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Synovium targeted colchicine therapy using pH responsive nanoparticles. 利用pH响应纳米颗粒治疗滑膜靶向秋水仙碱。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-30 DOI: 10.1080/09205063.2025.2611106
Syeda Komal Fatima, Naveed Ahmed, Kainat Gul, Abid Ur Rehman, Amna Khan Adil, Asim Ur Rehman

Conventional gout therapies are associated with severe systemic adverse effects, creating a need for sustained and targeted therapy. This research aimed to prepare Colchicine-EL-100-polymeric nanoparticles for pH-dependent release in gout. Molecular docking was performed to provide supportive insight into the COL-NLRP3 interaction. The nanoparticles were prepared and optimized using a Box-Behnken Design, characterized by FTIR, XRD, DSC, and FE-SEM. Incorporated into a characterized Carbopol934 hydrogel, it was evaluated for in vitro release, ex vivo permeation, and ex vivo fluorescence imaging. The nanoparticles were evaluated in an experimental MSU-induced gout model, along with biochemical and histopathological studies. Docking revealed favourable colchicine binding to NLRP3 (docking score of 39.3). Optimized nanoparticles exhibited favourable particle size (152 ± 2.8 nm) and zeta potential (-27.75 ± 0.25 mV), EE% (89.60 ± 0.3%), indicating physicochemical stability. FTIR showed no evidence of chemical incompatibility, XRD indicated amorphization, and DSC supported these findings. In vitro studies showed pH-dependent release (84.3 ± 2.67% at pH 6.8 vs. <20% at pH 7.4 in 24 h), restricted drug release at pH 7.4, with preferential release observed at pH 6.8. Ex vivo fluorescence imaging confirmed penetration (354 μm) within dermal layers with sponge-like restructuring of stratum corneum lipids. In vivo, the formulation reduced inflammation, with IL-6 suppression (92.5 ± 3.62 pg/mL vs. 495.23 ± 32.12 pg/mL). This formulation provides sustained, pH-responsive release and shows therapeutic potential for localized management of gout.

传统的痛风治疗与严重的全身不良反应相关,需要持续和靶向治疗。本研究旨在制备可用于痛风ph依赖性释放的秋水仙碱- el -100聚合纳米颗粒。进行分子对接,为COL-NLRP3相互作用提供支持。采用Box-Behnken设计对纳米颗粒进行了制备和优化,并用FTIR、XRD、DSC和FE-SEM对其进行了表征。将其加入表征的Carbopol934水凝胶中,评估其体外释放、体外渗透和体外荧光成像。纳米颗粒在实验性msu诱导的痛风模型中进行了评估,并进行了生化和组织病理学研究。对接显示秋水仙碱与NLRP3结合良好(对接评分为39.3)。优化后的纳米颗粒具有良好的粒径(152±2.8 nm)和zeta电位(-27.75±0.25 mV), EE%(89.60±0.3%),具有良好的物理化学稳定性。FTIR没有显示出化学不相容的证据,XRD显示非晶化,DSC支持这些发现。体外研究表明,pH值为6.8时,该药物的pH依赖性释放率为84.3±2.67%,离体荧光成像证实该药物在真皮内渗透(354 μm),角质层脂质呈海绵状重构。在体内,该制剂可减轻炎症,抑制IL-6(92.5±3.62 pg/mL vs. 495.23±32.12 pg/mL)。该配方提供持续的,ph响应释放,并显示出痛风局部管理的治疗潜力。
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引用次数: 0
A novel design of a hybrid hydrogel skin scaffold made from modified PVA/urea oligomer, incorporating protein and polysaccharide. 一种新型的由改性聚乙烯醇/尿素低聚物制成的混合水凝胶皮肤支架,结合蛋白质和多糖。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-28 DOI: 10.1080/09205063.2025.2604819
Fahimeh Dehghan Manshadi, Maryam Sharzehee, Seyed Abbas Mirjalili

