micelle

胶束
  • 文章类型: Journal Article
    目前,人们对促进健康的食品越来越感兴趣。卫生专业人员和营养学家积极倡导食品对人类健康的有益作用。这种日益增长的意识正在影响越来越多的功能性食品和对更多创新解决方案的追求。最近的研究表明,球形纳米颗粒具有在食品工业中用作功能生物材料的潜力,特别是用于封装疏水性天然植物化学物质。基于微米和纳米封装的技术和系统在食品和制药工业中非常重要。最重要的是封装材料在食品中的使用是安全的。这项研究的目的是使用蛋黄粉(EYP)进行乳化(作为卵磷脂的来源)和蛋清粉(EWP)进行稳定,以获得含有苦莓果渣提取物的胶束。使用傅里叶变换红外光谱(FTIR)表征所得粉末中胶束的结构性质。扫描电子显微镜(SEM)分析证实存在大小在500和1000nm之间的球形胶束结构。测定所得粉末的水活度和含水量,并研究了热(DSC)和抗氧化性能。结果表明,与通过不使用包封技术的简单混合获得的粉末相比,具有胶束结构的粉末具有更高的稳定性。
    There is currently a growing interest in health-promoting foods. The beneficial effects of food on human health are actively promoted by health professionals and nutritionists. This growing awareness is influencing the increasing range of functional foods and the pursuit of more innovative solutions. Recent research indicates that spherical nanoparticles have the potential to be used as functional biomaterials in the food industry, particularly for encapsulating hydrophobic natural phytochemicals. Techniques and systems based on micro- and nano-encapsulation are of great importance in the food and pharmaceutical industries. It is of paramount importance that encapsulation materials are safe for use in food. The aim of this study was to obtain micelles containing extracts from chokeberry fruit pomace using egg yolk powder (EYP) for emulsification (as a source of lecithin) and egg white powder (EWP) for stabilisation. The structural properties of the micelles in the resulting powders were characterised using Fourier transform infrared spectroscopy (FTIR). Scanning electron microscopy (SEM) analysis confirmed the presence of spherical micellar structures between 500 and 1000 nm in size. The water activity and water content of the obtained powders were determined, and the thermal (DSC) and antioxidant properties were investigated. The results indicated that the powder with the micellar structures had a higher stability compared to the powder obtained by simple mixing without the use of encapsulation techniques.
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  • 文章类型: Journal Article
    水凝胶是我们日常生活中最常用的材料之一,具有交联的三维网络结构,能够吸收大量流体。由于其突出的性能,比如灵活性,可调谐性,和生物相容性,水凝胶已广泛应用于生物医学研究和临床,特别是按需药物释放。然而,传统的水凝胶面临各种限制,例如,由于其高度亲水的内部环境,疏水性药物的递送。因此,已经设计和开发了含胶束的水凝胶,它具有亲水和疏水的微环境,能够储存不同的货物。基于胶束的功能,这些水凝胶可以分为胶束掺杂和化学/物理交联类型,据报道对各种刺激有反应,包括温度,pH值,辐照,电信号,磁场,等。这里,我们总结了含胶束水凝胶的研究进展,并根据我们自己实验室和其他机构的最新研究,对其在生物医学领域的应用提供了展望。
    Hydrogels are one of the most commonly used materials in our daily lives, which possess crosslinked three-dimensional network structures and are capable of absorbing large amounts of fluid. Due to their outstanding properties, such as flexibility, tunability, and biocompatibility, hydrogels have been widely employed in biomedical research and clinics, especially in on-demand drug release. However, traditional hydrogels face various limitations, e.g., the delivery of hydrophobic drugs due to their highly hydrophilic interior environment. Therefore, micelle-containing hydrogels have been designed and developed, which possess both hydrophilic and hydrophobic microenvironments and enable the storage of diverse cargos. Based on the functionalities of micelles, these hydrogels can be classified into micelle-doped and chemically/physically crosslinked types, which were reported to be responsive to varied stimuli, including temperature, pH, irradiation, electrical signal, magnetic field, etc. Here, we summarize the research advances of micelle-containing hydrogels and provide perspectives on their applications in the biomedical field based on the recent studies from our own lab and others.
