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Investigation of safety and efficacy of ZnO nanoparticle-loaded alginate-hyaluronic acid hydrogel for wound dressings: In vitro and in vivo studies 纳米氧化锌负载海藻酸透明质酸水凝胶用于伤口敷料的安全性和有效性研究:体外和体内研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-03-01 Epub Date: 2026-01-29 DOI: 10.1016/j.onano.2026.100284
Alaa Abuawad , Areen Alshweiat , Tamara Athamneh , Farah Bani Yaseen , Amin Omar , Hiba Alzoubi , Ali Hmedat , Lujain Aljarrah , Bara’a Magableh , Farah Alzoubi , Yamen Bani Younes , Ahmad Bani Younes
The integration of nanotechnology and biomaterials is valuable for the future of wound care. However, concerns regarding the biosafety of the nanoparticles remain unresolved. This study aims to evaluate the activity and safety of the alginate-hyaluronic acid (Alg/HA) hydrogel-loaded zinc oxide nanoparticles (ZnO-NPs) of three different size ranges (10-30, 35-45, 80-200 nm) and concentrations (5, 10, 20 mg/mL). Fourier Transform Infrared (FTIR) Spectroscopy, and X-ray fluorescence (XRF) Spectroscopy were used to confirm the successful loading and uniform distribution of ZnO-NPs within the hydrogel matrix. Minimum Biofilm Eradication Concentration (MBEC™) assay® against Staphylococcus aureus and Pseudomonas aeruginosa was used to evaluate antibacterial activity. The ZnO-NPs (10–30 nm, 20 mg/mL) loaded hydrogel and pure hydrogel achieved the highest antibacterial efficacy in planktonic states. However, MTT and scratch assays of ZnO-NPs loaded hydrogels indicated a significant reduction in cell viability and migration. The ZnO-NPs loaded hydrogel reduced cell viability up to 85% compared to 100% in the pure Alg/HA hydrogel. In scratch assay, the pure hydrogel showed 68% wound closure within 24 h compared to 55.77% for control group. The pure Alg/HA demonstrated superior in vitro performance. In vivo study showed promising efficacy of the pure Alg/HA hydrogel, promoting complete epithelial regeneration by day 15 (resulting in 95.68% wound closure), while ZnO-NPs hydrogels delayed healing (63.88% of wound closure). Overall, while ZnO-NPs show notable antibacterial properties, their potential cytotoxicity at higher concentrations limits their suitability for wound healing, which urges the reconsideration of using ZnO-NPs for wound dressing applications.
纳米技术和生物材料的结合对未来的伤口护理是有价值的。然而,对纳米颗粒生物安全性的担忧仍未得到解决。本研究旨在评价海藻酸透明质酸(Alg/HA)水凝胶负载氧化锌纳米颗粒(ZnO-NPs)的活性和安全性,该纳米颗粒的粒径范围为10-30、35-45、80-200 nm,浓度为5、10、20 mg/mL。傅里叶变换红外光谱(FTIR)和x射线荧光光谱(XRF)证实了ZnO-NPs在水凝胶基质内的成功加载和均匀分布。最小生物膜根除浓度(MBEC™)测定®对金黄色葡萄球菌和铜绿假单胞菌的抗菌活性。在浮游状态下,ZnO-NPs (10-30 nm, 20 mg/mL)负载的水凝胶和纯水凝胶的抗菌效果最高。然而,负载ZnO-NPs的水凝胶的MTT和划痕实验表明,细胞活力和迁移能力显著降低。ZnO-NPs负载的水凝胶将细胞活力降低了85%,而纯Alg/HA水凝胶的细胞活力为100%。在划痕实验中,纯水凝胶在24 h内伤口愈合率为68%,而对照组为55.77%。纯Alg/HA表现出优异的体外性能。体内研究显示,纯Alg/HA水凝胶具有良好的效果,在第15天促进上皮细胞完全再生(95.68%的伤口愈合),而ZnO-NPs水凝胶延迟愈合(63.88%的伤口愈合)。总体而言,虽然ZnO-NPs表现出显著的抗菌性能,但其在较高浓度下的潜在细胞毒性限制了其在伤口愈合中的适用性,这促使人们重新考虑将ZnO-NPs用于伤口敷料的应用。
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引用次数: 0
Eco-friendly synthesis of nitrogen-doped carbon dots from Cochlospermum regium for efficient photocatalytic removal of pharmaceutical contaminants and antibacterial performance 绿色环保地合成含氮碳点,用于高效光催化去除药物污染物和抗菌性能
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-03-01 Epub Date: 2026-02-05 DOI: 10.1016/j.onano.2026.100285
David Nugroho , Ponrawee Nakbang , A. Asrinawaty , Syamsun Jaya , Aphinya Thinthasit , Choosak Poonsawat , Rachadaporn Benchawattananon
Nitrogen-doped carbon dots (NCDs) were successfully synthesized from Cochlospermum regium petals via a facile hydrothermal method using L-phenylalanine as a nitrogen source. The structural, morphological, optical, and electrochemical properties of the prepared materials were systematically characterized using XRD, SEM–EDX, TEM, UV–Vis spectroscopy, XPS, BET, and electrochemical impedance spectroscopy. Compared with undoped carbon dots (CDs), the NCDs exhibited enhanced visible-light absorption, improved charge transfer capability, and a larger surface area, which significantly promoted their photocatalytic performance. Under visible light irradiation, the NCDs achieved 82% degradation of amoxicillin and 68% degradation of ciprofloxacin, outperforming CDs under identical conditions. Optimization studies revealed that catalyst dosage, pollutant concentration, and light intensity strongly influenced degradation efficiency, with maximum degradation reaching 99% for amoxicillin and 82% for ciprofloxacin under optimal conditions (45 W visible light). Reactive species trapping experiments confirmed that superoxide radicals (O₂⁻•) played a dominant role in ciprofloxacin degradation, whereas hydroxyl radicals (•OH) were primarily responsible for amoxicillin decomposition. In addition, NCDs exhibited strong antibacterial activity against both Gram-positive and Gram-negative bacteria, good biocompatibility in MTT assays, and moderate antioxidant properties. Photodegradation experiments conducted in real water samples demonstrated stable and consistent removal efficiencies, confirming the robustness of the system. These findings highlight NCDs as a promising green nanomaterial for antibiotic removal and sustainable wastewater treatment under visible-light conditions.
