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Flexible asymmetric liposomes as a platform for improved plasmid DNA delivery: An in vitro study 柔性不对称脂质体作为改进质粒DNA传递的平台:一项体外研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-27 DOI: 10.1016/j.onano.2026.100283
Denisse Gardea-Gutiérrez , Manuel Román-Aguirre , Raúl Loera-Valencia , Blanca Sánchez-Ramírez , Yocanxóchitl Perfecto-Avalos , Silvia L. Montes-Fonseca
As a versatile type of nanocarrier, liposomes have gained attention due to their biocompatibility, biodegradability, and ability to encapsulate a wide range of compounds. Asymmetric liposomes are characterized by distinct lipid compositions in their inner and outer layers, enhancing drug encapsulation and stability. Surfactant compounds and ethanol confer the flexibility of liposomes in their lipid layer. This characteristic allows liposomes to deform without breaking or releasing their contents, enabling them to cross complex barriers, such as the skin. This research investigates the innovative design and application of flexible asymmetric liposomes for transdermal DNA delivery. By using an adapted inverse emulsion technique, this study successfully encapsulated plasmid DNA within flexible asymmetric liposomes to evaluate its biocompatibility and skin permeation capacity in an in vitro model. Several formulations of liposomes containing DOTMA, DOPE, and/or cholesterol as the inner layer and DSPC, Span80, and/or ethanol as the outer layer were assessed through viability assay, transfection efficiency, and permeability testing using the Parallel Artificial Membrane Permeability Assay (PAMPA). All formulations demonstrated over 69% cell viability at a concentration of 5 μg, and transfection efficiency was significantly enhanced, reaching transfection rates of 32.37% ±3.32% in liposomes with all components. Permeability testing showed that the liposomal formulations exhibited high permeability, further improved by including ethanol and surfactants. Key findings indicate that cholesterol, Span 80, and ethanol substantially contribute to transfection rates and permeation. This research underscores the potential of flexible asymmetric liposomes for effective transdermal delivery of genetic material.
作为一种多用途的纳米载体,脂质体因其生物相容性、生物可降解性和包封多种化合物的能力而受到广泛关注。不对称脂质体的特点是其内层和外层的脂质组成不同,增强了药物的包封性和稳定性。表面活性剂化合物和乙醇赋予脂质体在其脂层中的柔韧性。这种特性允许脂质体在不破坏或释放其内容物的情况下变形,使它们能够穿过复杂的屏障,如皮肤。本研究探讨了柔性不对称脂质体的创新设计和应用,用于透皮DNA递送。本研究采用一种适应的反乳化技术,成功地将质粒DNA包裹在柔性不对称脂质体中,并在体外模型中评估其生物相容性和皮肤渗透能力。几种含有DOTMA、DOPE和/或胆固醇为内层,dsc、Span80和/或乙醇为外层的脂质体配方通过活力测定、转染效率和使用平行人工膜渗透性测定(PAMPA)的渗透性测试来评估。在浓度为5 μg时,各制剂的细胞存活率均在69%以上,转染效率显著提高,转染率为32.37%±3.32%。渗透性测试表明,脂质体配方具有较高的渗透性,并通过加入乙醇和表面活性剂进一步改善。主要研究结果表明,胆固醇、Span 80和乙醇对转染率和渗透有重要影响。这项研究强调了灵活的不对称脂质体在遗传物质的有效透皮递送方面的潜力。
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引用次数: 0
Transfersomal gel loading of amniotic mesenchymal stem cell metabolite product for diabetic wound healing in alloxan-induced diabetic mice 羊膜间充质干细胞代谢物在四氧嘧啶诱导的糖尿病小鼠伤口愈合中的转移体凝胶负载
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-13 DOI: 10.1016/j.onano.2026.100282
Andang Miatmoko , Dzihni Nahdliyyati , Sherly Maidasari , Tristiana Erawati , Dini Retnowati , Khoo Boon Yin , Margaret Ahmad , Djoko Legowo , Noorma Rosita

Purpose

Amniotic mesenchymal stem cell metabolite product (AMSC-MP), a metabolite derived from cell cultures, contains cytokines and growth factors that support skin regeneration, making it a promising therapeutic candidate for chronic wounds, such as diabetic foot ulcers. However, because of their large molecular size, AMSC-MPs cannot effectively penetrate the skin’s primary barrier, the stratum corneum. To address this issue, transfersomes have been developed as flexible vesicular carriers capable of delivering active compounds through intercellular gaps. This study aimed to evaluate the physicochemical properties of AMSC-MP transfersomes and their wound healing efficacy in a mouse model of diabetes.

