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Response surface methodology - optimized niosomes encapsulating whole tomato extract: Release profile and mechanistic insights for UVB protection and anti-melanogenesis applications 响应面方法-优化的包封整个番茄提取物的囊体:释放剖面和对UVB保护和抗黑素生成应用的机制见解
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-20 DOI: 10.1016/j.onano.2025.100267
Nattawadee Kanpipit , Sakornchon Mattariganont , Likit Temprom , Prutchayawoot Thopan , Khomsorn Lomthaisong , Sriprajak Krongsuk , Suthasinee Thapphasaraphong
This study presents the development and characterization of a novel niosome delivery system incorporating whole tomato extract for topical application. The formulation was optimized using a Box–Behnken design (BBD) by response surface methodology (RSM) to achieve high entrapment efficiency, small vesicle size, and low polydispersity index (PDI). The optimal formulation (2 mM Span 60, 1 mM cholesterol, 1 % extract) yielded an entrapment efficiency of 90.34 %, particle size of 222.06 nm, and PDI of 0.34. Fourier transform infrared spectroscopy (FTIR) and transmission electron microscopy (TEM) analyses confirmed successful encapsulation and nanoscale spherical morphology. In vitro release studies demonstrated distinct kinetic behaviors: the whole extract followed Higuchi model, while lycopene exhibited zero-order model. The optimized tomato extract–loaded niosomes (TNS) exhibited enhanced stability and demonstrated significant biological activity, including ultraviolet ̶ B (UVB) protection in immortalized human keratinocyte cell lines (HaCaT) and anti-melanogenic effects in murine melanoma cell lines (B16F10). Notably, tomato extract–loaded niosomes (TNS) significantly downregulated the expression of melanogenesis-related proteins, microphthalmia-associated transcription factor (MITF) and tyrosinase, as confirmed by Western blot analysis. These findings support the potential use of tomato extract-loaded niosomes (TNS) as multifunctional cosmetic ingredients for photoprotection and skin whitening applications.
本研究提出了一种新的niosome输送系统的发展和特性,该系统包含全番茄提取物用于局部应用。采用响应面法(RSM)对该配方进行Box-Behnken设计(BBD)优化,以获得高捕获效率、小囊泡尺寸和低多分散性指数(PDI)。最佳配方(2 mM Span 60, 1 mM胆固醇,1%提取物)的包封效率为90.34%,粒径为222.06 nm, PDI为0.34。傅里叶变换红外光谱(FTIR)和透射电子显微镜(TEM)分析证实了成功的封装和纳米级球形形貌。体外释放研究显示了不同的动力学行为:整个提取物符合Higuchi模型,而番茄红素则符合零级模型。优化后的番茄提取物负载niosomes (TNS)表现出更高的稳定性和显著的生物活性,包括对永生化人角质形成细胞系(HaCaT)的紫外线B (UVB)保护和对小鼠黑色素瘤细胞系(B16F10)的抗黑素生成作用。值得注意的是,经Western blot分析证实,番茄提取物装载的niosomes (TNS)显著下调了黑色素生成相关蛋白、小眼相关转录因子(MITF)和酪氨酸酶的表达。这些发现支持了番茄提取物负载niosomes (TNS)作为光保护和皮肤美白的多功能化妆品成分的潜在用途。
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引用次数: 0
Exploring the Therapeutic Potential of Green-fabricated CRL-AgNPs from Catharanthus roseus 红花绿色合成CRL-AgNPs的治疗潜力探讨
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-12-20 DOI: 10.1016/j.onano.2025.100278
Rokshana Ara Ruhi , Sk. Md. Atiqur Rahman , Mobasshir Noor Shehab , Md. Roqunuzzaman , Mohammad Saiful Islam , Md. Ragib Shariar , Md. Mahmudul Hasan Maruf , Firoz Ahmed , M Ahasanur Rabbi , Syed Rashel Kabir , Ananda Kumar Saha , Md. Anwarul Kabir Bhuiya , Md. Abu Reza
Despite the promise of green nanotechnology, the synthesis reproducibility with consistent pharmacological activity remains the key challenge. Therefore, the current project aimed to biosynthesize AgNPs using aqueous leaf extract of Catharanthus roseus as a reducing and capping agent to discover novel therapeutic leads. To attain this target, synthesis of C. roseus leaf-mediated AgNPs (CRL-AgNPs) was optimized using a 24 full factorial design, which yielded a highly significant and predictive statistical model. CRL-AgNPs synthesis was confirmed through chromism and UV-Vis spectroscopy. Further characterization by DLS, XRD, FTIR, FE-SEM, and EDX revealed an average particle size of 55.78±13.2 nm with high colloidal stability, scoring a zeta-potential of -54.5±0.57 mV. EDX study validated the elemental composition of synthesized CRL-AgNPs, demonstrating that a strong silver signal accounted for 84.09% of the weight. Cytotoxicity assessments using the MTT assay revealed a dose-dependent inhibition of MCF-7 breast cancer cell proliferation, with an IC50 value of 8.033μg/mL, indicating their potent anticancer activity. Furthermore, their anti-proliferative efficacy was validated in vivo on EAC cells bearing a mouse model, demonstrating that intra-peritoneal administration of CRL-AgNPs significantly reduced cancer cell growth by 63.20%. Apoptosis was ascertained by nuclear staining and gene expression, with upregulation of p53 and BAX and downregulation of Bcl2 and NF-κβ. Histopathology confirmed selective tissue protection for vital organs in treated mice. Therefore, these findings establish CRL-AgNPs as a sustainable, reproducible, and mechanistically validated nanoparticle that integrates green chemistry with functional biomaterials design, advancing the translational nanotherapeutic development.
尽管绿色纳米技术前景光明,但具有一致药理活性的合成可重复性仍然是关键的挑战。因此,本项目旨在利用花楸叶水提物作为还原和封盖剂生物合成AgNPs,以发现新的治疗线索。为了实现这一目标,采用24全因子设计优化了玫瑰叶介导的AgNPs (CRL-AgNPs)的合成,得到了一个高度显著和预测的统计模型。通过显色性和紫外-可见光谱证实了CRL-AgNPs的合成。进一步通过DLS、XRD、FTIR、FE-SEM和EDX等表征表明,该材料的平均粒径为55.78±13.2 nm,具有较高的胶体稳定性,ζ电位为-54.5±0.57 mV。EDX研究验证了合成的CRL-AgNPs的元素组成,表明强银信号占重量的84.09%。MTT法细胞毒性评估显示MCF-7对乳腺癌细胞增殖的抑制作用呈剂量依赖性,IC50值为8.033μg/mL,表明其具有较强的抗癌活性。此外,在小鼠EAC细胞模型上验证了它们的抗增殖作用,结果表明,腹膜内给药CRL-AgNPs可显著降低癌细胞生长63.20%。通过核染色和基因表达确定细胞凋亡,p53和BAX上调,Bcl2和NF-κβ下调。组织病理学证实了对小鼠重要器官的选择性组织保护。因此,这些发现确立了CRL-AgNPs是一种可持续的、可重复的、机械验证的纳米颗粒,它将绿色化学与功能性生物材料设计相结合,推动了转化纳米治疗的发展。
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引用次数: 0
Green-synthesized selenium nanoparticles overcoming methotrexate resistance in colorectal cancer 绿色合成纳米硒克服了结直肠癌对甲氨蝶呤的耐药性
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-22 DOI: 10.1016/j.onano.2025.100269
Mohammed S. Saddik , Basima A.A. Saleem , Ali Khames , Ahmed Adel Alaa-Eldin , Mohamed Ahmed , Hesham.A. Eliwa , Mostafa F. Al-Hakkani , Ahmed M. Ashour , Hamada Hashem , Mohamad A. Ismail , Amany A. Abdel-Rheem