以l -苯丙氨酸为氮源,采用水热法成功地合成了氮掺杂碳点(NCDs)。采用XRD、SEM-EDX、TEM、UV-Vis、XPS、BET、电化学阻抗谱等方法对材料的结构、形貌、光学和电化学性能进行了系统表征。与未掺杂的碳点(CDs)相比,NCDs的可见光吸收增强,电荷转移能力增强,比表面积增大,从而显著提高了其光催化性能。在可见光照射下,NCDs对阿莫西林的降解率为82%,对环丙沙星的降解率为68%,优于相同条件下的CDs。优化研究表明,催化剂用量、污染物浓度和光照强度对降解效率影响较大,在最佳条件下(45 W可见光),阿莫西林和环丙沙星的最大降解率分别达到99%和82%。反应性物种捕获实验证实,超氧自由基(O₂⁻)在环丙沙星的降解中起主导作用,而羟基自由基(•OH)则主要负责阿莫西林的分解。此外,NCDs对革兰氏阳性菌和革兰氏阴性菌均具有较强的抗菌活性,在MTT试验中具有良好的生物相容性,并具有中等的抗氧化性能。在实际水样中进行的光降解实验显示出稳定和一致的去除效率,证实了该系统的鲁棒性。这些发现强调了非传染性疾病作为一种有前景的绿色纳米材料,在可见光条件下用于抗生素去除和可持续废水处理。
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引用次数: 0
Natural nanocarriers in oncology: The targeting and delivery capabilities of extracellular vesicles 肿瘤中的天然纳米载体:细胞外囊泡的靶向和递送能力
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-03-01 Epub Date: 2026-02-10 DOI: 10.1016/j.onano.2026.100287
Sevval Kurt, Ilgin Kimiz-Gebologlu, Ozge Cinar, Suphi S. Oncel
Extracellular vesicles (EVs) are nanoscale structures naturally released by cells that mediate intercellular communication by transporting bioactive cargo, including nucleic acids, proteins, and lipids. Their natural origin provides high biocompatibility, low immunogenicity, enhanced stability in circulation, and evades immune clearance. Moreover, the presence of surface integrins, tetraspanins, and adhesion molecules endows EVs with intrinsic targeting capacity, enabling selective interaction with recipient cells. Beyond their role as biological messengers, accumulating evidence points to the active role of EVs in regulating key physiological and pathological processes, including angiogenesis, tumor invasion, metastasis, immune regulation and inflammatory responses within the tumor microenvironment. These unique properties have positioned EVs as promising natural nanocarriers for targeted drug delivery in cancer therapy, especially for improving the bioavailability, stability, and therapeutic index of anticancer agents. Here, this review comprehensively discusses EV biogenesis, isolation and characterization methods, cargo diversity, drug loading strategies, and targeting approaches, with particular emphasis on their application as natural nanocarriers in cancer treatment. Current challenges related to scalability, standardization, and clinical translation are also addressed, highlighting future directions for integrating EV-based systems into next-generation oncological treatments.