Methods

Transfersomes (Ts), composed of l-alpha phosphatidylcholine and sodium cholate, were prepared in different AMSC-MP concentrations, 5% (T-5) and 25% (T-25), using the thin-film hydration method, and hyaluronic acid (HA) was added.

Result

The results showed that the addition of HA increased particle size, polydispersity index, and pH, while reducing zeta potential, and maintaining high entrapment efficiency. In vivo wound healing evaluation showed that the T-25 HA gel formulation achieved the highest wound contraction percentage, followed by T-5 HA, THA, Blank gel, free AMSC-MPs (25% and 5%), and transfersomes without HA. Histopathological observations and collagen density analyses confirmed that HA improved healing by enhancing tissue regeneration, epithelialization, and collagen deposition.

Conclusion

In conclusion, the AMSC-MP transfersomal gel, particularly the 25% formulation with HA, demonstrated the most effective wound-healing performance and showed strong potential as a therapeutic strategy for chronic diabetic wounds.
羊膜间充质干细胞代谢物(AMSC-MP)是一种来源于细胞培养物的代谢物,含有支持皮肤再生的细胞因子和生长因子,使其成为慢性伤口(如糖尿病足溃疡)的有希望的治疗候选物。然而,由于其大分子大小,AMSC-MPs不能有效地穿透皮肤的主要屏障角质层。为了解决这个问题,转移体已被开发为能够通过细胞间隙传递活性化合物的柔性囊状载体。本研究旨在评价AMSC-MP转移体的理化性质及其在糖尿病小鼠模型中的创面愈合作用。方法采用薄膜水合法制备由l- α磷脂酰胆碱和胆酸钠组成的转运体(Ts),其浓度分别为5% (T-5)和25% (T-25),并加入透明质酸(HA)。结果HA的加入提高了样品的粒径、多分散性指数和pH值,同时降低了zeta电位,保持了较高的捕集效率。体内创面愈合评价显示,T-25 HA凝胶制剂创面收缩率最高,其次是T-5 HA、THA、Blank凝胶、游离AMSC-MPs(25%和5%)和不含HA的转移体。组织病理学观察和胶原密度分析证实,透明质酸通过促进组织再生、上皮化和胶原沉积来改善愈合。总之,AMSC-MP转移体凝胶,特别是25% HA的配方,具有最有效的伤口愈合性能,具有很强的潜力作为慢性糖尿病伤口的治疗策略。
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引用次数: 0
Development and in vitro evaluation of self-emulsifying drug delivery systems liquisolid lozenges of ibuprofen via design of experiments for solubility enhancement and oral epithelial cell permeation 布洛芬液体含片自乳化给药系统的开发及体外评价,通过设计溶解度增强和口腔上皮细胞渗透的实验
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2026-01-11 DOI: 10.1016/j.onano.2026.100281
Sukannika Tubtimsri, Poonsak Charoensak, Apichaya Sukontachard, Yotsanan Weerapol
Ibuprofen lozenges were developed by converting liquid self-emulsifying drug delivery systems (L-SEDDS) into liquisolid compacts (LSCs) to enhance aqueous solubility, support local anti-inflammatory action in the oral and throat regions, and reduce gastrointestinal irritation. The solubility of ibuprofen in oils and nonionic surfactants was evaluated. Tween 60 showed the highest solubility (285.53 ± 19.31 mg/g), whereas Imwitor® 742 (135.12 ± 0.21 mg/g) provided a suitable oil phase. L-SEDDS composed of ibuprofen, Tween 60, and Imwitor® 742 (9:1, w/w) formed nanoemulsions in simulated salivary fluid (SSF) with droplet sizes of approximately 200 nm. The L-SEDDS was loaded onto polyvinylpyrrolidone, magnesium aluminosilicate, sucrose, or F-Melt® C (FMC) to obtain LSC lozenges. A three-factor Box–Behnken design was employed to investigate the effects of L-SEDDS level, PVP content, and diluent type on tablet hardness and mean dissolution time (MDT). Suitable sucrose-LSC (Run7) and FMC-LSC (Run13) formulations showed rapid dissolution in SSF, with MDT values of 6.59 ± 0.15 and 5.91 ± 0.13 min, respectively, compared with 45.34 ± 1.11 min for ibuprofen powder. In a KON cell monolayer model, L-SEDDS and FMC-LSC (Run13) increased the apparent permeability coefficient of ibuprofen by approximately 3.6- and 3.5-fold, respectively, compared with ibuprofen powder. Both formulations maintained ibuprofen content, droplet size, dissolution behavior, and mechanical strength after 6 months of storage under both ambient and accelerated conditions. These results indicate that L-SEDDS-based LSC lozenges, particularly the FMC formulation, provide a stable dosage form that improves dissolution and mucosal permeation of poorly water-soluble ibuprofen.