Objective

Colorectal cancer (CRC) therapy with methotrexate (MTX) is limited by toxicity and resistance. This study developed eco-friendly selenium nanoparticles (SeNPs) to enhance MTX delivery and overcome resistance.

Methods

SeNPs were synthesized using a green reduction method and optimized via a Box–Behnken design. Characterization confirmed spherical nanoparticles with an average size of 20–30 nm. MTX loading efficiency (LE%) and release behavior were measured, and biological evaluation was conducted in HCT116 colorectal cancer cells through cytotoxicity, apoptosis (Annexin V/7-AAD), and efflux-transporter assays.

Results

Optimized SeNPs achieved an MTX loading efficiency of ≈48–52 %, with controlled early-phase release. MTX–SeNPs markedly enhanced cytotoxicity, reducing the IC₅₀ to 62.4 µg/mL, compared with 186.6 µg/mL for MTX alone—representing a ∼67 % reduction in required dose. Docking analysis showed selenium interacting with human glutathione reductase, supporting the observed increase in ROS and apoptosis.

Conclusions

Green-synthesized SeNPs significantly improve MTX efficacy by enhancing drug retention, suppressing efflux activity, and reducing resistance. These findings highlight MTX–SeNPs as a promising strategy for CRC treatment and justify further in vivo investigation.
目的甲氨蝶呤(MTX)治疗结直肠癌(CRC)存在一定的毒副作用和耐药性。本研究开发了生态友好的硒纳米颗粒(SeNPs)来增强MTX的递送和克服耐药性。方法采用绿色还原法合成senps,并采用Box-Behnken设计优化。表征证实了平均尺寸为20-30 nm的球形纳米颗粒。测定MTX的加载效率(LE%)和释放行为,并通过细胞毒性、凋亡(Annexin V/7-AAD)和外排转运体测定对HCT116结直肠癌细胞进行生物学评价。结果优化后的SeNPs的MTX加载效率为≈48 ~ 52%,早期释放可控。MTX - senps显着增强了细胞毒性,将IC₅0降低到62.4µg/mL,而单独使用MTX的IC₅0为186.6µg/mL,这意味着所需剂量减少了67%。对接分析显示,硒与人谷胱甘肽还原酶相互作用,支持观察到的ROS和细胞凋亡的增加。结论格林合成的SeNPs通过增强药物潴留、抑制外排活性、降低耐药,显著提高MTX的疗效。这些发现突出了MTX-SeNPs作为一种有前景的CRC治疗策略,并证明了进一步的体内研究的合理性。
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引用次数: 0
An overview of the alarming impediments encountered while establishing an apposite IVIVC of nanomedicines necessitated its regulatory approval 概述了在建立纳米药物的适当IVIVC时遇到的令人震惊的障碍,有必要批准其监管部门
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-22 DOI: 10.1016/j.onano.2025.100271
Nandakumar Selvasudha , Joseph Pushpa Sweety , Gover Antoniraj M , Kandasamy Ruckmani
<div><div>For the past three decades, the principle of nanotechnology has been widely employed to develop pharmaceuticals and bio-pharmaceuticals that are successful for many disease therapies. Several commercially available approved nanomedicines are more efficacious than conventional dosage forms and successfully manage many diseases. The patient's well-being and the certainty to resolve the unresolved challenges of medical science became realistic due to the advent of novel pharmaceutical products based on nanotechnology. These benefits are observed as in humans, the absorption profile of a drug fabricated into nanoparticles varies widely with that of its conventional dosage forms mainly due to the physicochemical modifications and results in highly deviating in-vitro and in-vivo data for the same drug when administered as nanoparticles. The researchers and regulators must frame new guidelines that guide the pharmaceutical industry to develop novel nanomedicines that conform to the desired safety and efficacy. The nanoparticles