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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 : 2025-09-24 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。
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引用次数: 0
Advancements in nanotechnology for sunscreens: Preparation, characterization, and mechanisms of UV protection 纳米技术在防晒方面的进展:制备、表征和防紫外线机制
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-09-24 DOI: 10.1016/j.onano.2025.100259
Feggy Yustika Sitinjak , Nur Aisyah , Diah Lia Aulifa , Arif Budiman
Nanotechnology based sunscreens have arisen as sophisticated alternatives to conventional formulations, overcoming constraints such as inadequate skin penetration, photoinstability, and potential toxicity of active components. Diverse nanocarrier systems such as liposomes, solid lipid nanoparticles, nanoemulsions, and polymeric nanoparticles exhibit significant advancements, including up to 50 % or more compared to conventional formulations increase in sun protection factor (SPF), particle dimensions ranging from 50 to 200 nm and encapsulation efficiencies surpassing 90 % for UV filters. These systems improve photostability, decrease systemic absorption, and mitigate whitening effects in comparison to conventional sunscreens. Characterization techniques, including dynamic light scattering, electron microscopy, and etc., yield insights into particle size distribution, shape, and stability, which are essential for guaranteeing safety and performance. This study emphasizes recent emphasizes novel developments in the preparation, characterization, and mechanisms of UV protection in nanotechnology based sunscreens, delineating current progress and prospective prospects for safer and more effective solutions.
基于纳米技术的防晒霜已经成为传统配方的复杂替代品,克服了诸如皮肤渗透不足、光不稳定性和活性成分潜在毒性等限制。不同的纳米载体系统,如脂质体、固体脂质纳米颗粒、纳米乳液和聚合物纳米颗粒表现出显著的进步,与传统配方相比,防晒系数(SPF)提高了50%或更多,颗粒尺寸从50到200纳米不等,紫外线过滤器的封装效率超过90%。与传统的防晒霜相比,这些系统提高了光稳定性,减少了系统吸收,减轻了美白效果。表征技术,包括动态光散射、电子显微镜等,可以深入了解颗粒的大小分布、形状和稳定性,这对保证安全性和性能至关重要。本研究着重介绍了纳米防晒剂在制备、表征和防紫外线机制方面的最新进展,描述了目前的进展和更安全、更有效的解决方案的前景。
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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 : 2025-09-17 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
A water-soluble, organosilane-based coating blocked acute and sub-chronic respirable crystalline silica-induced lung toxicity and systemic inflammation in an animal model 一种水溶性有机硅基涂层在动物模型中阻断急性和亚慢性可呼吸性结晶硅诱导的肺毒性和全身炎症
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-09-16 DOI: 10.1016/j.onano.2025.100256
James M. Antonini , Mohammad Shoeb , Breanna Alman , Gregory Zarus , Terry G. Meighan , Katherine A. Roach , Aleksandr Stefaniak , Lauren Bowers , Gregory Boyce , Jenny R. Roberts , Vamsi Kodali
Inhalation of respirable crystalline silica can cause pulmonary fibrosis and inflammation. Silica particles have a highly reactive surface that generates cell-damaging reactive oxygen species when fractured. The objective was to evaluate lung toxicity after exposure to silica coated with and without a water-soluble, organosilane-based coating (SIVO160). Male Sprague-Dawley rats were intratracheally instilled with silica (1 mg/rat), silica coated with SIVO160, SIVO160 alone, or saline (vehicle control). At 3, 10, 45, and 90 d after exposure, bronchoalveolar lavage (BAL) and histopathology were performed to assess lung toxicity. Whole blood was collected to evaluate systemic inflammation by differentiating circulating white blood cells. Also, samples of uncoated and coated silica were analyzed [(1) RapiFlex MALDI-ToF/ToF mass spectrometry; (2) digestion in phagolysosomal simulant fluid (PSF) and serum ultrafiltrate (SUF)] to confirm the SIVO160 coating on the surface of the silica particles after incubation in biological media. At each time point, silica significantly increased BAL fluid lactate dehydrogenase (lung injury) and the number of recovered lung macrophages and neutrophils (lung inflammation). These silica-induced elevations in lung toxicity were completely blocked at each time point when silica was coated with SIVO160 before exposure. At 45 d after exposure to uncoated silica, circulating total white blood cells, neutrophils, and lymphocytes were significantly elevated in the blood compared to the other groups. Lung exposure to silica pretreated with SIVO160 did not cause a significant elevation in any of the peripheral blood cell types at any time point when compared to the saline and SIVO160 alone. As assessed by mass spectrometry, multiple unique spectral peaks were detected on the surface of the silica+SIVO160 particle samples after an overnight incubation in saline. The peaks were absent in the uncoated silica sample spectra, confirming the coating’s presence on the particles. The time it took for removal by digestion of the SIVO160 coating on the silica was reflected by a short-term delay after incubation in both PSF and SUF, suggesting protection could be conveyed to lung cells by the coating during phagocytosis and particle deposition on lung tissue structures. Organosilane materials may be used as a possible mitigation strategy to potentially protect large numbers of workers exposed to respirable crystalline silica in multiple industries is important.
