Journal of Drug Targeting最新文献

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Chitosan nanoparticles for the treatment of ischemia-reperfusion injury: mechanisms, preclinical evidence, challenges, and future perspectives. 壳聚糖纳米颗粒治疗缺血再灌注损伤:机制、临床前证据、挑战和未来展望。
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-03 DOI: 10.1080/1061186X.2026.2723295
Yongxin Dong, Weidong Qiang
{"title":"Chitosan nanoparticles for the treatment of ischemia-reperfusion injury: mechanisms, preclinical evidence, challenges, and future perspectives.","authors":"Yongxin Dong, Weidong Qiang","doi":"10.1080/1061186X.2026.2723295","DOIUrl":"10.1080/1061186X.2026.2723295","url":null,"abstract":"<p><p>Ischaemia-reperfusion injury (IRI) is a complex pathological process involved in conditions such as organ transplantation, trauma, vascular surgery, myocardial infarction, and stroke. Although reperfusion is essential for restoring oxygen and nutrients to ischaemic tissues, it can paradoxically worsen tissue damage through oxidative stress, mitochondrial dysfunction, endothelial injury, inflammation, immune-cell infiltration, microvascular dysfunction, and regulated cell death. The multifactorial and rapidly evolving nature of IRI limits the effectiveness of traditional therapeutic approaches. Therefore, there is a strong need for strategies capable of simultaneously targeting multiple pathological pathways. Chitosan nanoparticles have emerged as promising nanocarriers for IRI therapy due to their biocompatibility, biodegradability, low toxicity, and ability to be chemically modified. They can encapsulate diverse therapeutic agents, including antioxidants, anti-inflammatory compounds, proteins, peptides, and nucleic acids, thereby improving drug stability, bioavailability, tissue retention, and enabling controlled or stimuli-responsive release. This review summarises current knowledge on IRI pathophysiology and highlights the therapeutic mechanisms of chitosan nanoparticles, particularly their effects on oxidative stress, inflammation, mitochondrial dysfunction, endothelial injury, and apoptosis. In addition, recent preclinical studies applying chitosan-based nanocarriers in cerebral, hepatic, renal, cardiac, and intestinal IRI are discussed.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-13"},"PeriodicalIF":4.7,"publicationDate":"2026-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148793993","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
Fatty acid vesicles as nanodrug delivery carriers: research progress and perspective. 脂肪酸囊泡作为纳米药物载体的研究进展与展望
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-02 DOI: 10.1080/1061186X.2026.2726885
Jiarong Hang, Lei Li, Lukuan Liu, Haiyan Ma, Ping Zhang, Ruiyang Lu, Nina Dou
{"title":"Fatty acid vesicles as nanodrug delivery carriers: research progress and perspective.","authors":"Jiarong Hang, Lei Li, Lukuan Liu, Haiyan Ma, Ping Zhang, Ruiyang Lu, Nina Dou","doi":"10.1080/1061186X.2026.2726885","DOIUrl":"10.1080/1061186X.2026.2726885","url":null,"abstract":"<p><p>Fatty acid vesicles (FAVs) are closed lipid bilayer nanostructures self-assembled from fatty acids and their ionised derivatives, featuring facile preparation, low cost and excellent biocompatibility, which endows them promising prospects in drug delivery. This study systematically compares FAVs with conventional phospholipid liposomes, highlighting the core limitations of FAVs including high pH sensitivity and poor structural stability in physiological environments. Common stabilisation strategies are summarised, mainly covering chemical modification and amphiphilic additive incorporation. Classic fabrication approaches such as thin-film hydration, alcohol-assisted vesiculation and spontaneous self-assembly from fatty-acid precursors are introduced, together with emerging industrial techniques represented by microfluidics and dynamic high-pressure microjets. The applications of FAVs in transdermal, oral and anticancer drug delivery are also reviewed. FAVs exhibit distinct advantages in improving the bioavailability of insoluble drugs, enhancing transdermal permeability and achieving targeted delivery. Nevertheless, physiological pH instability, inadequate <i>in vivo</i> pharmacokinetic and safety data, and underdeveloped industrial preparation technologies still hinder their clinical transformation. Future research should prioritise developing pH-stable FAVs and evaluating their <i>in vivo</i> performance to promote their clinical translation.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-16"},"PeriodicalIF":4.7,"publicationDate":"2026-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148840372","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
