Journal of Drug Delivery Science and Technology最新文献_第4页

Tunable nanospanlastics for 18α-Glycyrrhetinic acid brain targeted delivery to manage cognitive deficits and misfolded protein aggregates in Alzheimer's disease: In vitro optimization and in vivo pharmacodynamics assessment 可调纳米塑料用于18α-甘草次酸脑靶向递送，以管理阿尔茨海默病的认知缺陷和错误折叠蛋白聚集：体外优化和体内药效学评估

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-27 DOI: 10.1016/j.jddst.2025.107959

Hussein M. Eid , Mohammed H. El komy , Mohamed O. Mahmoud , Heba M. Aboud , Fares E.M. Ali , Ahmed M. Abdelhaleem Ali , Amany A. Azouz

18α-Glycyrrhetinic acid (18αGA), a bioactive triterpenoid, has demonstrated neuroprotective potential against Alzheimer's disease (AD). However, its clinical application is hindered by poor solubility, low absorption, and limited ability to cross biological barriers. This study aims to develop and optimize nanospanlastics (NSLs) as a novel nanovesicular system to enhance 18αGA delivery and therapeutic efficacy for AD management. 18αGA-loaded nanospanlastics (18αGA-NSLs) were developed via a thin-film hydration technique and refined through a D-optimal design. Key formulation parameters were evaluated to ascertain their impact on drug release, entrapment efficacy, and vesicle size. The optimized formulation underwent in vitro characterization, including short-term stability, in vitro drug release studies, and morphological evaluation. The pharmacodynamic efficacy was tested in an aluminum chloride-induced AD rat model. Behavioral tests (novel object recognition, Y-maze) and molecular analyses (real-time PCR, Western blotting) were conducted to evaluate key AD biomarkers. The optimized 18αGA-NSLs demonstrated a nanoscale vesicle size, high drug encapsulation efficiency, and prolonged release profile. In vivo, 18αGA-NSLs significantly improved cognitive function and attenuated AD-related neurodegeneration by reducing amyloid-beta accumulation, tau phosphorylation, and neuroinflammation markers. 18αGA-NSLs demonstrated superior neuroprotective effects compared to 18αGA suspension, suggesting their potential as a promising nanoplatform for AD treatment. This study highlights nanospanlastics as an effective strategy to enhance 18αGA delivery and optimize its therapeutic impact against neurodegeneration.

18α-甘草酸（18αGA）是一种生物活性三萜，已被证明具有抗阿尔茨海默病（AD）的神经保护潜力。然而，其溶解度差、吸收率低、跨越生物屏障的能力有限，阻碍了其临床应用。本研究旨在开发和优化纳米塑料（NSLs）作为一种新型纳米囊泡系统，以增强18αGA的递送和治疗AD的疗效。采用薄膜水化技术制备了负载18αGA-NSLs纳米塑料（18αGA-NSLs），并通过d优化设计对其进行了细化。对关键配方参数进行评价，以确定其对药物释放、包封效果和囊泡大小的影响。优化后的制剂进行了体外表征，包括短期稳定性、体外释药研究和形态学评价。采用氯化铝诱导的AD大鼠模型对其药效进行了检测。行为测试（新物体识别，y迷宫）和分子分析（实时PCR， Western blotting）评估AD的关键生物标志物。优化后的18α ga - nsl具有纳米级囊泡大小、高包封效率和缓释效果。在体内，18α ga - nsl通过减少淀粉样蛋白积累、tau磷酸化和神经炎症标志物，显著改善认知功能，减轻ad相关神经变性。与18αGA悬浮液相比，18αGA- nsl具有更好的神经保护作用，这表明它们有潜力成为治疗AD的纳米平台。本研究强调了纳米塑料作为一种有效的策略来增强18αGA的递送并优化其对神经退行性疾病的治疗效果。

{"title":"Tunable nanospanlastics for 18α-Glycyrrhetinic acid brain targeted delivery to manage cognitive deficits and misfolded protein aggregates in Alzheimer's disease: In vitro optimization and in vivo pharmacodynamics assessment","authors":"Hussein M. Eid , Mohammed H. El komy , Mohamed O. Mahmoud , Heba M. Aboud , Fares E.M. Ali , Ahmed M. Abdelhaleem Ali , Amany A. Azouz","doi":"10.1016/j.jddst.2025.107959","DOIUrl":"10.1016/j.jddst.2025.107959","url":null,"abstract":"<div><div>18α-Glycyrrhetinic acid (18αGA), a bioactive triterpenoid, has demonstrated neuroprotective potential against Alzheimer's disease (AD). However, its clinical application is hindered by poor solubility, low absorption, and limited ability to cross biological barriers. This study aims to develop and optimize nanospanlastics (NSLs) as a novel nanovesicular system to enhance 18αGA delivery and therapeutic efficacy for AD management. 18αGA-loaded nanospanlastics (18αGA-NSLs) were developed via a thin-film hydration technique and refined through a D-optimal design. Key formulation parameters were evaluated to ascertain their impact on drug release, entrapment efficacy, and vesicle size. The optimized formulation underwent <em>in vitro</em> characterization, including short-term stability, <em>in vitro</em> drug release studies, and morphological evaluation. The pharmacodynamic efficacy was tested in an aluminum chloride-induced AD rat model. Behavioral tests (novel object recognition, Y-maze) and molecular analyses (real-time PCR, Western blotting) were conducted to evaluate key AD biomarkers. The optimized 18αGA-NSLs demonstrated a nanoscale vesicle size, high drug encapsulation efficiency, and prolonged release profile. <em>In vivo</em>, 18αGA-NSLs significantly improved cognitive function and attenuated AD-related neurodegeneration by reducing amyloid-beta accumulation, tau phosphorylation, and neuroinflammation markers. 18αGA-NSLs demonstrated superior neuroprotective effects compared to 18αGA suspension, suggesting their potential as a promising nanoplatform for AD treatment. This study highlights nanospanlastics as an effective strategy to enhance 18αGA delivery and optimize its therapeutic impact against neurodegeneration.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107959"},"PeriodicalIF":4.9,"publicationDate":"2025-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145881101","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Smart nanocarriers for biosimilars: A new frontier in targeted drug delivery 生物仿制药的智能纳米载体：靶向药物递送的新前沿

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-27 DOI: 10.1016/j.jddst.2025.107955

Arbab Hassan, Muhammad Danish Zameer, Mandhal Khan, Taimoor Hassan, Muhammad Umair, Muhammad Nazaf Iqbal, Mohammad Javad Ahi, Parsa Gul, Naveed Ahmed

