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Current Pharmaceutical Design - Online First

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114 results

1 - 20 of 114 results

    • Design and Synthesis of Novel Spiropyridine Derivatives as Promising Anti-inflammatory and Gene-targeting Agents Against COVID-19

      https://doi.org/10.2174/0113816128379816250712091207
      Available online: 27 October 2025
      Background

      The COVID-19 pandemic, caused by SARS-CoV-2, has highlighted the urgent need for effective antiviral and anti-inflammatory therapies. Spiropyridine derivatives containing a chalcone moiety have shown potential in targeting key enzymes involved in viral replication and inflammation.

      Objective

      To evaluate the inhibitory effects of synthesized spiropyridine derivatives on SARS-CoV-2 main protease (Mpro), secreted phospholipase A2 (sPLA2), and cytosolic phospholipase A2 (cPLA2), and to assess their impact on inflammatory and oxidative stress markers in LPS-treated lung cells.

      Aim

      To develop novel therapeutic agents that can effectively manage COVID-19 and related inflammatory conditions.

      Methods

      The synthesized compounds () were tested for their inhibitory activity against SARS-CoV-2 Mpro, sPLA2, and cPLA2 using assays to determine IC values. Inflammatory markers (COX-2, IL-2, IL-4, TGF-1β, TNF-α) and oxidative stress markers (GSH, SOD, GR, MDA) were measured in LPS-treated lung cells. Gene expression levels of sPLA2 and cPLA2 were also assessed. Molecular docking studies were conducted to analyze the binding affinities and interactions of the compounds with the target enzymes.

      Results

      Compounds showed significant inhibitory activity against SARS-CoV-2 Mpro with IC values of 19.85 µM, 7.31 µM, and 3.73 µM, respectively. For comparison, baicalein's IC value was 13.63 µM. Additionally, these compounds inhibited sPLA2 with IC values of 8.36 µM, 7.31 µM, and 3.73 µM, and cPLA2 with IC values of 20.44 µM, 6.02 µM, and 4.61 µM, respectively. Baicalein's IC values for sPLA2 and cPLA2 were 11.73 µM and 5.89 µM, respectively. In LPS-treated lung cells, compounds significantly reduced COX-2 by up to 90.12%, IL-2 by 74.19%, IL-4 by 79.51%, TGF-1β by 44.57%, and TNF-α by 68.49%. They enhanced GSH by up to 194%, SOD by 357.19%, and GR by 445.87%, while reducing MDA by 77.90%. Gene expression of sPLA2 and cPLA2 was significantly downregulated by up to 82.31% and 64.59%, respectively. Molecular docking studies revealed binding affinities of -28.20, -28.20, and -28.07 kcal/mol for SARS-CoV-2 Mpro; -16.72, -17.21, and -15.89 kcal/mol for sPLA2; and -65.66, -66.95, and -79.24 kcal/mol for cPLA2, respectively.

      Discussion

      The results demonstrate that the structural integration of a spiropyridine core with a chalcone moiety yields compounds with superior multi-target inhibitory activity. The potent antiviral, anti-inflammatory, and antioxidant effects are significantly correlated with their strong binding interactions with the active sites of Mpro, sPLA2, and cPLA2, as validated by molecular docking. These findings align with and extend current research on targeting host-inflammatory pathways alongside viral replication for COVID-19 management.

      Conclusion

      The synthesized spiropyridine derivatives containing a chalcone moiety exhibit potent antiviral, anti-inflammatory, and antioxidant properties. These findings suggest that these compounds could be promising therapeutic agents for managing COVID-19 and related inflammatory conditions. Future studies should focus on experiments, clinical trials, and structural optimization to further develop these compounds for clinical use.

    • Integrating Telemedicine, Virtual Environments, and AI in Digital Healthcare: Advances and Future Directions

      https://doi.org/10.2174/0113816128392838250902182114
      Available online: 14 October 2025
      Objectives

      The delivery of healthcare services information and communication technology, or telemedicine, has grown to be an essential part of modern medicine. This study explores the evolving role of telemedicine, focusing on its expansion into the Metaverse, and evaluates its potential to improve healthcare accessibility, patient engagement, and medical outcomes.

      Methods

      A comprehensive analysis of the literature was conducted, evaluating studies investigating the efficacy of telemedicine in different medical fields, notably mental health, chronic disease management, and post-surgical follow-ups. This study assessed the impact of emerging technologies, specifically virtual reality (VR) and augmented reality (AR), on telemedicine, emphasizing their applications within the Metaverse. Furthermore, ethical considerations, insurance limitations, and technological disparities were assessed.

