with advantageous physicochemical and structural properties was successfully developed as a potential drug carrier. The system is also resistant to the destructive effects of ambient humidity, enabling preparation of suitable dosage forms. Full article

Background/Objectives: Liver cancer is considered one of the most dangerous types of cancer due to both the patients’ and the physician’s delay in diagnosis. Metal/ligand complexes represent antitumor drugs; however, they have several limitations such as a lack of specificity that results in damage to healthy organs. Therefore, there is a need for a material that improves specificity and decreases side effects. Magnetite nanoparticles (MNPs) show outstanding findings in the targeting and treatment of cancer-diseased organs. Methods: Herein, a metal/ligand palladium complex with antitumor activity was prepared and loaded onto magnetite nanoparticles for the treatment of liver cancer. The proposed structures with the lowest energy geometries were identified by density functional theory (DFT) utilizing the Gaussian09 program. Molecular docking simulation was conducted on an HP Pavilion dv6 Notebook PC equipped with an AMD Phenom™ N930 Quad processor. Afterward, the prepared nano-systems were investigated using FTIR and TEM. In vitro drug release measurement was evaluated in PBS at different time intervals. Eventually, the selectivity of these nano-systems was investigated using an animal rat model. Results: The results showed that MNPs with a crystalline structure and superparamagnetic characteristics (Ms = 71.273 emu/g) were created with a large surface area (63.75 m²/g), and they were validated to be acceptable for drug delivery applications. The palladium complex [Pd(DMEN)Cl₂] loaded onto magnetite released highly in acidic circumstances (pH 4.5), implying that it could be employed for targeted therapy of liver cancer. Conclusions: In vivo investigations in a rat model of liver cancer induced by diethylnitrosamine and thioacetamide (DEN/TAA) showed that the combination of the palladium complex and magnetite demonstrated a potent anticancer therapeutic activity on liver cancer in rats, improving liver function and structure while mitigating inflammation. Full article

Natural products possess potent pharmacological activities and health benefits. However, drawbacks such as water insolubility, poor stability, and low bioavailability limit their practical applications. This research is dedicated to the development of suitable natural self-assembled nano-delivery systems to encapsulate natural molecule drugs, improving their dispersion and stability in aqueous solution. As a model drug, curcumin (Cur) was encapsulated in zinc–adenine nanoparticles (Zn–Adenine), based on the self-assembly of a coordination matrix material. Hyaluronic acid (HA) was further functionalized on the surface of Cur@(Zn–Adenine) to realize a tumor-targeted delivery system. The morphology was characterized through TEM and zeta potential analyses, while the encapsulation mechanism of the nanoparticles was researched via XRD and FTIR. The formed Cur@(Zn–Adenine)@HA nanoparticles exhibited good drug loading efficiency and drug loading rate. Moreover, compared to free Cur, Cur-loaded (Zn–Adenine)@HA showed enhanced pH stability and thermal stability. In particular, Cur@(Zn–Adenine)@HA demonstrated excellent biocompatibility and strong specificity for targeting CD44 protein on cancer cells. The above results indicate that (Zn–Adenine)@HA NPs can serve as an effective nano-delivery system for hydrophobic substances. Full article

Despite remarkable advancements in cancer immunotherapy, its clinical efficacy remains constrained in solid tumors due to the immunosuppressive tumor microenvironment (TME). Reactive oxygen species (ROS), which exhibit dual regulatory roles in the TME by regulating immunogenic cell death (ICD) and reprogramming immune cell functionality, have emerged as a pivotal therapeutic target. Nano-enabled drug delivery systems present distinct advantages for TME modulation due to their structural versatility, tumor-specific targeting precision, and spatiotemporally controlled drug release. In particular, ROS-responsive nanoplatforms demonstrate multifaceted immunomodulatory potential by synergistically restoring ICD and remodeling immunosuppressive immune cell phenotypes within the TME. These platforms further amplify the therapeutic outcomes of conventional modalities including chemotherapy, radiotherapy, and photodynamic therapy (PDT) through ROS-mediated sensitization mechanisms. This review comprehensively examines recent breakthroughs in ROS-responsive nanosystems for antitumor immunotherapy, emphasizing their mechanistic interplay with TME components and clinical translation potential. Herein, we provide a framework for developing integrated therapeutic strategies to overcome the current limitations in cancer immunotherapy. Full article

