Stabilizers

稳定器
  • 文章类型: Journal Article
    纳米技术具有巨大的发展潜力,由于其改变表面特性和粒度的能力,促进功能性食品化合物的吸收和活性物质的受控释放,以减轻不利影响。纳米乳液,通过混合油形成的稳定胶体系统,乳化剂,和水,被认为是具有广阔应用前景的纳米技术。然而,研究表面活性剂对特性纳米乳液的影响需要更加多样化。这一研究差距需要进一步探索纳米技术食品的发展。帕利约托水果(麦地那speciosa),印度尼西亚的一种本土植物,尚未对其作为功能性和营养食品的潜在用途进行广泛的审查。花青素,巴利若托水果中的主要化合物,在降低心血管疾病糖尿病的风险方面表现出了功效,展示抗炎和抗氧化特性。本研究旨在研究从帕里霍托果实提取物中提取的纳米乳液制剂的特性,并评估各种吐温表面活性剂的最佳条件。这项研究的发现可以为从帕利佐托果实提取物中进一步发展花色苷纳米乳液提供有价值的见解。结果包括纳米乳液粒径的表征,多分散指数,ζ-电位,电导率,pH值,和粘度。通过数学建模和统计方法,RSM通过检查自变量和响应变量之间的关系和相互作用来优化纳米乳液。此外,纳米乳液的表征包括ζ电位,多分散性,颗粒大小,电导率,pH值,和粘度。表面活性剂浓度升高导致粒度减小和粒度分布更均匀,尽管达到了表面活性剂聚集和胶束形成的平台。表面活性剂类型的浓度增加,浓度,和parijoto提取物影响了纳米颗粒尺寸和多分散性的物理特性。用吐温类组成的纳米乳液的最佳工艺条件为吐温80,吐温浓度为12%,和帕利霍托果实提取物浓度为7.5%,产生0.74的可取性值,将其归类为中等。
    Nanotechnology has substantial potential for development due to its ability to modify surface characteristics and particle size, facilitating enhanced absorption of functional food compounds and controlled release of active substances to mitigate adverse effects. Nanoemulsion, a stable colloidal system formed by blending oil, emulsifier, and water, was identified as nanotechnology with promising applications. However, investigations into the impact of surfactants on characteristic nanoemulsions need to be more varied. This research gap necessitated further exploration in the advancement of nanotechnology-based foods. The parijoto fruit (Medinilla speciosa), an indigenous plant species in Indonesia, has yet to undergo extensive scrutiny for its potential use as a functional and nutraceutical food. Anthocyanins, a principal compound in the parijoto fruit, had exhibited efficacy in reducing the risk of cardiovascular disease diabetes, demonstrating anti-inflammatory and antioxidant properties. This study aimed to investigate the characteristics of nanoemulsion formulations derived from parijoto fruit extract and to evaluate an optimum condition with various tween surfactants. The findings from this investigation could furnish valuable insights for the further advancement of anthocyanin nanoemulsions from parijoto fruit extract. The results comprised the characterization of nanoemulsion particle size, polydispersity index, ζ-potential, conductivity, pH, and viscosity. Through mathematical modeling and statistical methods, RSM optimizes nanoemulsion by examining the relationships and interactions between independent and response variables. Furthermore, the characterization of nanoemulsion encompassed ζ-potential, polydispersity, particle size, conductivity, pH, and viscosity. Elevated surfactant concentrations resulted in diminished particle sizes and more uniform size distribution, albeit reaching a plateau where surfactant aggregation and micelle formation ensued. Increased concentrations of surfactant type, concentration, and parijoto extract impacted the physical characteristics of nanoparticle size and polydispersity. The optimal process conditions for nanoemulsion consisting of the type of Tween used are Tween 80, Tween concentration of 12%, and parijoto fruit extract concentration of 7.5%, yielding a desirability value of 0.74, categorizing it as moderate.
