Journal of Drug Targeting最新文献

In vitro and in vivo assessment of the bioavailability and efficacy of carvedilol-loaded novasomes as a therapy for diabetes mellitus-associated ischemic stroke. 卡维地洛负载novasome治疗糖尿病相关缺血性脑卒中的生物利用度和疗效的体内外评估

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2025-11-03 DOI: 10.1080/1061186X.2025.2578290

Amr Gamal Fouad, Amany Belal, Alaa Ismail, Fahad H Baali, Mohammed S Alharthi, Fatma I Abo El-Ela

{"title":"In vitro and in vivo assessment of the bioavailability and efficacy of carvedilol-loaded novasomes as a therapy for diabetes mellitus-associated ischemic stroke.","authors":"Amr Gamal Fouad, Amany Belal, Alaa Ismail, Fahad H Baali, Mohammed S Alharthi, Fatma I Abo El-Ela","doi":"10.1080/1061186X.2025.2578290","DOIUrl":"10.1080/1061186X.2025.2578290","url":null,"abstract":"Ischaemic stroke (IS) occurs when there is a deprivation of oxygen and nutrients in brain tissue. Diabetes mellitus (DM) is recognised as a possible factor contributing to this illness. Carvedilol exhibits anti-stroke effects; however, its insolubility and short half-life contribute to its ineffectiveness. The goal of this study was to create carvedilol-novasomes (CNF) nanovesicles for nasal spray as a potential DM-associated IS treatment that would increase sustainability, bioavailability, targeting and effectiveness of carvedilol. To optimise different CNF formulations, the Box-Behnken design was utilised. The optimal CNF formulation underwent in vivo evaluation in an experimental rat model of DM-associated IS. The optimal CNF formulation enhanced sustainability, bioavailability and permeability of carvedilol by 71.93%, 5.79-fold and 7.30-fold, respectively. The optimal CNF demonstrated anti-ischaemic effects by significantly enhancing various measures, including flexion, spontaneous motor activity, grip strength and target quadrant location time, with improvements of 93.72%, 88.53%, 96.57% and 353%, respectively, in comparison to the positive control group. The optimal CNF also improved the drug's targeting to the brain. These results indicate that a nasal spray formulation of the optimal CNF could serve as a promising therapy for DM-associated IS.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"817-833"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145345453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Advancement on nanoparticles-based approaches for the management of rheumatoid arthritis (RA): molecular mechanism, toxicity, and clinical perspectives. 纳米颗粒治疗类风湿性关节炎（RA）的进展：分子机制、毒性和临床前景

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2025-10-30 DOI: 10.1080/1061186X.2025.2577132

Sabya Sachi Das, Md Sadique Hussain, Srushti Tambe, Shubham Mundhe, Ankita Acharya, Adrija Bhunia, Sourav Mohanto, Mohammed Gulzar Ahmed

{"title":"Advancement on nanoparticles-based approaches for the management of rheumatoid arthritis (RA): molecular mechanism, toxicity, and clinical perspectives.","authors":"Sabya Sachi Das, Md Sadique Hussain, Srushti Tambe, Shubham Mundhe, Ankita Acharya, Adrija Bhunia, Sourav Mohanto, Mohammed Gulzar Ahmed","doi":"10.1080/1061186X.2025.2577132","DOIUrl":"10.1080/1061186X.2025.2577132","url":null,"abstract":"The nanoparticles (NPs) exhibited significant pharmacological potential due to their inherent physicochemical and biological characteristics in biomedical and tissue engineering applications. Rheumatoid arthritis (RA) is a chronic, inflammatory, genetically modulated disorder of the inflamed bone joints, resulting in discomfort and slow degeneration of the synovial membrane and cartilage. The conventional therapeutics for RA exhibited several limitations, predominantly inadequate pharmacokinetic properties and site-specific delivery. In this context, nanoparticles can enhance targeted drug delivery through the synovial membrane, regulate immune responses, provide real-time disease monitoring, and improve bioavailability. In addition, several therapeutics-loaded nanoparticles also promoted chondrocyte proliferation and matrix synthesis, which may support cartilage regeneration. Thus, the primary objective of this comprehensive review was to assess the various nanoparticle-based treatment approaches for RA management. The article initially delves into the primary molecular mechanism and genetic factors in RA progression, comprehends the recommended treatment protocol to justify the need for nanoparticles in RA treatment. This review discusses a comprehensive explication of advancement in nanoparticle treatment strategies and safety assessments. This article is a unique composition of different NPs effectiveness, toxicity assessment, focusing on the genetic modulation in RA management along with toxicity assessment and clinical perspectives.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"721-752"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145318351","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Carbon nanodots in breast cancer management: emerging tools for diagnosis and therapy. 碳纳米点在乳腺癌管理：新兴的诊断和治疗工具。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2025-11-10 DOI: 10.1080/1061186X.2025.2581988