Biosimilars are a significant intervention in facilitating patients’ access to critical treatments, as well as reducing expenditures in healthcare systems. However, biosimilars pose various challenges, such as the complexity of regulations, barriers to market acceptance, and issues with agnogenic immunogenicity and stability. The advancement of nanotechnology in biosimilars has revolutionized the horizon. These nanoscale delivery systems, including dendrimers, liposomes, micelles, polymeric nanoparticles, and quantum dots, are intended to enhance drug availability by promoting solubility, prolonging circulation in bodily fluids, and releasing active pharmaceutical ingredients in a controlled and targeted manner at specific physiological sites. Incorporating smart nanocarriers with biosimilar medications enhances biodistribution and targeting, while reducing systemic side effects and improving therapeutic efficacy. The review outlines various nanocarrier types, their valued characteristics, and their applications in various therapeutic domains, including autoimmune diseases and cancers. The challenges of conducting long-term, thorough safety and immunogenicity studies, navigating complex bureaucracy, and producing reproducible units on a large scale at a reasonable cost are also detailed. This review bridges the gap in the literature about the invention and utility of new smart nanocarrier technologies for smooth cooperation of numerous disciplines in research aimed at developing biosimilars, sophisticated AI algorithms, custom medicine, innovative materials, and intelligent targeting strategies. A strong focus is directed towards the role of nano platform-based strategies in biosimilars, which can significantly enhance access to advanced, safe, and efficient biopharmaceutical treatments worldwide.

生物仿制药是促进患者获得关键治疗以及减少医疗保健系统支出的重要干预措施。然而，生物仿制药带来了各种挑战，例如法规的复杂性，市场接受的障碍，以及不可知性免疫原性和稳定性问题。纳米技术在生物仿制药领域的进步已经彻底改变了人们的视野。这些纳米级递送系统，包括树状大分子、脂质体、胶束、聚合纳米粒子和量子点，旨在通过促进溶解度、延长体液循环和在特定生理部位以受控和靶向的方式释放活性药物成分来提高药物的可用性。将智能纳米载体与生物仿制药结合，可以增强生物分布和靶向性，同时减少全身副作用，提高治疗效果。本文概述了各种纳米载体类型，它们的价值特征，以及它们在各种治疗领域的应用，包括自身免疫性疾病和癌症。还详细介绍了进行长期、彻底的安全性和免疫原性研究、应对复杂的官僚机构以及以合理的成本大规模生产可复制单位的挑战。这篇综述填补了关于新型智能纳米载体技术的发明和应用的文献空白，旨在开发生物仿制药、复杂的人工智能算法、定制医学、创新材料和智能靶向策略等众多学科的研究合作。重点关注基于纳米平台的生物仿制药策略的作用，这可以显著提高全球先进、安全和高效的生物制药治疗的可及性。

{"title":"Smart nanocarriers for biosimilars: A new frontier in targeted drug delivery","authors":"Arbab Hassan, Muhammad Danish Zameer, Mandhal Khan, Taimoor Hassan, Muhammad Umair, Muhammad Nazaf Iqbal, Mohammad Javad Ahi, Parsa Gul, Naveed Ahmed","doi":"10.1016/j.jddst.2025.107955","DOIUrl":"10.1016/j.jddst.2025.107955","url":null,"abstract":"<div><div>Biosimilars are a significant intervention in facilitating patients’ access to critical treatments, as well as reducing expenditures in healthcare systems. However, biosimilars pose various challenges, such as the complexity of regulations, barriers to market acceptance, and issues with agnogenic immunogenicity and stability. The advancement of nanotechnology in biosimilars has revolutionized the horizon. These nanoscale delivery systems, including dendrimers, liposomes, micelles, polymeric nanoparticles, and quantum dots, are intended to enhance drug availability by promoting solubility, prolonging circulation in bodily fluids, and releasing active pharmaceutical ingredients in a controlled and targeted manner at specific physiological sites. Incorporating smart nanocarriers with biosimilar medications enhances biodistribution and targeting, while reducing systemic side effects and improving therapeutic efficacy. The review outlines various nanocarrier types, their valued characteristics, and their applications in various therapeutic domains, including autoimmune diseases and cancers. The challenges of conducting long-term, thorough safety and immunogenicity studies, navigating complex bureaucracy, and producing reproducible units on a large scale at a reasonable cost are also detailed. This review bridges the gap in the literature about the invention and utility of new smart nanocarrier technologies for smooth cooperation of numerous disciplines in research aimed at developing biosimilars, sophisticated AI algorithms, custom medicine, innovative materials, and intelligent targeting strategies. A strong focus is directed towards the role of nano platform-based strategies in biosimilars, which can significantly enhance access to advanced, safe, and efficient biopharmaceutical treatments worldwide.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107955"},"PeriodicalIF":4.9,"publicationDate":"2025-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145881036","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Nebulized liposomal co-delivery of nintedanib and tetrandrine for enhanced treatment of pulmonary fibrosis 雾化脂质体联合给药尼达尼布和粉防己碱增强肺纤维化治疗

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-26 DOI: 10.1016/j.jddst.2025.107956

Guoxing Deng , Zihao Xiong , Desheng Liang , Yishan Yan , Chuanzhou Fang , Siqi Zhu , Haijun Zhong , Feng Guo

Idiopathic pulmonary fibrosis (IPF) is a severe, chronic, progressive interstitial lung disease with few effective treatments. Although nintedanib is a first-line antifibrotic therapy for IPF, its efficacy is limited by poor oral bioavailability and serious gastrointestinal effects. This study developed an inhaled liposomal co-delivery system (N/T Lip) combining nintedanib-loaded liposomes (NDB Lip) and tetrandrine-loaded liposomes (TET Lip) to enhance anti-inflammatory and anti-fibrotic effects against pulmonary fibrosis. To maximize encapsulation efficiency, NDB Lip was prepared via ammonium sulfate-gradient remote loading, achieving above 96.09 ± 3.37 % encapsulation efficiency, while TET Lip, fabricated using a pH-gradient method, showed 78.76 ± 1.26 % efficiency. The optimized NDB Lip and TET Lip, demonstrating high encapsulation efficiency, were mixed at a 1:1 ratio to obtain N/T Lip. The N/T Lip exhibited favorable aerodynamic properties for nebulization, with a fine particle fraction >47 % and mass median aerodynamic diameter of ∼5.0 μm, ensuring efficient lung deposition. In vitro, N/T Lip significantly suppressed TGF-β1-induced myofibroblast activation, reducing α-SMA and Col-I expression and inhibiting migration. In vivo, in a bleomycin-induced pulmonary fibrosis model, N/T Lip effectively attenuated fibrosis progression by decreasing collagen deposition and downregulating fibrotic biomarkers, demonstrating superior efficacy compared to free drugs. These findings highlight the enhanced anti-fibrotic effects of N/T Lip, supporting its potential as a novel inhaled co-delivery strategy for clinical fibrosis treatment.