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  • 文章类型: Journal Article
    目的:使用多臂两亲性嵌段共聚物开发强大的药物递送系统,以增强癌症治疗的功效。材料和方法:两个系列的两亲聚合物胶束,PEG-b-PCLm和PEG-b-PCLm/TPGS,是合成的。通过溶剂透析实现阿霉素(DOX)加载到胶束中。结果:胶束表现出优异的生物相容性,窄尺寸分布,和均匀的形态。与游离DOX相比,负载DOX的胶束表现出增强的抗肿瘤功效和在肿瘤部位的药物积累增加。此外,图4A-PEG47-b-PCL21/TPGS胶束有效抑制耐药性MCF-7/ADR细胞。结论:本研究介绍了一种新型胶束制剂,具有出色的血清稳定性和抗耐药性的功效,有望用于癌症治疗。它强调了完善临床翻译和确保体内持续疗效和安全性的创新策略。
    [方框:见正文]。
    Aim: To develop a robust drug-delivery system using multi-arm amphiphilic block copolymers for enhanced efficacy in cancer therapy. Materials & methods: Two series of amphiphilic polymer micelles, PEG-b-PCLm and PEG-b-PCLm/TPGS, were synthesized. Doxorubicin (DOX) loading into the micelles was achieved via solvent dialysis. Results: The micelles displayed excellent biocompatibility, narrow size distribution, and uniform morphology. DOX-loaded micelles exhibited enhanced antitumor efficacy and increased drug accumulation at tumor sites compared with free DOX. Additionally, 4A-PEG47-b-PCL21/TPGS micelles effectively suppressed drug-resistant MCF-7/ADR cells. Conclusion: This study introduces a novel micelle formulation with exceptional serum stability and efficacy against drug resistance, promising for cancer therapy. It highlights innovative strategies for refining clinical translation and ensuring sustained efficacy and safety in vivo.
    [Box: see text].
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  • 文章类型: Journal Article
    奥洛他定(OLP)被广泛用作有效的抗组胺药物,用于减轻与过敏性结膜炎相关的眼部瘙痒。由于它在药店的频繁使用,迫切需要一种具有成本效益的,容易实现,高灵敏度的环境可持续检测方法。这项研究提出了一种新颖的荧光信号检测方法,用于检测纯形式和房水的OLP。所提出的方法依赖于增强OLP的弱本征荧光发射,与固有荧光相比,实现高达680%的显着增加。通过使用乙酸盐缓冲液(pH3.6)并掺入十二烷基硫酸钠(SDS)表面活性剂的溶液在质子化的OLP周围形成胶束来实现这种增强。在OLP的浓度与1.0至100.0ngmL-1的荧光强度之间观察到强相关性(R=0.9996),检测限为0.22ngmL-1。该方法成功地用于定量粉末形式和药物滴眼剂的OLP。此外,它在确定人工房水中的OLP方面表现出稳健的性能,回收率为99.05±1.51,基质干扰物的干扰最小。此外,评价所述方法的绿色度。
    Olopatadine (OLP) is widely utilized as an effective antihistaminic drug for alleviating ocular itching associated with allergic conjunctivitis. With its frequent usage in pharmacies, there arises a pressing need for a cost-effective, easily implementable, environmentally sustainable detection method with high sensitivity. This study presents a novel signal-on fluorimetric method for detecting OLP in both its pure form and aqueous humor. The proposed approach depends on enhancing the weak intrinsic fluorescence emission of OLP, achieving a remarkable increase of up to 680% compared to its intrinsic fluorescence. This enhancement is achieved by forming micelles around protonated OLP using an acetate buffer (pH 3.6) and incorporating a solution of sodium dodecyl sulfate (SDS) surfactant. A strong correlation (R = 0.9996) is observed between the concentration of OLP and fluorescence intensities ranging from 1.0 to 100.0 ng mL-1 with a limit of detection of 0.22 ng mL-1. This described method is successfully employed for quantifying OLP in both its powder form and pharmaceutical eye drops. Furthermore, it demonstrates robust performance in determining OLP in artificial aqueous humor with a percentage recovery of 99.05 ± 1.51, with minimal interference from matrix interferents. Moreover, the greenness of the described method was evaluated.