细胞外囊泡(EVs)是细胞自然释放的纳米级结构,通过运输生物活性物质介导细胞间通讯,包括核酸、蛋白质和脂质。它们的天然来源提供了高生物相容性,低免疫原性,增强循环稳定性,并逃避免疫清除。此外,表面整合素、四联蛋白和粘附分子的存在赋予电动汽车内在的靶向能力,使其能够与受体细胞选择性相互作用。除了作为生物信使的作用,越来越多的证据表明,EVs在调节关键的生理和病理过程中发挥积极作用,包括肿瘤微环境中的血管生成、肿瘤侵袭、转移、免疫调节和炎症反应。这些独特的特性使ev成为癌症治疗中靶向药物递送的天然纳米载体,特别是在提高抗癌药物的生物利用度、稳定性和治疗指数方面。本文综述了EV的生物发生、分离和表征方法、载货多样性、药物装载策略和靶向方法,重点介绍了EV作为天然纳米载体在癌症治疗中的应用。本文还讨论了当前与可扩展性、标准化和临床转化相关的挑战,强调了将基于ev的系统集成到下一代肿瘤治疗中的未来方向。
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引用次数: 0
Quality by design of ultra deformable nanovesicles loaded with flunarizine for brain targeting utilizing risk assessment and multivariate analytical methods 利用风险评估和多变量分析方法,设计装载氟桂利嗪的超可变形纳米囊泡用于脑靶向
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-12 DOI: 10.1016/j.onano.2025.100265
Mahmood A. Haiss, Shaimaa N. Abd Alhammid
The swiftly changing technological and regulatory environments in the development of pharmaceutical drugs require risk based approach that integrates multivariate analysis utilizing Quality by Design (QbD). Flunarizine, a poorly water-soluble calcium channel blocker utilized for migraine treatment, exhibits low bioavailability. Spanlastics, contemporary nonionic based surfactant nanovesicles, enhance medication penetration due to their fluidic nature. Consequently, we optimized flunarizine spanlastic nanovesicles (FNZ-SNVs) utilizing formulation by design principles and investigated the viability of nose-to-brain delivery for migraine management. Ishikawa diagram was utilized to identify the risk factors that may affect the critical quality attributes of FNZ-SNVs. The use of Plackett–Burman experimental design was employed to test eight distinct formula and process factors affecting vesicle size, zeta potential, vesicle deformability, and encapsulation efficiency. Utilizing Pareto charts, three critical parameters were identified: type of vesicle builder (Span 60), type of EA (Tween 60), and sonication duration. Three levels of these essential factors were tuned by formulation by design to minimize vesicle size and enhance encapsulation efficiency, and vesicle deformability of FNZ-SNVs. The optimized FNZ-SNVs exhibited a vesicle size of 95.5 nm, an encapsulation efficiency of 86%, a relative deformability of 4.8 minutes, and a dissolving efficiency of 90.2%. Consequently, the optimized formula was integrated into an insitu-gel (IG) and investigated for additional in vivo assessment, which demonstrated that the degree of FNZ-SIG intranasal delivered to the brain was significantly greater than that of the intravenous FNZ solution, exhibiting an exceptionally elevated drug targeting index (DTI) of 1.12 and (DTE%) 112.1. This study illustrates the successful implementation of risk management and Quality by Design (QbD) methodologies in the formulation of brain-targeting release of FNZ-SIGs.
药物开发中快速变化的技术和监管环境需要基于风险的方法,利用设计质量(QbD)集成多变量分析。氟桂利嗪是一种水溶性差的钙通道阻滞剂,用于偏头痛治疗,生物利用度低。西班牙塑料,当代非离子基表面活性剂纳米囊泡,由于其流体性质,增强药物渗透。因此,我们根据设计原则优化了氟桂利嗪弹性纳米囊泡(FNZ-SNVs)的配方,并研究了鼻到脑给药治疗偏头痛的可行性。石川图用于识别可能影响fnz - snv关键质量属性的风险因素。采用Plackett-Burman实验设计,考察8种不同的配方和工艺因素对囊泡大小、zeta电位、囊泡变形能力和包封效率的影响。利用帕累托图,确定了三个关键参数:囊泡构建器类型(Span 60), EA类型(Tween 60)和超声持续时间。通过配方设计调整这三个关键因素的水平,以减小fnz - snv的囊泡大小,提高囊泡的包封效率和囊泡变形能力。优化后的fnz - snv囊泡尺寸为95.5 nm,包封效率为86%,相对变形率为4.8 min,溶解效率为90.2%。因此,我们将优化后的配方整合到注射凝胶(IG)中,并进行了进一步的体内评估,结果表明,FNZ- sig经鼻给药到脑的程度显著高于静脉给药,药物靶向指数(DTI)异常升高,分别为1.12和112.1。本研究说明了风险管理和设计质量(QbD)方法在fnz - sig脑靶向释放制定中的成功实施。
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引用次数: 0
Recent advancements in drug nanocrystals: Innovation in formulation and drug delivery 药物纳米晶体的最新进展:配方和给药的创新
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-12-11 DOI: 10.1016/j.onano.2025.100277
Karan Vishwakarma , Preha Handa , Wena Shafeeq Tawfeeq , Mohammed Ahmed Hassan
Drug nanocrystals typically range in size smaller than 100 nm and have been used to enhance the solubility and bioavailability of various poorly water-soluble drugs, also enabling controlled release and specific drug delivery. They present several advantages, including high drug loading capacity and rapid dissolution, leading to quick absorption. Recent advances in the manufacturing of nanocrystals have emerged beyond traditional bottom-up and top-down methods. However, they have limitations, such as poor stability and safety concerns, that still need to be further explored. This review not only summarizes nanocrystal production and applications but also critically evaluates translational challenges, regulatory complexities, and emerging tools such as AI-enabled formulation design and personalized nanomedicine. Hence, this review will provide a detailed explanation of the various modifications carried out in the process of manufacturing drug nanocrystals, with their characterization and applications in drug delivery.