Engineered nano- and microparticles are considered as promising tools in biomedical applications, such as imaging, sensing, and drug delivery. Protein adsorption on these particles in biological media is an important factor affecting their properties, cellular interactions, and biological fate. Understanding the parameters determining the efficiency and pattern of protein adsorption is crucial for the development of effective biocompatible particle-based applications. This review focuses on the influence of the morphological and physicochemical properties of particles on protein adsorption, including the pattern and amount of the adsorbed protein species, as well as the relative abundance of proteins with specific functions or physicochemical parameters. The effects of functionalization of the particle surface with polyethylene glycol, zwitterions, zwitterionic polymers, or proteins on the subsequent protein adsorption are analyzed. In addition, the dependences of protein adsorption on the protein species, biological buffers, fluids, tissues, and other experimental conditions are looked into. The influence of protein adsorption on the targeting efficiency of particle-based delivery systems is also discussed. Finally, the effect of the adsorbed protein corona on the interaction of the engineered micro- and nanoparticles with cells and the roles of specific proteins adsorbed on the particle surface in the recognition of the particles by the immune system are considered. Full article

In this study, we present bi-layered hydrogel systems that incorporate different sizes and shapes of gold nanoparticles (nanospheres and nanorods) for potential use in areas such as photoactuators, soft robotics, artificial muscles, drug delivery and tissue engineering. The synthesized nano Au-PNiPAAm/PVA bi-layered hydrogel nanocomposites provide the unique ability to exhibit controlled motion upon light exposure, indicating that the above systems possess the capability of photo–thermal energy conversion. The chosen synthesis approach is a combination of chemical production of gold nanoparticles (AuNPs) followed by gamma radiation formation of crosslinked polymer networks around them, as the final step, which also allows for sterilization in a single technological step. According to the TEM analysis, the gold nanospheres (AuNSs) with mean diameters of around 17 and 30 nm, as well as nanorods (AuNRs) with an aspect ratio of around 4.5, were synthesized and used as nanofillers in the formation of nanocomposites. Their stability within the polymer matrix was confirmed by UV–Vis spectral studies, by the presence of local surface plasmon resonance (LSPR) bands, typical for nanoparticles of various shapes and sizes. Morphological studies (FE-SEM) of hydrogels revealed the formation of a porous structure with PNiPAAm hydrogel as an active layer and PVA hydrogel as a passive layer, as well as a stable interfacial layer with a thickness of around 80 μm. The synthesized bi-layered photoactuators showed a photo–thermal response upon exposure to irradiation of green lasers and lamps that simulate sunlight, resulting in bending motion. This bending response reveals the huge potential of the obtained materials as soft actuators, which are more flexible than rigid systems, making them effective for specific applications where controlled movement and flexibility are essential. Full article

Protein-bound nano-injectable solutions represent a cutting-edge advancement in nanomedicine, offering a versatile platform for precise and controlled drug delivery. By leveraging the biocompatibility and functional versatility of proteins such as albumin, gelatin, and casein, these nano systems enhance drug solubility, prolong circulation time, and improve site-specific targeting, which are particularly beneficial in cancer and inflammatory diseases. This review provides a comprehensive overview of their formulation strategies, physicochemical characteristics, and biological behavior. Emphasis is placed on therapeutic applications, regulatory considerations, fabrication techniques, and the underlying mechanisms of drug–protein interactions. This review also highlights improved pharmacokinetics and reduced systemic toxicity, while also critically addressing challenges like immunogenicity, protein instability, and production scalability. Recent FDA-approved formulations and emerging innovations in precision medicine and theranostics underscore the transformative potential of protein-based nanosuspensions in next-generation drug delivery systems. Full article