translational research conducted at the academic level is mainly developing, and the scale-up techniques of the clinically approved nanomedicines are yet to be optimized from the perspective of the manufacturer as well as the regulatory authorities. The IVIVC serves as a reference document that reinforces the pharmaceutical industries to substantiate and expedite the credentials of an oral dosage form about the New Drug Application (NDA), Abbreviated New Drug Application (ANDA), or Antibiotic Drug Application (AADA). A poor in-vitro in-vivo correlation (IVIVC) marks a constraint factor, which declines the clinical approval for nanomedicine and its commerce. As on date, neither any specific regulatory guidelines nor any specific calculation methods have been drafted that facilitate the determination of the IVIVC for nanomedicine. Most of the research scientists involved in developing nano/micro/macro formulations do not consider IVIVC an essential criterion. Therefore, a lag in assessing the formulation of assured quality for the next phase happens in the drug development cycle, which terminates the formulation mostly at its pilot scale rather than for its succession as a viable market product. In the pharmaceutical industries, the necessity for IVIVC has been expanded to a greater extent, and a strong IVIVC is recommended to approve the developed nanoformulations of poorly soluble drugs; thus, an appropriate IVIVC model shall be established to expedite the regulatory process for easy and rapid market approval of the developed nanomedicine.</div><div>The objective of the present review includes examining and considering the various associated factors involved in the development of an IVIVC model for nanomedicine, viz., Physico-chemical characteristics and bio-pharmaceutical factors (Formulation and physiological factors); to deliberate on the pros and cons of the various in-vitro dissolution study methods with due consid
在过去的三十年里,纳米技术的原理被广泛应用于开发药物和生物药物,这些药物和生物药物成功地治疗了许多疾病。几种市售的经批准的纳米药物比传统剂型更有效,并成功地治疗了许多疾病。由于基于纳米技术的新型医药产品的出现,病人的健康和解决医学未解决挑战的确定性变得现实。在人体中观察到这些益处,制成纳米颗粒的药物的吸收谱与其常规剂型的吸收谱差异很大,主要是由于物理化学修饰,并且当以纳米颗粒给药时,同一药物的体外和体内数据存在高度偏差。科学家和管理者必须制定新的指导方针,指导制药业开发符合预期安全性和有效性的新型纳米药物。学术层面的纳米颗粒转化研究主要处于发展阶段,临床批准的纳米药物的放大技术从生产企业和监管部门的角度来看都有待优化。IVIVC作为一份参考文件,加强制药行业证实和加快口服剂型关于新药申请(NDA)、简略新药申请(ANDA)或抗生素药物申请(AADA)的凭证。较差的体外体内相关性(IVIVC)是制约纳米药物临床批准和商业化的一个制约因素。迄今为止,还没有起草任何具体的监管指南或任何具体的计算方法来促进纳米药物IVIVC的确定。大多数参与开发纳米/微/宏观配方的研究科学家并不认为IVIVC是一个必要的标准。因此,在药物开发周期中,评估下一阶段质量有保证的配方会出现滞后,这主要是在其中试规模时终止配方,而不是在其作为可行市场产品的继承时终止配方。在制药行业,IVIVC的必要性已经扩大到更大的程度,并且建议使用强大的IVIVC来批准开发的难溶性药物的纳米配方;因此,应该建立一个合适的IVIVC模型,以加快监管过程,使所开发的纳米药物容易和快速地获得市场批准。本综述的目的包括审查和考虑纳米医学IVIVC模型开发中涉及的各种相关因素,即物理化学特性和生物制药因素(配方和生理因素);综合考虑各种体外溶出度研究方法的优缺点,并考虑受试者之间的差异,采用合适的方法准确预测体内吸收,以获得良好的IVIVC。这篇综述突出强调了与纳米药物监管批准相关的关键因素,并进一步探讨了遵守当前国际监管指南的各种研究工作。
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引用次数: 0
Nanodiagnostics and nanotoxicology: A systematic review and meta-analysis on nanoparticle applications and safety in metabolic organs 纳米诊断和纳米毒理学:纳米颗粒在代谢器官中的应用和安全性的系统综述和荟萃分析
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-11-19 DOI: 10.1016/j.onano.2025.100266
Sruti Murali , Jayamani Thomas , John Abraham , Vignesh Kanna , Sivaramakrishnan Ramachandiran , Suruthi SS