吸入可吸入的结晶二氧化硅可引起肺纤维化和炎症。二氧化硅颗粒具有高度活性的表面,当破裂时产生破坏细胞的活性氧。目的是评估暴露于有或没有水溶性有机硅基涂层(SIVO160)的二氧化硅后的肺毒性。雄性Sprague-Dawley大鼠气管内灌注二氧化硅(1 mg/只)、二氧化硅包被SIVO160、单独SIVO160或生理盐水(对照)。暴露后3、10、45和90 d,进行支气管肺泡灌洗(BAL)和组织病理学评估肺毒性。采集全血,通过区分循环白细胞来评估全身性炎症。(1) RapiFlex MALDI-ToF/ToF质谱分析;(2)在吞噬溶酶体模拟液(PSF)和血清超滤液(SUF)中进行消化,以确认生物培养基孵育后二氧化硅颗粒表面的SIVO160涂层。在每个时间点,二氧化硅显著增加BAL液乳酸脱氢酶(肺损伤)和恢复的肺巨噬细胞和中性粒细胞(肺炎症)的数量。当暴露前用SIVO160包覆二氧化硅时,这些二氧化硅引起的肺毒性升高在每个时间点都被完全阻断。暴露于未涂覆二氧化硅45天后,与其他组相比,血液中循环的白细胞总数、中性粒细胞和淋巴细胞显著升高。与单独使用生理盐水和SIVO160相比,肺暴露于经SIVO160预处理的二氧化硅在任何时间点都没有引起任何外周血细胞类型的显著升高。通过质谱分析,在生理盐水中孵育过夜后,二氧化硅+SIVO160颗粒样品表面检测到多个独特的光谱峰。在未涂覆的二氧化硅样品光谱中没有峰,证实了涂层在颗粒上的存在。在PSF和SUF中孵育后,SIVO160涂层通过消化去除二氧化硅所需的时间被反映为短期延迟,这表明在肺组织结构的吞噬和颗粒沉积过程中,涂层可以传递给肺细胞保护作用。有机硅烷材料可作为一种可能的缓解策略,以潜在地保护多个行业中暴露于可吸入结晶二氧化硅的大量工人,这一点很重要。
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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 : 2025-09-06 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
Myco-nanotechnology at the crossroads: eco-friendly synthesis, agricultural applications, and AI-driven risk mitigation of fungal-derived nanoparticles 十字路口的微生物纳米技术:生态友好合成、农业应用和人工智能驱动的真菌衍生纳米颗粒风险缓解
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-09-01 DOI: 10.1016/j.onano.2025.100254
Lakshika Sharma , Abhishek Dadhich , Irra Dhar , Rashmi Choudhary , Mamta Dhiman , Madan Mohan Sharma
Fungal-based nanotechnology is emerging as a promising and sustainable approach in agriculture, environmental cleanup, and biotechnology. Nanoparticles produced by fungi known as Myco-nanoparticles offer a greener method of synthesis, along with good stability and strong biological activity. However, their increasing use has raised concerns about possible environmental risks and long-term effects. This review highlights recent advances in the eco-friendly production of Myco-nanoparticles and their potential to support plant growth, improve nutrient uptake, and boost resistance to stress and disease. While small amounts of these particles may be helpful, higher doses can lead to harmful effects such as oxidative stress and damage to plant DNA. Compared to nanoparticles made by plants or bacteria, fungal-derived particles are often more stable and easier to produce, though they still pose similar safety concerns. This review uniquely connects fungal nanobiotechnology with AI-driven toxicity prediction and omics-based pathway mapping an integrated approach that lays the groundwork for precision myconanotechnology with reduced ecological impact.