Urea compounds, which help control bacterial growth and maintain tissue moisture, were used to create a stable polyvinyl alcohol (PVA) hydrogel. By combining urea, sulfamic acid, and phosphorus acid under molten conditions, urea linkage oligomers (ULO) are formed. These compounds, with NH2 and OH as active functional groups at two ends of their chain, can react with the hydroxyl groups of polyvinyl alcohol. Also, crosslinking networks produce a resistant hydrogel in an aqueous medium. Egg white was found to be an ideal protein for the scaffold and was reacted with ULO to enhance mixing and prevent coagulation. The base polymer consisted of 8 g PVA, 5 g ULO, 2 g urea, and 1 g egg white powder, with one gram of a biopolymer (gelatin, collagen, or chitosan) as the sole variable. Characterization involved swelling behavior, gel fraction, and tensile strength measurements in dry states, alongside FT-IR, XRD, SEM, and EDAX analyses. Biodegradation and MTT tests evaluated the growth of fibroblast cells on the hydrogels. The samples made with the selected bio-compounds showed great promise for wound healing, with swelling rates ranging from 300% to 900% and gel factor variations from 43% to 56%. Cell growth exceeded 90-110% after one day of culture. The higher presence of functional groups in the chitosan biopolymer enhanced crosslinking conditions, resulting in better physical, mechanical, and biological properties compared to other biopolymers.

尿素化合物有助于控制细菌生长和保持组织水分,用来制造稳定的聚乙烯醇(PVA)水凝胶。尿素、氨基磺酸和磷酸在熔融条件下结合,形成尿素连锁低聚物(ULO)。这些化合物在链的两端以NH2和OH为活性官能团,可与聚乙烯醇的羟基反应。此外,交联网络在水介质中产生抗性水凝胶。蛋白被发现是一种理想的支架蛋白质,并与ULO反应,以加强混合和防止凝血。基础聚合物由8g PVA, 5g ULO, 2g尿素和1g蛋清粉组成,1克生物聚合物(明胶,胶原蛋白或壳聚糖)作为唯一变量。表征包括膨胀行为、凝胶分数和干燥状态下的拉伸强度测量,以及FT-IR、XRD、SEM和EDAX分析。生物降解和MTT试验评估成纤维细胞在水凝胶上的生长情况。用选定的生物化合物制成的样品显示出伤口愈合的巨大希望,肿胀率从300%到900%不等,凝胶因子变化从43%到56%不等。培养1天后细胞生长超过90-110%。壳聚糖生物聚合物中较高的官能团增强了交联条件,与其他生物聚合物相比,具有更好的物理、机械和生物性能。
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引用次数: 0
Astragaloside-loaded PCL microspheres prepared from microchips for promoting collagen regenerating. 微芯片制备含黄芪甲苷PCL微球促进胶原蛋白再生。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-23 DOI: 10.1080/09205063.2025.2604821
Die Xie, Xin Che, Li Zha, Qian Zhang, Mengxing Chen, Lihong Wang

Polycaprolactone (PCL) microspheres are effective in stimulating collagen regeneration. However, the local inflammation they induce upon subcutaneous injection, particularly during the initial post-injection phase, cannot be overlooked. In this study, we designed and fabricated Astragaloside (AS)-loaded PCL microspheres using microfluidic technology for subcutaneous injection to promote collagen regeneration. The incorporation of AS and the application of microfluidic technology endowed the AS/PCL microspheres with a significantly reduced incidence of initial inflammation, thereby enhancing their safety profile. We prepared the AS/PCL microspheres via microfluidic technology and conducted characterization alongside in vitro and in vivo studies. Results demonstrated that the AS/PCL microspheres exhibited a circularity index of 0.90 ± 0.03, an average particle size of 30.45 ± 5.49 μm, and the polydispersity index (PDI) was 0.26 ± 0.03. The AS/PCL microspheres significantly enhanced the proliferation and migration of L929 fibroblasts. In vivo pharmacodynamic studies revealed that the inclusion of AS effectively mitigated the initial inflammatory response triggered by PCL microspheres and promoted superior collagen regeneration. Consequently, the microfluidically fabricated AS/PCL microspheres developed in this study demonstrate enhanced safety and efficacy for subcutaneous injection in promoting collagen regeneration.