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  • 文章类型: Journal Article
    染料通常在医学中用于染色细胞,组织,和细胞器。由于这些化合物也被称为光敏剂(PS),它们在光子照射时表现出光响应性,人们非常希望将这些分子配制成纳米颗粒(NP),以实现用于新型成像和治疗应用的改善的递送效率和增强的稳定性。此外,已经表明,这些分子的一些光物理性质可以在NP形成时改变,从而在其应用的结果中起主要作用。在这次审查中,我们主要专注于介绍染料类别,它们的配方策略以及这些策略如何在光热和非光热应用的背景下影响它们的光物理性质。更具体地说,最近的进展显示了染料超分子组装在光声和荧光成像等模态中的潜力,将概述光热和光动力疗法以及它们在光消融中作为一种新颖的方式。除了它们的光物理活性,我们研究了染料作为药物稳定剂的新兴应用,其中这些分子与聚集剂分子一起使用以形成稳定的纳米颗粒。
    Dyes have conventionally been used in medicine for staining cells, tissues, and organelles. Since these compounds are also known as photosensitizers (PSs) which exhibit photoresponsivity upon photon illumination, there is a high desire towards formulating these molecules into nanoparticles (NPs) to achieve improved delivery efficiency and enhanced stability for novel imaging and therapeutic applications. Furthermore, it has been shown that some of the photophysical properties of these molecules can be altered upon NP formation thereby playing a major role in the outcome of their application. In this review, we primarily focus on introducing dye categories, their formulation strategies and how these strategies affect their photophysical properties in the context of photothermal and non-photothermal applications. More specifically, the most recent progress showing the potential of dye supramolecular assemblies in modalities such as photoacoustic and fluorescence imaging, photothermal and photodynamic therapies as well as their employment in photoablation as a novel modality will be outlined. Aside from their photophysical activity, we delve shortly into the emerging application of dyes as drug stabilizing agents where these molecules are used together with aggregator molecules to form stable nanoparticles.
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  • 文章类型: Journal Article
    本研究的目的是使用纳米悬浮液开发和评估具有增加的溶解度和渗透速率的纳米氟康唑(FLZ)制剂。使用各种浓度的各种稳定剂和表面活性剂稳定FLZ纳米悬浮液。使用粒径对FLZ纳米混悬液进行了体外表征,zeta电位,X-射线粉末衍射(XRPD),和溶解度。此外,分析了FLZ通过山羊角膜的离体眼部渗透。结果显示,所有纳米混悬剂制剂的粒径在174.5±1.9至720.2±4.77nm的纳米范围内;未处理药物的粒径为18.34μm。zeta电位值是可以接受的,这表明制剂的合适稳定性。与未处理的药物相比,纳米悬浮液的溶解度高达5.7倍。FLZ纳米悬浮液的离体眼部扩散的结果显示,在使用Kollicoat稳定纳米悬浮液制剂之后,经由山羊角膜渗透的FLZ的百分比增加。因此,当使用Kollicoat的纳米混悬剂时,该药物的抗真菌活性增强。
    The aim in this study was to develop and evaluate a nanofluconazole (FLZ) formulation with increased solubility and permeation rate using nanosuspensions. The FLZ nanosuspensions were stabilized using a variety of stabilizing agents and surfactants in various concentrations. The FLZ nanosuspension was characterized in vitro using particle size, zeta potential, X-ray powder diffraction (XRPD), and solubility. In addition, the ex vivo ocular permeation of FLZ through a goat cornea was analyzed. The results showed that the particle size of all nanosuspension formulations was in the nanometer range from 174.5 ± 1.9 to 720.2 ± 4.77 nm; that of the untreated drug was 18.34 μm. The zeta potential values were acceptable, which indicated suitable stability for formulations. The solubility of the nanosuspensions was up to 5.7-fold higher compared with that of the untreated drug. The results of the ex vivo ocular diffusion of the FLZ nanosuspensions showed the percentage of FLZ penetrating via the goat cornea increased after using Kollicoat to stabilize the nanosuspension formulation. Consequently, when using a nanosuspension formulation of Kollicoat, the antifungal activity of the drug strengthens.
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  • 文章类型: Journal Article
    小分子对蛋白质-蛋白质相互作用的调节是药物发现中发展最迅速的领域之一。在这次审查中,我们讨论了过去十年(2014-2023年)的进展,重点是分子胶(MGs)-诱导接近的单价小分子,通过稳定天然相互作用或通过诱导新形态相互作用。我们包括偶然发现和理性发现,并描述了用于识别它们的不同方法。我们将化合物分为三大类:降解性MGs,非降解性MGs或PPI稳定剂,和诱导自我联想的MGs。多样化,详细描述了具有结构数据的说明性示例,强调分子识别和界面处的协同结合元素,这是MG作用机制的基础。
    The modulation of protein-protein interactions with small molecules is one of the most rapidly developing areas in drug discovery. In this review, we discuss advances over the past decade (2014-2023) focusing on molecular glues (MGs)-monovalent small molecules that induce proximity, either by stabilizing native interactions or by inducing neomorphic interactions. We include both serendipitous and rational discoveries and describe the different approaches that were used to identify them. We classify the compounds in three main categories: degradative MGs, non-degradative MGs or PPI stabilizers, and MGs that induce self-association. Diverse, illustrative examples with structural data are described in detail, emphasizing the elements of molecular recognition and cooperative binding at the interface that are fundamental for a MG mechanism of action.