药物纳米晶体的尺寸通常小于100纳米,可用于提高各种水溶性差药物的溶解度和生物利用度,还可实现控释和特异性药物递送。它们有几个优点,包括高载药量和快速溶解,导致快速吸收。纳米晶体制造的最新进展已经超越了传统的自下而上和自上而下的方法。然而,它们也有局限性,比如稳定性差和安全问题,这些仍需要进一步探索。这篇综述不仅总结了纳米晶体的生产和应用,而且批判性地评估了转化挑战、监管复杂性和新兴工具,如人工智能支持的配方设计和个性化纳米医学。因此,本文将详细介绍在制造药物纳米晶体过程中进行的各种修饰,以及它们的表征和在药物传递中的应用。
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引用次数: 0
Hydrogel film-forming spray formulation containing propolis-based nanostructured lipid carriers of α-mangostin for diabetic wound repair 含蜂胶纳米结构α-山竹苷脂质载体的水凝胶成膜喷雾剂用于糖尿病创面修复
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-12-08 DOI: 10.1016/j.onano.2025.100275
Cecep Suhandi , Gofarana Wilar , Ahmed Fouad Abdelwahab Mohammed , Muchtaridi Muchtaridi , Shaharum Shamsuddin , Sabreena Safuan , Ronny Lesmana , Nurhasni Hasan , Khaled M. Elamin , Nasrul Wathoni
Diabetic wounds are difficult to treat due to persistent inflammation, delayed tissue repair, and high susceptibility to infection. α-Mangostin (αM), a xanthone with strong anti-inflammatory and wound-healing properties, shows improved solubility and therapeutic performance when encapsulated in propolis-based nanostructured lipid carriers (Nanopropolis-αM). Incorporating these nanoparticles into a hydrogel film-forming spray (HFFS) offers uniform application and sustained delivery. This study aimed to formulate, characterize, and evaluate an αM-loaded propolis-based NLC HFFS (HFFS-Nanopropolis-αM). The spray was prepared using chitosan, Carbopol 940, and sodium carboxymethyl cellulose. Physicochemical evaluations included pH, viscosity, spray angle, weight uniformity, particle size, zeta potential, and entrapment efficiency. The optimized formulation also underwent TEM imaging, in vitro release testing, cytocompatibility assessment using the WST-8 assay in NIH-3T3 cells, and 14-day in vivo wound-healing studies in alloxan-induced diabetic mice. The optimal HFFS containing 0.1 % Carbopol 940 exhibited suitable pH (7.30 ± 0.01), viscosity (19.97 ± 2.12 mPa.s), spray angle (62.02 ± 3.83°), film formation time (113.000 ± 11.372 s), particle size (85.17 ± 2.55 nm), zeta potential (−13.90 ± 2.18 mV), and entrapment efficiency (91.31 ± 0.58 %). It showed good 28-day stability and followed Higuchi release kinetics (R² = 0.998). Cytocompatibility was acceptable at experimentally testable concentrations, and the viability value at the intended dose reflects a modeled estimate due to assay dilution limits. In vivo, HFFS-Nanopropolis-αM significantly accelerated wound closure (99.53 ± 1.04 %) compared with silver sulfadiazine (89.24 ± 3.04 %, p < 0.01), supported by improved histological regeneration. Overall, the formulation demonstrates strong promise for diabetic wound management.
糖尿病伤口由于持续的炎症、延迟的组织修复和对感染的高易感性而难以治疗。α-山竹苷(αM)是一种具有较强抗炎和创面愈合性能的山竹酮,被包裹在基于蜂胶的纳米结构脂质载体(纳米蜂胶-αM)中,可以改善其溶解性和治疗性能。将这些纳米颗粒结合到水凝胶成膜喷雾(HFFS)中可以提供均匀的应用和持续的递送。本研究旨在制备、表征和评价一种负载α m的新型纳米蜂胶HFFS (HFFS- nanopropolis -αM)。以壳聚糖、卡波波尔940和羧甲基纤维素钠为原料制备喷雾。物理化学评价包括pH值、粘度、喷雾角度、重量均匀性、粒径、zeta电位和捕获效率。对优化后的配方进行了TEM成像、体外释放测试、NIH-3T3细胞WST-8细胞相容性评估以及四氧嘧啶诱导的糖尿病小鼠体内14天的伤口愈合研究。含0.1%卡波波尔940的最佳HFFS pH值为7.30±0.01,粘度为19.97±2.12 mPa。s)、喷涂角度(62.02±3.83°)、成膜时间(113.000±11.372 s)、粒径(85.17±2.55 nm)、zeta电位(−13.90±2.18 mV)、包封效率(91.31±0.58%)。28 d稳定性良好,符合Higuchi释放动力学(R²= 0.998)。在实验可测试的浓度下,细胞相容性是可接受的,并且在预期剂量下的活力值反映了由于测定稀释限制而建立的模型估计。在体内,与磺胺嘧啶银(89.24±3.04%,p < 0.01)相比,hffs - nano蜂胶-αM显著加速伤口愈合(99.53±1.04%),这是由于组织再生的改善。总体而言,该配方显示出糖尿病伤口管理的强大前景。
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引用次数: 0
Dual mechanistic approach utilizing pH- and time- responsive bromelain laden polymeric nanoparticles for colon cancer management 双重机制的方法利用pH和时间响应菠萝蛋白酶负载聚合物纳米颗粒结肠癌的管理
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-26 DOI: 10.1016/j.onano.2025.100272
Manu Sharma, Namita Badoniya