Background

Nanotechnology is reshaping the biomedical landscape by offering unprecedented capabilities in disease diagnostics, targeted therapy, and biosensing. Nanoparticles (NPs), owing to their unique physicochemical properties, enable ultra-sensitive biomarker detection, real-time monitoring, and minimally invasive assays across oncology, infectious diseases, and neurology. However, their biological interactions also raise significant concerns regarding organ-specific toxicity, particularly in metabolic systems.

Objective

This systematic review and meta-analysis aim to integrate current evidence on nanoparticle-based diagnostic applications with emerging insights into their toxicological impacts on key metabolic organs — liver, kidney, pancreas, spleen, and adipose tissue. It further examines mechanistic pathways, dose-dependent effects, and translational challenges to bridge the gap between innovation and biosafety.

Methods

A comprehensive literature search was conducted across PubMed, Scopus, Web of Science, and Google Scholar from January 2015 to October 2025 following PRISMA 2020 guidelines. Eligible studies reported quantitative diagnostic performance metrics (e.g., limit of detection, sensitivity, multiplexing capacity) or biological outcomes (e.g., oxidative stress, apoptosis, fibrosis, endocrine disruption) related to NP exposure. Meta-analytic synthesis was performed on 42 studies reporting comparable quantitative toxicity data.

Results

Diagnostic applications of metallic, polymeric, photonic, and hybrid nanoparticles demonstrated up to a 1000-fold improvement in sensitivity over conventional assays, with mean detection limits reaching the femtomolar range. However, pooled toxicity analysis revealed significant organ-specific risks: hepatic ROS generation (standardized mean difference [SMD] = 1.42, 95 % CI: 1.10–1.75), renal tubular apoptosis (SMD = 1.27, 95 % CI: 0.94–1.61), and β-cell impairment (SMD = 1.18, 95 % CI: 0.88–1.49). Translational challenges remain due to poor clearance kinetics, chronic inflammation, and incomplete regulatory frameworks.