特发性肺纤维化（IPF）是一种严重的、慢性的、进行性间质性肺疾病，很少有有效的治疗方法。虽然尼达尼布是治疗IPF的一线抗纤维化药物，但其口服生物利用度差和严重的胃肠道效应限制了其疗效。本研究开发了一种吸入式脂质体共递送系统（N/T Lip），该系统结合了负载尼达尼脂质体（NDB Lip）和负载粉防己碱脂质体（TET Lip），以增强抗炎和抗纤维化的肺纤维化作用。为了提高包封效率，采用硫酸铵梯度远程负载法制备NDB Lip，包封效率达到96.09±3.37%以上，而采用ph梯度法制备TET Lip的包封效率为78.76±1.26%。优化后的NDB Lip和TET Lip包封效率高，以1:1的比例混合得到N/T Lip。N/T Lip具有良好的雾化气动性能，细颗粒分数为47%，质量中值气动直径为~ 5.0 μm，确保了有效的肺沉积。在体外，N/T Lip显著抑制TGF-β1诱导的肌成纤维细胞活化，降低α-SMA和col - 1表达，抑制迁移。在体内，在博莱霉素诱导的肺纤维化模型中，N/T Lip通过减少胶原沉积和下调纤维化生物标志物有效地减缓了纤维化进展，与游离药物相比，显示出优越的疗效。这些发现强调了N/T Lip增强的抗纤维化作用，支持其作为临床纤维化治疗的新型吸入共给药策略的潜力。

{"title":"Nebulized liposomal co-delivery of nintedanib and tetrandrine for enhanced treatment of pulmonary fibrosis","authors":"Guoxing Deng , Zihao Xiong , Desheng Liang , Yishan Yan , Chuanzhou Fang , Siqi Zhu , Haijun Zhong , Feng Guo","doi":"10.1016/j.jddst.2025.107956","DOIUrl":"10.1016/j.jddst.2025.107956","url":null,"abstract":"<div><div>Idiopathic pulmonary fibrosis (IPF) is a severe, chronic, progressive interstitial lung disease with few effective treatments. Although nintedanib is a first-line antifibrotic therapy for IPF, its efficacy is limited by poor oral bioavailability and serious gastrointestinal effects. This study developed an inhaled liposomal co-delivery system (N/T Lip) combining nintedanib-loaded liposomes (NDB Lip) and tetrandrine-loaded liposomes (TET Lip) to enhance anti-inflammatory and anti-fibrotic effects against pulmonary fibrosis. To maximize encapsulation efficiency, NDB Lip was prepared via ammonium sulfate-gradient remote loading, achieving above 96.09 ± 3.37 % encapsulation efficiency, while TET Lip, fabricated using a pH-gradient method, showed 78.76 ± 1.26 % efficiency. The optimized NDB Lip and TET Lip, demonstrating high encapsulation efficiency, were mixed at a 1:1 ratio to obtain N/T Lip. The N/T Lip exhibited favorable aerodynamic properties for nebulization, with a fine particle fraction >47 % and mass median aerodynamic diameter of ∼5.0 μm, ensuring efficient lung deposition. <em>In vitro</em>, N/T Lip significantly suppressed TGF-β1-induced myofibroblast activation, reducing α-SMA and Col-I expression and inhibiting migration. <em>In vivo</em>, in a bleomycin-induced pulmonary fibrosis model, N/T Lip effectively attenuated fibrosis progression by decreasing collagen deposition and downregulating fibrotic biomarkers, demonstrating superior efficacy compared to free drugs. These findings highlight the enhanced anti-fibrotic effects of N/T Lip, supporting its potential as a novel inhaled co-delivery strategy for clinical fibrosis treatment.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107956"},"PeriodicalIF":4.9,"publicationDate":"2025-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145880991","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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 lincomycin delivery through innovative nanocarriers: A review 通过创新的纳米载体增强林可霉素的递送：综述

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-24 DOI: 10.1016/j.jddst.2025.107948

Mehrab Pourmadadi , Mahsa Molaei Nasr , Fatemeh Yazdian , Abbas Rahdar , Luiz Fernando Romanholo Ferreira

Antibiotic resistance has been brought on by misuse of antibiotics, even though lincomycin (LIN), a lincosamide antibiotic, is effective in treating Gram-positive bacterial infections. The advent of this basic problem has limited the efficacy of typical uses of this class of antibiotics, making their application in healthcare more difficult. To tackle this issue, the design of innovative drug delivery systems based on nanomaterials, including polymeric, lipid-based, and inorganic nanoparticles such as chitosan, hydrogels, liposomes, Ag-nanoparticles (Ag-NPs), Au-NPs, titanium oxide nanoparticles (TiO₂-NPs), and others, has been proposed. Under some conditions, correct release of drugs at infection sites is possible via systems of drug delivery that are sensitive to environmental stimuli like pH variation. Recent investigation research suggests that co-formulation of LIN with other therapeutics or co-delivery of LIN can potentially defeat drug resistance and adverse effects with improved therapeutic efficacy in inflammatory and cancer diseases. While these research developments challenge existing such as those related to industrial manufacturing of these systems, in vivo reliability, and safety evaluation. This review emphasizes the importance of continued research in this field to offer more potent treatments by focusing on methods for managing drug resistance and improving the use of the antibiotic LIN.

抗生素耐药性是由于滥用抗生素引起的，尽管林可霉素是一种林可沙胺类抗生素，可有效治疗革兰氏阳性细菌感染。这一基本问题的出现限制了这类抗生素的典型使用效果，使其在医疗保健中的应用更加困难。为了解决这一问题，已经提出了基于纳米材料的创新药物递送系统的设计，包括聚合物、脂基和无机纳米颗粒，如壳聚糖、水凝胶、脂质体、银纳米颗粒（Ag-NPs）、金纳米颗粒、氧化钛纳米颗粒（TiO2-NPs）等。在某些条件下，通过对环境刺激（如pH变化）敏感的药物输送系统，在感染部位正确释放药物是可能的。最近的调查研究表明，LIN与其他治疗药物合用或共给药可以潜在地克服耐药和不良反应，提高炎症和癌症疾病的治疗效果。虽然这些研究进展挑战了现有的诸如这些系统的工业制造，体内可靠性和安全性评估相关的研究进展。这篇综述强调了在这一领域继续研究的重要性，以提供更有效的治疗方法，重点是控制耐药性和改善抗生素LIN的使用。