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  • 文章类型: Journal Article
    赖氨酸是蛋白质表面上最丰富的残基之一,其位点选择性官能化极具挑战性。现有的功能化方法依赖于赖氨酸对蛋白质的差异反应性,使得不可能选择性地标记反应性较低的赖氨酸。我们在这里报道了模拟蛋白质翻译后修饰中涉及的酶的聚合物纳米颗粒,这些酶可以区分赖氨酸的化学和超分子环境,并将标记试剂精确地传递到其ε氨基。通过可交联表面活性剂胶束的分子印迹制备纳米粒子,加上一个原位,在压印之前肽模板的胶束上衍生化。这些程序对聚合物纳米颗粒进行编码,具有序列识别和精确标记所需的所有超分子信息,允许在混合物中的靶蛋白上的预定赖氨酸的单位点官能化。
    Lysine is one of the most abundant residues on the surface of proteins and its site-selective functionalization is extremely challenging. The existing methods of functionalization rely on differential reactivities of lysine on a protein, making it impossible to label less reactive lysines selectively. We here report polymeric nanoparticles that mimic enzymes involved in the posttranslational modifications of proteins that distinguish the chemical and supramolecular contexts of a lysine and deliver the labeling reagent precisely to its ε amino group. The nanoparticles are prepared through molecular imprinting of cross-linkable surfactant micelles, plus an in situ, on-micelle derivatization of the peptide template prior to the imprinting. The procedures encode the polymeric nanoparticles with all the supramolecular information needed for sequence identification and precise labeling, allowing single-site functionalization of a predetermined lysine on the target protein in a mixture.
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  • 文章类型: Journal Article
    载体材料总是占大多数,特别是在纳米配方中,与活性成分部分一起施用可能导致代谢相关的毒性。生物活性赋形剂的使用不仅可以降低副作用,而且还可以提供额外的治疗效果。在本研究中,使用生物活性茄尼醇衍生物开发了基于三萜的胶束药物递送系统。首先制备溶剂胺,然后使用马来酸酰胺键与聚(乙二醇)缀合。两亲性药物载体聚乙二醇化(2-丙基-3-甲基马来酸)-嵌段-茄尼醇胺(mPEG-CDM-NH-SOL)可以形成胶束,并在内部负载多柔比星(DOX)。胶束的尺寸为约112nm,并且载药量为约5.97wt%。对于负载DOX的pH敏感胶束mPEG-CDM-NH-SOL-DOX明显观察到酸触发的药物释放行为。而对于没有pH敏感性的DOX负载胶束(mPEG-NHS-NH-SOL)则没有。CCK8实验表明,聚乙二醇化茄尼胺胶束在高浓度下对肿瘤细胞有一定的抑制作用,pH敏感的胶束似乎更具毒性。体内研究表明,pH敏感型mPEG-CDM-NH-SOL-DOX具有优越的抗肿瘤作用,表明其在癌症治疗中的巨大潜力。
    Carrier materials always account for the majority particularly in nanosized formulations, which are administrated along with the active ingredient part might result in metabolism related toxicity. The usage of bioactive excipients could not only reduce the sided effect but also provide additional therapeutic effects. In the present study, a triterpene based micellar drug delivery system was developed using a bioactive solanesol derivative. Solanesylamine was prepared firstly followed by conjugating with poly (ethylene glycol) using maleic acid amide linkage. The amphiphilic drug carrier PEGylated (2-propyl-3-methylmaleic acid)-block-solanesol amine (mPEG-CDM-NH-SOL) could be formed into micelles and loaded with doxorubicin (DOX) inside. The micelles were about 112 nm in size and the drug loading content was about 5.97 wt%. An acid triggered drug release behavior was obviously observed for the DOX loaded pH-sensitive micelle mPEG-CDM-NH-SOL-DOX. While not for DOX-loaded micelles without pH-sensitivity (mPEG-NHS-NH-SOL). CCK8 assay showed that the micelles of PEGylated solanesylamines exhibited certain inhibitory effect on tumor cells at high concentration and the pH sensitive ones seemed more toxic. In vivo studies showed that the pH sensitive mPEG-CDM-NH-SOL-DOX had a superior anti-tumor effect, indicating its great potential in cancer treatment.