Conclusion

Nanoparticles hold transformative potential in precision diagnostics, but their clinical adoption demands a nuanced understanding of toxicological trade-offs. Future research must focus on biodegradable and renal-clearable materials, mechanistically guided design strategies, standardized toxicological protocols, and AI-driven predictive models. This review provides a dual-perspective framework that integrates diagnostic breakthroughs with biosafety imperatives, guiding the next phase of nanomedicine toward safe and effective clinical translation.
纳米技术在疾病诊断、靶向治疗和生物传感方面提供了前所未有的能力,正在重塑生物医学领域。纳米粒子(NPs),由于其独特的物理化学性质,使超灵敏的生物标志物检测,实时监测和微创分析跨越肿瘤学,感染性疾病和神经病学。然而,它们的生物相互作用也引起了对器官特异性毒性的重大关注,特别是在代谢系统中。本系统综述和荟萃分析旨在整合纳米颗粒诊断应用的现有证据,以及纳米颗粒对关键代谢器官(肝、肾、胰腺、脾脏和脂肪组织)毒理学影响的新见解。它进一步研究了机制途径、剂量依赖效应和转化挑战,以弥合创新与生物安全之间的差距。方法按照PRISMA 2020指南,于2015年1月至2025年10月对PubMed、Scopus、Web of Science和谷歌Scholar进行综合文献检索。符合条件的研究报告了与NP暴露相关的定量诊断性能指标(如检测限、灵敏度、多路复用能力)或生物学结果(如氧化应激、细胞凋亡、纤维化、内分泌干扰)。对42项报告可比较定量毒性数据的研究进行荟萃分析综合。结果金属、聚合物、光子和混合纳米颗粒的诊断应用表明,与传统分析相比,灵敏度提高了1000倍,平均检测限达到飞摩尔范围。然而,综合毒性分析显示了显著的器官特异性风险:肝脏ROS生成(标准化平均差[SMD] = 1.42, 95% CI: 1.10-1.75)、肾小管凋亡(SMD = 1.27, 95% CI: 0.94-1.61)和β细胞损伤(SMD = 1.18, 95% CI: 0.88-1.49)。由于清除动力学差、慢性炎症和不完整的调控框架,转化挑战仍然存在。纳米颗粒在精确诊断方面具有变革性潜力,但其临床应用需要对毒理学权衡有细致的了解。未来的研究必须集中在可生物降解和肾脏清除材料、机械指导设计策略、标准化毒理学方案和人工智能驱动的预测模型上。这篇综述提供了一个双重视角的框架,将诊断突破与生物安全要求结合起来,指导纳米医学的下一阶段走向安全有效的临床转化。
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引用次数: 0
Study of various forms of propolis nanoparticles and their antibacterial effectiveness 研究了不同形式的蜂胶纳米颗粒及其抗菌效果
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-01 Epub Date: 2025-12-09 DOI: 10.1016/j.onano.2025.100276
Ammar Fadhil , Sriwidodo , Khaled M. Elamin , Ahmed Fouad Abdelwahab Mohammed , Safwat A Mahmoud , Nasrul Wathoni
Most bacteria are beneficial to human health, but some have pathogenic properties. Pathogenic bacteria cause diseases in the host by directly damaging tissues or cells during replication via toxin production. Propolis nanoparticles is a method that has the potential to be an effective antibacterial. Advantages of using nanotechnology include boosting the drug delivery system and absorption of active herbal medicine substances, which have poor bioavailability owing to their high molecular weight, improved solubility, rapid penetration with low cytotoxicity, reduced drug dosage, and fewer side effects. This study reviews the literature on the effectiveness of propolis in various forms of nanoparticle technology as an antibacterial agent, which may help researchers to develop nanoparticle technology in the pharmaceutical industry. We conducted this research using search engines, including Scopus, PubMed, and ScienceDirect, with the keywords " Nanoparticles,”" Propolis,”and "Antibacterial,” without limiting the year of publication. We conducted a search between April and June 2025. They related the reviewed articles to knowledge of nanoparticle use. Propolis is a natural resinous substance produced by honeybees in various forms. These parameters were used to extract 1699 articles, which were reviewed and examined. The study identified eight types of propolis nanoparticles with antibacterial properties: nanoemulsions, nanostructured lipid carriers (NLC), nanosheets, metal nanoparticles, chitosan nanoparticles, nanoencapsulation, solid lipid nanoparticles (SLN), and polymer nanoparticles. The effectiveness of antibacterial propolis nanoparticles varies agents. The metallic form of propolis nanoparticles is the most effective nanoparticles. Metallic propolis nanoparticles can inhibit 19 types of bacteria and can be applied in eight different forms.
大多数细菌对人体健康有益,但也有一些具有致病性。致病菌在复制过程中通过产生毒素直接破坏宿主的组织或细胞,从而引起宿主的疾病。蜂胶纳米颗粒是一种有潜力成为有效抗菌药物的方法。使用纳米技术的优点包括促进药物传递系统和活性草药物质的吸收,这些活性草药物质由于其高分子量、提高溶解度、快速渗透和低细胞毒性、减少药物剂量和较少副作用而具有较差的生物利用度。本研究综述了蜂胶在各种形式的纳米颗粒技术中作为抗菌剂的有效性的文献,这可能有助于研究人员在制药工业中开发纳米颗粒技术。我们使用搜索引擎进行了这项研究,包括Scopus, PubMed和ScienceDirect,关键词是“纳米颗粒”,“蜂胶”和“抗菌”,没有限制发表年份。我们在2025年4月到6月间进行了搜索。他们将所评论的文章与纳米粒子的应用知识联系起来。蜂胶是一种天然的树脂状物质,由蜜蜂以各种形式产生。利用这些参数提取了1699篇文章,并对其进行了回顾和检验。研究确定了八种具有抗菌性能的蜂胶纳米颗粒:纳米乳液、纳米结构脂质载体(NLC)、纳米片、金属纳米颗粒、壳聚糖纳米颗粒、纳米胶囊、固体脂质纳米颗粒(SLN)和聚合物纳米颗粒。不同药剂的蜂胶纳米颗粒抗菌效果不同。金属形式的蜂胶纳米颗粒是最有效的纳米颗粒。金属蜂胶纳米颗粒可以抑制19种细菌,并可以以8种不同的形式应用。
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引用次数: 0