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  • 文章类型: Journal Article
    这项研究旨在开发基于咪康唑的微乳剂,该乳剂使用油酸作为天然亲脂性相,并使用包含Tween20和PEG400的稳定剂混合物来溶解咪康唑作为抗真菌剂,并提高其生物利用度。配方和制备过程与使用23全因子计划的数学方法相结合。流体和凝胶状微乳液获得和分析考虑pH,电导率,和折射率,其次是对液滴大小的广泛分析,zeta电位,流变行为,和测角法.进行体外释放测试以评估其生物制药特性。独立变量编码X1-油酸(%,w/w),X2-吐温20(%,w/w),和X3-PEG400(%,w/w)与三个主要输出的关系进行了分析,如平均液滴尺寸,粘合功,通过将统计工具与响应面方法相结合,得到扩散系数。含咪康唑碱-2%的微乳液,油酸-5%,吐温20-40%,PEG400-20%,33%的水表现出119.6nm的平均液滴尺寸,71.98mN/m的附着力功,扩散系数为2.11·10-5cm2/s,以及用较高油浓度配制的两种凝胶样系统的显著属性,将微乳液的最终优化步骤建模为口腔输送的潜在系统。
    This research aimed to develop miconazole-based microemulsions using oleic acid as a natural lipophilic phase and a stabilizer mixture comprising Tween 20 and PEG 400 to solubilize miconazole as an antifungal agent known for its activity in oral candidiasis and to improve its bioavailability. The formulation and preparation process was combined with a mathematical approach using a 23-full factorial plan. Fluid and gel-like microemulsions were obtained and analyzed considering pH, conductivity, and refractive index, followed by extensive analyses focused on droplet size, zeta potential, rheological behavior, and goniometry. In vitro release tests were performed to assess their biopharmaceutical characteristics. Independent variables coded X1-Oleic acid (%, w/w), X2-Tween 20 (%, w/w), and X3-PEG 400 (%, w/w) were analyzed in relationship with three main outputs like mean droplet size, work of adhesion, and diffusion coefficient by combining statistical tools with response surface methodology. The microemulsion containing miconazole base-2%, oleic acid-5%, Tween 20-40%, PEG 400-20%, and water-33% exhibited a mean droplet size of 119.6 nm, a work of adhesion of 71.98 mN/m, a diffusion coefficient of 2.11·10-5 cm2/s, and together with remarked attributes of two gel-like systems formulated with higher oil concentrations, modeled the final optimization step of microemulsions as potential systems for buccal delivery.
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  • 文章类型: English Abstract
    OBJECTIVE: The movements and stability of the human shoulder are a complex dynamic interaction between several joints, muscles and ligaments, which on the one hand enable extensive mobility and on the other hand must provide the necessary stability. Furthermore, the complexity of the shoulder is increased by a large number of normal variants. This article aims to explain the relevant anatomical structures and the radiological examination techniques necessary to visualize them.
    UNASSIGNED: Various modalities contribute to the examination of the shoulder. These include X‑rays, computed tomography (CT), magnetic resonance imaging (MRI) and ultrasound.
    UNASSIGNED: It is important to use the various procedures appropriately. Especially with MRI arthrography, it is necessary to pay attention to suitable sequences and possibly additional examination positions.
    CONCLUSIONS: The multimodal examination of the shoulder can contribute to the diagnosis of numerous clinical pictures. Anatomical and methodological foundations are essential for this.
    UNASSIGNED: KLINISCHES PROBLEM: Die Bewegungen und Stabilität der menschlichen Schulter sind ein komplexes dynamisches Zusammenspiel zwischen mehreren Gelenken, Muskeln und Bändern, die zum einen eine umfangreiche Beweglichkeit ermöglichen, zum anderen für die nötige Stabilität sorgen müssen. Darüber hinaus wird die Komplexität der Schulter durch eine Vielzahl an Normvarianten erhöht. Dieser Artikel soll die relevanten anatomischen Strukturen sowie die zu deren Darstellung notwendigen radiologischen Untersuchungstechniken erläutern.