基于真菌的纳米技术在农业、环境清理和生物技术领域正成为一种有前途的可持续方法。由真菌产生的纳米颗粒被称为真菌纳米颗粒,提供了一种更环保的合成方法,同时具有良好的稳定性和很强的生物活性。然而,它们越来越多的使用引起了人们对可能的环境风险和长期影响的担忧。这篇综述重点介绍了生态友好型纳米真菌生产的最新进展,以及它们在支持植物生长、改善养分吸收和增强对胁迫和疾病的抵抗力方面的潜力。虽然少量的这些颗粒可能有帮助,但高剂量会导致有害的影响,如氧化应激和对植物DNA的损害。与植物或细菌制造的纳米颗粒相比,真菌衍生的颗粒通常更稳定,更容易生产,尽管它们仍然存在类似的安全问题。这篇综述独特地将真菌纳米生物技术与人工智能驱动的毒性预测和基于组学的途径映射联系起来,这是一种综合方法,为减少生态影响的精确真菌纳米技术奠定了基础。
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引用次数: 0
Solvothermally grown ZnO/BiOCl photocatalyst for solar-light-responsive degradation of tetracycline antibiotic 溶剂热生长的ZnO/BiOCl光催化剂用于四环素类抗生素的光敏降解
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-08-10 DOI: 10.1016/j.onano.2025.100253
Lalitphan Hongtanee , Khemika Wannakan , Sattra Nonthing , Atchawadee Panchakeaw , Supinya Nijpanich , Suwat Nanan
Binary photocatalyst based on ZnO/BiOCl was constructed very easily using a solvothermal route by addition of solid ZnO to the reaction mixture during the formation of BiOCl. The two-component heterojunction was then applied for sunlight-active removal of tetracycline (TC) drug. The synthesized heterostructure showed mainly the characteristic XRD peaks of BiOCl with the band gap of 3.50 eV, compared to 3.30 eV of the bare BiOCl. The binary photocatalyst comprising 0.05 g of ZnO per 1.0 g of BiOCl (denoted as 0.05ZnO/BiOCl) displayed the lowest photoluminescence signal, compared to the synthesized BiOCl and ZnO. This indicates the greatest carrier separation rate at the interface detected in the binary ZnO/BiOCl, compared to other photocatalysts. The result corelates well with the maximum photoactivity detected in the 0.05ZnO/BiOCl. High photocatalytic performance of 100% was detected under 100 min of UV light (135 W, a mercury lamp). In addition, 98% removal of TC under natural sunlight was also achieved within 240 min. The photodegradation of TC agrees perfectly with the first-order kinetic model providing a rate constant of 0.0546 min–1. This is about 1.9 times higher than those obtained from either ZnO or BiOCl photocatalysts. The binary ZnO/BiOCl heterostructure still exhibits the promising photodegradation efficiency after five runs. The scavenger experiment reveals that the photogenerated electrons are the major species which play a crucial role in TC degradation. This work emphasizes a facile route to fabricate the two-component heterostructure, with promising performance, for removal of TC antibiotic in natural water.