Nanocarrier based topical gel of clofazimine: advanced therapeutic strategy for the treatment of leprosy. 纳米载体外用氯法齐明凝胶:治疗麻风病的先进治疗策略。
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-01 Epub Date: 2026-02-08 DOI: 10.1080/1061186X.2026.2626359
Shailesh Chalikwar, Tanaya Dhole, Pankaj Jain, Kailas Moravkar, Pradip Nirbhavane
{"title":"Nanocarrier based topical gel of clofazimine: advanced therapeutic strategy for the treatment of leprosy.","authors":"Shailesh Chalikwar, Tanaya Dhole, Pankaj Jain, Kailas Moravkar, Pradip Nirbhavane","doi":"10.1080/1061186X.2026.2626359","DOIUrl":"10.1080/1061186X.2026.2626359","url":null,"abstract":"<p><p>This study aims to formulate Clofazimine (CLOF)-loaded nanostructured lipid carriers (NLCs) for transdermal application, thereby improving the overall efficacy of the drug. NLCs loaded with clofazimine were developed using biocompatible lipids, characterised w.r.t. particle size, PDI and % entrapment efficiency and optimised using 'Box-Behnken design'. The optimum formulation was assessed for <i>in vitro</i> drug release, dermatokinetics & <i>in vivo</i> biocompatibility study. The characterisation of NLCs formulation revealed their globular shape with a particle size of around 192 nm, zeta potential of approximately of -30 mV and % EE of around 88.45%. Drug release demonstrated biphasic drug release from NLCs and follows the Higuchi release kinetics with a non-fickian release mechanism. The <i>ex vivo</i> study confirmed a 3.5 folds increase in permeation as compared with conventional gel formulation. Thus, the NLC based formulation exhibited around 350% increase in permeation as compared to plain gel of drug. The developed formulation was found to be biocompatible and exhibited no signs of irritancy or toxicity, according to the skin irritation study. Furthermore, formulation has good physicochemical stability with a shelf life of about 27 months. In conclusion the study suggests that NLC-loaded CLOF was applied topically to treat leprosy, providing improved skin penetration and effectiveness.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1494-1510"},"PeriodicalIF":4.7,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146119051","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
Finasteride-loaded phospholipid-bile salt mixed micelles for targeted follicular delivery in androgenetic alopecia. 非那雄胺负载磷脂-胆汁盐混合胶束用于雄激素性脱发的靶向卵泡输送。
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-01 Epub Date: 2026-06-24 DOI: 10.1080/1061186X.2026.2622535
Mohammad Saleh Sadeghi, Naghmeh Jabarimani, Helia Behrouzfar, Farid Dorkoosh, Hamid Akbari Javar
{"title":"Finasteride-loaded phospholipid-bile salt mixed micelles for targeted follicular delivery in androgenetic alopecia.","authors":"Mohammad Saleh Sadeghi, Naghmeh Jabarimani, Helia Behrouzfar, Farid Dorkoosh, Hamid Akbari Javar","doi":"10.1080/1061186X.2026.2622535","DOIUrl":"10.1080/1061186X.2026.2622535","url":null,"abstract":"<p><p>Androgenetic alopecia (AGA) is driven by elevated scalp dihydrotestosterone. Although oral finasteride (FNS) is clinically effective, its long-term use is limited by sexual and psychological adverse effects. Topical delivery has the potential to reduce systemic exposure; however, conventional formulations still permit considerable transdermal absorption. To overcome this limitation, phospholipid-bile salt mixed micelles composed of egg phosphatidylcholine (EPC) and sodium cholate (SC) were developed using a remote-loading strategy to enhance follicular targeting while restricting systemic uptake. The optimised formulation, containing EPC-to-SC and lipid-to-drug molar ratios of 0.7:0.3 and 20:1, respectively, produced uniform spherical micelles (285 ± 10.9 nm; polydispersity index 0.385 ± 0.01; -36.3 ± 0.6 mV). High-performance liquid chromatography analysis indicated an encapsulation efficiency of 98.5 ± 0.5% and confirmed sustained FNS release over 48 h. Confocal microscopy of fluorescein isothiocyanate-loaded micelles demonstrated efficient follicular deposition with minimal lateral diffusion. In an AGA mouse model, the micelles markedly improved hair regrowth, increased follicle number and length, and enhanced follicular proliferation compared with a hydroalcoholic FNS solution. Notably, serum dihydrotestosterone levels remained higher in the micelle-treated group, indicating reduced systemic absorption. Collectively, these findings support the strong translational potential of EPC-SC micelles as a safer and more effective topical strategy for AGA management.