Vrutti Parmar, Krina Patel, Sachin Sharma, Kundan Kumar Chaubey, Shailendra Thapliyal, Devesh U Kapoor

{"title":"Carbon nanodots in breast cancer management: emerging tools for diagnosis and therapy.","authors":"Vrutti Parmar, Krina Patel, Sachin Sharma, Kundan Kumar Chaubey, Shailendra Thapliyal, Devesh U Kapoor","doi":"10.1080/1061186X.2025.2581988","DOIUrl":"10.1080/1061186X.2025.2581988","url":null,"abstract":"Breast cancer is still a major global health issue and calls for innovative approaches for both early detection and effective treatment. Because of their distinct optical characteristics, biocompatibility and ease of surface functionalisation, carbon nanodots (CANDs), a novel class of carbon-based nanomaterials, have become effective agents in cancer nanomedicine. This review comprehensively explores the synthesis, physicochemical characteristics and functionalisation strategies of CANDs relevant to oncological applications. The review entails their mechanisms of action, including cellular uptake, tumour microenvironment (TME) modulation and reactive oxygen species generation. CANDs offer remarkable potential in breast cancer diagnosis through fluorescence imaging, photoacoustic and MRI enhancement, and biosensing, with advances towards point-of-care diagnostics. Therapeutically, CANDs serve as carriers for drug, gene and small interfering RNA (siRNA) delivery, and enable modalities such as photothermal, photodynamic and chemo-phototherapy, with emerging applications in immunotherapy. Additionally, theranostic systems integrating diagnostic and therapeutic functionalities are highlighted. The review also addresses clinical progress, patents and translational challenges while projecting future directions involving AI and hybrid nanodots, paving the way for next-generation breast cancer management.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"767-786"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145409141","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Use of methotrexate carried in lipid core nanoparticles in rats with endotoxemia: a possible new strategy for the treatment of the cardiac dysfunction in sepsis. 在内毒素血症大鼠中使用脂核纳米颗粒携带的甲氨蝶呤：一种治疗败血症心功能障碍的可能新策略。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2025-11-17 DOI: 10.1080/1061186X.2025.2585040

Natalia de Menezes Lopes, Maria Carolina Guido, Priscila de Oliveira Carvalho, Camila Inagaki Albuquerque, Leonardo Jensen, Victor Debbas, Ludhmila Abrahão Hajjar, Raul Cavalcante Maranhão

{"title":"Use of methotrexate carried in lipid core nanoparticles in rats with endotoxemia: a possible new strategy for the treatment of the cardiac dysfunction in sepsis.","authors":"Natalia de Menezes Lopes, Maria Carolina Guido, Priscila de Oliveira Carvalho, Camila Inagaki Albuquerque, Leonardo Jensen, Victor Debbas, Ludhmila Abrahão Hajjar, Raul Cavalcante Maranhão","doi":"10.1080/1061186X.2025.2585040","DOIUrl":"10.1080/1061186X.2025.2585040","url":null,"abstract":"Cardiac dysfunction is a major cause of death in endotoxemia. Previously, we showed that methotrexate (MTX) carried in lipid-core nanoparticles (LDE) can modulate immune response and increase myocardial angiogenesis. The aim was to test the effects of LDE-methotrexate (LDEMTX) in rats with endotoxemia. Twenty male rats received I.P. injections of lipopolysaccharides (LPS, 10 mg/kg twice, 24h interval) and were allocated to 3 groups: LPS-LDEMTX, injected I.P. with 1 mg/kg MTX associated with LDE; LPS-MTX with conventional MTX (1 mg/kg, I.P.); LPS-LDE, injected with LDE only. A control group (CT) without endotoxemia was included. Echocardiography was performed 72h after endotoxemia induction. Animals were euthanized for analysis. LPS-LDE developed LV diastolic dysfunction, which was prevented in both LPS-LDEMTX and LPS-MTX groups. LPS-LDEMTX, but not LPS-MTX, developed compensatory LV hypertrophy. In LPS-LDEMTX, cellular hypoxia was lower, and angiogenesis was higher than in LPS-MTX and LPS-LDE, indicated by expression of hypoxia-inducible factor 1α, vascular endothelial growth factor and angiopoietin 1/2, respectively. Intracellular adenosine was increased in LPS-LDEMTX, with higher adenosine receptor expression. LPS-MTX but not LPS-LDEMTX showed hepatic toxicity. In conclusion, both LDEMTX and MTX prevented diastolic dysfunction in endotoxemia, but LDEMTX was further capable of improving several other parameters and had no toxicity.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"899-911"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145482301","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Astragaloside-Soluplus/TPGS/glycyrrhizic acid ammonium salt mixed micelles: preparation and pharmacodynamic evaluation. 黄芪甲苷/TPGS/甘草酸铵盐混合胶束的制备及药效学评价