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  • 文章类型: Journal Article
    有效应对复杂病理状况的关键方面之一是在空间和时间上精确地递送所需的治疗化合物。因此,对核靶向运载系统的关注已经成为一项潜力巨大的有希望的战略,特别是在基因治疗和癌症治疗中。这里,我们探索了超分子纳米组装体作为载体的设计,以将特定化合物传递到细胞核,特别关注暴露核定位信号的聚合物和基于肽的载体。这样的纳米组装体旨在最大化细胞核内遗传和治疗剂的浓度,从而优化治疗结果,同时最小化脱靶效应。复杂的情况,包括细胞摄取,内体逃逸,和核易位,需要微调纳米载体的属性。首先,我们介绍了核导入的原理和核孔复合物的作用,揭示了纳米系统靶向核的策略。然后,我们概述了依赖于核定位以实现最佳活性的货物,因为它们的完整性和积累是设计合适的输送系统时需要考虑的关键参数。考虑到他们正处于研究的早期阶段,我们提出了各种货物负载的肽和聚合物纳米组装,促进核靶向,强调它们增强治疗反应的潜力。最后,我们简要讨论了更精确和有效的核输送的进一步进展。
    One of the key aspects of coping efficiently with complex pathological conditions is delivering the desired therapeutic compounds with precision in both space and time. Therefore, the focus on nuclear-targeted delivery systems has emerged as a promising strategy with high potential, particularly in gene therapy and cancer treatment. Here, we explore the design of supramolecular nanoassemblies as vehicles to deliver specific compounds to the nucleus, with the special focus on polymer and peptide-based carriers that expose nuclear localization signals. Such nanoassemblies aim at maximizing the concentration of genetic and therapeutic agents within the nucleus, thereby optimizing treatment outcomes while minimizing off-target effects. A complex scenario of conditions, including cellular uptake, endosomal escape, and nuclear translocation, requires fine tuning of the nanocarriers\' properties. First, we introduce the principles of nuclear import and the role of nuclear pore complexes that reveal strategies for targeting nanosystems to the nucleus. Then, we provide an overview of cargoes that rely on nuclear localization for optimal activity as their integrity and accumulation are crucial parameters to consider when designing a suitable delivery system. Considering that they are in their early stages of research, we present various cargo-loaded peptide- and polymer nanoassemblies that promote nuclear targeting, emphasizing their potential to enhance therapeutic response. Finally, we briefly discuss further advancements for more precise and effective nuclear delivery.
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  • 文章类型: Journal Article
    三重态-三重态湮没上转换(TTA-UC)的当前研究面临诸如有机溶剂的过度使用和分子氧对激发的三重态敏化剂的猝灭等困难。在这里,为了克服这些问题,我们提出了一种高效,简便的TTA-UC微乳制备策略。设备简单,制备过程短,在由TritonX114,四氢呋喃和上转换发色团(铂八乙基卟啉和9,10-二苯基蒽)共组装的微乳液中,实现了空气稳定的TTA-UC,上转换效率高达16.52%。这与TTA-UC微乳液体系有史以来报道的最高UC效率相当。TX114-THF的优异UC性能可归因于两个方面。首先,小尺寸胶束容纳发色团在有机相中达到高浓度,这促进了有效的分子碰撞。此外,532nm处的高吸收率确保了激发光的充分利用,获得更多的长波长光子参与TTA-UC过程。此外,空气稳定的TTA-UC在具有各种表面活性剂的微乳液中也表现良好,包括非离子表面活性剂(吐温20,吐温80,TritonX-110,TritonX-114),离子表面活性剂(十二烷基硫酸钠,十六烷基三甲基溴化铵)和嵌段共聚物(pluronicF127,pluronicP123),根据表面活性剂分子的结构特征,通过三个猜想组装模型(浓缩,未压实和分散)。这些发现可为TTA-UC相关领域表面活性剂的选择提供参考。
    Current research of triplet-triplet annihilation upconversion (TTA-UC) faces difficulty such as overuse of organic solvents and quenching of excited triplet sensitizers by molecular oxygen. Herein, we propose an efficient and facile preparation strategy of TTA-UC microemulsion to overcome these issues. With simple device and short preparation process, air-stable TTA-UC with a high upconversion efficiency of 16.52% was achieved in microemulsion coassembled from TritonX114, tetrahydrofuran and upconverting chromophores (platinum octaethyl-porphyrin and 9,10-diphenylanthracene). This is comparable to the highest UC efficiency ever reported for TTA-UC microemulsion systems. The excellent UC performance of TX114-THF could be attributed to two perspectives. Firstly, small-size micelle accommodated chromophores up to high concentrations in organic phase, which promoted efficient molecular collision. Additionally, high absorbance at 532 nm ensured full use of excitation light, getting more long wavelength photons involved in the TTA-UC process. Moreover, air-stable TTA-UC also performed well in microemulsion with various surfactants, including nonionic surfactants (Tween 20, Tween 80, Triton X-110, Triton X-114), ionic surfactants (sodium dodecyl sulfate, cetyltrimethyl ammonium bromide) and block copolymers (pluronic F127, pluronic P123), through three conjectural assembly models according to the structural characteristics of surfactant molecules (concentrated, uncompacted and scattered). These discoveries could provide estimable reference for selection of surfactants in relevant fields of TTA-UC.