布洛芬含片是通过将液体自乳化给药系统(L-SEDDS)转化为液体固体压片(LSCs)来提高水溶性,支持口腔和喉咙区域的局部抗炎作用,并减少胃肠道刺激而开发的。考察了布洛芬在油脂和非离子表面活性剂中的溶解度。Tween 60的溶解度最高(285.53±19.31 mg/g), Imwitor®742的溶解度最高(135.12±0.21 mg/g)。由布洛芬、Tween 60和Imwitor®742 (9:1,w/w)组成的L-SEDDS在模拟唾液液(SSF)中形成纳米乳液,液滴大小约为200 nm。L-SEDDS被加载到聚乙烯吡烷酮、铝硅酸镁、蔗糖或F-Melt®C (FMC)上,得到LSC含片。采用三因素Box-Behnken设计考察L-SEDDS含量、PVP含量和稀释剂类型对片剂硬度和平均溶出时间的影响。合适的蔗糖- lsc (Run7)和FMC-LSC (Run13)制剂在SSF中溶出快速,MDT值分别为6.59±0.15和5.91±0.13 min,而布洛芬粉的MDT值为45.34±1.11 min。在KON细胞单层模型中,与布洛芬粉末相比,L-SEDDS和FMC-LSC (Run13)分别使布洛芬的表观通透系数提高了约3.6倍和3.5倍。两种制剂在常温和加速条件下储存6个月后均保持布洛芬含量、滴度、溶出行为和机械强度不变。这些结果表明,基于l - seds的LSC含片,特别是FMC配方,提供了一种稳定的剂型,可以改善水溶性差的布洛芬的溶解和粘膜渗透。
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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 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
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 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。
{"title":"Exploring the Therapeutic Potential of Green-fabricated CRL-AgNPs from Catharanthus roseus","authors":"Rokshana Ara Ruhi ,&nbsp;Sk. Md. Atiqur Rahman ,&nbsp;Mobasshir Noor Shehab ,&nbsp;Md. Roqunuzzaman ,&nbsp;Mohammad Saiful Islam ,&nbsp;Md. Ragib Shariar ,&nbsp;Md. Mahmudul Hasan Maruf ,&nbsp;Firoz Ahmed ,&nbsp;M Ahasanur Rabbi ,&nbsp;Syed Rashel Kabir ,&nbsp;Ananda Kumar Saha ,&nbsp;Md. Anwarul Kabir Bhuiya ,&nbsp;Md. Abu Reza","doi":"10.1016/j.onano.2025.100278","DOIUrl":"10.1016/j.onano.2025.100278","url":null,"abstract":"<div><div>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 <em>Catharanthus roseus</em> as a reducing and capping agent to discover novel therapeutic leads. To attain this target, synthesis of <em>C. roseus</em> leaf-mediated AgNPs (CRL-AgNPs) was optimized using a 2<sup>4</sup> 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 IC<sub>50</sub> value of 8.033μg/mL, indicating their potent anticancer activity. Furthermore, their anti-proliferative efficacy was validated <em>in vivo</em> 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.</div></div>","PeriodicalId":37785,"journal":{"name":"OpenNano","volume":"27 ","pages":"Article 100278"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145938369","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
Enantiomeric lysine-based cationic lipids: Design, synthesis, and characterization for in vitro gene delivery 基于赖氨酸的阳离子脂质对映体:设计、合成和表征体外基因传递
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-28 DOI: 10.1016/j.onano.2025.100280
Berenice Erendira Oseguera-Guerra , Oliver Lopez-Villegas , Manuel Román-Aguirre , Alfredo Aguilar-Elguezabal , Raúl Loera-Valencia , Silvia Lorena Montes-Fonseca