      Results

      Telemedicine has significantly enhanced healthcare access, especially in remote and underserved regions. Patient satisfaction and purpose to continue with telemedicine services are elevated, particularly in specialized areas like Tele-stroke and mental health counseling.

      Discussion

      The Metaverse has the potential to transform telemedicine through the establishment of immersive and interactive healthcare settings. VR and AR have the potential to facilitate virtual consultations, enhancing the interaction between patients and healthcare professionals. Additionally, the integration of data may lead to improvements in diagnostic accuracy and treatment planning. However, issues such as data privacy, cybersecurity hazards, and the digital gap must be addressed to provide adequate access.

      Conclusion

      Telemedicine has demonstrated significant utility within modern healthcare, and its incorporation with the Metaverse offers novel prospects for improving patient care, advancing medical education, and facilitating collaborative research. Despite the promising benefits, it is crucial to address technological, ethical, and regulatory challenges to ensure widespread adoption and successful implementation.

    • The Effect of Tricyclic Antidepressants on Fracture Healing: An Experimental Study

      https://doi.org/10.2174/0113816128410083250919102413
      Available online: 10 October 2025
      Introduction

      Disorders of mood and post-traumatic stress disorder (PTSD) are common after major trauma, and one of the treatments used is Tricyclic Antidepressants (TCA). These medications work by inhibiting the re-uptake of neurotransmitters like serotonin and noradrenaline. Serotonin is known to have measurable effects on bone tissue due to the presence of specific receptors on bone cells. However, there are conflicting reports about how serotonin signaling affects bone tissue and the process of fracture healing. This study aimed to evaluate the effect of TCAs on fracture healing.

      Method

      Twelve skeletally mature Wistar rats were used in the study. All rats underwent intra-medullary pinning of the right tibia, and a complete mid-diaphyseal fracture was created. The rats were then randomly split into two groups: a control group and a study group. For twenty-eight days, the study group received a daily dose of 10 mg/kg of amitriptyline intraperitoneal infusion, while the control group received an equal volume of plain saline the same route. On day twenty-eight, five hours after the final dose, all rats were euthanized to assess fracture healing using radiological, microscopic, and histological methods.

      Results

      The study found a significant difference in the total volume of new bone formation between the two groups on day twenty-eight. The control group had a mean bone formation volume of 1.077 mm3, whereas the amitriptyline-treated group had a significantly higher mean volume of 1.824 mm3 (<0.01).

      Discussion

      The results suggest that TCAs positively influence the early phases of fracture healing. The increased new bone formation observed in the amitriptyline group indicates a potential therapeutic benefit beyond their known psychiatric effects. This finding adds to the existing literature on the complex relationship between serotonin signaling and bone metabolism, providing evidence that this class of antidepressants may enhance the process of bone repair.

      Conclusion

      Tricyclic Antidepressants, specifically amitriptyline, significantly increase new bone formation in the early stages of fracture healing in Wistar rats.

    • Cataract Management in the Modern Era: Therapeutic Advances and Unmet Needs

      https://doi.org/10.2174/0113816128409580250812000816
      Available online: 09 October 2025

      Cataract remains one of the leading causes of blindness worldwide. Studies have shown that its onset is predominantly age-related, particularly affecting the elderly. According to the latest report by the World Health Organization (WHO), more than fifty percent of global blindness cases are attributed to cataracts alone. If timely and appropriate measures are not implemented, this percentage is projected to double in the coming decades. Therefore, there is an urgent need to develop alternative approaches to manage cataracts more effectively, beyond the current reliance on surgical intervention. In recent years, researchers have been actively exploring simpler, non-surgical treatment options that could potentially dissolve cataracts in their early stages. The successful development of such therapies would mark a significant breakthrough and offer immense benefits to humanity. This article highlights the evolution of surgical techniques used in cataract management, from traditional practices to modern innovations, while also discussing emerging non-invasive strategies such as lanosterol-based pharmacotherapy, nanomedicine-driven drug delivery systems, and regenerative approaches like stem cell therapy. These advances signal a promising future for safer, more accessible, and more effective cataract care.

    • Unveiling the Therapeutic Targets and Active Components of Xianlinggubao Capsule in Osteoarthritis and Osteoporosis through Network Pharmacology and Bioinformatic Analysis

      https://doi.org/10.2174/0113816128406157250911093530
      Available online: 08 October 2025
      Introduction

      The Xianling Gubao capsule (XLGB), a traditional Chinese medicine formulation approved by the China Food and Drug Administration, has been effectively used to treat two common medical conditions: osteoarthritis (OA) and osteoporosis (OP). However, due to the complex ingredients, the molecular mechanisms underlying its therapeutic effects for OA and OP remain unknown.