Prostate cancer is the most common tumor in men in developed countries and it often responds poorly to conventional treatments. Monoclonal antibody (MoAb) therapy, for this pathology, has grown tremendously in the past decades, exploiting naked and conjugated antibodies to cytotoxic payloads to form antibody drug conjugates (ADCs). Several studies have been carried out conjugating biomolecules against prostate-specific membrane antigen (PSMA), highly expressed in this tumor, to cytotoxic drugs. Nano-based formulations show high potential in targeted drug delivery to enhance the bioavailability of drugs. Our research aimed to evaluate the feasibility of setting up a nanoparticle-based multimodal tool for targeted drug delivery, describing the step-by-step approach and to perform a first screening of these fluorescent PEGylated silica nanoparticles employed in selective cancer cell targeting and killing. These nanoparticles featured a core–shell structure to contemporarily conjugate the antibody and the cytotoxic payload monomethyl auristatin E (MMAE) using a step-by-step approach. We compared the cytotoxic effect of this multimodal nanotool near the antibody-MMAE and free MMAE. We found a lower cytotoxicity effect of the nanoparticle-based construct compared to free drugs, likely because of the preservation of the previously observed receptor-mediated endocytosis. Nanomedicine is confirmed as a powerful alternative to organic drug delivery systems, even if some aspects, such as drug loading efficacy, release, scalable manufacturing and long-term stability, need to be deepened. Full article

Kinase inhibitors are small molecules that block kinase activity and have significant applications in both therapy and diagnostics. Recent studies suggest that these inhibitors hold great potential as targets for treating a range of diseases, including autoimmune disorders, cardiovascular conditions, cancer, and inflammatory diseases like ulcerative colitis. Ongoing research focuses on developing effective carriers for tyrosine kinase inhibitors (TKIs) to enhance treatment outcomes while reducing side effects. The nano-scale drug carriers have demonstrated the ability to encapsulate a wide range of imaging and therapeutic agents, enhancing tumor diagnosis and treatment. Notably, the incorporation of drugs with poor pharmacokinetics into nanocarriers enhances their solubility and stability, offering a renewed opportunity to assess their full therapeutic potential. The entrapped agents can be released in a controlled manner to maintain a specific drug concentration within a treatment framework or triggered by specific stimuli such as time or pH to target particular tissues or cells. The multifunctionality of nanosystems offers a promising avenue for developing innovative tyrosine kinase inhibitor (TKI) delivery strategies that serve as alternative treatment options for cancer and other inflammatory diseases. This review aims to provide a comprehensive overview of innovative nano-scale delivery systems for TKIs, both as standalone treatments and in combination with other therapeutic agents or drug delivery approaches. We discuss their comparative advantages and limitations for future small-molecule TKIs research. Full article

This review summarizes the research progress in the co-delivery of natural products (NPs) and small RNAs in cancer therapy. NPs such as paclitaxel, camptothecin, and curcumin possess multi-target antitumor effects, but their applications are limited by drug resistance and non-specific distribution. Small RNAs can achieve precise antitumor effects through gene regulation, yet their delivery efficiency is low, and they are prone to degradation by nucleases. Nanomaterial-based drug delivery systems (nano-DDSs) provide an efficient platform for the co-delivery of both, which can enhance the targeting of their delivery and improve the synergistic antitumor effects simultaneously. The mechanisms of the antitumor action of natural compounds and small RNAs, the design and application of nanocarriers, and the latest research progress in co-delivery systems are introduced in detail in this paper. The application prospects of the co-delivery of natural compounds and small RNAs in cancer therapy are also discussed. Full article

