Journal of Drug Targeting最新文献_第4页

Recent advances in chitosan-based nanomaterials and conjugates for active and passive targeting of cancer cells. 壳聚糖基纳米材料及其主动和被动靶向癌细胞缀合物的研究进展。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-04-01 Epub Date: 2025-10-27 DOI: 10.1080/1061186X.2025.2573841

Himali Horo, Jiwanjot Sharma

{"title":"Recent advances in chitosan-based nanomaterials and conjugates for active and passive targeting of cancer cells.","authors":"Himali Horo, Jiwanjot Sharma","doi":"10.1080/1061186X.2025.2573841","DOIUrl":"10.1080/1061186X.2025.2573841","url":null,"abstract":"Chitosan-based materials have gained significant attention in drug delivery owing to their exceptional properties, including biocompatibility, biodegradability, mucoadhesiveness, and tuneable physicochemical characteristics. Their structural versatility allows formulation into various delivery tools, such as nanoparticles, microparticles, hydrogels, micelles, and conjugates. These attributes make chitosan an ideal biopolymeric candidate as a drug carrier with engineered characteristics, facilitating active and passive targeting. Chitosan nanoparticles contribute to passive targeting via enhanced permeation and retention (EPR) effect and actively participate in receptor-mediated targeting when functionalized with ligands such as small molecules, peptides, polymers, aptamers, and antibodies. This dual-targeting capability makes chitosan-based drug delivery systems highly advantageous for cancer therapy and other site-specific treatments. This review compiles recent advancements in the synthesis of various types of chitosan-based materials and their study in cancer-targeting efficacy. It explores passive targeting mechanisms through modified chitosan nanoparticles and discusses active targeting strategies achieved via conjugation with cancer cell-specific ligands. Special emphasis is placed on formulation strategies, targeting efficiency, and evaluating therapeutic outcomes through cell viability assays and cellular uptake studies.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"529-554"},"PeriodicalIF":3.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145274587","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

Design and in vivo evaluation of a multi-epitope vaccine that suppresses tumour growth in a murine colorectal cancer model. 抑制小鼠结直肠癌模型肿瘤生长的多表位疫苗的设计和体内评价

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-04-01 Epub Date: 2025-10-15 DOI: 10.1080/1061186X.2025.2573054

Alisa Khodadadi, Saeid Afshar, Rezvan Najafi, Alireza Zamani, Razieh Dalirfardouei, Meysam Soleimani

{"title":"Design and in vivo evaluation of a multi-epitope vaccine that suppresses tumour growth in a murine colorectal cancer model.","authors":"Alisa Khodadadi, Saeid Afshar, Rezvan Najafi, Alireza Zamani, Razieh Dalirfardouei, Meysam Soleimani","doi":"10.1080/1061186X.2025.2573054","DOIUrl":"10.1080/1061186X.2025.2573054","url":null,"abstract":"Harnessing the immune system through cancer vaccines offers a promising strategy to overcome tumour heterogeneity, which remains one of the most significant challenges in achieving effective treatment for colorectal cancer (CRC). In this study, we designed and validated a novel multi-epitope vaccine against CRC using integrated computational and experimental approaches. The final construct was developed through in silico prediction and optimisation, followed by recombinant expression and in vivo testing in a CRC mouse model. Mice receiving the multi-dose vaccine exhibited a mean tumour volume approximately 80% lower than that of the untreated cancer group. Additionally, IL-4 levels were significantly elevated (p < 0.0001), consistent with activation of humoral immune responses. Histopathological assessment showed largely preserved tissue architecture in the spleen, kidney, and liver. The multi-dose vaccine group achieved 100% survival, compared with 60% survival in the untreated cancer group. These results suggest the vaccine can suppress tumour progression, enhance immune responses, and provide systemic protection, supporting further preclinical development.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"680-695"},"PeriodicalIF":3.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145251192","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

Formulation and optimisation of nanoemulsions for enhancing topical delivery of methotrexate in CFA induced arthritis rat model. 增强甲氨蝶呤在CFA性关节炎大鼠模型中的局部递送的NEs的配方和优化。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-04-01 Epub Date: 2025-09-29 DOI: 10.1080/1061186X.2025.2565409