    UNASSIGNED: Zur Untersuchung der Schulter tragen verschiedene Modalitäten bei. Hierzu gehören die Röntgenuntersuchung, Computertomographie (CT), Magnetresonanztomographie (MRT) und der Ultraschall.
    UNASSIGNED: Es gilt die verschiedenen Verfahren passend einzusetzen. Insbesondere bei der MRT-Arthrographie ist es notwendig, auf passende Sequenzen und evtl. zusätzliche Untersuchungspositionen zu achten. EMPFEHLUNG FüR DIE PRAXIS: Die multimodale Untersuchung der Schulter kann zur Diagnose zahlreicher Krankheitsbilder beitragen. Anatomische und methodische Grundlagen sind hierfür essenziell.
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  • 文章类型: Review
    纳米悬浮液(NSps)是颗粒的胶态分散体,其具有解决与它们在水中的低溶解度或由于环境因素的不稳定性相关的活性成分的递送问题的潜力。必须考虑它们的化学成分和制备方法,因为它们直接影响药物负载,尺寸,形态学,溶解度,和稳定性;纳米混悬剂的这些特性影响活性成分的递送和生物利用度。NSps提供高负荷的药物,防止降解剂,快速溶解,高颗粒稳定性,和活性成分在生物膜上的高生物利用度。此外,与其他纳米载体相比,它们的毒性较低,如脂质体或聚合物纳米颗粒,并且可以改变药代动力学曲线,从而提高其安全性和有效性。本审查旨在解决与NSps组成有关的所有方面,不同的生产方法,以及影响其稳定性的主要因素。此外,最近的研究被描述为活性成分的载体及其生物活性。
    Nanosuspensions (NSps) are colloidal dispersions of particles that have the potential to solve the delivery problems of active ingredients associated with their low solubility in water or instability due to environmental factors. It is essential to consider their chemical composition and preparation methods because they directly influence drug loading, size, morphology, solubility, and stability; these characteristics of nanosuspensions influence the delivery and bioavailability of active ingredients. NSps provides high loading of drugs, protection against degrading agents, rapid dissolution, high particle stability, and high bioavailability of active ingredients across biological membranes. In addition, they provide lower toxicity compared to other nanocarriers, such as liposomes or polymeric nanoparticles, and can modify the pharmacokinetic profiles, thus improving their safety and efficacy. The present review aims to address all aspects related to the composition of NSps, the different methods for their production, and the main factors affecting their stability. Moreover, recent studies are described as carriers of active ingredients and their biological activities.
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  • 文章类型: Journal Article
    野生型转甲状腺素蛋白(TTR)和超过130种遗传TTR变体的聚集是一组致命疾病的基础,称为TTR淀粉样变性(ATTR)。TTR化学伴侣是对改变ATTR进展过程具有巨大前景的分子。在以往的研究中,我们结合了合理的设计和分子动力学模拟,以产生一系列TTR选择性动力学稳定剂,显示出极高的亲和力。为了支持先前开发的具有最佳药代动力学特性的分子,我们进行了结构设计优化,导致PITB的发展。PITB以高亲和力结合TTR,有效抑制野生型蛋白和两种最普遍的疾病相关TTR变体的四聚体解离和聚集。重要的是,PITB选择性结合并稳定血浆中的TTR,胜过托卡彭,目前正在接受ATTR临床试验的药物。对小鼠进行的药代动力学研究证实,PITB表现出令人鼓舞的药代动力学特性,正如最初的意图。此外,PITB显示出优异的口服生物利用度和缺乏毒性。这些组合属性将PITB定位为未来临床试验的先导化合物,作为ATTR的疾病改善疗法。
    The aggregation of wild-type transthyretin (TTR) and over 130 genetic TTR variants underlies a group of lethal disorders named TTR amyloidosis (ATTR). TTR chemical chaperones are molecules that hold great promise to modify the course of ATTR progression. In previous studies, we combined rational design and molecular dynamics simulations to generate a series of TTR selective kinetic stabilizers displaying exceptionally high affinities. In an effort to endorse the previously developed molecules with optimal pharmacokinetic properties, we conducted structural design optimization, leading to the development of PITB. PITB binds with high affinity to TTR, effectively inhibiting tetramer dissociation and aggregation of both the wild-type protein and the two most prevalent disease-associated TTR variants. Importantly, PITB selectively binds and stabilizes TTR in plasma, outperforming tolcapone, a drug currently undergoing clinical trials for ATTR. Pharmacokinetic studies conducted on mice confirmed that PITB exhibits encouraging pharmacokinetic properties, as originally intended. Furthermore, PITB demonstrates excellent oral bioavailability and lack of toxicity. These combined attributes position PITB as a lead compound for future clinical trials as a disease-modifying therapy for ATTR.