Nucleic acid delivery is crucial for gene therapy, vaccination, and cancer treatment. Despite advances in cationic lipid-based vectors, their transfection efficiency is often limited by structural complexity. In this study, we synthesized lysine-based cationic lipids by esterifying d- or l-lysine with alcohols of varying chain lengths. The compounds were characterized by infrared spectroscopy and mass spectrometry, incorporated into liposomes, and evaluated for transfection efficiency, particle size, morphology, and cytotoxicity in vitro. Transfection performance increased with chain length, peaking at 20 carbons, with no significant differences between d- and l-enantiomers. Compared to Lipofectamine 2000, the optimized liposomes showed superior gene delivery while preserving cell viability. They displayed predominantly spherical to oval morphologies, particle sizes of 30–130 nm, and negligible cytotoxicity. These results suggest lysine-based cationic lipids are promising, safe, and effective nonviral vectors for nucleic acid delivery.
核酸传递对基因治疗、疫苗接种和癌症治疗至关重要。尽管阳离子脂质载体取得了进展,但其转染效率往往受到结构复杂性的限制。在本研究中,我们通过将d-赖氨酸或l-赖氨酸与不同链长的醇酯化合成了基于赖氨酸的阳离子脂质。通过红外光谱和质谱对化合物进行了表征,并将其纳入脂质体中,并在体外对转染效率、粒径、形态和细胞毒性进行了评估。转染性能随着链长的增加而增加,在20个碳处达到峰值,d-和l-对映体之间没有显著差异。与Lipofectamine 2000相比,优化后的脂质体在保持细胞活力的同时具有更好的基因传递能力。它们主要呈球形到椭圆形形态,粒径为30-130 nm,细胞毒性可以忽略不计。这些结果表明,基于赖氨酸的阳离子脂质是一种有前途的、安全的、有效的核酸传递的非病毒载体。
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引用次数: 0
Development of new delivery systems of hyaluronic acid based on silica hydrogels: In vitro kinetics of release and enzymatic degradation of the drug 基于二氧化硅水凝胶的透明质酸新递送系统的开发:药物的体外释放动力学和酶降解
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-12-27 DOI: 10.1016/j.onano.2025.100279
Ekaterina Dolinina, Elena Parfenyuk
Hyaluronic acid (HA) is a well-known anti-inflammatory drug that is widely used clinically to treat various diseases and as a component in cosmetic products. However some properties of HA (rapid release and enzymatic degradation) significantly reduce its functioning in the body and, consequently, its therapeutic effect. To develop new soft delivery system of HA with improved functional properties, the drug was encapsulated into silica hydrogels with various surface chemistry of silica matrix. The hydrogels of silica modified with aminopropyl and mercaptopropyl groups, as well as unmodified silica were studied as HA carriers. The effects of silica matrix modification, average molecular weight and concentration HA on the kinetics of its release from the formed composite hydrogels, as well as enzymatic degradation were revealed in vitro. It was found that the encapsulation of HA into silica hydrogels significantly slows down release process of the acid and, in most cases, its enzyme-induced degradation. The release controlled by delayed (pseudo-Fickian) diffusion as well as the protective effect of the silica hydrogel matrixes on the enzymatic degradation showed that the silica hydrogels are promising materials for creation of new soft formulations of HA.
透明质酸(HA)是一种众所周知的抗炎药物,在临床上广泛用于治疗各种疾病,并作为化妆品的成分。然而,透明质酸的某些特性(快速释放和酶降解)显着降低了其在体内的功能,从而降低了其治疗效果。为了开发新的功能性能更好的透明质酸软性给药系统,将药物包封在具有不同表面化学性质的二氧化硅基质的二氧化硅水凝胶中。研究了氨基丙基和巯基改性二氧化硅水凝胶和未改性二氧化硅水凝胶作为HA载体。研究了二氧化硅基质改性、平均分子量和HA浓度对其从复合水凝胶中释放的动力学以及体外酶降解的影响。研究发现,将透明质酸包封在二氧化硅水凝胶中,显著减缓了酸的释放过程,在大多数情况下,还减缓了酶诱导的降解。延迟(拟菲克式)扩散控制的释放以及二氧化硅水凝胶基质对酶解的保护作用表明,二氧化硅水凝胶是制备新型软质透明质酸的有前景的材料。
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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 : 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
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 : 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
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 : 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":"2025-11-28","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}
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