Enhanced oral bioavailability of Irbesartan via nano-bilosomes: A potential breakthrough in hypertension treatment 通过纳米胆管体提高厄贝沙坦的口服生物利用度:高血压治疗的潜在突破
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-11-01 Epub Date: 2025-09-06 DOI: 10.1016/j.onano.2025.100255
Heba A. Ghanem , Mahmoud M.A. Elsayed , Shadeed Gad , Mamdouh Ghorab , Nashwa H. Abd Elwahab , Abd El hakim Ramadan , Maha Alsunbul , Amira Abdel Motaal , Ali M. Nasr
Irbesartan (IRB), a widely used antihypertensive medication, exhibits limited therapeutic efficacy due to poor solubility and stability characteristics, which compromise patient adherence. This investigation focused on developing and optimizing a nano bilosomal formulation of IRB to enhance oral bioavailability, extend release duration, and improve pharmacological performance. Through D-optimal design methodology, the study examined key formulation variables including bile salt concentration, cholesterol content, bile salt type, edge activator type, and soybean phosphatidylcholine to bile salt ratio (SPC). These parameters were evaluated against key performance indicators: particle size (PS), zeta potential (ZP), and encapsulation efficiency (EE%). Physicochemical characterization included DSC analysis, TEM imaging, and in vitro release studies. The optimized bilosomal formulation demonstrated favorable characteristics with a particle size of 109.99 nm, zeta potential of -30.999 mV, and encapsulation efficiency of 94.54 %. Physicochemical characterization confirmed the absence of IRB-excipient interactions, while DSC analysis revealed IRB amorphization. TEM imaging validated spherical morphology of the formulated structures. The IRB-loaded bilosomes exhibited sustained biphasic release over 24 h, achieving relative bioavailability 1.42-fold and 1.30-fold higher compared to IRB solution and commercial formulation, respectively. The nano bilosomal formulation significantly enhances IRB solubility, stability, and bioavailability, offering a promising approach for improved oral delivery and therapeutic outcomes. Additional research addressing scalability and clinical efficacy is warranted.
厄贝沙坦(Irbesartan, IRB)是一种广泛使用的降压药,由于其溶解度和稳定性差,其治疗效果有限,影响了患者的依从性。本研究的重点是开发和优化IRB的纳米二质体配方,以提高口服生物利用度,延长释放时间,改善药理性能。通过d -最优设计方法,研究考察了关键配方变量,包括胆盐浓度、胆固醇含量、胆盐类型、边缘活化剂类型和大豆磷脂酰胆碱与胆盐比(SPC)。根据关键性能指标:粒径(PS)、ζ电位(ZP)和包封效率(EE%)对这些参数进行评估。理化表征包括DSC分析、TEM成像和体外释放研究。结果表明,优化后的包封率为94.54%,粒径为109.99 nm, zeta电位为-30.999 mV。理化表征证实了IRB-赋形剂之间不存在相互作用,而DSC分析显示了IRB的非晶化。透射电镜成像证实了配方结构的球形形貌。负载IRB的双相释放持续超过24 h,相对生物利用度分别比IRB溶液和商业配方高1.42倍和1.30倍。纳米二质体制剂显著提高了IRB的溶解度、稳定性和生物利用度,为改善口服给药和治疗结果提供了一种有希望的方法。进一步的研究解决可扩展性和临床疗效是必要的。
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引用次数: 0
Green synthesis of antioxidant and low-toxicity gold and silver nanoparticles using floral extracts 利用花卉提取物绿色合成抗氧化和低毒的金、银纳米颗粒
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-11-01 Epub Date: 2025-09-24 DOI: 10.1016/j.onano.2025.100258
Geovanna Arroyo , Yolanda Angulo , Blanca Naranjo , Fernanda Toscano , Marbel Torres Arias , Alexis Debut , Carlos Reinoso , Carina Stael , Joselyn Soria , Andrés Izquierdo
In this study, gold (AuNPs) and silver (AgNPs) nanoparticles were synthesized using floral extracts of H. sabdariffa and P. domesticum, aiming to develop eco-friendly nanomaterials with antioxidant and low toxicity properties. The green synthesis method produced stable nanoparticles larger than 30 nm, which were characterized by high antioxidant activity, low cytotoxicity, and minimal ecotoxic effects compared to those obtained via conventional chemical reducers (trisodium citrate and tannic acid). Among the most promising results, promising results, AuNPs and AgNPs synthesized with H. sabdariffa exhibited the highest antioxidant capacity (up to 43.13% more than P. domesticum) and negligible cytotoxicity in both A549 and HFF cell lines, with AuNPs even enhancing cell viability. AgNPs from P. domesticum showed improved resistance to UV exposure buy slightly higher cytotoxicity. In contrast, chemically synthesized NPs (Q1 and Q2) induced significant cell death and exhibited increased oxidative states under UV–Vis-NIR radiation. Toxicity tests on cyanobacteria (Fisherella musicola) confirmed the biocompatibility of green synthesis NPs, with no significant growth inhibition observed for AuNPs:Hs and AgNPs:Hs. Overall, this work confirms that anthocyanin rich floral extracts can act as effective reducing and stabilizing agents, producing multifunctional nanoparticles suitable for biomedical and cosmetic applications. These findings highlight the potential of green nanotechnology to deliver safer and more sustainable nanoparticle formulations.