Amruta Parmar, Brijesh Sukumaran

{"title":"Formulation and optimisation of nanoemulsions for enhancing topical delivery of methotrexate in CFA induced arthritis rat model.","authors":"Amruta Parmar, Brijesh Sukumaran","doi":"10.1080/1061186X.2025.2565409","DOIUrl":"10.1080/1061186X.2025.2565409","url":null,"abstract":"Methotrexate (MTX) is widely used in treating cancers and inflammatory conditions like psoriasis and rheumatoid arthritis (RA), however is associated with side effects. Nanoemulsions (NEs) offer enhanced stability, protection and improved permeation via various delivery routes. MTX-loaded oil-in-water NEs (O/W NEs) were formulated to improve entrapment efficiency, permeation ability and efficacy in CFA-induced arthritis model. The area of NEs was identified by pseudoternary phase diagrams, optimisation of MTX-NEs was performed using I-optimal mixture design, and characterised for %entrapment efficiency, droplet size, polydispersity index, zeta potential, morphology and %transmittance. The MTX-NE gel was evaluated for rheology, in vitro drug release, ex vivo permeation and efficacy in a CFA-induced arthritic rats. The MTX-NEs were prepared using Smix ratio of 3:1 with 0.2 N sodium hydroxide as aqueous phase. It showed >90% entrapment efficiency, size of 161.4 ± 13.5 nm, and 94 ± 1.8% of %transmittance. MTX-NE gel showed sustained release of 86 ± 1.8% MTX, and cumulative permeation of 77.6 ± 1.4% with a flux of 0.184 µg/cm2·h. Efficacy studies in a CFA-induced rat model resulted in significant reduction of paw oedema, radiographic, histopathological and inflammatory biomarkers. The optimised MTX-NE gel showed enhanced delivery, sustained release and significant anti-arthritic effects, supporting its potential as an effective for RA therapy.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"577-593"},"PeriodicalIF":3.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145131185","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

Fisetin topical delivery via ascorbyl palmitate/hyaluronan-enhanced limosomes: a novel paradigm for preventing UVB-induced skin photoaging. 通过抗坏血酸棕榈酸/透明质酸增强的脂质体局部递送非瑟汀：预防uvb诱导的皮肤光老化的新范例。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-04-01 Epub Date: 2025-10-22 DOI: 10.1080/1061186X.2025.2573053

Asmaa H Elwan, Soha M El-Masry, Doaa A Habib, Marwa M Essawy, Mariam Zewail

{"title":"Fisetin topical delivery via ascorbyl palmitate/hyaluronan-enhanced limosomes: a novel paradigm for preventing UVB-induced skin photoaging.","authors":"Asmaa H Elwan, Soha M El-Masry, Doaa A Habib, Marwa M Essawy, Mariam Zewail","doi":"10.1080/1061186X.2025.2573053","DOIUrl":"10.1080/1061186X.2025.2573053","url":null,"abstract":"This study investigates the topical delivery of Fisetin (FIS) to counteract UVB-induced skin photoaging. Due to FIS's poor solubility and high lipophilicity, it was encapsulated in D-limonene-modified phospholipid carriers, limosomes (LIMOs), co-formulated with Ascorbyl Palmitate (AP) and Hyaluronan (HYA) to improve FIS's solubility, skin penetration, and photoprotective efficacy. FIS-AP-HYA-LIMOs exhibited small size (81.50 ± 0.98 nm), high entrapment (98.93 ± 0.13%), and sustained release over 24 h. FT-IR and DSC confirmed the successful formation of FIS-AP-HYA-LIMOs. The ex vivo permeation study showed high flux (10.54 ± 0.40 µg.cm-2.h-1), reflecting evident skin penetration. Confocal microscopy proved the ability of FIS-AP-HYA-LIMOs to deposit FIS to a skin depth of 128 µm with a strong FIS fluorescence in skin layers. FIS-AP-HYA-LIMOs showed potent in vitro antioxidant activity, high biocompatibility, and remained stable for 6 months. In vivo studies revealed the downregulation of MMP9, TNFα, and NF-κB, accompanied by increased SOD and CAT levels, indicating superior anti-ageing, anti-inflammatory, and antioxidant effects compared to FIS suspension. FIS-AP-HYA-LIMOs decreased JNK expression, preserved the integrity of skin layers, and reduced collagen degradation. This is the first report on FIS-loaded limosomes, modified with AP and HYA to synergistically prevent UVB-induced photoaging.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"659-679"},"PeriodicalIF":3.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145274549","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