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1428-1439"},"PeriodicalIF":4.7,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147326316","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
Alendronate-conjugated liposome for targeting of osteoblastic prostate cancer: evaluation of binding to bone matrix and in vivo targeting in a mouse model. 靶向成骨前列腺癌的阿仑膦酸偶联脂质体:与骨基质结合的评估和小鼠模型的体内靶向。
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-01 Epub Date: 2026-03-02 DOI: 10.1080/1061186X.2026.2636002
Kitz Paul D Marco, Jossana A Damasco, Guoyu Yu, Joy Vanessa D Perez, Elizabeth M Whitley, Francisco M Heralde, Sue-Hwa Lin, Marites P Melancon
{"title":"Alendronate-conjugated liposome for targeting of osteoblastic prostate cancer: evaluation of binding to bone matrix and <i>in vivo</i> targeting in a mouse model.","authors":"Kitz Paul D Marco, Jossana A Damasco, Guoyu Yu, Joy Vanessa D Perez, Elizabeth M Whitley, Francisco M Heralde, Sue-Hwa Lin, Marites P Melancon","doi":"10.1080/1061186X.2026.2636002","DOIUrl":"10.1080/1061186X.2026.2636002","url":null,"abstract":"<p><p>Prostate cancer bone metastases are predominantly osteoblastic, placing them in a unique position for bone-targeted drug delivery. Bone-targeted nanoparticles may be able to accumulate in aberrant bone formation inside these osteoblastic tumours, but this has not been explored. Here, we developed an alendronate-conjugated liposome (Lip-Cy5.5-Aln) encapsulating the near-infra-red dye Cy5.5 as a model payload to evaluate targeting. Binding to bone matrix was assessed <i>in vitro</i> using hydroxyapatite, MC3T3-E1-derived osteoblasts and 2H11-derived osteoblast-like cells. <i>In vivo</i> targeting of bone and bone-forming tumours was assessed in male nude mice with or without subcutaneous C4-2B (non-osteoblastic) or C4-2B-BMP4 (osteoblastic) tumours using optical imaging and non-targeted liposomes as control. Lip-Cy5.5-Aln selectively bound to bone matrix <i>in vitro</i> as opposed to control (57.4% vs. 0.6%, <i>p</i> < 0.0001). <i>In vivo</i>, Lip-Cy5.5-Aln exhibited increased musculoskeletal accumulation (51.0% vs. 39.8%, <i>p</i> < 0.0001) and reduced kidney localisation (18.4% vs. 29.9%, <i>p</i> < 0.0001). However, there was no significant difference in Cy5.5 signal between Lip-Cy5.5-Aln and control in bone-forming C4-2B-BMP4 tumours, nor was localisation greater in osteoblastic versus non-osteoblastic tumours. Overall, the alendronate-conjugated liposome showed enhanced musculoskeletal accumulation, but it does not seem to effectively target pathologic intratumour bone formation in metastatic prostate cancer.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1540-1549"},"PeriodicalIF":4.7,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147276012","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
Nanomedicine strategies for mitigating cancer therapy-related cardiovascular toxicity. 减轻癌症治疗相关心血管毒性的纳米药物策略。
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-01 Epub Date: 2026-03-17 DOI: 10.1080/1061186X.2026.2638328
QuZhe Lu, ZhaoWu Li, Zhi Hu, Chao Liu, Hui Yin
{"title":"Nanomedicine strategies for mitigating cancer therapy-related cardiovascular toxicity.","authors":"QuZhe Lu, ZhaoWu Li, Zhi Hu, Chao Liu, Hui Yin","doi":"10.1080/1061186X.2026.2638328","DOIUrl":"10.1080/1061186X.2026.2638328","url":null,"abstract":"<p><p>Cancer therapy-induced cardiotoxicity represents a serious clinical complication driven by oxidative injury, topoisomerase IIβ-mediated DNA damage, endoplasmic reticulum (ER) stress, mitochondrial dysfunction and sustained inflammatory signalling. These pathogenic processes can lead to a range of adverse outcomes, including myocarditis, vascular and valvular alterations, myocardial