{"title":"Enhancing lincomycin delivery through innovative nanocarriers: A review","authors":"Mehrab Pourmadadi , Mahsa Molaei Nasr , Fatemeh Yazdian , Abbas Rahdar , Luiz Fernando Romanholo Ferreira","doi":"10.1016/j.jddst.2025.107948","DOIUrl":"10.1016/j.jddst.2025.107948","url":null,"abstract":"<div><div>Antibiotic resistance has been brought on by misuse of antibiotics, even though lincomycin (LIN), a lincosamide antibiotic, is effective in treating Gram-positive bacterial infections. The advent of this basic problem has limited the efficacy of typical uses of this class of antibiotics, making their application in healthcare more difficult. To tackle this issue, the design of innovative drug delivery systems based on nanomaterials, including polymeric, lipid-based, and inorganic nanoparticles such as chitosan, hydrogels, liposomes, Ag-nanoparticles (Ag-NPs), Au-NPs, titanium oxide nanoparticles (TiO<sub>2</sub>-NPs), and others, has been proposed. Under some conditions, correct release of drugs at infection sites is possible via systems of drug delivery that are sensitive to environmental stimuli like pH variation. Recent investigation research suggests that co-formulation of LIN with other therapeutics or co-delivery of LIN can potentially defeat drug resistance and adverse effects with improved therapeutic efficacy in inflammatory and cancer diseases. While these research developments challenge existing such as those related to industrial manufacturing of these systems, in vivo reliability, and safety evaluation. This review emphasizes the importance of continued research in this field to offer more potent treatments by focusing on methods for managing drug resistance and improving the use of the antibiotic LIN.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107948"},"PeriodicalIF":4.9,"publicationDate":"2025-12-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145921251","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Bilirubin-loaded, dual-responsive nanoparticles promote macrophage Re-polarization for efficient rheumatoid arthritis therapy 装载胆红素的双反应纳米颗粒促进巨噬细胞再极化，有效治疗类风湿性关节炎

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-24 DOI: 10.1016/j.jddst.2025.107952

Lixia Zhang , Xiangrui Yang , Yufei Li , Yangfei Yi , Kewei Lei , Dukun Liu , Yue Tan , Shichao Wu , Xiaojun Tao

Rheumatoid arthritis (RA) frequently demonstrates an inadequate response to conventional therapies, and long-term pharmacological interventions are often accompanied by severe adverse effects. The pathological progression of RA is characterized by infiltration of M1 macrophages and secretion of pro-inflammatory cytokines, which play central roles in driving inflammation. In this study, we developed folic acid (FA)-modified bilirubin (BR)-loaded nanoparticles (FA-BNPs) for efficient RA therapy via a dual-response strategy. FA-BNPs specifically targeted M1 macrophages through FA receptor-mediated endocytosis. Subsequently, BR was responsively released within the inflammatory microenvironment due to the high reactive oxygen species (ROS) levels. The released BR not only scavenged excess ROS and remodeled the immune microenvironment but also significantly promoted the re-polarization of M1 macrophages toward the M2 phenotype. This resulted in reduced levels of TNF-α, IL-6, and IL-1β, demonstrating a notable joint-protective effect alongside a favorable safety profile. This study established a novel synergistic strategy based on “targeted delivery—oxidative stress modulation—immune remodeling” for RA treatment and provided new perspectives for advancing nanotherapies utilizing endogenous substances.

类风湿性关节炎（RA）经常对常规治疗反应不足，长期的药物干预往往伴随着严重的不良反应。RA的病理进展以M1巨噬细胞浸润和促炎细胞因子分泌为特征，促炎细胞因子在炎症驱动中起核心作用。在这项研究中，我们开发了叶酸（FA）修饰胆红素（BR）负载纳米颗粒（FA- bnps），通过双反应策略有效治疗RA。FA- bnps通过FA受体介导的内吞作用特异性靶向M1巨噬细胞。随后，由于高活性氧（ROS）水平，BR在炎症微环境中被响应性释放。释放的BR不仅清除了过量的ROS，重塑了免疫微环境，而且显著促进了M1巨噬细胞向M2表型的再极化。这导致TNF-α、IL-6和IL-1β水平降低，显示出显著的关节保护作用和良好的安全性。本研究建立了一种基于“靶向递送-氧化应激调节-免疫重塑”的新型RA治疗协同策略，为利用内源性物质推进纳米治疗提供了新的视角。

{"title":"Bilirubin-loaded, dual-responsive nanoparticles promote macrophage Re-polarization for efficient rheumatoid arthritis therapy","authors":"Lixia Zhang , Xiangrui Yang , Yufei Li , Yangfei Yi , Kewei Lei , Dukun Liu , Yue Tan , Shichao Wu , Xiaojun Tao","doi":"10.1016/j.jddst.2025.107952","DOIUrl":"10.1016/j.jddst.2025.107952","url":null,"abstract":"<div><div>Rheumatoid arthritis (RA) frequently demonstrates an inadequate response to conventional therapies, and long-term pharmacological interventions are often accompanied by severe adverse effects. The pathological progression of RA is characterized by infiltration of M1 macrophages and secretion of pro-inflammatory cytokines, which play central roles in driving inflammation. In this study, we developed folic acid (FA)-modified bilirubin (BR)-loaded nanoparticles (FA-BNPs) for efficient RA therapy via a dual-response strategy. FA-BNPs specifically targeted M1 macrophages through FA receptor-mediated endocytosis. Subsequently, BR was responsively released within the inflammatory microenvironment due to the high reactive oxygen species (ROS) levels. The released BR not only scavenged excess ROS and remodeled the immune microenvironment but also significantly promoted the re-polarization of M1 macrophages toward the M2 phenotype. This resulted in reduced levels of TNF-α, IL-6, and IL-1β, demonstrating a notable joint-protective effect alongside a favorable safety profile. This study established a novel synergistic strategy based on “targeted delivery—oxidative stress modulation—immune remodeling” for RA treatment and provided new perspectives for advancing nanotherapies utilizing endogenous substances.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107952"},"PeriodicalIF":4.9,"publicationDate":"2025-12-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145881035","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Antheraea mylitta silk sericin grafted polyaniline/Polyvinyl Alcohol based scaffolds as emerging biomaterials for bone tissue regeneration 柞蚕丝胶接枝聚苯胺/聚乙烯醇基支架作为骨组织再生的新兴生物材料

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-24 DOI: 10.1016/j.jddst.2025.107954