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  • 文章类型: Journal Article
    已经开发了一种高度敏感的胶束诱导的感觉,用于检测长链醛作为呼吸道癌症的潜在生物标志物。通过CTAB和S2表面活性剂的部分自组装制备了胶束状传感器,含有荧光肼官能化染料(Naph-NH2)。原则上,具有两亲特性的长链醛充当诱导配合表面活性剂,形成良好包埋的胶束颗粒,以及与Naph-NH2反应形成腙衍生物,导致荧光增强。胶束Naph-NH2/CTAB/S2平台的检测限(LOD)计算为〜64.09-80.98µM,用于检测长链醛,在肺癌细胞(A549)中显示荧光成像。这种胶束感觉探针证明了在人血液样品中长链醛传感的实际适用性,可接受的回收率为〜94.02-102.4%。超越Naph-NH2/CTAB/S2传感器,milcellar混合传感器是通过将胶束样平台与超分子凝胶结合到基于羧酸盐的胶凝剂(Gel1),灵敏度提高了十倍。期望,通过这些传感平台确定长链醛对于即时癌症诊断和治疗具有重要的前景.
    A highly sensitive micelle-induced sensory has been developed for detection of long-chain aldehydes as potential biomarkers of respiratory cancers. The micelle-like sensor was fabricated through the partial self-assembly of CTAB and S2 surfactants, containing a fluorescent hydrazine-functionalized dye (Naph-NH2). In principle, long-chain aldehydes with amphiphilic character act as the induced-fit surfactants to form well-entrapped micellar particles, as well as react with Naph-NH2 to form hydrazone derivatives resulting in fluorescent enhancement. The limit of detection (LOD) of micellar Naph-NH2/CTAB/S2 platform was calculated to be ∼  64.09-80.98 µM for detection of long-chain aldehydes, which showed fluorescent imaging in lung cancer cells (A549). This micellar sensory probe demonstrated practical applicability for long-chain aldehyde sensing in human blood samples with an accepted percent recovery of ~ 94.02-102.4%. Beyond Naph-NH2/CTAB/S2 sensor, the milcellar hybrid sensor was successfully developed by incorporating a micelle-like platform with supramolecular gel regarding to carboxylate-based gelators (Gel1), which showed a tenfold improvement in sensitivity. Expectedly, the determination of long-chain aldehydes through these sensing platforms holds significant promise for point-of-care cancer diagnosis and therapy.
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  • 文章类型: Journal Article
    由于细胞毒性,离子洗涤剂能够在生物圈中应用并造成伤害。离子和非离子去污剂头部基团之间的共价组合在调节细胞毒性中的效用仍然是推测性的,因为还很少探索合成。我们缩小了这一差距,建立了离子/非离子混合洗涤剂的模块化合成。我们将组合的甲基烯丙基二氯一锅法偶联重组为两步偶联,这减少了副产品,提高产品产量,并实现了不对称的克级制备,阳离子/非离子和阴离子/非离子混合洗涤剂。我们的模块化合成为离子洗涤剂的设计提供了新的模式,包括确定应用程序的属性的前所未有的扩展,如电荷,临界胶束浓度(cmc),增溶性能,硬水耐受性,和细胞相容性。我们发现,屏蔽离子头基中的电荷可以将对细胞有毒的洗涤剂物种从单体转换为单体和胶束组件的混合物。建立离子/非离子混合洗涤剂的化学提供了离子和非离子洗涤剂的结构比较中缺失的进化环节,能够轻松合成不对称混合材料的尚未开发的化学空间,并为设计超分子纳米材料的毒性提供了新的模式。
    Ionic detergents enable applications and cause harm in biospheres due to cell toxicity. The utility of covalent combinations between ionic and non-ionic detergent headgroups in modulating cell toxicity remains speculative due to the yet rarely explored synthesis. We close this gap and establish the modular synthesis of ionic/non-ionic hybrid detergents. We restructure a combinatorial methallyl dichloride one-pot coupling into a two-step coupling, which reduces by-products, improves product yields, and enables the gram-scale preparation of asymmetric, cationic/non-ionic and anionic/non-ionic hybrid detergents. Our modular synthesis delivers new modalities for the design of ionic detergents, including an unprecedented scaling of properties that determine applications, such as charge, critical micelle concentration, solubilizing properties, hard water tolerance, and cell compatibility. We uncover that shielding the charge in ionic headgroups can switch the detergent species that is toxic to cells from monomers to mixtures of monomers and micellar assemblies. Establishing the chemistry of ionic/non-ionic hybrid detergents provides a missing evolutionary link in the structural comparison of ionic and non-ionic detergents, enables an easy synthesis access to yet unexplored chemical spaces of asymmetric hybrid materials, and delivers new modalities for designing the toxicity of supramolecular nanomaterials.
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