      Methods

      This study identified XLGB-related therapeutic target genes and pathways for OA and OP by using bioinformatics and network pharmacology. Molecular docking assessed the interactions between core genes and compounds, while quantitative real-time PCR and Western blotting analyses validated the mRNA and protein expression of key target genes.

      Results

      Bioinformatics analysis identified 473 unique genes common to OA and OP. Network pharmacology analysis identified 30 intersecting genes as the principal target genes for anti-OA and anti-OP effects. Ten hub genes were identified using protein-protein interaction as potential therapeutic targets. These genes were related to transcription regulation and enriched in certain signaling pathways, such as interleukin-17 and tumor necrosis factor. Molecular docking analysis revealed danshenxinkun B to exhibit a strong affinity for , , and , while miltirone displayed a strong affinity for . The experimental results have been verified using cellular experiments.

      Discussion

      This study showed , , and to be mainly enriched in interleukin-17 and tumor necrosis factor signaling pathways. Moreover, danshenxinkun B and miltirone significantly modulated the expression levels of these genes.

      Conclusion

      This study has demonstrated that danshenxinkun B and miltirone may be pivotal agents in treating OA and OP by down-regulating the expressions of , , and .

    • Mechanisms, Mediators, and Pharmacological Approaches Targeting Brain Cholesterol Transport in Alzheimer’s Disease

      https://doi.org/10.2174/0113816128411158250909151734
      Available online: 01 October 2025

      Cholesterol transport within the brain represents a highly regulated process essential for maintaining neuronal function and central nervous system (CNS) homeostasis. Unlike peripheral tissues, the brain

      relies on cholesterol synthesis, primarily by astrocytes and other glial cells, which supply neurons high-density lipoprotein (HDL)-like particles, identified in the human cerebrospinal fluid (CSF). The major component of HDL-like lipoproteins is the apolipoprotein E (ApoE), whose E4 isoform represents the strongest genetic risk factor for late-onset Alzheimer’s disease (AD). Growing evidence suggests that impaired cholesterol transport contributes to the pathogenesis of various neurodegenerative disorders, particularly AD, a major public health concern due to increasing prevalence and the lack of effective treatments. Indeed, the unconvincing outcomes of the amyloid-targeting monoclonal antibodies underscore the urgency of identifying alternative therapeutic strategies. This review provides a comprehensive analysis of cholesterol transport mechanisms within the brain and their dysregulation in AD by examining the astrocyte-to-neuron cholesterol supply pathways, including endogenous biosynthesis, cholesterol efflux from astrocytes, neuronal uptake, and intracellular processing. Key molecular players involved in each step are discussed, focusing on their roles in AD pathophysiology and potential as therapeutic targets. Furthermore, the review critically evaluates recent preclinical studies exploring pharmacological interventions able to modulate cerebral cholesterol homeostasis. These emerging approaches offer promising alternatives to amyloid-based treatments and may open new perspectives for preventing or mitigating neurodegeneration in AD. By providing an integrated overview of cholesterol transport in the brain, this review highlights novel directions for research and drug development targeting CNS cholesterol metabolism.

    • Exploring the Mechanism of Bu Zhong Yi Qi Decoction in Treating Sepsis-induced Acute Lung Injury based on Network Pharmacology and Experimental Verification

      https://doi.org/10.2174/0113816128397243250902131510
      Available online: 30 September 2025
      Introduction

      Sepsis-induced acute lung injury (S-ALI) is one of the diseases with a very high fatality rate. However, the traditional Chinese medicine compound Buzhong Yiqi Decoction (BZYQD) has an excellent effect in the treatment of S-ALI. Nevertheless, its mechanism of action is still unclear. In this study, we explored the molecular mechanisms of S-ALI injury treated with buzhong yiqi decoction through network pharmacology, in combination with in vivo experimental validation.