聚己内酯(PCL)微球能有效刺激胶原蛋白再生。然而,它们在皮下注射时引起的局部炎症,特别是在注射后的初始阶段,是不能忽视的。本研究采用微流体技术设计并制备了载黄芪甲苷(Astragaloside, AS) PCL微球,用于皮下注射促进胶原再生。AS的掺入和微流控技术的应用使AS/PCL微球的初始炎症发生率显著降低,从而提高了其安全性。我们通过微流体技术制备了AS/PCL微球,并进行了体外和体内研究。结果表明,AS/PCL微球的圆度指数为0.90±0.03,平均粒径为30.45±5.49 μm,多分散性指数(PDI)为0.26±0.03。AS/PCL微球能显著促进L929成纤维细胞的增殖和迁移。体内药理学研究表明,AS的加入有效减轻了PCL微球引发的初始炎症反应,促进了优质胶原的再生。因此,本研究开发的微流体制备的AS/PCL微球在皮下注射促进胶原再生方面具有更高的安全性和有效性。
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引用次数: 0
Correction. 修正。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-19 DOI: 10.1080/09205063.2025.2606461
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引用次数: 0
Evaluation of in vitro antioxidant activity of chrysin and in vivo wound healing potential of an optimized chrysin emulgel formulation. 菊花素体外抗氧化活性及优化后的菊花素乳状剂体内创面愈合潜力的评价。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-15 DOI: 10.1080/09205063.2025.2603346
Neha Singh, Phool Chandra

The present study evaluated the in vivo wound healing activity of an optimized chrysin emulgel formulation. Antioxidant potential was confirmed through ferrous ion chelation and DPPH radical scavenging assays, showing dose-dependent activity with IC50 values of 1755.78 µg/ml and 141.68 µg/ml, respectively. Acute dermal toxicity testing (OECD Guideline 402) revealed no signs of dermal or systemic toxicity at 2000 mg/kg. Wound healing efficacy was assessed using incision and excision models in Wistar albino rats, with animals divided into control (emulgel base), standard (1% silver sulfadiazine), and test (chrysin emulgel) groups. In the incision model, the test group achieved a tensile strength of 561.17 ± 1.11 g, comparable to the standard (565.33 ± 0.88 g). In the excision model, the chrysin emulgel achieved 97.93% wound contraction by day 12 with an epithelization period of 14.83 ± 0.30 days, similar to the standard (98.17%; 14.33 ± 0.42 days). Overall, the optimized chrysin emulgel demonstrated strong antioxidant activity, effective wound healing, and excellent safety, suggesting its potential as a natural alternative to silver sulfadiazine for topical wound management.

本研究评估了一种优化的菊花素乳凝胶配方的体内伤口愈合活性。通过铁离子螯合和DPPH自由基清除实验证实了其抗氧化潜力,显示出剂量依赖性活性,IC50值分别为1755.78µg/ml和141.68µg/ml。急性皮肤毒性试验(经合组织指南402)显示2000mg /kg时没有皮肤或全身毒性迹象。采用Wistar白化病大鼠切口和切除模型,将动物分为对照组(凝胶基)、标准组(1%磺胺嘧啶银)和试验组(菊花素凝胶),评估伤口愈合效果。在切口模型中,实验组的抗拉强度为561.17±1.11 g,与标准(565.33±0.88 g)相当。在切除模型中,黄菊花乳凝胶在第12天创面收缩率为97.93%,上皮形成周期为14.83±0.30天,与标准(98.17%;14.33±0.42天)相似。综上所述,优化后的菊花素凝胶具有较强的抗氧化活性,有效的伤口愈合,并且具有良好的安全性,这表明它有可能作为磺胺嘧啶银的天然替代品用于局部伤口治疗。
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引用次数: 0
Co-encapsulation of bromelain and doxorubicin in acid-responsive nanogels for enhanced chemotherapy via tumor ECM degradation. 菠萝蛋白酶和阿霉素在酸反应纳米凝胶中的共包封,通过肿瘤ECM降解增强化疗。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-12 DOI: 10.1080/09205063.2025.2599287
Lijun Wang, Miao Lei, Jie Hao, Xiaojun Zhang, Wei Jiang, Zhenming Hu

