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Preparation and biochemical evaluation of daily-thiosulfinate/polyoxyethylene conjugated pH-responsive micelle with enhanced stability, hydrosolubility and antibacterial properties 具有更高的稳定性、水溶性和抗菌性的日硫代硫酸酯/聚氧乙烯共轭 pH 响应胶束的制备和生化评估
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-17 DOI: 10.1007/s00396-024-05298-z
Souptik Bhattacharya, Sayamdipta DasChowdhury

Diallyl thiosulfinate (DT), a major organosulfur chemical with several notable therapeutic characteristics, is highly unstable and easily degradable which restricts its extensive use in biopharmaceutical commodities. Therefore, utilizing the self-assembly nature of polyoxyethylene (Brij S20 and Brij 58), appropriate pH-responsive micelle carrier systems have been designed to entrap and improve DT’s stability at an ambient temperature (25 °C) while preserving its quantity and biological activity. Comparing with the Brij S20 with the Brij 58 micelle carrier system, the latter demonstrated superior stability and entrapment of DT. In addition, it was found that DT’s stability in micellized condition is significantly influenced by both pH and temperature (p < 0.05). The micelle system was capable enough to reduce degradation significantly. Additionally, the liberation of DT from micelle is greatly aided by acidic pH 1.5. Around 77% DT was released from Brij 58 system. Various biochemical analyses were done. The liberation of DT from the micelle in a controlled manner using lower pH as stimuli may facilitate its biological action at an individual’s gastrointestinal lumen or near cancer cell environment having lower pH. Additionally, it was made sure that the micellization method did not impair DT’s bioactivity or reduce appropriate biocompatibility. The current study increases the likelihood of creating a commercially available DT-loaded, micelle-based formulation for application in biopharma and food-related industries.

Graphical Abstract

硫代硫酸二烯丙酯(DT)是一种主要的有机硫化学品,具有多种显著的治疗特性,但它极不稳定且容易降解,这限制了它在生物制药商品中的广泛应用。因此,我们利用聚氧乙烯(Brij S20 和 Brij 58)的自组装特性,设计了适当的 pH 响应胶束载体系统,以在保持 DT 的数量和生物活性的同时,夹带 DT 并提高其在环境温度(25 °C)下的稳定性。与 Brij S20 和 Brij 58 胶束载体系统相比,后者显示出更高的稳定性和对 DT 的吸附能力。此外,研究还发现 DT 在胶束化条件下的稳定性受到 pH 值和温度的显著影响(p < 0.05)。胶束系统能够显著减少降解。此外,pH 值为 1.5 的酸性环境对 DT 从胶束中的释放有很大帮助。大约 77% 的 DT 从 Brij 58 系统中释放出来。进行了各种生化分析。利用较低的 pH 值作为刺激,以可控方式从胶束中释放 DT,这可能会促进 DT 在个人胃肠道腔内或 pH 值较低的癌细胞环境附近的生物作用。此外,还要确保胶束化方法不会损害 DT 的生物活性或降低适当的生物相容性。目前的研究提高了开发出商用 DT 胶束制剂的可能性,该制剂可应用于生物制药和食品相关行业。
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引用次数: 0
Synthesis and characterization of cellulose nanocrystals derived from ginger stick for berberine delivery: exploring interactions with human holo-transferrin 用于递送小檗碱的姜汁纤维素纳米晶体的合成与表征:探索与人类全转铁蛋白的相互作用
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-17 DOI: 10.1007/s00396-024-05297-0
Samaneh Tavana, Alaleh Riyahi, Shadi Nikjoo, Sahar Shafi-Moghaddam, Reza Taheri, Zahra Akhavannezhad, Parisa Mokaberi, Jamshidkhan Chamani

As an antioxidative isoquinoline quaternary alkaloid, berberine (BR) is derived from certain types of plants, such as Berberis aristate, and despite its ability to inhibit cell proliferation, its poor aqueous solubility has limited its effectiveness in treatments. This study attempted to extract cellulose nanocrystals (CNCs) from ginger sticks to perform BR delivery and proceeded by characterizing the prepared CNCs and CNCs-BR by the results of DLS, TEM, FESEM, XRD, and FTIR. Moreover, various biophysical methods were used to investigate the interaction of BR-loaded CNCs with human serum holo-transferrin (HTF). The obtained outcomes confirmed the effectiveness of our spherical CNCs in reducing the size of the drug from 403.06 to 203.42 nm in CNCs-BR and consequently improving the solubility of BR. The XRD analysis approved the successful elimination of amorphous regions in cellulose, while the diminution of crystallinity index after the loading of BR indicated the occurrence of their interaction. The induced alterations in the functional groups and hydrophilicity enhancement of CNCs and CNCs-BR were displayed by FTIR. The fluorescence studies indicated the capability of CNCs-BR in interacting with HTF and quenching its fluorescence emission intensity through a static quenching process, which was revealed by the inverse correlation between Ksv values and temperature. In conformity to the results of synchronous fluorescence spectroscopy, CNCs-BR caused more changes in the vicinity of Trp residue in contrast to Tyr, while the FRET analysis determined the energy transfer between HTF and CNCs-BR to be 0.18, and their distance to be 2.41 nm. The drawn conclusion from these observations confirmed the suitability of CNCs as a carrier for BR along with their improved bioavailability caused by the effective interaction between HTF and BR-loaded CNCs. The results also showed that loading BR on CNCs not only improved its water solubility but also led to a sustained release behavior in a simulated gastrointestinal condition of the body.