本研究以金花和家花提取物为原料合成了金(AuNPs)和银(AgNPs)纳米粒子,旨在开发具有抗氧化和低毒性的环保型纳米材料。绿色合成方法制备的纳米颗粒稳定,直径大于30 nm,与传统化学还原剂(柠檬酸三钠和单宁酸)相比,具有高抗氧化活性、低细胞毒性和最小生态毒性的特点。其中,最有希望的结果是,在A549和HFF细胞系中,用黄麻合成的AuNPs和AgNPs均表现出最高的抗氧化能力(比家麻高出43.13%),而细胞毒性可以忽略不计,AuNPs甚至可以提高细胞活力。家蝇AgNPs的抗紫外线能力增强,但细胞毒性略高。相比之下,化学合成的NPs (Q1和Q2)在UV-Vis-NIR辐射下诱导了显著的细胞死亡,并表现出增加的氧化状态。对蓝藻(fishella musicola)的毒性试验证实了绿色合成NPs的生物相容性,对AuNPs:Hs和AgNPs:Hs没有明显的生长抑制。总的来说,这项工作证实了花青素丰富的花卉提取物可以作为有效的还原和稳定剂,生产适合生物医学和化妆品应用的多功能纳米颗粒。这些发现突出了绿色纳米技术在提供更安全和更可持续的纳米颗粒配方方面的潜力。
{"title":"Green synthesis of antioxidant and low-toxicity gold and silver nanoparticles using floral extracts","authors":"Geovanna Arroyo ,&nbsp;Yolanda Angulo ,&nbsp;Blanca Naranjo ,&nbsp;Fernanda Toscano ,&nbsp;Marbel Torres Arias ,&nbsp;Alexis Debut ,&nbsp;Carlos Reinoso ,&nbsp;Carina Stael ,&nbsp;Joselyn Soria ,&nbsp;Andrés Izquierdo","doi":"10.1016/j.onano.2025.100258","DOIUrl":"10.1016/j.onano.2025.100258","url":null,"abstract":"<div><div>In this study, gold (AuNPs) and silver (AgNPs) nanoparticles were synthesized using floral extracts of <em>H. sabdariffa</em> and <em>P. domesticum</em>, aiming to develop eco-friendly nanomaterials with antioxidant and low toxicity properties. The green synthesis method produced stable nanoparticles larger than 30 nm, which were characterized by high antioxidant activity, low cytotoxicity, and minimal ecotoxic effects compared to those obtained via conventional chemical reducers (trisodium citrate and tannic acid). Among the most promising results, promising results, AuNPs and AgNPs synthesized with <em>H. sabdariffa</em> exhibited the highest antioxidant capacity (up to 43.13% more than <em>P. domesticum</em>) and negligible cytotoxicity in both A549 and HFF cell lines, with AuNPs even enhancing cell viability. AgNPs from <em>P. domesticum</em> showed improved resistance to UV exposure buy slightly higher cytotoxicity. In contrast, chemically synthesized NPs (Q1 and Q2) induced significant cell death and exhibited increased oxidative states under UV–Vis-NIR radiation. Toxicity tests on cyanobacteria (<em>Fisherella musicola</em>) confirmed the biocompatibility of green synthesis NPs, with no significant growth inhibition observed for AuNPs:Hs and AgNPs:Hs. Overall, this work confirms that anthocyanin rich floral extracts can act as effective reducing and stabilizing agents, producing multifunctional nanoparticles suitable for biomedical and cosmetic applications. These findings highlight the potential of green nanotechnology to deliver safer and more sustainable nanoparticle formulations.</div></div>","PeriodicalId":37785,"journal":{"name":"OpenNano","volume":"26 ","pages":"Article 100258"},"PeriodicalIF":0.0,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145363049","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
Targeted gene removal by SpCas9 transduced by a protein-RNA complex transduction system NanoMEDIC 蛋白- rna复合物转导系统NanoMEDIC介导的SpCas9靶向基因去除
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-11-01 Epub Date: 2025-09-17 DOI: 10.1016/j.onano.2025.100257
Mayuko Yagi , China Tomita , Minami Hama , Rafal Krol , Peter Gee , Akitsu Hotta , Jun Komano
The CRISPR-Cas9 system offers powerful genome editing capabilities, but off-target effects remain a key limitation. Direct delivery of Cas9 protein complexed with guide RNA (gRNA) can mitigate these effects by limiting exposure time. We previously developed NanoMEDIC, a virus-like particle system shown to deliver Cas9/gRNA ribonucleoprotein (RNP) complexes both in vitro and in vivo. In the present study, we compared NanoMEDIC-mediated delivery with plasmid-based transfection using a gene excision reporter in the human embryonic kidney-derived cell line 293FT and the human glioblastoma-derived cell line NP-2. In this model, the DNA sequence targeted by Cas9/gRNA was derived from a human oncogenic retrovirus, human T-cell leukemia virus type I (HTLV-1). NanoMEDIC achieved efficient gene removal-editing with