Emerging evidences confirming bromelain’s potential to induce apoptosis and inhibit tumor progression highlights its prospective as adjunctive therapeutic in colorectal cancer malignancies. Despite, high oral doses coupled with poor bioavailability remarkably limits bromelain’s clinical utility, underscoring the necessity of use of innovative delivery strategies. Therefore, the current invention was designed to develop dual pH- and time-responsive bromelain-loaded nanoformulation (Br-PNPs) for controlled and precise delivery to colon with high drug loading capacity and enhanced therapeutic efficacy. pH responsive spherical shaped mucoadhesive nanosized (89.02±6.23 nm) Br-PNPs underscores their potential of minimizing gastric exposure while swelling and mucoadhesivity assured sustained release in colon. Lower IC50 (16.25µg/ml) along with enhanced colon drug concentration attained by Br-PNPs assured their effective colon targeting potential. Br-PNPs significantly reduced disease activity index, tumor burden, aberrant crypt foci and hyperplastic lesions in colon alongside oxidative stress and immunological biomarkers in chemically induced colon cancer model (DMH+DSS) in Wistar rat. The preclinical findings suggested that Br-PNPs have opened up new horizons for establishment of promising contender for colon cancer management in near future.
新出现的证据证实菠萝蛋白酶具有诱导细胞凋亡和抑制肿瘤进展的潜力,这突出了其作为结直肠癌恶性肿瘤辅助治疗的前景。尽管如此,高口服剂量加上较差的生物利用度显著限制了菠萝蛋白酶的临床应用,强调了使用创新给药策略的必要性。因此,本发明旨在开发双重pH和时间响应的菠萝蛋白酶负载纳米制剂(Br-PNPs),以控制和精确地递送到结肠,具有高载药能力和增强的治疗效果。pH响应球形黏附纳米Br-PNPs(89.02±6.23 nm)强调了它们在减少胃暴露的同时肿胀和黏附确保在结肠中持续释放的潜力。Br-PNPs具有较低的IC50(16.25µg/ml)和较高的结肠药物浓度,确保了其有效的结肠靶向潜力。在化学诱导结肠癌模型(DMH+DSS)中,Br-PNPs显著降低Wistar大鼠的疾病活动指数、肿瘤负担、异常隐窝灶和结肠增殖性病变,以及氧化应激和免疫生物标志物。临床前研究结果表明,Br-PNPs为在不久的将来建立有希望的结肠癌治疗竞争者开辟了新的视野。
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引用次数: 0
Diosgenin-functionalized zinc oxide nanoparticles produced using Hibiscus tiliaceus leaf extract: evaluation of anticancer and antibacterial activities 用芙蓉叶提取物制备的薯蓣皂苷元功能化氧化锌纳米颗粒:抗癌和抗菌活性的评价
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-28 DOI: 10.1016/j.onano.2025.100274
Oktavina Kartika Putri , Dewi Wulansari , Arif Fadlan , Mardi Santoso , Hesti Lina Wiraswati , Yuly Kusumawati
Diosgenin is a potentially safer treatment for breast cancer. ZnO nanoparticles (ZnONPs) can overcome their limited water solubility. This study was undertaken to prepare and characterize ZnONPs and ZnONP@dios (ZnONPs loaded with diosgenin), to examine their cytotoxicity against MCF-7 (breast cancer cells), and to test their antimicrobial activity against Escherichia coli and Staphylococcus aureus. The research began with the phyto-production of ZnONPs using Hibiscus tiliaceus leaf extract media, followed by the preparation of ZnONP@dios. X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and UV–Vis diffuse reflectance spectroscopy (DRS) were performed for the characterization of the nanoparticles. The cytotoxic response induced by ZnONPs and ZnONP@dios was analyzed using the 3-(4,5-dimethyl-diazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The agar well diffusion method was utilized to assess antibacterial activity. The ZnONPs were highly pure and revealed hexagonal and rod-shaped appearances, with nanoscale sizes (45–125 nm). FTIR analysis confirmed the successful preparation of ZnONP@dios, as evidenced by the distinct absorption band at 1570 cm⁻¹, while TEM images revealed a thin coating layer surrounding the ZnONPs. Cytotoxicity assays against MCF-7 cells showed dose-dependent inhibition, with diosgenin-functionalized composites demonstrating greater potency. ZnONPsMA@dios (ZnONPs derived from H. tiliaceus methanol extract, with zinc acetate precursor and loaded with diosgenin) exhibited the most substantial effect (reducing its IC₅₀ from 48.2 to 37.2 µg/mL). Similarly, diosgenin loading improved the activity of ZnONPs1:1 N (ZnONPs derived from H. tiliaceus water:ethanol 1:1 (v/v) extract, zinc nitrate precursor), reducing its IC₅₀ from 98.8 to 46.7 µg/mL. The inhibition zones against E. coli were 13, 14, 16, 14, 12, and 11 mm for ZnONPsMA (ZnONPs derived from H. tiliaceus methanol extract, zinc acetate precursor), ZnONPMA@dios, ZnONPs1:1 N, ZnONP1:1N@dios (ZnONPs derived from H. tiliaceus water: ethanol of 1:1 (v/v) extract, zinc nitrate precursor and loaded with diosgenin), ZnOcom (commercial ZnO), and ZnOcom@dios (commercial ZnO loaded with diosgenin), respectively. In the case of S. aureus, no inhibition zone was observed. These findings highlight that diosgenin-functionalized ZnONPs can enhance anticancer efficacy. All types of ZnONPs and ZnONP@dios have potential as antibacterial agents against E. coli, but were ineffective against S. aureus.