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  • 文章类型: Journal Article
    研究了源自热处理和高压均质化泥的水相(血清)相的水溶性生物聚合物的乳液形成和稳定能力。对血清生物聚合物进行表征,然后在简单的水包油乳液中用作乳化剂/稳定剂。将所得乳液在4°C下储存并监测2周。结果表明,与西兰花相比,胡萝卜和番茄血清中的果胶含量更高,蛋白质含量更低。血清果胶生物聚合物表现出不同的分子结构,取决于蔬菜的来源。鉴于这些天然生物聚合物的组成和特性,在pH3.5时观察到小液滴大小的乳液。然而,乳液在pH6.0显示大的平均液滴尺寸,除了用胡萝卜血清配制的乳液。不管pH值如何,含有胡萝卜血清生物聚合物的乳液表现出很高的形成精细乳液的能力,这些乳液在低温下储存2周期间是稳定的。这项研究清楚地表明,从蔬菜泥的血清相中分离出的天然水溶性生物聚合物形成细乳液液滴并在储存期间保持其稳定性的能力,尤其是在胡萝卜血清生物聚合物的情况下。
    The emulsion forming and stabilizing capacities of water-soluble biopolymers originating from the aqueous (serum) phase of heat-treated and high pressure homogenized purées were investigated. The serum biopolymers were characterized and then utilized as emulsifier/stabilizer in simple oil-in-water emulsions. The resulting emulsions were stored at 4 °C and monitored for 2 weeks. Results revealed that carrot and tomato sera contained higher amounts of pectin and lower protein compared to broccoli. The serum pectic biopolymers exhibited distinct molecular structures, depending on the vegetable origin. Given these natural biopolymer composition and characteristics, emulsions with small droplet sizes were observed at pH 3.5. However, emulsions at pH 6.0 showed large mean droplet sizes, except for the emulsion formulated with carrot serum. Regardless of the pH, emulsions containing carrot serum biopolymers exhibited high capacity to form fine emulsions that were stable during the 2-week storage period at low temperature. This study clearly shows the capacity of natural water-soluble biopolymers isolated from the serum phase of vegetable purées to form fine emulsion droplets and maintain its stability during storage, especially in the case of carrot serum biopolymers.
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  • 文章类型: Journal Article
    植物化学品,如白藜芦醇,姜黄素,还有槲皮素,对健康有很多好处,但是由于它们的水溶性和稳定性差,它们中的大多数具有低生物利用度,快速新陈代谢,和间隙,这限制了其潜在的应用范围。为了克服这些问题,不同类型的纳米粒子(NPs),特别是生物相容性和可生物降解的NP,已经开发了。NP可以携带植物化学物质并增加其溶解度,稳定性,目标特异性,和口服生物利用度。然而,NP容易发生不可逆的聚集,导致NP不稳定和功能丧失。为了弥补这个缺点,稳定剂如聚合物和表面活性剂被引入到NP上。稳定剂不仅增加了NP的稳定性,但也改善了他们的特点。当前的评论集中在讨论合成基于植物化学的NP及其常用稳定剂的研究中的最新技术。此外,还讨论了这些NP中的稳定剂的应用,影响,和潜在的机制。本综述旨在为未来稳定剂和NPs的开发提供更多的参考。
    Phytochemicals, such as resveratrol, curcumin, and quercetin, have many benefits for health, but most of them have a low bioavailability due to their poor water solubility and stability, quick metabolism, and clearance, which restricts the scope of their potential applications. To overcome these issues, different types of nanoparticles (NPs), especially biocompatible and biodegradable NPs, have been developed. NPs can carry phytochemicals and increase their solubility, stability, target specificity, and oral bioavailability. However, NPs are prone to irreversible aggregation, which leads to NP instability and loss of functions. To remedy this shortcoming, stabilizers like polymers and surfactants are incorporated on NPs. Stabilizers not only increase the stability of NPs, but also improve their characteristics. The current review focused on discussing the state of the art in research on synthesizing phytochemical-based NPs and their commonly employed stabilizers. Furthermore, stabilizers in these NPs were also discussed in terms of their applications, effects, and underlying mechanisms. This review aimed to provide more references for developing stabilizers and NPs for future research.
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