Trishna Bal , Sutapa Satpathi , Soumyadip Ghosh , Akash Mondal , Karmabeer Jena , Joydeep Bhattacharyya , Aman Kumar , Jiban Jyoti Panda , Rajdeep Saha , Biswatrish Sarkar , Balaji Ayyanar Chinnappan , Kajal Kumari , Riya Kumari , Tejaswani Sahoo

Bone tissue regeneration remains a significant challenge due to the limitations of autografts, allografts, and conventional biomaterials. To address this, we developed Antheraea mylitta silk sericin (SER)-polyvinyl alcohol (PVA) blend grafted with polyaniline (PANI) based biomaterials. The graft copolymer (SER–PVA–g–PANI) was synthesized using ammonium persulfate-initiated oxidative radical polymerization in an acidic medium under microwave irradiation, with optimized monomer ratios to achieve effective grafting. The composite material was characterized using Fourier-transform infrared spectroscopy, solid-state 13C nuclear magnetic resonance, X-ray diffraction, field-emission scanning electron microscopy, and thermal analysis to confirm grafting, crystallinity, and stability. Mechanical testing showed a tensile strength of 8.2 ± 0.27 MPa and Young's modulus of 2.98 ± 0.12 MPa, indicating its suitability for load-bearing biomedical applications. The optimized formulation exhibited a critical micelle concentration of 0.099 ± 0.002 mg/mL, demonstrated superhydrophilicity with a contact angle of 0°, and showed hemocompatibility with less than 2 % hemolysis. In vitro assays revealed 72–80 % viability of MG-63 cells at concentrations up to 10 μg/mL, accompanied by enhanced alkaline phosphatase activity and mineralization over seven days. Comprehensive zebrafish assays revealed no evidence of acute toxicity, and regenerative studies demonstrated effective tail regrowth following treatment. This study establishes SER-PVA-g-PANI graft copolymer as an effective scaffold with a unique combination of biodegradability, biocompatibility, and regenerative efficacy, positioning it as a next-generation silk sericin-based biomaterial for tissue regeneration applications.

由于自体移植物、同种异体移植物和传统生物材料的局限性，骨组织再生仍然是一个重大挑战。为了解决这一问题，我们开发了柞蚕丝胶(SER)-聚乙烯醇（PVA）共混接枝聚苯胺（PANI）基生物材料。在微波辐照下，采用过硫酸铵引发氧化自由基聚合的方法，在酸性介质中合成了接枝共聚物SER-PVA-g-PANI，优化了单体配比，实现了有效接枝。采用傅里叶变换红外光谱、固态13C核磁共振、x射线衍射、场发射扫描电镜和热分析对复合材料进行了表征，以确定接枝、结晶度和稳定性。力学试验结果表明，该材料抗拉强度为8.2±0.27 MPa，杨氏模量为2.98±0.12 MPa，适合生物医学承重应用。优化后的配方胶束临界浓度为0.099±0.002 mg/mL，接触角为0°的超亲水性，溶血率小于2%的血液相容性。体外实验显示，MG-63细胞在10 μg/mL浓度下的存活率为72 - 80%，碱性磷酸酶活性和矿化在7天内增强。全面的斑马鱼试验没有发现急性毒性的证据，再生研究表明治疗后尾巴再生有效。本研究确定SER-PVA-g-PANI接枝共聚物作为一种有效的支架，具有独特的生物可降解性、生物相容性和再生功效，将其定位为下一代丝胶蛋白基生物材料，用于组织再生应用。

{"title":"Antheraea mylitta silk sericin grafted polyaniline/Polyvinyl Alcohol based scaffolds as emerging biomaterials for bone tissue regeneration","authors":"Trishna Bal , Sutapa Satpathi , Soumyadip Ghosh , Akash Mondal , Karmabeer Jena , Joydeep Bhattacharyya , Aman Kumar , Jiban Jyoti Panda , Rajdeep Saha , Biswatrish Sarkar , Balaji Ayyanar Chinnappan , Kajal Kumari , Riya Kumari , Tejaswani Sahoo","doi":"10.1016/j.jddst.2025.107954","DOIUrl":"10.1016/j.jddst.2025.107954","url":null,"abstract":"<div><div>Bone tissue regeneration remains a significant challenge due to the limitations of autografts, allografts, and conventional biomaterials. To address this, we developed <em>Antheraea mylitta</em> silk sericin (SER)-polyvinyl alcohol (PVA) blend grafted with polyaniline (PANI) based biomaterials. The graft copolymer (SER–PVA–g–PANI) was synthesized using ammonium persulfate-initiated oxidative radical polymerization in an acidic medium under microwave irradiation, with optimized monomer ratios to achieve effective grafting. The composite material was characterized using Fourier-transform infrared spectroscopy, solid-state 13C nuclear magnetic resonance, X-ray diffraction, field-emission scanning electron microscopy, and thermal analysis to confirm grafting, crystallinity, and stability. Mechanical testing showed a tensile strength of 8.2 ± 0.27 MPa and Young's modulus of 2.98 ± 0.12 MPa, indicating its suitability for load-bearing biomedical applications. The optimized formulation exhibited a critical micelle concentration of 0.099 ± 0.002 mg/mL, demonstrated superhydrophilicity with a contact angle of 0°, and showed hemocompatibility with less than 2 % hemolysis. <em>In vitro</em> assays revealed 72–80 % viability of MG-63 cells at concentrations up to 10 μg/mL, accompanied by enhanced alkaline phosphatase activity and mineralization over seven days. Comprehensive zebrafish assays revealed no evidence of acute toxicity, and regenerative studies demonstrated effective tail regrowth following treatment. This study establishes SER-PVA-g-PANI graft copolymer as an effective scaffold with a unique combination of biodegradability, biocompatibility, and regenerative efficacy, positioning it as a next-generation silk sericin-based biomaterial for tissue regeneration applications.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107954"},"PeriodicalIF":4.9,"publicationDate":"2025-12-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145836994","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Novel 3D-Printed medicated straw platform with an optimized lyophilized drug cake for dysphagic patients 新型3d打印药物吸管平台，为吞咽困难患者优化冻干药物蛋糕

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-24 DOI: 10.1016/j.jddst.2025.107950

Tanikan Sangnim , Kittipat Suwanpitak , Pornsak Sriamornsak , Inderbir Singh , Pattiya Prapakun , Laksana Jamnongsut , Krittiyaporn Lekprasert , Kampanart Huanbutta

Non-compliance with medication is a significant issue found among both pediatric and geriatric patients. One of the main factors is dysphagia, which could lead to treatment failure. The aim of this study is to investigate and develop a pharmaceutical formulation in a medicated straw for geriatric and pediatric patients using 3D printing technology combined with lyophilization. The process began with the design and computer simulation of a suitable medicated straw, followed by the development of the formulation using the Design of Experiment (DOE) approach using the Box-Behnken design to analyze the relationship between formulation components and various properties of straw and drug cake loaded inside. These included water-to-solid content ratio, sodium starch glycolate-to-mannitol ratio and gelatin amount, to key tablet properties. Based on experimental results and Partial Least Squares (PLS), the study identified that water-to-solid content ratio significantly influences sipping time, pore volume, tablet density and weight loss percentage. The sodium starch glycolate-to-mannitol ratio primarily affects drug dissolution percentage, while the gelatin content was identified as the most influential factor in enhancing the hardness of the tablets. The optimal formulation was identified with a water-to-solid content ratio of 4.918, a sodium starch glycolate-to-mannitol ratio of 0.075, and a gelatin content of 0.225 mg per unit. The findings enabled the development of an optimal medicated straw and formulation for pediatric and geriatric patients.