DNAJA1 as a modulator of CD8⁺ T-cell function and prognosis in lung cancer: implications for immune regulation and therapeutic targeting. DNAJA1作为CD8+ t细胞功能和肺癌预后的调节剂：免疫调节和治疗靶向的意义

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-04-01 Epub Date: 2025-10-20 DOI: 10.1080/1061186X.2025.2571546

Shengkai Yang, Lian Liu, Yubiao Guo, Luqi Dai

{"title":"DNAJA1 as a modulator of CD8+ T-cell function and prognosis in lung cancer: implications for immune regulation and therapeutic targeting.","authors":"Shengkai Yang, Lian Liu, Yubiao Guo, Luqi Dai","doi":"10.1080/1061186X.2025.2571546","DOIUrl":"10.1080/1061186X.2025.2571546","url":null,"abstract":"In lung adenocarcinoma (LUAD), dysfunctional CD8+ T-cells and an immunosuppressive tumour microenvironment (TME) are major barriers to effective immunotherapy, yet the molecular regulators coordinating T cell exhaustion and macrophage polarisation remain undefined. To address this, we integrated single-cell RNA sequencing, TCGA transcriptome and methylation data, co-culture assays, chromatin profiling, functional assays, and xenograft models to investigate the role of DNAJA1 in immune regulation and tumour progression. Our results demonstrated that DNAJA1 was upregulated in exhausted CD8+ T-cells in lung cancer tissues and correlated positively with exhaustion markers including PD-1, TIM-3, and LAG-3. Notably, exhausted CD8+ T-cells exhibited DNAJA1 promoter hypomethylation and enrichment of activating histone modifications H3K4me3 and H3K27ac, while inhibiting the activation of H3K4me3 and H3K27ac reduced DNAJA1 expression. Additionally, DNAJA1 overexpression upregulated M2-associated genes (CD206 and IL-10), while its knockdown enhanced the expression of M1-associated genes (CD86 and IL-12). Furthermore, DNAJA1 promoted tumour cell proliferation, and its expression level showed a moderate positive correlation with PD-L1. Collectively, these findings establish DNAJA1 as an epigenetically activated regulator that drives CD8+ T-cell exhaustion and protumor macrophage polarisation, highlighting its dual role as a functional immunomodulator and potential biomarker for stratifying LUAD patients with immune-dysregulated TME.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"594-609"},"PeriodicalIF":3.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145251180","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 nanodrug delivery strategies for precision chemotherapy in prostate cancer. 前列腺癌精准化疗的靶向纳米药物递送策略。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-04-01 Epub Date: 2025-10-27 DOI: 10.1080/1061186X.2025.2576111

Tianfeng Bi, Xiaoyu Wang, Lili Chen, Luchen Zhang, Chunzhao Liu, Chunlei Liu

{"title":"Targeted nanodrug delivery strategies for precision chemotherapy in prostate cancer.","authors":"Tianfeng Bi, Xiaoyu Wang, Lili Chen, Luchen Zhang, Chunzhao Liu, Chunlei Liu","doi":"10.1080/1061186X.2025.2576111","DOIUrl":"10.1080/1061186X.2025.2576111","url":null,"abstract":"Prostate cancer is one of the most common malignancies globally, with chemotherapy remaining a cornerstone treatment for advanced and metastatic cases. However, traditional chemotherapy is limited by poor targeting, low bioavailability, and systemic toxicity, necessitating the development of precise chemotherapy strategies. Nanotechnology has emerged as a promising platform to address these limitations by enabling targeted drug delivery. This review systematically synthesises advancements in nanotechnology-based drug delivery systems and their targeting strategies, emphasising their application in prostate cancer therapy. Active targeting approaches leverage cell membrane receptors, such as prostate-specific membrane antigen (PSMA), folate receptor, transferrin receptor, and CD44, as biomarkers. Corresponding ligands, including PSMA ligands, folate derivatives, transferrin, hyaluronic acid, chondroitin sulphate, and DUP-1, are used to modify nanocarriers, conferring precise targeting capabilities to loaded chemotherapeutics. Additionally, bioinspired strategies employing cell membrane encapsulation and magnetic field-guided delivery are discussed. Meanwhile, the review comprehensively summarises the research advancements of nanodelivery systems in combination therapy involving chemotherapy and radiotherapy, photodynamic therapy, immunotherapy, and other modalities. Through a categorised analysis of the developments and challenges of these nanotechnologies, this review intends to furnish references and new orientations for the research and application of precise chemotherapy in prostate cancer.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"555-576"},"PeriodicalIF":3.9,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145301330","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