fibrosis, electrophysiological remodelling and related cardiac abnormalities. A growing body of experimental evidence indicates that nanocarriers can markedly reduce unintended cardiac exposure to cytotoxic agents. These systems exploit the enhanced permeability and retention (EPR) effect in the tumour microenvironment while lowering free drug concentrations in the myocardium. Progress in targeting strategies, spanning surface-functionalised ligands and antibodies to stimuli-responsive nanoparticles, further constrains off-target distribution and enables spatially controlled drug release at the tumour site. In parallel, nanoparticles co-loaded with cardioprotective agents, including antioxidants, Top2β inhibitors, small molecules and selected natural products, demonstrate additive benefits by intercepting central mediators of cardiomyocyte injury. Such dual co-delivery platforms may also augment antitumour efficacy. Nanocarriers incorporating these cardioprotective agents may similarly attenuate radiotherapy-induced cardiotoxicity. This review critically evaluates these multifaceted nanomedicine strategies and outlines a comprehensive roadmap for harnessing nanoparticle technologies to prevent and mitigate cardiotoxicity associated with cancer therapy.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1377-1393"},"PeriodicalIF":4.7,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147317207","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
Iontophoresis-enhanced transdermal delivery of curcumin micelles: mechanisms of penetration and wound healing. 离子渗透-增强姜黄素胶束的透皮递送:渗透和伤口愈合的机制。
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-01 DOI: 10.1080/1061186X.2026.2724404
Pingping Zhao, Wenhao Yuan, Yuhong Xu, Caifei Jin, Chu Chu, Yan Yang
{"title":"Iontophoresis-enhanced transdermal delivery of curcumin micelles: mechanisms of penetration and wound healing.","authors":"Pingping Zhao, Wenhao Yuan, Yuhong Xu, Caifei Jin, Chu Chu, Yan Yang","doi":"10.1080/1061186X.2026.2724404","DOIUrl":"10.1080/1061186X.2026.2724404","url":null,"abstract":"<p><p>The transdermal delivery of poorly water-soluble drugs is limited by low aqueous solubility and the stratum corneum permeability barrier. In this study, curcumin was formulated into self-assembled micelles using Tween 20 and polyethylene glycol 400, which exhibited a particle size of 12.5 nm, a zeta potential of -12.5 mV, and a 170-fold increase in solubility. The curcumin micelles (CM) were combined with constant-current iontophoresis (0.45 mA/cm<sup>2</sup>), to investigate the synergistic enhancement effects and underlying mechanisms. The results showed a 44.2-fold increase in cumulative release over 60 min, with a linear flux-current density relationship (<i>R</i><sup>2</sup> = 0.99). CM exhibited electro-responsive release with an approximate 20-min lag. Under a fixed 2 h total stimulation, pulsed current (4 pulses) nearly doubled the 8-h cumulative release compared to continuous current. Furthermore, both current density and electrode configuration were shown to influence penetration depth and width. Iontophoresis enabled CM to penetrate rat skin to a depth of 270 μm and increased intradermal retention by 258%. In a rat second-degree burn model, the combination therapy significantly accelerated wound healing <i>via</i> promoting angiogenesis, downregulating inflammatory cytokines, and enhancing collagen deposition.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-15"},"PeriodicalIF":4.7,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148793969","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 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-01 Epub 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":"<p><p>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 <i>in vivo</i> 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.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1608-1621"},"PeriodicalIF":4.7,"publicationDate":"2026-09-01","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
Formulation and optimization of leflunomide-loaded NLC-gel for improved skin permeation and anti-inflammatory efficacy. 来氟米特负载nlc凝胶提高皮肤渗透和抗炎效果的配方及优化。
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-01 Epub Date: 2026-02-06 DOI: 10.1080/1061186X.2026.2622536
Vivek Mewada, Jigar Shah, Aakash Kumar, Snehal Patel, Anroop Nair, Hiral Shah