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2025-10-27 DOI: 10.1080/1061186X.2025.2576120

Hong Chen, Michael Adu-Frimpong, Lili Yuan, Yaping Yang, Jollibekov Berdiyar, Jiangnan Yu, Xia Cao, Qilong Wang, Ximing Xu

{"title":"Astragaloside-Soluplus/TPGS/glycyrrhizic acid ammonium salt mixed micelles: preparation and pharmacodynamic evaluation.","authors":"Hong Chen, Michael Adu-Frimpong, Lili Yuan, Yaping Yang, Jollibekov Berdiyar, Jiangnan Yu, Xia Cao, Qilong Wang, Ximing Xu","doi":"10.1080/1061186X.2025.2576120","DOIUrl":"10.1080/1061186X.2025.2576120","url":null,"abstract":"Astragaloside, a natural flavonol glycoside isolated from plants, exhibits significant tumour-suppressive activity. However, its low solubility and poor bioavailability have hindered its practical application. To improve its bioavailability and therapeutic efficacy, this study prepared Ast-loaded Soluplus/TPGS/Gas hybrid polymer micelles (Ast-STG-M) via the thin-film hydration method. The resulting Ast-STG-M nanoparticles were spherical and uniformly dispersed, characterised by a small particle size (50.92 ± 0.13 nm) and a high encapsulation efficiency (95.24 ± 0.53%). In vitro release profiles demonstrated that the cumulative release rate of Ast from Ast-STG-M was higher than that of free Ast under various pH conditions. After oral administration, compared with free Ast, Ast-STG-M exhibited delayed in vivo elimination and significantly increased bioavailability. Furthermore, results from in vitro and in vivo anti-tumour studies indicated that Ast-STG-M could significantly inhibit the viability of TPC-1 cells, thereby effectively suppressing the growth of solid tumours. In conclusion, Ast-STG-M holds substantial potential as a delivery system for Ast to tumour sites, which not only enhances the oral bioavailability of Ast but also strengthens its anti-cancer activity.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"805-816"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145337074","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Nanotechnology-based PD-L1 siRNA codelivery systems for improving cancer immunotherapy. 基于纳米技术的PD-L1 siRNA共递送系统改善癌症免疫治疗。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2026-02-16 DOI: 10.1080/1061186X.2025.2581984

Naghmeh Jabarimani, Mohammad Saleh Sadeghi, Maryam Edalat, Fatemeh Atyabi, Farhad Jadidi-Niaragh, Farid Abedin Dorkoosh

{"title":"Nanotechnology-based PD-L1 siRNA codelivery systems for improving cancer immunotherapy.","authors":"Naghmeh Jabarimani, Mohammad Saleh Sadeghi, Maryam Edalat, Fatemeh Atyabi, Farhad Jadidi-Niaragh, Farid Abedin Dorkoosh","doi":"10.1080/1061186X.2025.2581984","DOIUrl":"10.1080/1061186X.2025.2581984","url":null,"abstract":"Immune checkpoint blockade targeting the PD-1/PD-L1 (Programmed cell death protein 1/Programmed death-ligand 1) axis has transformed cancer therapy. However, antibodies non-specifically bind to PD-1 or PD-L1 on both malignant and normal cells, resulting in immune-related adverse events and limited therapeutic selectivity. Additionally, antibodies only target cell-surface PD-1/PD-L1, whereas intracellular proteins can translocate to the membrane, enabling immune evasion. In contrast, small interfering RNA (siRNA) can specifically silence PD-1 or PD-L1 on the cell surface and within the cytoplasm, mitigating immune suppression, reducing drug resistance, and limiting systemic off-target effects. Despite the clinical success of immune checkpoint inhibitors, monotherapy benefits only a fraction of patients. Combination therapies incorporating chemotherapy, radiotherapy, or photo-mediated therapy have shown improved efficacy. Nanoparticles offer a promising approach for combination therapy by overcoming RNA delivery challenges, enabling efficient tumour-targeting capacity, providing tumour-responsive behaviour, and versatility for combination therapy. This review presents an overview of different nanoparticles, including polymer and lipid nanoparticles, developed for the codelivery of PD-L1 siRNA and other therapeutic modalities with different properties. Furthermore, discusses mechanisms underlying PD-L1-mediated tumour therapy, and finally, highlights current challenges and perspectives for translating nanoparticle-based combinatorial immunotherapy into clinical applications.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"753-766"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145767984","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Retraction: Chitosan tamarind-based nanoparticles as a promising approach for topical application of curcumin intended for burn healing: in vitro and in vivo study. 撤回：壳聚糖罗望子纳米颗粒作为姜黄素局部应用的一种有前途的方法，用于烧伤愈合：体外和体内研究。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2026-03-23 DOI: 10.1080/1061186X.2026.2647484