      Methods

      Traditional Chinese medicine system pharmacology (TCMSP) database was used to screen thechemical composition of BZYQD and its action targets; Multiple databases were used to collect target genesfor-S-ALI, including OMIM, TTD, GeneCards, and DrugBank; The STRING database was used for the protein-protein interaction (PPI) analysis of the common targets of the BZYQD and the S-ALI; The DAVID databasewas used for GO and KEGG analysis; molecular docking was used to detect the binding capacity of corecomponents and targets. HE staining was used to visualize the pathology of lung tissue in each group; ELISA wasused to detect the levels of inflammatory factors (IL-1β, IL-6, IL-8, NF-κB and TNF-α) and oxidative stressrelatedfactors (LDH, CK-MB, SOD, GSH-Px); The qPCR and Western blot were used to examine the mRNAand protein expression of IL-1β, IL-6, TNF-α NF-κB, p-NF-κB, PI3K, p-PI3K, AKT, and IKKα.

      Results

      113 chemical components and 226 targets were screened from BZYQD; 9059 S-ALI-related geneswere screened out, with a total of 228 intersecting targets between BZYQD and S-ALI. Stigmasterol, quercetin, and isorhamnetin are the core components of BZYQD, PPI analysis shows that AKT1, IL6, TNF, andIL1B are the core targets of BZYQD for treating S-ALI, and molecular docking results show that the corecomponents have high binding activity with the target; Enrichment analysis shows that these core targets arerelated to the TNF signaling pathway. In vivo experimental studies have found that BZYQD can improve thedegree of inflammatory infiltration and edema in lung tissue of S-ALI model mice, reduce the expression ofIL-6, IL-1β, IL-8, TNF-α, LDH, CK-MB, and NF-κB in serum (P0.05), as well as the mRNA and proteinexpression of IL-6, IL-1β, TNF-α, NF-κB, p-NF-κB, PI3K, p-PI3K, AKT, and IKKα in lung tissue (P0.05),and levels of SOD and GSH-Px were increased (P0.05).

      Discussion

      The action targets of the main chemical components of BZYQD are TNF, AKT, and IL6. Thesetargets can promote the activation of PI3K and TNF pathways and mediate the occurrence of inflammationand oxidative stress, which provides inspiration for the treatment of S-ALI. However, the results of this study still need to be verified in combination with in vitro approaches.

      Conclusion

      This study suggests that the mechanism of BZYQD in treating S-ALI may be achieved by inhibiting the TNF and PI3K signaling pathway and reducing inflammation and oxidative stress levels.

    • Salvianolic Acid B-Loaded Albumin Nanoparticles Reduce Portal Hypertension in Cirrhotic Mice and Inhibit the Proliferation and Contraction of Hepatic Stellate Cells

      https://doi.org/10.2174/0113816128364560250124055417
      Available online: 29 September 2025
      Introduction

      Salvianolic acid B (SAB), as one of the major water-soluble compounds of , has proved to effectively reduce elevated portal pressure in cirrhotic rats. However, the short half-life and retention time of SAB affect its pharmacodynamics. Therefore, in this study, we prepared albumin nanoparticles loaded with SAB (SAB-ALB-NPs) to improve the retention time of the drug and enhance bioavailability.

      Methods

      We prepared and characterized SAB-ALB-NPs, including particle size, polydispersity index (PDI), zeta potential, stability, EE, release, and pharmacokinetics. Subsequently, we investigated the effects and potential mechanisms of SAB-ALB-NPs in CCl-induced portal hypertension (PHT) mice models, and it was found that angiotensin-II (Ang-II) induced proliferation and contraction in hepatic stellate cells (HSCs). The CCl (0.3:1 in corn oil, 1mL/kg) was injected repeatedly, leading to the PHT mice model. The effect of SAB-ALB-NPs on PHT mice was evaluated by hematoxylin-eosin, Sirius red staining, immunohistochemistry, and Western blot.

      Results

      We successfully prepared SAB-loaded albumin nanoparticles with smaller-sized particles, lower PDI and zeta potential with stable properties, and higher EE. Importantly, the SAB-ALB-NPs notably prolonged the release of SAB. SAB-ALB-NPs significantly reduced portal pressure, inhibited inflammation (decrease the concentration of TNF-α and IL-6) and hepatotoxicity of the liver (down-regulated the level of ALT and AST) against fibrous tissue hyperplasia, and reduced collagen deposition in the liver. Afterward, we used Ang-II to facilitate the proliferation of HSCs and induce HSC cell contraction. Cotreatment of SAB-ALB-NPs markedly inhibited Ang II-induced effects on cell proliferation and contraction and improved apoptosis. Importantly, SAB-ALB-NPs were preliminarily found to inhibit the expression of RhoA and ROCK II in Ang-II-treated HSC and CCl-induced PHT mice, suggesting that SAB-ALB-NPs may participate in the regulation of RhoA/ROCK II pathway.