不遵医嘱是儿科和老年患者中发现的一个重要问题。其中一个主要因素是吞咽困难，这可能导致治疗失败。本研究的目的是利用3D打印技术结合冻干技术，研究和开发一种用于老年和儿科患者的药物吸管的药物配方。该过程首先设计和计算机模拟合适的药物吸管，然后采用实验设计（design of Experiment， DOE）方法开发配方，采用Box-Behnken设计方法分析配方成分与稻草和药饼内负载的各种性能之间的关系。这些指标包括水固含量比、乙醇酸钠淀粉与甘露醇比和明胶量，以及关键的片剂性能。基于实验结果和偏最小二乘法（PLS），研究发现水固含量比显著影响吸药时间、孔隙体积、片剂密度和失重率。乙醇酸淀粉钠与甘露醇的比例主要影响药物溶出度，明胶含量是提高片剂硬度的最主要因素。优选出的最佳配方水固比为4.918，甘露醇比为0.075，明胶含量为0.225 mg /单位。这一发现为儿童和老年患者开发了一种最佳的药物吸管和配方。

{"title":"Novel 3D-Printed medicated straw platform with an optimized lyophilized drug cake for dysphagic patients","authors":"Tanikan Sangnim , Kittipat Suwanpitak , Pornsak Sriamornsak , Inderbir Singh , Pattiya Prapakun , Laksana Jamnongsut , Krittiyaporn Lekprasert , Kampanart Huanbutta","doi":"10.1016/j.jddst.2025.107950","DOIUrl":"10.1016/j.jddst.2025.107950","url":null,"abstract":"<div><div>Non-compliance with medication is a significant issue found among both pediatric and geriatric patients. One of the main factors is dysphagia, which could lead to treatment failure. The aim of this study is to investigate and develop a pharmaceutical formulation in a medicated straw for geriatric and pediatric patients using 3D printing technology combined with lyophilization. The process began with the design and computer simulation of a suitable medicated straw, followed by the development of the formulation using the Design of Experiment (DOE) approach using the Box-Behnken design to analyze the relationship between formulation components and various properties of straw and drug cake loaded inside. These included water-to-solid content ratio, sodium starch glycolate-to-mannitol ratio and gelatin amount, to key tablet properties. Based on experimental results and Partial Least Squares (PLS), the study identified that water-to-solid content ratio significantly influences sipping time, pore volume, tablet density and weight loss percentage. The sodium starch glycolate-to-mannitol ratio primarily affects drug dissolution percentage, while the gelatin content was identified as the most influential factor in enhancing the hardness of the tablets. The optimal formulation was identified with a water-to-solid content ratio of 4.918, a sodium starch glycolate-to-mannitol ratio of 0.075, and a gelatin content of 0.225 mg per unit. The findings enabled the development of an optimal medicated straw and formulation for pediatric and geriatric patients.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107950"},"PeriodicalIF":4.9,"publicationDate":"2025-12-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145881104","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Effect of compositions on stability, lipid digestion, and bioavailability of progesterone-loaded self-nanoemulsifying drug delivery systems 组合物对黄体酮负载的自纳米乳化给药系统的稳定性、脂质消化和生物利用度的影响

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-23 DOI: 10.1016/j.jddst.2025.107951

Nguyen-Thach Tung , Cao-Son Tran , Van-Trang Nguyen , Thanh-Tung Nguyen , Thi-Thanh-Thuy Vu

The first objective of the study is to formulate and determine the stability of self-nanoemulsifying drug delivery systems containing progesterone in both in-vitro and in-vivo lipolysis simulated conditions. Another aim of the study was to compare the bioavailability of raw material, SNEDDS, and the reference product in the rabbit model. The high amount of cosolvent played an important role in maintaining the high nanoemulsion formation area, monodispersity, and drug loading capacity of SNEDDSs consisting of oleic acid, Tween 80, and ethanol. Under different in vitro severe conditions, including a hot-cold cycle, freeze-thaw cycle, and different pHs of gastrointestinal simulated mediums, there was no appearance of drug precipitation and phase separation of optimal SNEDDS. The cryo-TEM and dynamic light scattering study indicated that the size of the nanoemulsion was under 150 nm and monodispersity. The in vivo lipolysis simulated study then showed that the lower the amount of drug content loaded in SNEDDSs, the higher the proportion of Progesterone (PGT) existed in the colloidal phase, and the lower the risk of drug precipitation in the gastrointestinal medium. Especially, the percentage of PGT in the colloidal phase obtained from the digestion process of optimal SNEDDS was much higher than that from the reference product. Besides, the majority of drugs digested from Ultrogestan® existed in the precipitation phase. These in vitro results were consistent with a pharmacokinetics study in the rabbit model, which indicated that the oral bioavailability of SNEDDS was improved by around 2.95 and 5.40 times compared to the reference product and raw material, respectively.