引用次数: 0

In vitro and in vivo evaluation of the therapeutic efficacy of in-situ pH-sensitive carvedilol-loaded novasomes as a therapy for diabetes-associated coronary artery disease. 体外和体内评价原位ph敏感卡维地洛负载novassomes治疗糖尿病相关冠状动脉疾病的疗效

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2025-11-06 DOI: 10.1080/1061186X.2025.2581985

Amr Gamal Fouad, Amany Belal, Alaa Ismail, Fahad H Baali, Mohammed S Alharthi, Fatma I Abo El-Ela

{"title":"In vitro and in vivo evaluation of the therapeutic efficacy of in-situ pH-sensitive carvedilol-loaded novasomes as a therapy for diabetes-associated coronary artery disease.","authors":"Amr Gamal Fouad, Amany Belal, Alaa Ismail, Fahad H Baali, Mohammed S Alharthi, Fatma I Abo El-Ela","doi":"10.1080/1061186X.2025.2581985","DOIUrl":"10.1080/1061186X.2025.2581985","url":null,"abstract":"Hyperglycaemia contributes to vascular dysfunction in coronary artery disease (CAD) by causing damage to endothelial cells and smooth muscle in the blood vessels. Carvedilol (CRD), a non-selective β- and α1-blocker, is approved for treating diabetes-associated CAD. However, CRD's short half-life and poor solubility limit its oral bioavailability and effectiveness. This study aimed to develop a nasal formulation of in-situ pH-sensitive CRD-loaded novasomes (ISCLN) to enhance CRD's sustainability, bioavailability, and efficacy as a therapy for diabetes-associated CAD. The Box-Behnken design was employed to determine the optimised formulation of CRD-loaded novasomes. This formulation was subsequently combined with chitosan and glyceryl monooleate to create ISCLN. The ISCLN was then evaluated in vivo using a rat model of experimental diabetes and CAD. Compared to free CRD, ISCLN significantly improved sustainability, bioavailability, targeting, and permeability of CRD. Relative to the positive control group, the ISCLN group exhibited decreased levels of glucose, cholesterol, triglycerides, low-density lipoprotein, lactate dehydrogenase, and creatine kinase-MB. Additionally, this group showed increased levels of high-density lipoprotein. Histopathological and toxicity studies confirmed the efficacy and safety of the ISCLN. These findings suggest that a nasal ISCLN formulation may serve as a potential therapy for diabetes-associated CAD.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"885-898"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145400955","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Targeted colon cancer therapy using lapatinib-encapsulated chitosan nanoparticles conjugated with lactoferrin and melatonin with integrated in silico in vitro and in vivo evaluation. 拉帕替尼包封壳聚糖纳米颗粒结合乳铁蛋白和褪黑素的体外和体内评价

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2025-11-04 DOI: 10.1080/1061186X.2025.2578296

Upasana, Sankha Bhattacharya, Vishal Beldar, Preeti Chidambar Sangave, Shashikant Bagade, Satyam Sharma, Rehan Khan