      Conclusion

      SAB-ALB-NPs improved portal hypertension by suppressing inflammation and inhibiting HSCs activation and proliferation to attenuate liver fibrosis. This therapeutic function of SAB-ALB-NPs may be owing to SAB-ALB-NPs regulating the RhoA/ROCK2 pathway, which may be one of its molecular mechanisms for reducing portal hypertension.

    • Para-probiotics as Novel Anti-Inflammatory Agents: Insight into Health Benefits and Therapeutic Applications

      https://doi.org/10.2174/0113816128411949250909113034
      Available online: 29 September 2025

      Para-probiotics, also referred to as non-viable microbial cells or cell components that confer health benefits, are emerging as promising agents in the prevention and management of inflammation-associated diseases. Unlike traditional probiotics, which require viability for efficacy, these inactivated forms offer significant advantages in terms of safety, stability, and applicability in vulnerable populations, including immunocompromised individuals. Recent studies have highlighted their capacity to modulate immune responses, enhance mucosal defense mechanisms, and reinforce intestinal barrier integrity through interactions involving microbial-associated molecular patterns (MAMPs) and host pattern recognition receptors. Such interactions influence signaling cascades like NF-κB, MAPKs, and inflammasome pathways, contributing to anti-inflammatory and immunomodulatory effects. One of the key advantages is the reduced risk of adverse effects and concerns associated with live probiotic use. In addition, their robust physicochemical stability under industrial processing conditions supports their incorporation into a range of functional foods and nutraceuticals. Despite these advantages, their mechanisms of action remain incompletely understood and require further investigation. This review synthesizes current evidence on their anti-inflammatory properties, highlights preclinical and clinical studies, and discusses technological approaches for their production. Overall, these bioactives represent a safe, stable, and efficacious alternative to traditional probiotics in managing inflammatory disorders.

    • YF Reduces Alveolar Epithelial Cell Apoptosis and PF by Inactivating JAK2/STAT3

      https://doi.org/10.2174/0113816128403995250828105423
      Available online: 25 September 2025
      Introduction

      Pulmonary fibrosis (PF) is a chronic pulmonary disorder with unknown etiology and an irreversible course. Traditional Chinese medicine (TCM) possesses promising clinical benefits for PF treatment through a multi-component and multi-target approach. This study evaluates the efficacy of Yangyin Yifei Tongluo Wan (YF), a traditional formulation, in the treatment of PF, and further explores the underlying mechanism.

      Methods

      A bleomycin (BLM)-induced PF mouse model was established. Mice were administered with low-, medium-, and high-dose YF (1.5, 3, and 6 g/kg/d, respectively). The fibrosis degree of mouse lung tissues was evaluated by morphometric measurements and hydroxyproline (HYP) analysis. Network pharmacology-based bioinformatics were employed for constructing a network involving components, targets, and disease, and YF's potential mechanism and molecular targets for PF therapy were explored. This was further validated by TUNEL staining, Western blot, RT-qPCR, and ELISA in BLM-treated mice.

      Results

      YF could relieve PF in BLM-treated mice in a dose-dependent manner, evidenced by a notable decrease in collagen deposition, and collagen I and III, HYP, fibronectin, vimentin, and α-SMA expressions. Network pharmacology revealed that JAK2/STAT3 signaling pathway-mediated alveolar epithelial cell apoptosis may be a potential therapeutic target for YF in treating PF. assays confirmed that YF's anti-fibrosis effect on BLM-induced PF was ascribed to the suppression of alveolar epithelial cell apoptosis and disruption of the JAK2/STAT3 signaling pathway.

      Discussion

      YF can block alveolar epithelial cell apoptosis through inactivation of the JAK2/STAT3 signaling, subsequently enhancing the resolution of PF.

      Conclusion

      YF may be a promising therapeutic candidate for PF treatment.

    • Preparation and Evaluation of Sodium Alginate Nanoparticles Containing Recombinant Diphtheria Toxoid (CRM) and their Immunogenicity in Mice

      https://doi.org/10.2174/0113816128402345250905072744
      Available online: 18 September 2025
      Introduction

      Recombinant protein vaccines against infectious diseases, based on immunogenic antigen identification and employing polymeric nanoparticles as a delivery system, can provoke immune responses comparable to or better than traditional vaccines. The production of a safe and immunogenic vaccine against diphtheria was achieved by preparing sodium alginate nanoparticles containing recombinant diphtheria toxoid (CRM).