本研究的第一个目标是在体外和体内脂肪分解模拟条件下，制定并确定含有黄体酮的自纳米乳化药物递送系统的稳定性。本研究的另一个目的是比较原料SNEDDS和参比产品在家兔模型中的生物利用度。高用量的助溶剂对油酸、吐温80和乙醇组成的snedds的高纳米乳形成面积、单分散性和载药量起着重要作用。在不同的体外严酷条件下，包括冷热循环、冻融循环以及胃肠道模拟培养基的不同ph值，最优SNEDDS均未出现药物沉淀和相分离现象。低温透射电镜和动态光散射研究表明，纳米乳液的粒径在150 nm以下，具有单分散性。体内脂解模拟研究表明，snedss中载药量越低，胶体相中孕酮（PGT）的比例越高，药物在胃肠道介质中沉淀的风险越低。其中，最优sndds溶出过程中得到的胶体相PGT的含量明显高于参比产物。此外，从乌曲孕酮®消化的大部分药物存在于沉淀相。这些体外结果与兔模型药代动力学研究结果一致，表明SNEDDS的口服生物利用度分别比参比品和原料药提高约2.95倍和5.40倍。

{"title":"Effect of compositions on stability, lipid digestion, and bioavailability of progesterone-loaded self-nanoemulsifying drug delivery systems","authors":"Nguyen-Thach Tung , Cao-Son Tran , Van-Trang Nguyen , Thanh-Tung Nguyen , Thi-Thanh-Thuy Vu","doi":"10.1016/j.jddst.2025.107951","DOIUrl":"10.1016/j.jddst.2025.107951","url":null,"abstract":"<div><div>The first objective of the study is to formulate and determine the stability of self-nanoemulsifying drug delivery systems containing progesterone in both in-vitro and in-vivo lipolysis simulated conditions. Another aim of the study was to compare the bioavailability of raw material, SNEDDS, and the reference product in the rabbit model. The high amount of cosolvent played an important role in maintaining the high nanoemulsion formation area, monodispersity, and drug loading capacity of SNEDDSs consisting of oleic acid, Tween 80, and ethanol. Under different in vitro severe conditions, including a hot-cold cycle, freeze-thaw cycle, and different pHs of gastrointestinal simulated mediums, there was no appearance of drug precipitation and phase separation of optimal SNEDDS. The cryo-TEM and dynamic light scattering study indicated that the size of the nanoemulsion was under 150 nm and monodispersity. The in vivo lipolysis simulated study then showed that the lower the amount of drug content loaded in SNEDDSs, the higher the proportion of Progesterone (PGT) existed in the colloidal phase, and the lower the risk of drug precipitation in the gastrointestinal medium. Especially, the percentage of PGT in the colloidal phase obtained from the digestion process of optimal SNEDDS was much higher than that from the reference product. Besides, the majority of drugs digested from Ultrogestan® existed in the precipitation phase. These in vitro results were consistent with a pharmacokinetics study in the rabbit model, which indicated that the oral bioavailability of SNEDDS was improved by around 2.95 and 5.40 times compared to the reference product and raw material, respectively.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107951"},"PeriodicalIF":4.9,"publicationDate":"2025-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145880993","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Chitosan/hazelnut shell powder composites as innovative dressing in the treatment of wounds 壳聚糖/榛子壳粉复合材料在创面治疗中的应用

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-22 DOI: 10.1016/j.jddst.2025.107943

Anna Imbriano , Alessandro Di Michele , Debora Puglia , Francesca Luzi , Francesco Cottone , Giorgia Licciardi , Samuele Bonafè , Maurizio Ricci , Sara Primavilla , Cinzia Pagano , Luana Perioli

Wound management by drug-free dressings is a useful approach for elderly people, children, pregnant women and otherwise fragile patients, for whom pharmacological treatment is often not an option. Polymeric films combining the biopolymer chitosan to glycerol were developed and characterized, and hazelnut shell powder (HSP) was upcycled as a valuable, feasible and novel filler.

Reference chitosan/glycerol films with or without the traditional bentonite (BENT) filler were prepared and characterized in terms of porosity, water vapor transmission rate (WVTR), swelling ability, morphology, mechanical properties, bioadhesion and conductivity. The HSP-film can absorb up to ∼80 % by weight of the simulated wound fluid, and retain its integrity for up to 6 days. Data obtained from porosity (92.58 %) and WVTR (28.88 ± 2.95 g/m² • h) measurements showed that the HSP-film can prevent wound dehydration, ensuring the level of moisture necessary to support the healing. The film also demonstrated a bioadhesion capacity useful for self-adhesion to skin. Mechanical characterization showed that the tensile characteristics are improved in presence of HSP when compared to chitosan/glycerol, resulting in a detectable increase in elastic modulus and breaking strength. Antimicrobial activity studies showed that the film suppress the growth of both studied strains, Streptococcus pyogenes and Staphylococcus aureus, within 48 h. The electrical conductivity of HSP-film was detected by sheet resistance measurements, making them exploitable also as bioelectric dressing.

对老年人、儿童、孕妇和其他身体虚弱的病人来说，用无药敷料处理伤口是一种有用的方法，对他们来说，药物治疗往往不是一种选择。制备了生物聚合物壳聚糖-甘油复合聚合物薄膜，并对其进行了表征，将榛子壳粉（HSP）作为一种有价值的、可行的新型填料进行了再生利用。制备了添加或不添加传统膨润土（BENT）填料的壳聚糖/甘油参考膜，并对其孔隙率、水蒸气透过率（WVTR）、膨胀能力、形貌、力学性能、生物粘附性和电导率进行了表征。热休克蛋白膜可以吸收高达80%的模拟伤口液的重量，并保持其完整性长达6天。从孔隙率（92.58%）和WVTR（28.88±2.95 g/m2•h）测量中获得的数据表明，hsp膜可以防止伤口脱水，确保支持愈合所需的水分水平。该薄膜还显示了一种生物粘附能力，有助于皮肤的自粘附。力学表征表明，与壳聚糖/甘油相比，HSP的存在改善了拉伸特性，导致弹性模量和断裂强度明显增加。抗菌活性研究表明，该膜在48 h内抑制了所研究的两种菌株，化脓性链球菌和金黄色葡萄球菌的生长。热休克蛋白膜的电导率通过薄片电阻测量来检测，使其也可用于生物电敷料。

{"title":"Chitosan/hazelnut shell powder composites as innovative dressing in the treatment of wounds","authors":"Anna Imbriano , Alessandro Di Michele , Debora Puglia , Francesca Luzi , Francesco Cottone , Giorgia Licciardi , Samuele Bonafè , Maurizio Ricci , Sara Primavilla , Cinzia Pagano , Luana Perioli","doi":"10.1016/j.jddst.2025.107943","DOIUrl":"10.1016/j.jddst.2025.107943","url":null,"abstract":"<div><div>Wound management by drug-free dressings is a useful approach for elderly people, children, pregnant women and otherwise fragile patients, for whom pharmacological treatment is often not an option. Polymeric films combining the biopolymer chitosan to glycerol were developed and characterized, and hazelnut shell powder (HSP) was upcycled as a valuable, feasible and novel filler.</div><div>Reference chitosan/glycerol films with or without the traditional bentonite (BENT) filler were prepared and characterized in terms of porosity, water vapor transmission rate (WVTR), swelling ability, morphology, mechanical properties, bioadhesion and conductivity. The HSP-film can absorb up to ∼80 % by weight of the simulated wound fluid, and retain its integrity for up to 6 days. Data obtained from porosity (92.58 %) and WVTR (28.88 ± 2.95 g/m<sup>2</sup> • h) measurements showed that the HSP-film can prevent wound dehydration, ensuring the level of moisture necessary to support the healing. The film also demonstrated a bioadhesion capacity useful for self-adhesion to skin. Mechanical characterization showed that the tensile characteristics are improved in presence of HSP when compared to chitosan/glycerol, resulting in a detectable increase in elastic modulus and breaking strength. Antimicrobial activity studies showed that the film suppress the growth of both studied strains, <em>Streptococcus pyogenes</em> and <em>Staphylococcus aureus</em>, within 48 h. The electrical conductivity of HSP-film was detected by sheet resistance measurements, making them exploitable also as bioelectric dressing.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107943"},"PeriodicalIF":4.9,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145836998","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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