{"title":"Targeted colon cancer therapy using lapatinib-encapsulated chitosan nanoparticles conjugated with lactoferrin and melatonin with integrated in silico in vitro and in vivo evaluation.","authors":"Upasana, Sankha Bhattacharya, Vishal Beldar, Preeti Chidambar Sangave, Shashikant Bagade, Satyam Sharma, Rehan Khan","doi":"10.1080/1061186X.2025.2578296","DOIUrl":"10.1080/1061186X.2025.2578296","url":null,"abstract":"Colorectal cancer is major cause of mortality, necessitating improved treatments. Lapatinib-loaded chitosan nanoparticles conjugated with lactoferrin and melatonin (LAP-CS-LF-MLT-NPs) developed using ionic gelation and carbodiimide coupling to improve bioavailability and minimise toxicity. Nanoparticles had a size of 184.36 ± 1.25 nm, a zeta potential of +31.88 ± 1.21 mV, and an entrapment efficiency of 68.23 ± 1.69%. FTIR, XRD, DSC, Raman, and NMR validated drug encapsulation, whereas FE-SEM, TEM, and AFM displayed uniform, smooth, spherical structures. In vitro, LAP-CS-LF-MLT-NPs displayed an IC50 of 0.17 µg/mL in HCT116 cells compared to 127 µg/mL for free lapatinib, indicating a 700-fold enhancement in potency. Further investigations revealed a 48.29% arrest in G1-phase, a 233.44% disruption of mitochondrial membrane potential, and a 4.15% occurrence of late apoptosis, while ROS levels decreased to 54.13%, indicating melatonin's facilitation of ROS-independent apoptosis. Molecular docking demonstrated strong binding to EGFR (-12.014), SRC (-10.778), and MAPK14 (-10.298). Pharmacokinetic studies in Wistar rats showed a longer half-life (9.69 vs. 5.28 h), higher AUC0-∞ (452.880 vs. 159.715 µg/mL·h), and improved MRT (15.260 vs. 7.696 h). Focused colon retention (8.20 ± 1.38 µg/g), minimal toxicity, and confirmed safety and stability underscore its potential as an accurate, efficient treatment for colon cancer.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"834-884"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145438209","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Ivabradine, a hyperpolarization-activated channel blocker, attenuates mechanical, but not heat, hypersensitivity in hyperglycaemic and normoglycemic rat models of diabetic neuropathy. 伊伐布雷定是一种超极化激活通道阻滞剂，可减轻高血糖和正常血糖大鼠糖尿病神经病变模型的机械性超敏反应，但不能减轻热敏反应。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-06-01 Epub Date: 2025-11-19 DOI: 10.1080/1061186X.2025.2587701

Dina Elsayegh, Omar Tluli, Maram Elzayyat, Abdelrahman Karen, Layan Albarghouthi, Abdulla Al-Emadi, Mubarak AlMaadid, Haya Al-Mohannadi, Laiche Djouhri

{"title":"Ivabradine, a hyperpolarization-activated channel blocker, attenuates mechanical, but not heat, hypersensitivity in hyperglycaemic and normoglycemic rat models of diabetic neuropathy.","authors":"Dina Elsayegh, Omar Tluli, Maram Elzayyat, Abdelrahman Karen, Layan Albarghouthi, Abdulla Al-Emadi, Mubarak AlMaadid, Haya Al-Mohannadi, Laiche Djouhri","doi":"10.1080/1061186X.2025.2587701","DOIUrl":"10.1080/1061186X.2025.2587701","url":null,"abstract":"Diabetic peripheral neuropathic pain (DPNP) is a debilitating complication of longstanding type 1 (T1DM) and type 2 (T2DM) diabetes mellitus. DPNP patients experience mechanical and thermal pain hypersensitivity. Despite its clinical significance and high prevalence, treatment for DPNP remains challenging due to its unclear pathogenesis. We investigated whether hyperpolarization-activated cyclic nucleotide-gated (HCN) ion channels, known to be involved in other PNP types, also contribute to DPNP. We used two DPNP rat models: (a) streptozotocin (STZ) model of T1DM induced by a single STZ injection (60 mg/kg, i.p.), and (b) high fat diet-fed STZ model (HFD/STZ) of T2DM induced by feeding the rats with HFD (60% calories as fat) for 2 weeks followed by a low-dose STZ injection (35 mg/kg, i.p.). We found that: (a) diabetic (hyperglycaemic) and non-diabetic (normoglycemic) STZ rats, as well as normoglycemic HFD/ZTZ rats, exhibit mechanical and heat hypersensitivity, evidenced by reduced paw withdrawal thresholds and latencies, respectively, and (b) ivabradine (10 mg/kg, i.p.), the clinically approved HCN blocker, was as effective as the positive control gabapentin in attenuating mechanical, but not heat, hypersensitivity, in both models. These findings reinforce that factors beyond hyperglycaemia contribute to DPNP and highlight HCN channels as potential therapeutic targets for treating DPNP.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"926-937"},"PeriodicalIF":3.9,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145495735","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0