Graphical abstract

小檗碱(BR)是一种具有抗氧化作用的异喹啉季生物碱,提取自某些类型的植物,如小檗,尽管它具有抑制细胞增殖的能力,但其较差的水溶性限制了其在治疗中的有效性。本研究尝试从生姜条中提取纤维素纳米晶体(CNCs)来进行 BR 递送,并通过 DLS、TEM、FESEM、XRD 和 FTIR 对制备的 CNCs 和 CNCs-BR 进行表征。此外,还使用了多种生物物理方法来研究负载了溴代苯的氯化萘与人血清全转铁蛋白(HTF)的相互作用。结果证实,我们的球形 CNCs 能有效地将 CNCs-BR 中药物的尺寸从 403.06 纳米减小到 203.42 纳米,从而提高 BR 的溶解度。XRD 分析表明,纤维素中的无定形区域被成功消除,而负载 BR 后结晶度指数的降低则表明二者发生了相互作用。傅立叶变换红外光谱(FTIR)显示了 CNCs 和 CNCs-BR 的官能团变化和亲水性增强。荧光研究表明,CNCs-BR 能够与 HTF 发生相互作用,并通过静态淬灭过程淬灭 HTF 的荧光发射强度,Ksv 值与温度之间的反相关关系也揭示了这一点。与同步荧光光谱的结果一致,CNCs-BR 在 Trp 残基附近引起的变化比 Tyr 更多,而 FRET 分析确定 HTF 与 CNCs-BR 之间的能量传递为 0.18,它们之间的距离为 2.41 nm。通过这些观察得出的结论证实了 CNCs 适合作为 BR 的载体,而且 HTF 与负载 BR 的 CNCs 之间的有效相互作用提高了 BR 的生物利用率。研究结果还表明,在 CNCs 上负载 BR 不仅能提高其水溶性,还能在模拟人体胃肠道条件下实现持续释放。
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引用次数: 0
Convective heat transfer of tri-hybrid nanofluid through a curved expanding surface with the impact of velocity slip and exponential heat source 三混合纳米流体通过受速度滑移和指数热源影响的弯曲膨胀表面的对流传热
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-16 DOI: 10.1007/s00396-024-05291-6
Subhalaxmi Dey, Surender Ontela, P. K. Pattnaik, S. R. Mishra

Obtaining an efficient heat transfer fluid is currently a significant challenge in various industries, including production processes and biomedical applications such as drug delivery systems. In line with this, the study aims to investigate the velocity slip impact along with convective heat transfer on the flow of tri-hybrid nanofluid over an expanding curved surface. Electrically conducting fluid suspended with nanoparticles enhances thermal properties; however, incorporating an exponential heat source with convective heat transfer properties further energises heat transport phenomena. The proposed model, described by nonlinear differential equations, is transformed into non-dimensional nonlinear ordinary differential equations using suitable similarity rules. These equations are then solved by using a semi-analytical technique, i.e., the Adomian decomposition method with controlled parameters. Moreover, the important outcomes are that the combined effect of all the nanoparticles forms the tri-hybrid nanofluid overrides the fact of nanofluid and hybrid nanofluid in all cases of velocity and temperature distribution. Further, the fluid temperature augments significantly for the enhanced magnetization, but the impact is reversed for the fluid velocity.

Graphical Abstract

  • The two-dimensional flow of tri-hybrid nanofluid in association with the role of velocity slip and convective heat transport properties shows a greater impact for the higher thermal conductivity.

  • The electrically conducting fluid, due to the imposition of the transverse magnetic field along with an exponential heat source, has several industrial as well as engineering applications.

  • The dissipative heat effect, including Joule dissipation, is vital in cancer therapy, drug delivery systems, peristaltic pumping processes, etc.

目前,获得高效的导热流体是各行各业(包括生产过程和生物医学应用,如药物输送系统)面临的一项重大挑战。有鉴于此,本研究旨在探讨三混合纳米流体在不断扩大的曲面上流动时的速度滑移影响以及对流传热。悬浮着纳米颗粒的导电流体可增强热特性;然而,加入具有对流传热特性的指数热源可进一步增强热传输现象。所提出的模型由非线性微分方程描述,利用适当的相似性规则将其转化为非维非线性常微分方程。然后利用半解析技术,即参数受控的阿多米分解法,对这些方程进行求解。此外,重要的结果是,在速度和温度分布的所有情况下,所有纳米粒子形成的三混合纳米流体的综合效应超过了纳米流体和混合纳米流体。此外,流体温度在磁化增强的情况下会显著升高,但在流体速度方面的影响则相反。 由于横向磁场和指数热源的作用,导电流体在工业和工程领域有多种应用。 包括焦耳耗散在内的耗散热效应在癌症治疗、药物输送系统、蠕动泵过程等方面至关重要。
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引用次数: 0
Synthesis and evaluation of salt tolerant delayed-crosslinking fracturing fluid system in ultra-deep high temperature wells 超深高温井中耐盐延迟交联压裂液体系的合成与评估
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-16 DOI: 10.1007/s00396-024-05296-1
Cheng Jian, Yi Yu, Dingze Yu, Ping Chen, Jing Yan, Xuefeng Chen