Understanding cellular interaction with nanomaterials represents a subject of great interest for the validation of new diagnostic and therapeutic tools. A full characterization of a designed product includes the evaluation of its impact on specific biological systems, including the study of cell behavior as a response to that particular interaction. Copper and copper-based nanoparticles (CuO NPs) have emerged as valuable building blocks for various biomedical applications such as antibacterial and disinfecting agents for infectious diseases, and the evaluation of the metabolism of food, including the iron required for proteins and enzymes or as drug delivery systems in cancer therapy. In this study, the biological impact of manganese-doped crystalline copper oxide (CuO:Mn) nano-platelets on human normal BJ fibroblasts and human A375 skin melanoma was assessed. The particles were synthesized at room temperature via the hydrothermal method. A complete physicochemical characterization of the materials was performed by employing various techniques including X-ray diffraction, electron microscopy, X-Ray photoelectron spectroscopy, and dynamic light scattering. Morphological investigations revealed a flat structure with nearly straight edges, with sizes spanning in the nanometer range. XRD analysis confirmed the formation of the CuO phase with good crystallinity, while XPS provided insights into the Mn doping. The findings indicate that nano-platelets interact with cells actively by mediating essential molecular processes. The exogenous manganese triggers increased MnSOD production in mitochondria, compensating ROS produced by external stress factors (Cu²⁺ ions), and mimics the endogenous SODs production, which compensates internal ROS production as it normally results from cell biochemistry. The effect is differentiated in normal cells compared to malignant cells and deserves investigation. Full article

Photodynamic therapy (PDT) is an innovative treatment that has recently been approved for clinical use and holds promise for cancer patients. It offers several benefits, such as low systemic toxicity, minimal invasiveness, and the ability to stimulate antitumor immune responses. For certain types of cancer, it has shown positive results with few side effects. However, PDT still faces some challenges, including limited light penetration into deeper tumor tissues, uneven distribution of the photosensitizer (PS) that can also affect healthy cells, and the difficulties posed by the hypoxic tumor microenvironment (TME). In hypoxic conditions, PDT’s effectiveness is reduced due to insufficient production of reactive oxygen species, which limits tumor destruction and can lead to relapse. This review highlights recent advances in photosensitizers and nanotechnologies that are being developed to improve PDT. It focuses on multifunctional nanoplatforms and nanoshuttles that have shown promise in preclinical studies, especially for treating solid tumors. One of the key areas of focus is the development of PSs that specifically target mitochondria to treat deep-seated malignant tumors. New mitochondria-targeting nano-PSs are designed with better water solubility and extended wavelength ranges, allowing them to target tumors more effectively, even in challenging, hypoxic environments. These advancements in PDT are opening new doors for cancer treatment, especially when combined with other therapeutic strategies. Moving forward, research should focus on optimizing PDT, creating more efficient drug delivery systems, and developing smarter PDT platforms. Ultimately, these efforts aim to make PDT a first-choice treatment option for cancer patients. Full article

Currently, inflammation diseases are one of the leading causes of mortality worldwide. The therapeutic drugs for inflammation are mainly steroidal and non-steroidal anti-inflammatory drugs. However, the use of these anti-inflammatory drugs over a prolonged period is prone to causing serious side effects. Accordingly, it is particularly critical to design an intelligent target-specific drug delivery system to control the release of drugs in order to mitigate the side effects of anti-inflammatory drugs without limiting their activity. Meanwhile, cyclodextrin-based nano-delivery systems have garnered significant attention in contemporary pharmaceutical research owing to their capacity to enhance drug bioavailability, enable site-specific targeted accumulation, prolong the systemic circulation duration, facilitate synergistic therapeutic outcomes, and exhibit superior biocompatibility profiles. It is worth noting that cyclodextrin-based drug delivery systems show great potential in inflammation-related diseases. However, few studies have systematically reviewed their design strategies and application advancements. Here, we summarize the structural and chemical modification strategies of cyclodextrins, as well as cyclodextrin-based drug delivery systems and their applications in inflammation-related diseases. In summary, the aim is to provide a bit of insight into the development of cyclodextrin-based drug delivery systems for inflammation-related diseases. Full article