The therapeutic efficacy of chemotherapy in solid tumors such as osteosarcoma is hindered by the dense, collagen-rich extracellular matrix (ECM). In this work, we report an acid-responsive nanogel that co-encapsulates bromelain (BL), a proteolytic enzyme, and doxorubicin (DOX) with spatially distinct localization and independent pH-responsive release mechanisms. BL is encapsulated within the nanogel network, whereas DOX is covalently grafted onto the nanogel surface via an acid-labile linker, enabling the nanocarrier (ng(BL-DOX)) to remain stable under physiological conditions while promoting controlled release in the mildly acidic tumor microenvironment. The released BL degrades collagenous ECM components and reduces matrix density, thereby improving the penetration and intratumoral distribution of the concurrently released DOX. In a murine osteosarcoma model, the PEG-rich nanogels showed prolonged circulation and increased tumor accumulation via the enhanced permeability and retention (EPR) effect, accompanied by collagen I degradation and effective tumor growth inhibition, with final tumor volumes reduced to approximately one-tenth of those in the control group and without observable systemic toxicity. This microencapsulation approach provides an enzyme-drug co- encapsulation system that combines ECM degradation with chemotherapy in a single nanogel platform and may be adapted to other proteolytic enzymes and cytotoxic agents for the treatment of stroma-rich solid tumors.

化疗对骨肉瘤等实体瘤的治疗效果受到密集的、富含胶原的细胞外基质(ECM)的阻碍。在这项工作中,我们报道了一种酸反应纳米凝胶,它共包被菠萝蛋白酶(BL)、一种蛋白水解酶和阿霉素(DOX),具有不同的空间定位和独立的ph反应释放机制。BL被封装在纳米凝胶网络中,而DOX则通过酸不稳定的连接剂共价接枝到纳米凝胶表面,使纳米载体(ng(BL-DOX))在生理条件下保持稳定,同时促进在温和酸性肿瘤微环境中的控制释放。释放的BL降解了胶原ECM成分,降低了基质密度,从而改善了同时释放的DOX的渗透和肿瘤内分布。在小鼠骨肉瘤模型中,富含peg的纳米凝胶通过增强渗透性和滞留性(EPR)效应,表现出延长循环和增加肿瘤积累,伴随着胶原I降解和有效的肿瘤生长抑制,最终肿瘤体积减少到对照组的十分之一左右,并且没有观察到的全身毒性。这种微囊化方法提供了一种酶-药物共囊化系统,将ECM降解与化疗结合在一个纳米凝胶平台上,可能适用于其他蛋白水解酶和细胞毒性药物,用于治疗富含基质的实体瘤。
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引用次数: 0
From water to medicine: the transformative role of hydrogels in diabetic wound healing. 从水到医学:水凝胶在糖尿病伤口愈合中的转化作用。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-08 DOI: 10.1080/09205063.2025.2599294
Prince Kumar Maurya, Kishore Hazarika, Sanchita Bandyopadhyay-Ghosh, Samit Kumar Nandi, Subrata Bandhu Ghosh

Slow tissue repair, chronic inflammation, poor angiogenesis, and increased susceptibility to infection make diabetic wound healing a significant global medical concern. Hydrogel-based dressing is an innovative approach to diabetic wound treatment, replacing traditional treatments like surgery, antibiotics, and dressings that often fail to restore the complex wound microenvironment. This review focuses on significant advancements in hydrogel formulations, including their composition, properties, and medical uses. It begins with an overview of the diabetic wound healing process and current treatment strategies. Hydrogels provide moist environment for healing, which are three-dimensional networks of hydrophilic polymers that can hold almost 90% of water and are categorized according to their crosslinking technique (physical and chemical) and their source (natural, synthetic, or hybrid). Among these, injectable hydrogels are popular due to their simplicity of use, capacity to fill a variety of irregularly shaped wounds, and in situ gelation, promoting tissue regeneration and reducing the risk of infection. Finally, we conclude with clinical case studies utilizing hydrogels derived from sodium alginate, placenta-derived mesenchymal stem cells (PDMSC), and collagen-polyacrylate-metal-organic frameworks (MOFs) have shown notable results in wound healing, including improved tissue repair, enhanced chronic wound management, and reduced infection. Despite these advancements, hydrogels continue to encounter issues with mechanical strength, degradation control, and large-scale production. Hydrogel-based wound dressings have potential for individualized treatment of diabetic wounds keeps growing as research and biomaterial technologies advance. This review also highlights novel classification, real-world case studies, and emerging clinical trends, providing a comprehensive perspective that is not commonly addressed in existing literature.