      Methods

      Alginate nanoparticles loaded with CRM were prepared using the ionic-gelation method and thoroughly characterized. Safety and immunogenicity studies were conducted in an animal model for comparison with commercial vaccines. Antibody responses were evaluated using both qualitative and quantitative measurements, as determined by the toxin neutralization test (TNT) and indirect ELISA, respectively. IgG subclasses in the sera of immunized mice and possible pathological lesions in vital tissues of all immunized mouse groups were investigated.

      Results

      Nanoparticles with or without CRM were synthesized by the ionic gelation method. LE and LC measurements showed ˃80% and ˃20%, respectively, indicating stable and persistent release without a bursting pattern. studies showed safety and enhanced immunogenicity in mice immunized with the CRM-loaded sodium alginate nanoparticles, with higher levels of total anti-CRM IgG and subclasses than those induced by conventional vaccines.

      Discussion

      Reducing antigen usage in vaccine production while increasing immunogenicity and safety compared with traditional vaccines are the goals of new vaccine development, which were achieved in the current study.

      Conclusion

      Engineered alginate nanoparticles loaded with recombinant diphtheria antigen (CRM) demonstrated controlled and slow release, as well as safety and immunogenicity profiles against diphtheria. Nanoparticles containing CRM antigens equivalent to adult and children doses showed high levels of IgG1 and IgG2a, confirming the combined responses of the humoral and cellular immune systems.

    • Quantification and Engineering of Lipid Nanocapsule Formulations for the Delivery of Niclosamide as an Anti-Cancer Drug

      https://doi.org/10.2174/0113816128385620250829061535
      Available online: 12 September 2025
      Introduction

      Recent studies indicate that niclosamide demonstrates considerable promise as both an anthelmintic agent and a possible anticancer medication. Given the increasing interest in nano-sized drug delivery methods for cancer therapy, lipid nanocapsules (LNCs) have emerged as a viable approach to enhance the bioavailability of poorly soluble pharmaceuticals due to their beneficial properties. This research intends to develop niclosamide-loaded lipid nanocapsules (NIC-LNCs) using the phase inversion technique, followed by the optimization of these formulations the Box-Behnken experimental design.

      Methods

      A reverse-phase high-performance liquid chromatography (RP-HPLC) method was devised and validated for quantifying niclosamide in the LNC formulations. Optimal chromatographic separation was attained utilizing an Agilent Eclipse XDB-C18 column (150×4.6 mm, 5 µm i.d.) with a mobile phase of a 50:50 mixture of acetonitrile and 0.1% HPO phosphate buffer, at a flow rate of 1.2 mL/min. The detection wavelength was set at 335 nm, and the analysis was performed at 35°C. The developed analytical methodology was validated through a comprehensive evaluation of accuracy, linearity, precision, limit of detection, limit of quantitation, specificity, and stability.

      Results

      The optimization of the NIC-LNC formulation through the Box-Behnken design resulted in an optimal formulation labeled LNC5, consisting of 4% niclosamide, 20% lipid, and 20% surfactant. The proven RP-HPLC method enables accurate quantification of NIC in the LNC formulations. The refined NIC-LNC formulation exhibited developed attributes as assessed by the design.

      Discussion

      NIC-LNCs were successfully prepared with particle sizes below 100 nm, narrow size distributions (PDI<0.2), and negative zeta potential values in accordance with the literature. All formulations exhibited high encapsulation efficiency and sustained drug release profiles. The optimum formulation revealed a particle size of 43.29 ± 0.32 nm, encapsulation efficiency of 99.99 ± 0.02%, and drug release at one week of 68.85 ± 1.76%. The formulation maintained stability throughout the short-term study period.

      Conclusion

      The findings indicate that LNC systems are a promising method for drug administration, especially for anticancer drugs with limited solubility in water.

    • Ranking the Diabetes-related Safety Profile of Different Statin Drugs

      https://doi.org/10.2174/0113816128430202250902074509
      Available online: 12 September 2025
      Introduction

      Statins are widely prescribed for cardiovascular disease prevention, but their potential to increase diabetes risk has prompted regulatory warnings. Different statin drugs have varying physicochemical properties, yet comprehensive comparative assessments of their individual diabetes-related safety profiles remain limited in post-marketing surveillance data. Therefore, this study aimed to evaluate and compare the risk of diabetes-related adverse events among different statin drugs using pharmacovigilance data.