在BiOCl形成过程中,通过在反应混合物中加入固体ZnO,可以很容易地构建出基于ZnO/BiOCl的二元光催化剂。然后将双组分异质结应用于日光活性脱除四环素(TC)药物。合成的异质结构主要表现为BiOCl的特征XRD峰,带隙为3.50 eV,而裸BiOCl的带隙为3.30 eV。与合成的BiOCl和ZnO相比,含有0.05 g ZnO/ 1.0 g BiOCl的二元光催化剂(表示为0.05ZnO/BiOCl)的光致发光信号最低。这表明与其他光催化剂相比,二元ZnO/BiOCl在界面处检测到最大的载流子分离率。该结果与在0.05ZnO/BiOCl中检测到的最大光活性具有良好的相关性。在紫外光(135 W,汞灯)照射100 min下,检测到100%的高光催化性能。另外,在240 min内,TC的去除率也达到98%。TC的光降解完全符合一级动力学模型,速率常数为0.0546 min - 1。这比使用ZnO或BiOCl光催化剂得到的结果高1.9倍。经过5次实验后,ZnO/BiOCl二元异质结构仍表现出良好的光降解效率。清道夫实验表明,光生电子是在TC降解过程中起关键作用的主要电子种。本工作强调了一种简单的制备双组分异质结构的方法,该方法具有良好的性能,可用于去除天然水中的TC抗生素。
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引用次数: 0
Recent progress in supersaturation-based SNEDDS: Formulation, mechanism, and biopharmaceutical performance 过饱和型SNEDDS的最新进展:配方、机制和生物制药性能
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-07-16 DOI: 10.1016/j.onano.2025.100252
Sani Ega Priani , Adilah Nurhaliza , Ratih Aryani , Gofarana Wilar , Anis Yohana Chaerunisaa , Iyan Sopyan
This review highlights supersaturation-based SNEDDS (self-nanoemulsifying drug delivery systems), focusing on formulation strategies, supersaturation generation, stabilization mechanisms, and their impact on drug release, permeation, and bioavailability. The discussion is based on articles from reputable databases published between 2020 and 2025. Supersaturation-based SNEDDS are classified into supersaturable and supersaturated types, differing in the onset of supersaturation and approaches to precipitation inhibition. Widely developed for BCS Class II and IV drugs, these systems increase thermodynamic activity and enhance drug absorption in the gastrointestinal tract. Although metastable and prone to precipitation, precipitation inhibitors (PIs) such as HPMC or PVP can stabilize the supersaturated state, suppressing nucleation and crystal growth. Proper screening is essential to identify the most suitable PIs for each formulation. Supersaturable and supersaturated SNEDDS have improved drug release and intestinal permeation, enhancing bioavailability compared to pure drugs, conventional SNEDDS, or marketed formulations.
这篇综述重点介绍了基于过饱和的自纳米乳化给药系统(SNEDDS),重点是配方策略、过饱和的产生、稳定机制以及它们对药物释放、渗透和生物利用度的影响。该讨论基于2020年至2025年间发表的知名数据库中的文章。基于过饱和的SNEDDS分为过饱和型和过饱和型,在过饱和的开始和沉淀抑制的方法上有所不同。广泛用于BCS II类和IV类药物,这些系统增加了热力学活性并促进了药物在胃肠道的吸收。虽然亚稳且容易析出,但沉淀抑制剂(PIs)如HPMC或PVP可以稳定过饱和状态,抑制成核和晶体生长。适当的筛选对于确定每种制剂最合适的pi至关重要。与纯药物、传统SNEDDS或上市制剂相比,过饱和和过饱和SNEDDS改善了药物释放和肠道渗透,提高了生物利用度。
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引用次数: 0
Entrapment efficiency methodology for lipid nanoparticles – a literature review 脂质纳米颗粒的捕集效率方法-文献综述
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-07-01 DOI: 10.1016/j.onano.2025.100251
Niklas Baltz , Regina Scherließ
Lipid nanoparticles have been used for decades to deliver lipophilic drugs. The success of particle formation and drug loading is determined by excipient selection and the production process. Entrapment efficiency (EE) as a measure for process effectiveness and drug load are critical quality attributes of lipid nanoparticles. To determine EE, the nanodispersion must be separated to determine the amount of drug inside the nanoparticles or to measure the amount of un-encapsulated drug in the medium. This review systematically analyses opportunities and challenges of different EE methods. 109 studies were included. The methodology used for EE appears to be chosen on a case-by-case basis and is often reported without a thorough method description. 78 studies (72 %) reported the EE method with enough detail to readily attempt experimental reproduction. This review underlines the need for thorough reporting of the principles and method used to determine entrapment efficiency to allow data interpretation.