薯蓣皂苷元可能是一种更安全的乳腺癌治疗方法。ZnO纳米颗粒(ZnONPs)可以克服其有限的水溶性。本研究对ZnONPs和ZnONP@dios(负载薯蓣皂苷元的ZnONPs)进行了制备和表征,并检测了它们对MCF-7(乳腺癌细胞)的细胞毒性,以及对大肠杆菌和金黄色葡萄球菌的抗菌活性。本研究首先以木槿叶提取物为培养基,制备ZnONPs,然后制备ZnONP@dios。采用x射线衍射(XRD)、傅里叶变换红外光谱(FTIR)、扫描电子显微镜(SEM)和紫外可见漫反射光谱(DRS)对纳米颗粒进行表征。采用3-(4,5-二甲基-二唑-2-基)-2,5-二苯基溴化四唑(MTT)法分析ZnONPs和ZnONP@dios诱导的细胞毒性反应。采用琼脂孔扩散法测定其抑菌活性。ZnONPs纯度高,呈六边形和棒状,尺寸为纳米级(45-125 nm)。FTIR分析证实了ZnONP@dios的成功制备,在1570 cm(⁻¹)处有明显的吸收带,而TEM图像显示ZnONPs周围有一层薄薄的涂层。对MCF-7细胞的细胞毒性试验显示出剂量依赖性抑制,薯蓣皂苷元功能化复合物显示出更大的效力。ZnONPsMA@dios (ZnONPs源自H. tiliaceus甲醇提取物,带有乙酸锌前体并装载薯蓣皂苷元)表现出最显著的效果(将其IC₅0从48.2降至37.2µg/mL)。同样,薯蓣皂苷元负载提高了ZnONPs1:1 N (ZnONPs源自H. tiliaceus水:乙醇1:1 (v/v)提取物,硝酸锌前体)的活性,将其IC₅0从98.8降低到46.7µg/mL。ZnONPsMA(紫丁香甲醇提取物、醋酸锌前体)、ZnONPMA@dios、znonps1∶1N、ZnONP1∶1N@dios(紫丁香水:1:1 (v/v)乙醇提取物、硝酸锌前体和负载薯蓣皂苷元)、ZnOcom(商用氧化锌)和ZnOcom@dios(负载薯蓣皂苷元的商用氧化锌)对大肠杆菌的抑制区分别为13、14、16、14、12和11 mm。在金黄色葡萄球菌的情况下,没有观察到抑制带。这些发现表明薯蓣皂苷元功能化的ZnONPs可以增强抗癌效果。所有类型的ZnONPs和ZnONP@dios对大肠杆菌具有潜在的抗菌作用,但对金黄色葡萄球菌无效。
{"title":"Diosgenin-functionalized zinc oxide nanoparticles produced using Hibiscus tiliaceus leaf extract: evaluation of anticancer and antibacterial activities","authors":"Oktavina Kartika Putri ,&nbsp;Dewi Wulansari ,&nbsp;Arif Fadlan ,&nbsp;Mardi Santoso ,&nbsp;Hesti Lina Wiraswati ,&nbsp;Yuly Kusumawati","doi":"10.1016/j.onano.2025.100274","DOIUrl":"10.1016/j.onano.2025.100274","url":null,"abstract":"<div><div>Diosgenin is a potentially safer treatment for breast cancer. ZnO nanoparticles (ZnO<img>NPs) can overcome their limited water solubility. This study was undertaken to prepare and characterize ZnO<img>NPs and ZnO<img>NP@dios (ZnO<img>NPs loaded with diosgenin), to examine their cytotoxicity against MCF-7 (breast cancer cells), and to test their antimicrobial activity against <em>Escherichia coli</em> and <em>Staphylococcus aureus</em>. The research began with the phyto-production of ZnO<img>NPs using <em>Hibiscus tiliaceus</em> leaf extract media, followed by the preparation of ZnO<img>NP@dios. X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and UV–Vis diffuse reflectance spectroscopy (DRS) were performed for the characterization of the nanoparticles. The cytotoxic response induced by ZnO<img>NPs and ZnO<img>NP@dios was analyzed using the 3-(4,5-dimethyl-diazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The agar well diffusion method was utilized to assess antibacterial activity. The ZnO<img>NPs were highly pure and revealed hexagonal and rod-shaped appearances, with nanoscale sizes (45–125 nm). FTIR analysis confirmed the successful preparation of ZnO<img>NP@dios, as evidenced by the distinct absorption band at 1570 cm⁻¹, while TEM images revealed a thin coating layer surrounding the ZnO<img>NPs. Cytotoxicity assays against MCF-7 cells showed dose-dependent inhibition, with diosgenin-functionalized composites demonstrating greater potency. ZnO<img>NPs<sub>MA</sub>@dios (ZnO<img>NPs derived from <em>H. tiliaceus</em> methanol extract, with zinc acetate precursor and loaded with diosgenin) exhibited the most substantial effect (reducing its IC₅₀ from 48.2 to 37.2 µg/mL). Similarly, diosgenin