组织修复缓慢、慢性炎症、血管生成不良以及对感染的易感性增加使糖尿病伤口愈合成为一个重要的全球医学问题。水凝胶敷料是糖尿病伤口治疗的一种创新方法,它取代了手术、抗生素和敷料等传统治疗方法,这些方法往往不能恢复复杂的伤口微环境。本文综述了水凝胶制剂的重大进展,包括它们的组成、性质和医学用途。它开始与糖尿病伤口愈合过程和当前的治疗策略的概述。水凝胶为愈合提供了湿润的环境,它是亲水性聚合物的三维网络,可以容纳近90%的水,并根据其交联技术(物理和化学)及其来源(天然,合成或混合)进行分类。其中,可注射水凝胶因其使用简单,能够填充各种不规则形状的伤口,以及原位凝胶,促进组织再生和降低感染风险而广受欢迎。最后,我们总结了临床案例研究,利用海藻酸钠衍生的水凝胶、胎盘源性间充质干细胞(PDMSC)和胶原-聚丙烯酸-金属-有机框架(mof)在伤口愈合方面显示出显著的效果,包括改善组织修复、增强慢性伤口管理和减少感染。尽管取得了这些进步,但水凝胶在机械强度、降解控制和大规模生产方面仍然存在问题。随着研究和生物材料技术的进步,基于水凝胶的伤口敷料具有个性化治疗糖尿病伤口的潜力。这篇综述还强调了新的分类、现实世界的病例研究和新出现的临床趋势,提供了一个在现有文献中不常见的全面视角。
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引用次数: 0
Natural amphiphilic co-polymers as sustainable nanocarriers for enhanced solubility of hydrophobic drugs. 天然两亲共聚物作为增强疏水药物溶解度的可持续纳米载体。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-08 DOI: 10.1080/09205063.2025.2597238
Avnish Kumar, Anurag Verma, Gulshan Rathore

A major barrier to effective therapy is the limited water solubility of many Biopharmaceutics Classification System (BCS) Class II and IV medications, which results in poor bioavailability and inconsistent patient outcomes. Better solubilization and stability are provided by traditional synthetic nanocarriers such as PLGA, poloxamers, and PEG-PLA; however, these have disadvantages such as toxicity, cost, reliance on petrochemical resources, and regulatory barriers. Natural amphiphilic co-polymers (NACPs) are a sustainable and amiable alternative to proteins, polysaccharides, and phospholipids. Because of their innate amphiphilicity, which promotes self-assembly into micelles, vesicles, nanogels, and hydrogels, hydrophobic drugs can be effectively encapsulated and released under controlled conditions.This review focuses on the structural foundations of amphiphilicity in graft and block copolymers, naturally occurring self-assembling systems, and chemically modified derivatives that enhance solubility and drug-polymer interactions. In contrast to synthetic carriers, NACPs have other benefits such as mucoadhesion, enzymatic degradability, pH/enzyme responsiveness, and generally recognized as safe (GRAS) regulatory status, even though problems with scalability, reproducibility, and long-term stability still exist. Their versatility includes oral, parenteral, transdermal, pulmonary, nasal, and ocular drug delivery, with notable improvements in solubility, bioavailability, and therapeutic accuracy. Recent advancements include stimuli-responsive designs, hybrid natural-synthetic systems, and artificial intelligence (AI)-driven modeling for predicting drug-polymer compatibility. Collectively, NACPs present a sustainable strategy for next-generation nanomedicine that strikes a balance between therapeutic efficacy and environmental responsibility. By addressing solubility concerns with environmentally acceptable carriers, NACPs have a substantial translational potential to promote pharmaceutical innovation and green drug delivery systems.