significantly lower Cas9 input per cell regardless of whether the target DNA was transiently transfected or integrated into chromosomal DNA. Sequencing of edited loci revealed that NanoMEDIC-mediated Cas9/gRNA delivery produced 58.3 – 87.5 % removal-edited DNA without insertions or deletions (indels), compared with 8.3 – 29.4 % using plasmid transfection. These data suggest a high editing precision of NanoMEDIC-mediated Cas9/gRNA delivery. This likely reflects the transient presence of Cas9, which enables rapid repair through non-homologous end joining (NHEJ) without prolonged nuclease activity. Collectively, our findings highlight the potential of NanoMEDIC for applications requiring precise, indel-free genome modifications and support its use as a safer alternative to DNA-based delivery or systems involving sustained Cas9 expression.
CRISPR-Cas9系统提供了强大的基因组编辑能力,但脱靶效应仍然是一个关键的限制。直接递送Cas9蛋白与引导RNA (gRNA)的复合物可以通过限制暴露时间来减轻这些影响。我们之前开发了NanoMEDIC,这是一种病毒样颗粒系统,可以在体外和体内传递Cas9/gRNA核糖核蛋白(RNP)复合物。在本研究中,我们在人胚胎肾源性细胞系293FT和人胶质母细胞瘤源性细胞系NP-2中比较了nanomedic介导的传递与基于基因切除报告基因的质粒转染。在这个模型中,Cas9/gRNA靶向的DNA序列来源于一种人类致癌逆转录病毒,人类t细胞白血病病毒I型(HTLV-1)。无论目标DNA是瞬时转染还是整合到染色体DNA中,NanoMEDIC都实现了高效的基因去除编辑,每个细胞的Cas9输入量显著降低。编辑位点的测序显示,nanomedic介导的Cas9/gRNA递送产生58.3% - 87.5%的无插入或缺失的去除编辑DNA (indels),而使用质粒转染则为8.3 - 29.4%。这些数据表明,nanomedic介导的Cas9/gRNA传递具有很高的编辑精度。这可能反映了Cas9的短暂存在,它可以通过非同源末端连接(NHEJ)快速修复,而不延长核酸酶活性。总的来说,我们的研究结果突出了NanoMEDIC在需要精确、无indel基因组修饰的应用中的潜力,并支持其作为基于dna的递送或涉及持续Cas9表达的系统的更安全替代方案。
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引用次数: 0
Phytochemical-capped silver nanoparticles from the medicinal plant Embelia laeta disrupting 3D tumorspheres and inducing ROS-mediated apoptosis in MCF-7 breast cancer cells 来自药用植物叶红的植物化学覆盖银纳米颗粒破坏3D肿瘤球并诱导ros介导的MCF-7乳腺癌细胞凋亡
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-11-01 Epub Date: 2025-10-18 DOI: 10.1016/j.onano.2025.100262
Thi Thanh Huong Le , Van Hung Hoang , Thi Quynh Nguyen , Dac Trung Nguyen , Viet Hoang , Thu Huong Trinh , Thi Tam Khieu , Phu Hung Nguyen
Plant-based green nanotechnology provides a promising strategy that integrates phytochemicals with metallic nanoparticles for targeted cancer therapy. In this study, silver nanoparticles (Eml-AgNPs) synthesized using Embelia laeta (L.) Mez. leaf extract were investigated for their anticancer potential. The Eml-AgNPs were spherical, crystalline, and averaged 13.4 ± 4.6 nm in size, as confirmed by UV–Vis spectroscopy (absorption peak at 453 nm), XRD, FTIR, and TEM analyses. UPLC-QToF-MS profiling revealed 13 bioactive molecules bound to the nanoparticle surface, contributing to their stability and anticancer efficacy. Eml-AgNPs demonstrated potent, concentration-dependent cytotoxicity against HepG2, AGS, MCF-7, and MKN45 cancer cell lines, with IC₅₀ values ranging from 0.78 µg/mL to 1.67 µg/mL. In 3D tumorsphere cultures, treatment with Eml-AgNPs (2–5 µg/mL) significantly disrupted spheroid morphology and cellular cohesion. Mechanistic studies indicated ROS-mediated apoptosis, evidenced by a 36.7 % increase in Annexin V-FITC-positive cells (p < 0.01) and a 32.7 % elevation in ROS generation following treatment with 5 µg/mL Eml-AgNPs (p < 0.01). Furthermore, expression of pro-apoptotic genes including CASP8, CASP9, GADD45, and BAX was significantly upregulated. Collectively, these findings highlight the potential of Eml-AgNPs as a green nanotherapeutic platform, leveraging phytochemical synergy to induce oxidative stress-driven apoptosis in cancer cells. Further in vivo studies are needed to confirm the efficacy and safety of Eml-AgNPs for potential biomedical applications.
基于植物的绿色纳米技术提供了一种很有前途的策略,将植物化学物质与金属纳米粒子结合起来用于靶向癌症治疗。在本研究中,银纳米粒子(Eml-AgNPs)是由Eml-AgNPs合成的。Mez。研究了叶提取物的抗癌作用。通过紫外可见光谱(吸收峰在453nm处)、XRD、FTIR和TEM分析证实,Eml-AgNPs为球形结晶,平均尺寸为13.4±4.6 nm。UPLC-QToF-MS分析显示,13种生物活性分子结合在纳米颗粒表面,有助于其稳定性和抗癌功效。Eml-AgNPs对HepG2, AGS, MCF-7和MKN45癌细胞系表现出有效的浓度依赖性细胞毒性,IC₅0值范围为0.78 μ g/mL至1.67 μ g/mL。在3D肿瘤球培养中,Eml-AgNPs(2-5µg/mL)显著破坏了球体形态和细胞内聚。机制研究表明ROS介导的细胞凋亡,Annexin v - fitc阳性细胞增加36.7% (p < 0.01), 5µg/mL Eml-AgNPs处理后ROS生成增加32.7% (p < 0.01)。此外,促凋亡基因CASP8、CASP9、GADD45和BAX的表达显著上调。总之,这些发现突出了Eml-AgNPs作为绿色纳米治疗平台的潜力,利用植物化学协同作用诱导癌细胞氧化应激驱动的细胞凋亡。需要进一步的体内研究来证实Eml-AgNPs在潜在生物医学应用中的有效性和安全性。
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引用次数: 0
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