loading improved the activity of ZnO<img>NPs<sub>1:1</sub> <sub>N</sub> (ZnO<img>NPs derived from <em>H. tiliaceus</em> water:ethanol 1:1 (v/v) extract, zinc nitrate precursor), reducing its IC₅₀ from 98.8 to 46.7 µg/mL. The inhibition zones against <em>E. coli</em> were 13, 14, 16, 14, 12, and 11 mm for ZnO<img>NPs<sub>MA</sub> (ZnO<img>NPs derived from <em>H. tiliaceus</em> methanol extract, zinc acetate precursor), ZnO<img>NP<sub>MA</sub>@dios, ZnO<img>NPs<sub>1:1</sub> <sub>N</sub>, ZnO<img>NP<sub>1:1N</sub>@dios (ZnO<img>NPs derived from <em>H. tiliaceus</em> water: ethanol of 1:1 (v/v) extract, zinc nitrate precursor and loaded with diosgenin), ZnO<sub>com</sub> (commercial ZnO), and ZnO<sub>com</sub>@dios (commercial ZnO loaded with diosgenin), respectively. In the case of <em>S. aureus</em>, no inhibition zone was observed. These findings highlight that diosgenin-functionalized ZnO<img>NPs can enhance anticancer efficacy. All types of ZnO<img>NPs and ZnO<img>NP@dios have potential as antibacterial agents against <em>E. coli,</em> but were ineffective against <em>S. aureus</em>.</div></div>","PeriodicalId":37785,"journal":{"name":"OpenNano","volume":"27 ","pages":"Article 100274"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145691259","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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 characterization of dolutegravir sodium-loaded nanostructured lipid carrier in situ gel for targeted brain delivery via intranasal route dolute重力韦钠负载纳米结构脂质载体原位凝胶的制备和表征
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-20 DOI: 10.1016/j.onano.2025.100270
Salam Shanta Taher, Khalid K. Al-Kinani
Effective delivery of antiretroviral drugs to the brain is a major hurdle in treating central nervous system (CNS) HIV infections. This study developed an intranasal in situ gel containing dolutegravir sodium-loaded nanostructured lipid carriers (DTGs-NLCs) for targeted nose-to-brain delivery. DTGs-NLCs were prepared using a modified melt emulsification-ultrasonication method, yielding nanocarriers with a size of 80.8 ± 10.4 nm, zeta potential of –13±1.4 mV, and entrapment efficiency of 80.7 ± 0.48 %. These NLCs were incorporated into a thermosensitive in situ gel matrix composed of poloxamer 407 and carbopol 934P. The in vitro drug release from the gel was significantly enhanced compared to the free drug (p < 0.05). Rheological studies confirmed the formulation’s non-Newtonian behavior, good spreadability (5.9 ± 0.13 cm), and strong mucoadhesiveness (1116.86 ± 20 dyne/cm²). Safety evaluations demonstrated excellent hemocompatibility and biocompatibility. Pharmacokinetic studies revealed that intranasal administration achieved higher brain concentrations (Cmax: 35.4 ± 3.6 µg/g; AUC₀–₄₈: 193.22±14.66 µg·h/g) and faster absorption (Tmax: 1 h) than intravenous delivery. These results indicate that the DTGs-NLC in situ gel offers a safe, non-invasive, and efficient approach for enhanced brain targeting, showing great promise for treating CNS complications of HIV, including neuroAIDS.