有效治疗的主要障碍是许多生物制药分类系统(BCS) II类和IV类药物的水溶性有限,这导致生物利用度差和患者预后不一致。传统的合成纳米载体如PLGA、poloxamers和PEG-PLA提供了更好的增溶性和稳定性;然而,这些方法存在毒性、成本、对石化资源的依赖以及监管障碍等缺点。天然两亲共聚物(NACPs)是一种可持续的、友好的蛋白质、多糖和磷脂的替代品。由于疏水药物具有天生的两亲性,可以促进自组装成胶束、囊泡、纳米凝胶和水凝胶,因此疏水药物可以在受控条件下被有效地封装和释放。本文综述了接枝共聚物和嵌段共聚物两亲性的结构基础,自然形成的自组装体系,以及增强溶解度和药物-聚合物相互作用的化学修饰衍生物。与合成载体相比,NACPs还有其他优点,如黏附性、酶降解性、pH/酶响应性,以及公认的安全(GRAS)监管状态,尽管存在可扩展性、可重复性和长期稳定性方面的问题。它们的用途广泛,包括口服、肠外、透皮、肺、鼻和眼给药,具有显著的溶解度、生物利用度和治疗准确性。最近的进展包括刺激响应设计、混合天然合成系统以及用于预测药物-聚合物相容性的人工智能(AI)驱动建模。总的来说,NACPs为下一代纳米医学提供了一个可持续的战略,在治疗效果和环境责任之间取得平衡。通过解决环境可接受载体的溶解度问题,NACPs具有促进制药创新和绿色给药系统的巨大转化潜力。
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引用次数: 0
Novel drug-loaded nano-polymer comparison: amoxicillin between ceftriaxone for MCF-7 breast cancer cytotoxicity. 新型载药纳米聚合物比较:阿莫西林与头孢曲松对MCF-7乳腺癌的细胞毒性。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-08 DOI: 10.1080/09205063.2025.2599290
Khawla I Abd Nusaif, Bahaa K Al-Ghanimi, Zaid M Abbas, Mohammad N Al-Baiati

The rising challenges of conventional chemotherapy, including drug resistance and systemic toxicity, necessitate the exploration of novel therapeutic strategies. Repurposing existing antibiotics offers a promising, cost-effective approach in oncology. In this study, we investigate the anticancer potential of two common β-lactam antibiotics, amoxicillin and ceftriaxone, by conjugating them to a novel glycerol-phthalic anhydride nano-polymer. Successful conjugation and nanoscale formulation (∼97 nm) were confirmed through FT-IR, NMR, and DLS. When evaluated against aggressive MCF-7 breast cancer cells, the ceftriaxone conjugate demonstrated superior efficacy, showing 14% greater cytotoxicity (IC50 = 38.52 vs. 44.8 µg/mL) and inducing extensive apoptosis, evidenced by membrane blebbing and nuclear fragmentation. Molecular docking revealed a mechanistic basis for this enhanced activity, with ceftriaxone forming stronger binding interactions (-7.8 kcal/mol) with key breast cancer proteins, including π-sulfur and hydrogen bonds. This work establishes a scalable nano-polymer platform for antibiotic repurpose, identifies ceftriaxone as a superior candidate for breast cancer therapy, and provides a critical mechanistic bridge between drug chemistry and tumor biology. With its established clinical safety, this ceftriaxone-based system represents a viable candidate for rapid translation to in vivo studies.