      Methods

      We analyzed adverse event reports from the FDA Adverse Event Reporting System (FAERS) database from 2004 to 2022. Diabetes-related adverse events were identified using relevant MedDRA Preferred Terms. Four pharmacovigilance algorithms—Reporting Odds Ratio (ROR), Medicines and Healthcare products Regulatory Agency (MHRA) standard method, Bayesian Confidence Propagation Neural Network, and Multi-Item Gamma Poisson Shrinkage—were employed to detect signals. Positive signals were defined when all four methods showed significance. Outcome severity and time-to-event were also analyzed.

      Results

      Among 13,438,409 ADE reports, 63,583 identified statins as primary suspect drugs, with 11,562 reporting diabetes-related events. Positive signals were detected for atorvastatin, rosuvastatin, simvastatin, pravastatin, and pitavastatin. Signal strength ranking showed atorvastatin had the strongest association (ROR 36.70; 95% CI 35.92-37.51), followed by rosuvastatin (ROR 9.63; 95% CI 9.10-10.19), pitavastatin (ROR 5.46; 95% CI 4.03-7.41), simvastatin (ROR 2.96; 95% CI 2.54-3.45), and pravastatin (ROR 2.82; 95% CI 2.14-3.71). In patients under 45, only atorvastatin showed a positive signal. Atorvastatin was associated with a higher risk of serious adverse events (PRR=1.37; 95% CI: 1.09-1.71) with a median time to event of 1,012 days.

      Discussion

      Our findings revealed differences in diabetes-related risk profiles among statins, with atorvastatin demonstrating the strongest signals across different age groups. The observed risk hierarchy may be attributed to differences in lipophilicity, potency, and metabolic effects. The age-dependent patterns and extended time-to-event for diabetic events underscore the importance of long-term monitoring, complementing clinical trial data with post-marketing surveillance evidence for improved statin selection.

      Conclusion

      Different statins demonstrate varying associations with diabetes-related adverse events, with atorvastatin showing the strongest signal across age groups. These findings may inform clinical decision-making when prescribing statins, particularly for patients with pre-existing diabetes risk factors.

    • Nasal Microbiota as a Potential Therapeutic Target for Allergic Rhinitis: An Emerging Perspective

      https://doi.org/10.2174/0113816128388496250812102820
      Available online: 11 September 2025

      Allergic Rhinitis (AR) represents a significant global health challenge with extensive prevalence and profound impacts, necessitating the development of novel therapeutic approaches beyond conventional symptomatic treatment. Emerging research has elucidated the crucial role of nasal microbiota dysbiosis in both the pathogenesis and progression of AR. Although the dominant microbial phyla remain largely consistent, significant changes in microbial abundance, composition, and diversity are often observed. In addition, studies have shown a correlation between changes in nasal microbiota and immune markers such as immunoglobulin E levels, suggesting that microbiota changes can reflect the severity of AR. Therefore, targeted modulation of the aberrant nasal microbiota may offer a promising therapeutic approach for this disease. However, further research is crucial for elucidating the causal relationships between specific microbial characteristics, disease severity, and potential comorbidities. This article summarizes recent studies examining the pathogenic role of nasal microbiota dysbiosis, the differential microbial composition across nasal mucosal sites, and potential therapeutic targets in AR. The ultimate goal is to develop precision medicine-based therapeutic interventions that target the underlying pathophysiological mechanisms of AR through specific modulation of dysbiotic nasal microbiota, thereby potentially preventing disease progression and reducing the risk of associated comorbidities.

    • Unraveling the Complexity of Polycystic Ovary Syndrome: Biomarkers for Diagnosis, Prognosis, and Treatment

      https://doi.org/10.2174/0113816128382284250822045319
      Available online: 09 September 2025

      Polycystic ovary syndrome is distinguished by alterations in ovarian morphology, ovulatory failure, and increased androgen levels. The National Institutes of Health (NIH) defines it as ovulatory dysfunction accompanied by hyperandrogenism. Women with PCOS may have obesity, type 2 diabetes, anxiety, hypertension, insulin resistance, and pregnancy-related complications. PCOS is additionally linked with a greater chance of cardiovascular and metabolic disorders. Several factors, including LH/FSH ratio, FAI levels, and ovarian USG, should be considered when diagnosing PCOS. The Rotterdam criterion is employed to determine the condition when two of the three features are present and other etiologies are eliminated. Biomarkers have developed as a means of optimizing PCOS diagnosis and treatment results. This review has examined a number of biomarkers associated with PCOS, such as insulin, anti-Mullerian hormone, oxidative stress markers, inflammatory markers, and others. Controlling these disease-related markers may aid in lessening the symptoms of PCOS.