几十年来,脂质纳米颗粒一直被用于输送亲脂性药物。颗粒形成和药物装载的成功与否取决于辅料的选择和生产工艺。包封效率(EE)作为衡量工艺有效性和药物负荷的指标是脂质纳米颗粒的关键质量属性。为了确定EE,必须分离纳米分散体以确定纳米颗粒内的药物量或测量介质中未封装药物的量。本文系统分析了不同的情感表达方法所面临的机遇和挑战。纳入109项研究。用于情感表达的方法似乎是根据具体情况选择的,并且经常在没有详细方法描述的情况下进行报道。78项研究(72%)报告了EE方法的足够细节,可以随时尝试实验复制。这项审查强调需要全面报告用于确定捕获效率的原则和方法,以便对数据进行解释。
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引用次数: 0
Effect of unsaturated fatty acids on the topical delivery of caspofungin ufasomes: In vitro/ Ex vivo evaluation and anti-fungal study against Candida albicans 不饱和脂肪酸对caspofunins ufasomes局部递送的影响:体外/体外评估和抗白色念珠菌的研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-06-25 DOI: 10.1016/j.onano.2025.100250
Sumayah Al-Mahmood , Nawal Ayash Rajab
Cutaneous candidiasis presents a considerable challenge in today’s medical landscape, particularly for patients with weakened immune systems or chronic illnesses. As antifungal resistance continues to rise, the development of new topical therapies has become increasingly urgent. Caspofungin (CSP), an echinocandin antifungal, exhibits fungicidal activity against Candida species by inhibiting β-1,3-d-glucan synthase, a key enzyme in fungal cell wall synthesis. However, its poor stability and requirement for intravenous administration limit its clinical application. To address these limitations, novel formulations such as ufasomes (unsaturated fatty acid vesicles) have been developed to enhance caspofungin's stability and skin penetration. In this study, ufasomes were prepared using three oils: oleic acid, linoleic acid, and palmitoleic acid, along with caspofungin and cholesterol, using the thin-film method. Among the formulations, F34, composed of 500 mg palmitoleic acid and 10 mg cholesterol, exhibited promising results. It demonstrated a particle size (PS) of 87.65± 2.65 nm, a polydispersity index (PDI) of 0.22 ± 0.00, a zeta potential (ZP) of -7.46± 0.4 mV, a drug content of 97 ± 1.34 %, and an encapsulation efficiency (EE %) of 92 ± 0.82 %. Furthermore, the optimized formulation F34 showed a sustained drug release of 81.5 ± 0.4 over 600 min (10 h) compared to 100 %±0.01 of caspofungin. The permeation of F34 in 600 min (10 h) was 94 %±0.81 compared to the caspofungin 87.85 %±0.85. The antifungal activity showed that the inhibition zone diameter, MIC and MBC for caspofungin-loaded ufasomes was 29 mm±0.8, 0.153 μg/mL±0.01, 0.283 μg/mL±0.02 compared to 25 mm±0.8, 0.214 μg/mL±0.01, 0.409±0.01 for pure caspofungin. The histopathological study revealed a positive response towards the optimized formulation. In conclusion, this optimized formulation holds potential as a novel therapeutic approach for treating topical fungal infections.
皮肤念珠菌病在当今的医疗领域提出了相当大的挑战,特别是对于免疫系统较弱或慢性疾病的患者。随着抗真菌耐药性的持续上升,开发新的局部治疗方法变得越来越紧迫。Caspofungin (CSP)是一种棘白菌素抗真菌药物,通过抑制真菌细胞壁合成的关键酶β-1,3-葡聚糖合成酶,对念珠菌具有杀真菌活性。但其稳定性差,需要静脉给药,限制了其临床应用。为了解决这些限制,新的配方如不饱和脂肪酸囊泡(不饱和脂肪酸囊泡)已经被开发出来,以提高caspofunins的稳定性和皮肤渗透性。本研究以油酸、亚油酸、棕榈油酸三种油类为原料,与caspofunins、胆固醇为原料,采用薄膜法制备ufasomes。其中,由500 mg棕榈油酸和10 mg胆固醇组成的F34具有良好的效果。其粒径(PS)为87.65±2.65 nm,多分散指数(PDI)为0.22±0.00,ζ电位(ZP)为-7.46±0.4 mV,药含量为97±1.34%,包封率(EE %)为92±0.82%。优化后的F34在600 min (10 h)内的缓释量为81.5±0.4,而卡泊芬素的缓释量为100%±0.01。F34在600 min (10 h)内的通透率为94%±0.81,而caspofungin为87.85%±0.85。抑菌活性表明,载caspofunins的抑菌带直径、MIC和MBC分别为29 mm±0.8、0.153 μg/mL±0.01、0.283 μg/mL±0.02,而纯caspofunins的抑菌带直径、MIC和MBC分别为25 mm±0.8、0.214 μg/mL±0.01、0.409±0.01。组织病理学研究显示了对优化配方的积极反应。总之,这个优化的配方具有潜力作为治疗局部真菌感染的一种新的治疗方法。
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