Platelet-rich plasma ameliorates knee osteoarthritis in rats by modulating the abundance of gut Lactobacillus murinus. 富血小板血浆通过调节肠道乳酸杆菌的丰度改善大鼠膝骨关节炎。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-03-27 DOI: 10.1080/1061186X.2026.2648088

Xueyuan Sun, Qishan Li, Mengjie Wang, Yaochi Nie, Lin Na, Dongmei Yan, Hui Wang

引用次数: 0

Erythrocyte membrane-camouflaged doxorubicin nanoparticles for enhancing therapeutic efficacy in primary liver cancer. 红细胞膜伪装的阿霉素纳米颗粒增强原发性肝癌的治疗效果。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-03-26 DOI: 10.1080/1061186X.2026.2647068

Ting-Ting Hu, Ying Ding, Yi-Ren Yao, Xin Zhang, Xi-Wen Zhang, Yang Gu

{"title":"Erythrocyte membrane-camouflaged doxorubicin nanoparticles for enhancing therapeutic efficacy in primary liver cancer.","authors":"Ting-Ting Hu, Ying Ding, Yi-Ren Yao, Xin Zhang, Xi-Wen Zhang, Yang Gu","doi":"10.1080/1061186X.2026.2647068","DOIUrl":"10.1080/1061186X.2026.2647068","url":null,"abstract":"Doxorubicin (DOX), an anthracycline antibiotic, stands as one of the most potent and clinically ubiquitous chemotherapeutic agents for cancer treatment. Despite advances in clinical supportive care, strategies to prevent DOX-induced toxicity remain inadequate - with cardiotoxicity being a particularly devastating complication that can progress to heart failure. To address this unmet need, we engineered a novel core-shell biomimetic nanoparticle (NP) camouflaged with erythrocyte membranes, tailored for the targeted delivery of DOX to treat liver cancer while mitigating DOX-induced cardiotoxicity. This erythrocyte membrane-camouflaged biomimetic NP system exhibits an average diameter of 262.4 nm - an optimal size for prolonged systemic circulation - and possesses exceptional biocompatibility, coupled with enhanced responsiveness to the acidic tumour microenvironment. These synergistic features collectively augment the anti-tumour efficacy of DOX against hepatocellular carcinoma (HCC). Our findings highlight that the erythrocyte membrane-camouflaged NP serves as a promising biomimetic nanocarrier: it enables efficient delivery of chemotherapeutics to tumour sites while attenuating their off-target side effects (e.g. DOX-induced cardiotoxicity). This work thus provides a valuable strategy for improving the therapeutic index of anthracycline-based cancer treatments.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-12"},"PeriodicalIF":3.9,"publicationDate":"2026-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147468082","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

Beyond drug delivery: nanoparticles as active modulators of immunometabolism for treating inflammatory diseases. 超越药物递送：纳米颗粒作为治疗炎症性疾病的免疫代谢活性调节剂。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-03-25 DOI: 10.1080/1061186X.2026.2647069