    • Flavonoids as Dual Inhibitors of MELK and LYN Kinases in Cervical Cancer: An Molecular Docking Analysis

      https://doi.org/10.2174/0113816128387273250823102532
      Available online: 05 September 2025
      Introduction

      Cervical cancer (CC) is among the most prevalent cancers affecting women globally, with a substantial number of deaths reported annually. Despite advancements in treatment, the persistently high mortality rate underscores the urgent need for novel and effective therapeutic strategies.

      Methods

      This study screened a library of 240 flavonoids against maternal embryonic leucine zipper kinase (MELK) and LYN using molecular docking methods to achieve precise calculations. These proteins play critical roles in CC progression, and their simultaneous inhibition could mark a significant step forward in multitargeted drug design.

      Results

      Molecular docking revealed binding affinities ranging from -10.0649 to -8.14296 kcal/mol for MELK and -10.2748 to -8.5237 kcal/mol for LYN. The screening process was complemented by pharmacokinetics and interaction fingerprinting analyses, which confirmed that the flavonoids effectively bound to optimal sites, forming stable complexes through multiple interactions. Molecular dynamics simulations extended to 100 ns further validated the stability of these protein-ligand complexes.

      Discussion

      The findings indicate that the top-ranked compounds exhibit strong binding affinities and stable interactions, highlighting their potential as multitargeted therapeutic agents against CC.

      Conclusion

      These findings set the stage for future experimental and clinical studies to validate our results and facilitate the development of novel, flavonoid-based therapeutic strategies against cervical cancer, potentially revolutionizing the treatment landscape of this disease.

    • Green Tea Catechins and COVID-19: Epidemiological Trends and Therapeutic Perspectives

      https://doi.org/10.2174/0113816128412495250824132514
      Available online: 01 September 2025
      Introduction

      Pharmacological studies demonstrate the preventive and therapeutic potential of green tea and its constituent epigallocatechin-3-gallate (EGCG) in the fight against coronavirus disease 2019 (COVID-19). Previously reported correlations between green tea consumption and COVID-19 morbidity/mortality suggest similar effects . Considering that some recent SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2) sub-variants are less influenced by EGCG, this study aimed to determine whether this affects the aforementioned correlations, focusing on comparisons between the periods before (2021) and after (2022-2024) the emergence of the Omicron variant.

      Methods

      Correlations between green tea consumption and COVID-19 morbidity/mortality were calculated using multiple regression models accounting for several confounding factors in a subset (n=84) of countries/territories worldwide with Human Development Index (HDI) above 0.55.

      Results

      Higher green tea consumption was associated with lower COVID-19 morbidity and mortality. Statistically significant correlations were observed in 2021-2024. Compared with 2021, the strength of both correlations decreased; the relative decrease in the strength of the correlation between green tea consumption and COVID-19 mortality was notably less pronounced.

      Discussion

      This differential decrease at the epidemiological level supports the idea that green tea consumption may have not only preventive but also therapeutic value regarding COVID-19. This aligns with in pharmacological evidence indicating that green tea constituents target distinct molecular pathways responsible for the entry of the virus and its replication.

      Conclusion

      While promising, these findings require further assessment in observational and interventional studies focused on potential therapeutic benefits.

    • Watermelon Rind: Nutritional Composition, Therapeutic Potential, Environmental Impact, and Commercial Applications in Sustainable Industries

      https://doi.org/10.2174/0113816128371677250806001232
      Available online: 27 August 2025

      (watermelon) is a fruit with remarkable therapeutic potential, as each part of it- rind, peel, flesh, and seeds contain bioactive compounds. Despite its wide range of benefits, the utilization of watermelon, particularly its rind, remains limited due to a lack of awareness and an underrated perspective. The rind, situated between the green outer peel and the red flesh, is light green in color and rich in bioactive compounds, minerals, and phytochemicals. These constituents are associated with various therapeutic properties, including antioxidant, antineoplastic, cardiovascular, and neuroprotective effects. In addition to its therapeutic applications, watermelon rind offers significant commercial value in the food, cosmetic, and pharmaceutical industries, as well as in industrial applications such as biofuel production and eco-friendly packaging. Its versatility makes watermelon rind an exciting area of research for uncovering new applications and enhancing existing ones. However, limitations in its usage and handling need to be addressed for its broader adoption. This review comprehensively discusses the global research conducted to date on the nutritional composition, therapeutic potential, environmental impact, and commercial applications of watermelon rind. Additionally, it highlights challenges and future directions for advancing the utilization of this promising 
resource.

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