Development, quality and safety assessments of nanoemulsions containing capsaicin for the treatment of burning mouth syndrome 用于治疗灼口综合征的含辣椒素纳米乳剂的开发、质量和安全性评估

IF 4.9 3区医学 Q1 PHARMACOLOGY & PHARMACY

Journal of Drug Delivery Science and Technology

Pub Date : 2025-12-22 DOI: 10.1016/j.jddst.2025.107944

F.L. Schneider , J.C. Facchini , E.C.J. Ferreira , B.A.F. Souza , F. Visioli , L.A. Frank , C.V. Garcia

This study developed a nanoemulsion containing capsaicin (NE-C) for the treatment of burning mouth syndrome (BMS). The composition of the NE-C was ultra-purified water, Span 80 and Tween 80 for the aqueous phase, as the oily phase consisted of copaiba oil, Span 80 and capsaicin raw material. A blank nanoemulsion (NE-B) and a capsaicin solution were also prepared for comparative analyses. The aims were to develop and validate an analytical method, characterize the NE-C and NE-B formulations through a preliminary stability study, investigate their local irritation effects using the HET-CAM assay, evaluate permeation and penetration with Franz cells and assess cell viability. The analytical validation results were excellent, with r = 0.999, and all other parameters considered satisfactory. The particle size values were appropriate for the expected nanoemulsion parameters, with 155.17 ± 1.23 nm determined by dynamic light scattering and 141.67 ± 3.21 nm by laser beam diffraction. Similarly, the PDI (0.246 ± 0.001) and SPAN (1.365 ± 0.001) values were within acceptable ranges. The zeta potential values were (-10.49 ± 1.24 mV). The preliminary stability results were favorable with minor variations observed under refrigerator and in the climatic chamber. The HET-CAM assay demonstrated a moderate irritation for NE-C, slight irritation for NE-B and severe irritation for capsaicin solution, indicating a reduction in local irritation due to nanotechnology. Additionally, the penetration and permeation results were considered acceptable. However, the formulations exhibited significant cytotoxic effects on cell viability at both evaluation times (12 and 24 h) in HaCaT and fibroblast cell lines. Overall, this study generates several promising aspects for the development of an innovative formulation for the treatment of BMS.

本研究开发了一种含有辣椒素（NE-C）的纳米乳，用于治疗灼口综合征（BMS）。NE-C的水相组成为超纯水、Span 80和Tween 80，油相由copaiba油、Span 80和辣椒素原料组成。制备空白纳米乳（NE-B）和辣椒素溶液进行对比分析。目的是开发和验证一种分析方法，通过初步的稳定性研究来表征NE-C和NE-B配方，使用ht - cam试验研究它们的局部刺激效应，评估Franz细胞的渗透性和穿透性，并评估细胞活力。分析验证结果优良，r = 0.999，其他参数均满意。动态光散射法测定的粒径为155.17±1.23 nm，激光衍射法测定的粒径为141.67±3.21 nm，符合纳米乳液的预期参数。同样，PDI（0.246±0.001）和SPAN（1.365±0.001）值也在可接受范围内。zeta电位为（-10.49±1.24 mV）。初步的稳定性结果是有利的，在冰箱和气候室中观察到的变化很小。HET-CAM实验显示，NE-C有中度刺激，NE-B有轻微刺激，辣椒素溶液有严重刺激，表明纳米技术减少了局部刺激。此外，穿透和渗透结果被认为是可以接受的。然而，在HaCaT和成纤维细胞系的评估时间（12和24小时），这些配方对细胞活力都有显著的细胞毒性作用。总的来说，这项研究为开发治疗BMS的创新配方提供了几个有希望的方面。

{"title":"Development, quality and safety assessments of nanoemulsions containing capsaicin for the treatment of burning mouth syndrome","authors":"F.L. Schneider , J.C. Facchini , E.C.J. Ferreira , B.A.F. Souza , F. Visioli , L.A. Frank , C.V. Garcia","doi":"10.1016/j.jddst.2025.107944","DOIUrl":"10.1016/j.jddst.2025.107944","url":null,"abstract":"<div><div>This study developed a nanoemulsion containing capsaicin (NE-C) for the treatment of burning mouth syndrome (BMS). The composition of the NE-C was ultra-purified water, Span 80 and Tween 80 for the aqueous phase, as the oily phase consisted of copaiba oil, Span 80 and capsaicin raw material. A blank nanoemulsion (NE-B) and a capsaicin solution were also prepared for comparative analyses. The aims were to develop and validate an analytical method, characterize the NE-C and NE-B formulations through a preliminary stability study, investigate their local irritation effects using the HET-CAM assay, evaluate permeation and penetration with Franz cells and assess cell viability. The analytical validation results were excellent, with r = 0.999, and all other parameters considered satisfactory. The particle size values were appropriate for the expected nanoemulsion parameters, with 155.17 ± 1.23 nm determined by dynamic light scattering and 141.67 ± 3.21 nm by laser beam diffraction. Similarly, the PDI (0.246 ± 0.001) and SPAN (1.365 ± 0.001) values were within acceptable ranges. The zeta potential values were (-10.49 ± 1.24 mV). The preliminary stability results were favorable with minor variations observed under refrigerator and in the climatic chamber. The HET-CAM assay demonstrated a moderate irritation for NE-C, slight irritation for NE-B and severe irritation for capsaicin solution, indicating a reduction in local irritation due to nanotechnology. Additionally, the penetration and permeation results were considered acceptable. However, the formulations exhibited significant cytotoxic effects on cell viability at both evaluation times (12 and 24 h) in HaCaT and fibroblast cell lines. Overall, this study generates several promising aspects for the development of an innovative formulation for the treatment of BMS.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"116 ","pages":"Article 107944"},"PeriodicalIF":4.9,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145837387","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"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