有效地将抗逆转录病毒药物输送到大脑是治疗中枢神经系统(CNS) HIV感染的主要障碍。本研究开发了一种含多替重力韦钠负载纳米结构脂质载体(DTGs-NLCs)的鼻内原位凝胶,用于靶向鼻至脑递送。采用改进的熔融乳化-超声法制备了DTGs-NLCs,得到的纳米载体尺寸为80.8±10.4 nm, zeta电位为-13±1.4 mV,包封效率为80.7±0.48%。这些NLCs被掺入由poloxam407和carbopol 934P组成的热敏原位凝胶基质中。与游离药物相比,凝胶的体外药物释放明显增强(p < 0.05)。流变学研究证实了该配方具有非牛顿力学性质,良好的涂覆性(5.9±0.13 cm)和较强的黏附性(1116.86±20达因/cm²)。安全性评价显示其具有良好的血液相容性和生物相容性。药代动力学研究表明,与静脉给药相比,鼻内给药具有更高的脑浓度(Cmax: 35.4±3.6µg/g; AUC₀-₄₈:193.22±14.66µg·h/g)和更快的吸收(Tmax: 1 h)。这些结果表明,DTGs-NLC原位凝胶为增强脑靶向提供了一种安全、无创、有效的方法,在治疗包括神经艾滋病在内的HIV中枢神经系统并发症方面显示出巨大的希望。
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引用次数: 0
Snail-collagen/chitosan nanocomposite film with silver nanoparticles for antimicrobial and regenerative wound healing 蜗牛-胶原/壳聚糖纳米复合膜与银纳米粒子抗菌和再生伤口愈合
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-11 DOI: 10.1016/j.onano.2025.100264
Dina Mohamed Mahmoud , Mohamed Mahmoud Abdelfatah , Tamer Mohamed Mahmoud , Omiya Ali Hasan , Randa Mohammed Zaki , Obaid Afzal , Mostafa Asim Darwish , Mohamed G. Ewees , Mostafa Nasr Taha , Mahmoud Mohamed Omar
Infected wounds pose a significant clinical challenge, driving the need for advanced dressings that actively combat infection and promote healing. This study developed a novel bio-composite film by integrating silver nanoparticle-enhanced, metronidazole-loaded lipidic nanovesicles into a snail slime collagen-chitosan matrix. A Design of Experiment optimized lipidic nanovesicle formulation (loaded with metronidazole) (Lop) was fabricated and characterized (DLS, drug release). Silver nanoparticles (AgNPs) were incorporated to form optimized nanovesicle formulation incorporating Silver Nanoparticles (Lop-AgNPs), which were embedded into a snail slime collagen (SSC)-chitosan (CS) matrix to create the final Lop.M film (optimized bio-composite film (Lop-AgNPs in a Snail Slime Collagen-Chitosan matrix). The film was tested for physicochemical properties, antimicrobial activity (disc diffusion), and efficacy in a rat wound model. The optimized formulation (Lop) showed a vesicle size of 339.5 ± 3.1 nm, zeta potential of -58.2 ± 2.8 mV, and entrapment efficiency of 88.6 ± 4.5% w/w, with 45.9 ± 3.2% w/w cumulative metronidazole release after 4 h. Upon silver incorporation, vesicle size increased to 358.9 ± 5.7 nm and zeta potential to -62.1 ± 3.2 mV. The composite film (Lop.M) exhibited a swelling index (SI) of 18.2 ± 0.4% w/w, film thickness of 0.71 ± 0.05 mm, and folding endurance > 50 folds. Antimicrobial zones of inhibition reached 50 mm for P. aeruginosa and 45 mm for Escherichia coli. In vivo, Lop.M-treated wounds demonstrated 96.4 ± 2.3% closure by day 14 compared to 68.1 ± 3.8% in controls. The Lop.M film, which demonstrated 96.4% wound closure in 14 days and potent antimicrobial activity, presents a strategy for wound management that combines robust antimicrobial action with active promotion of tissue regeneration.
感染的伤口是一个重大的临床挑战,推动需要先进的敷料,积极对抗感染和促进愈合。本研究通过将纳米银粒子增强、甲硝唑负载的脂质纳米囊泡整合到蜗牛黏液胶原-壳聚糖基质中,开发了一种新型生物复合膜。制备了含甲硝唑(Lop)的脂质纳米囊泡配方,并对其进行了表征(DLS,药物释放)。将银纳米颗粒(Lop-AgNPs)包埋在蜗牛黏液胶原蛋白(SSC)-壳聚糖(CS)基质中,形成最终的Lop纳米囊泡。M膜(优化的生物复合膜(蜗牛黏液胶原-壳聚糖基质中的Lop-AgNPs)。在大鼠伤口模型中测试了该膜的理化性质、抗菌活性(圆盘扩散)和功效。最佳配方(Lop)的囊泡大小为339.5±3.1 nm, zeta电位为-58.2±2.8 mV,包封效率为88.6±4.5% w/w, 4 h后甲硝唑的累积释放量为45.9±3.2% w/w。加入银后,囊泡大小增加至358.9±5.7 nm, zeta电位为-62.1±3.2 mV。复合膜(lopm)的膨胀指数(SI)为18.2±0.4% w/w,膜厚为0.71±0.05 mm,可折叠50次。铜绿假单胞菌和大肠杆菌的抑菌区分别为50 mm和45 mm。在体内,Lop。m治疗的伤口在第14天愈合率为96.4±2.3%,而对照组为68.1±3.8%。垂下的。M膜在14天内显示出96.4%的伤口愈合和有效的抗菌活性,提出了一种将强大的抗菌作用与积极促进组织再生相结合的伤口管理策略。
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