Hailing Wang, Ahequeli Gemingnuer, Yinan Wang, Yan Liu, Xin Meng

{"title":"Beyond drug delivery: nanoparticles as active modulators of immunometabolism for treating inflammatory diseases.","authors":"Hailing Wang, Ahequeli Gemingnuer, Yinan Wang, Yan Liu, Xin Meng","doi":"10.1080/1061186X.2026.2647069","DOIUrl":"10.1080/1061186X.2026.2647069","url":null,"abstract":"Immunometabolism is central to chronic inflammatory diseases, with metabolic reprogramming including dysregulated glycolysis, mitochondrial dysfunction and excessive reactive oxygen species (ROS) production driving pathology in conditions like inflammatory bowel disease (IBD), rheumatoid arthritis and psoriasis. Although metabolic regulators hold therapeutic promise, their efficacy is limited by poor site-specific delivery and bioavailability. Nanotechnology-based platforms (e.g. liposomes, polymeric nanoparticles (NPs), nanoemulsions and metal NPs) address these barriers by enhancing bioavailability and forming a protein corona that modulates NP uptake by macrophages and T cells, directly influencing metabolic fate. Advanced organelle-targeting strategies such as mitochondria-directed liposomes and lysosome-responsive polymers enable precise metabolic rescue by restoring mitochondrial respiration or modulating nutrient-sensing pathways. By targeting key metabolic nodes including HIF-1α, mTOR and AMPK, nanocarriers actively shift immune cells from pro-inflammatory glycolysis towards anti-inflammatory oxidative phosphorylation, minimising toxicity and restoring immune homeostasis. Thus, nanocarriers function not as passive delivery vehicles but as sophisticated immunometabolism modulators. Despite progress, a comprehensive review bridging nanomaterial design and metabolic intervention remains lacking. This review addresses that gap by highlighting nanoscale phenomena such as stimulus-responsive release, membrane perturbation and organelle-specific targeting.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-17"},"PeriodicalIF":3.9,"publicationDate":"2026-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147468164","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

Enhancing the efficacy and bioavailability of isoxsuprine for the treatment of cardiotoxicity: in vitro and in vivo studies. 提高异苏嘌呤治疗心脏毒性的疗效和生物利用度：体外和体内研究。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2026-03-24 DOI: 10.1080/1061186X.2026.2646189

Asmaa M El-Kalaawy, Marwa H Elkarmalawy, Amr Gamal Fouad, Amany Belal, Alaa Ismail, Rasha Hallal Alziyadi, Suhaib Mohammadmustafa Bukhari, Yasmine K Rabea, Fatma I Abo El-Ela, Asmaa Ramadan Abdel-Sattar, Alshimaa Mohamed Abdelmohymen

{"title":"Enhancing the efficacy and bioavailability of isoxsuprine for the treatment of cardiotoxicity: in vitro and in vivo studies.","authors":"Asmaa M El-Kalaawy, Marwa H Elkarmalawy, Amr Gamal Fouad, Amany Belal, Alaa Ismail, Rasha Hallal Alziyadi, Suhaib Mohammadmustafa Bukhari, Yasmine K Rabea, Fatma I Abo El-Ela, Asmaa Ramadan Abdel-Sattar, Alshimaa Mohamed Abdelmohymen","doi":"10.1080/1061186X.2026.2646189","DOIUrl":"10.1080/1061186X.2026.2646189","url":null,"abstract":"Isoxsuprine (ISX) is a blood flow-improving beta-adrenergic agonist that provides cardiotoxicity protection. However, the limited effectiveness of ISX can be attributed to a short half-life and low bioavailability. The focus of this study was to create ISX-loaded transbilosomes (ILT), improving sustainability, permeability, bioavailability, safety, and ISX therapeutic efficacy as a safe option for managing cardiotoxicity. Different ILT formulations were developed using design expert software. Additionally, a rat model of cardiotoxicity was used to conduct an in vivo study to assess its bioavailability, safety, and efficacy. An optimised ILT formulation was identified, consisting of 275 mg phospholipid, 20 mg cholesterol, 25 mg Span 60, and 20 mg sodium deoxycholate. This formulation achieved a release rate of 29.22%, a permeation rate of 95.66%, and resulted in a 3.55-fold increase in bioavailability. Compared to the disease group, the optimised ILT significantly reduced mortality and levels of troponin-1, LDH, CK-MB, and MDA by 23.89%, 99.03%, 94.77%, 96.77%, and 96.57%, respectively. Furthermore, it enhanced the GSH, SOD, and CAT by 3.69-fold, 3.54-fold, and 3.57-fold, respectively. These findings suggest that nasal ILT could be an innovative avenue to consider for treating cardiotoxicity.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-14"},"PeriodicalIF":3.9,"publicationDate":"2026-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147468087","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