传统化疗的挑战日益增加,包括耐药性和全身毒性,需要探索新的治疗策略。重新利用现有抗生素为肿瘤学提供了一种有前途的、具有成本效益的方法。在这项研究中,我们通过将两种常见的β-内酰胺类抗生素阿莫西林和头孢曲松偶联到一种新型的甘油-邻苯二酸酐纳米聚合物上,研究了它们的抗癌潜力。通过FT-IR, NMR和DLS证实了成功的偶联和纳米级配方(~ 97 nm)。当对侵袭性MCF-7乳腺癌细胞进行评估时,头孢曲松偶联物表现出卓越的疗效,显示出14%的细胞毒性(IC50 = 38.52 vs. 44.8µg/mL),并诱导广泛的细胞凋亡,表现为膜起泡和核断裂。分子对接揭示了这种增强活性的机制基础,头孢曲松与关键乳腺癌蛋白形成更强的结合相互作用(-7.8 kcal/mol),包括π-硫键和氢键。这项工作建立了一个可扩展的纳米聚合物平台,用于抗生素的再用途,确定了头孢曲松作为乳腺癌治疗的优越候选者,并在药物化学和肿瘤生物学之间提供了一个关键的机制桥梁。由于其已建立的临床安全性,这种基于头孢曲松的系统代表了快速转化为体内研究的可行候选。
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引用次数: 0
Enhanced cardioprotective efficacy of Rosmarinus officinalis-loaded polydopamine nanoparticles for targeted therapy of myocardial infarction. 迷迭香负载的聚多巴胺纳米颗粒靶向治疗心肌梗死的心脏保护作用增强。
IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Pub Date : 2025-12-05 DOI: 10.1080/09205063.2025.2590717
Ming Zhang, Zhiling Zhang, Jie Hu, Shulan Zhou

Myocardial infarction (MI) is a predominant cause of mortality and heart failure in cardiovascular disorders. This article presents a novel polydopamine (PD) nanoparticles, tagged with cyclic RGD peptides (RP), for the targeted delivery of Rosmarinus officinalis L. (RO) (RP-PD@RO NPs). RO is a therapeutic accessory for cerebrovascular and cardiovascular diseases. RP-PD@RO NPs were developed and characterized using transmission electron microscope (TEM), zeta potentials, and FT-IR spectral analysis. The cell viability was investigated using cell counting kit-8 (CCK-8) analysis. The migration ability was assessed through in vitro wound assays and migration assays. MI targeted therapy was examined using wild-type C57 BL/6J mice. The expression of specific proteins was confirmed using an enzyme-linked immunosorbent assay (ELISA). PD is an efficient carrier recognized for its superior surface modifiability and cytocompatibility. RO was incorporated into PD via π-π stacking, while RP was conjugated via a Michael addition process, yielding stable RP-PD@RO NPs with a mean diameter of 204.51 ± 3.52 nm. Targeting investigations have shown a 2.19-fold enhancement in the efficiency of NPs accumulation within cellular uptake. The study revealed a 1.46-fold enhancement in cell proliferation, a 1.48-fold rise in the rate of angiogenesis, and a notable decrease in the MI site. These data indicate that RP-PD@RO NPs can reduce the MI site and enhance endothelial cell (EC) function via targeted distribution.

心肌梗死(MI)是心血管疾病中死亡和心力衰竭的主要原因。本文提出了一种新的聚多巴胺(PD)纳米颗粒,标记环状RGD肽(RP),用于靶向递送迷迭香(RO) (RP-PD@RO NPs)。RO是一种治疗脑血管和心血管疾病的辅助药物。RP-PD@RO NPs通过透射电子显微镜(TEM)、zeta电位和FT-IR光谱分析进行了表征。采用细胞计数试剂盒-8 (CCK-8)检测细胞活力。通过体外伤口试验和迁移试验评估其迁移能力。用野生型C57 BL/6J小鼠检测心肌梗死靶向治疗。特异蛋白的表达通过酶联免疫吸附试验(ELISA)得到证实。PD是一种高效的载体,具有良好的表面修饰性和细胞相容性。通过π-π叠加将RO掺入PD中,通过Michael加成法共轭RP,得到稳定的RP-PD@RO NPs,平均直径为204.51±3.52 nm。靶向研究表明,细胞摄取内NPs积累的效率提高了2.19倍。该研究显示细胞增殖增强1.46倍,血管生成率增加1.48倍,心肌梗死部位明显减少。这些数据表明RP-PD@RO NPs可以通过靶向分布降低心肌梗死位点并增强内皮细胞(EC)功能。
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Journal of Biomaterials Science, Polymer Edition
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