{"title":"Formulation and optimization of leflunomide-loaded NLC-gel for improved skin permeation and anti-inflammatory efficacy.","authors":"Vivek Mewada, Jigar Shah, Aakash Kumar, Snehal Patel, Anroop Nair, Hiral Shah","doi":"10.1080/1061186X.2026.2622536","DOIUrl":"10.1080/1061186X.2026.2622536","url":null,"abstract":"<p><p>Arthritis is a chronic-inflammatory disorder that impairs joint function and necessitates efficient localised treatment. This research aimed to formulate and optimise leflunomide-loaded nanostructured lipid carriers (NLCs) for topical delivery. Dynasan 114 and corn oil were used as the solid and liquid lipids, respectively, and NLCs were formulated using high-speed homogenisation and probe sonication. Dual experimental design (1) Plackett-Burman for screening, and (2) Box-Behnken for formulation optimisation were employed. The optimised NLCs showed particle size (125.5 nm), PDI (0.188), zeta potential (-15.5 mV), and entrapment efficiency (92.20 ± 1.28%). FT-IR, DSC, P-XRD, and TEM validated the amorphous dispersion of leflunomide within the lipid matrix and the spherical morphology of the NLCs. The optimised NLCs were integrated into a Carbopol 980 NF (0.75%) gel base, demonstrating appropriate rheological properties such as extrudability (176 g), adhesiveness (-112 g), and pH (6.92). The gel formulation demonstrated prolonged drug release (96% over 24 h) and increased ex-vivo permeation with flux of 0.3632 mg/cm<sup>2</sup>/hour, hence validating enhanced diffusion through the skin barrier. The in-vivo pharmacodynamic study using a carrageenan-induced paw edoema model exhibited an 89.40% reduction in inflammation, exceeding the efficacy of the marketed leflunomide formulation. These findings suggest that the leflunomide-loaded NLC-based gel offers a promising platform for dermal drug distribution and enhanced anti-inflammatory activity.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1440-1455"},"PeriodicalIF":4.7,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146064061","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
Potential therapeutic benefits of lutein-loaded hydrogel in diabetic-induced dermal wound healing. 叶黄素负载水凝胶在糖尿病诱导的皮肤伤口愈合中的潜在治疗效益。
IF 4.7 4区 医学
Journal of Drug Targeting Pub Date : 2026-09-01 Epub Date: 2026-03-13 DOI: 10.1080/1061186X.2026.2639022
Zuha Rahman, Vidhu Aeri
{"title":"Potential therapeutic benefits of lutein-loaded hydrogel in diabetic-induced dermal wound healing.","authors":"Zuha Rahman, Vidhu Aeri","doi":"10.1080/1061186X.2026.2639022","DOIUrl":"10.1080/1061186X.2026.2639022","url":null,"abstract":"<p><p>Research on wound-healing agents is a growing area in modern biomedical sciences, and oxidative stress plays a significant role in the challenges of chronic wound healing. These challenges include dry dressings that lack functionality and cause increased pain by adhering to wounds. Hydrogels are widely utilised for wound healing because they mimic the native extracellular matrix (ECM) and help maintain a moist environment. <i>In silico</i> docking studies revealed that lutein forms strong and stable interactions with proteins involved in ECM degradation, inflammation and oxidative stress. The optimised hydrogel formulations demonstrated excellent physicochemical stability and improved topical delivery of the drug. <i>In vitro</i> and <i>ex vivo</i> studies confirmed superior skin permeation and sustained release of lutein from the fermented hydrogel compared with controls. <i>In vivo</i> experiments using F2 formulation (0.5% lutein) on diabetic rat models demonstrated rapid wound contraction, achieving 92.1% closure by day 9 and complete healing by day 11, with minimal scarring and enhanced tissue regeneration. Histopathological analysis supported these results, revealing dense granulation tissue, minimal inflammatory infiltration and notable dermal remodelling in the treatment group. These findings suggest that lutein-loaded hydrogels are promising biotherapeutic options for the effective management of diabetic wounds.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1568-1577"},"PeriodicalIF":4.7,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147306563","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
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