The Tarim area, characterized by deep reservoirs, high temperatures, and limited fresh water resources, necessitates a fracturing fluid system that exhibits excellent temperature shear resistance, low friction, and salinity tolerance. This study presents the development of a zwitterionic hydrophobic polymer, HPC-5, as an effective thickener using five types of polymeric monomers, including AM, AA, DMC, AMPS, and a non-ionic hydrophobic monomer. The method employed for synthesis was free-radical polymerization in solution. A series of experiments including viscosity measurement with variation of salinity, solubility and drag reduction test, crosslinking test, thermal and shear resistance, sand-carrying test, gel breaking evaluation, and core damage test were conduct under the simulated reservoir conditions. The zwitterionic design imparts great salt tolerance to HPC-5, and the apparent viscosities of HPC-5 solutions can maintain comparably high values with 10×104 ppm NaCl and CaCl2 concentration. Meanwhile, the molecules of HPC-5 associate with each other to form tight net structures, resulting in an excellent viscoelasticity of the solution. To achieve high pump rate during hydraulic fracturing operation in ultra-deep reservoirs, the delayed crosslinking agent ZDC-L was prepared for forming a delayed crosslinking gel fracturing fluid system using reservoir brine, and the drag reduction rate can reach over 70% before crossing link within 4 min. Under pH = 4 conditions, the crosslinking time can be significantly delayed to over 4 min while maintaining exceptional temperature resistance up to 160 ℃ for the gel. These properties make it highly suitable for hydraulic fracturing operations in ultra-deep wells with temperatures reaching up to 7000 m depth at pump rates of 4~5m3/min.

Graphical abstract

塔里木地区储层深、温度高、淡水资源有限,因此需要一种具有出色的耐温剪切性、低摩擦性和耐盐性的压裂液体系。本研究利用五种聚合物单体(包括 AM、AA、DMC、AMPS 和一种非离子疏水单体),开发了一种有效的增稠剂--齐聚物疏水聚合物 HPC-5。合成方法是在溶液中进行自由基聚合。在模拟储层条件下进行了一系列试验,包括随盐度变化的粘度测量、溶解度和阻力降低试验、交联试验、耐热性和耐剪切性、携砂试验、凝胶破裂评估和岩心损害试验。HPC-5的齐聚物设计赋予其极强的耐盐性,在10×104 ppm的NaCl和CaCl2浓度下,HPC-5溶液的表观粘度仍能保持相当高的数值。同时,HPC-5 分子之间相互结合形成紧密的网状结构,从而使溶液具有极佳的粘弹性。为了在超深储层水力压裂作业中实现高泵率,制备了延迟交联剂 ZDC-L,利用储层盐水形成延迟交联凝胶压裂液体系,在 4 分钟内,交联前的阻力降低率可达 70% 以上。在 pH = 4 的条件下,交联时间可显著延迟至 4 分钟以上,同时凝胶还能保持优异的耐温性,最高可达 160 ℃。这些特性使其非常适合在温度高达 7000 米、泵速为 4~5m3/min 的超深井中进行水力压裂作业。
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引用次数: 0
Preparation and property of PVA-based colorful coating composite reinforced with silica aerogel particles filled by high-loaded flame retardant 高负载阻燃剂填充二氧化硅气凝胶颗粒增强的 PVA 基多彩涂料复合材料的制备与性能
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-10 DOI: 10.1007/s00396-024-05292-5
Yilin Feng, Ran Xu, Ying Li, Beibo Zhang, Jiali Wang, Zhi Chen, Luoxin Wang, Hua Wang

Hydrophilic mesoporous silica aerogel particles were synthesized via self-assembly of amphiphilic polymer (Ph8-PEG6-PEOS) and its instantaneous hydrolysis and condensation in the alkaline environment. Meanwhile, the capture and encapsulation of flame retardant (IPPP) and oil soluble dyes were successively completed during the two processes above. Observed by thermal field scanning electron microscopy (TFESEM), the average diameter of aerogel particles reached about 10 µm. BET surface area analysis displayed that the existence of oil-phase component (IPPP) can result in the expansion of pore diameter, and promote the evolution of mesopores into macropores. Then, IPPP@SiO2 aerogel particles were utilized to improve the flame retardancy of polyvinyl alcohol (PVA) coatings implemented onto cotton yarns, by employing developed knife coating procedure in an aqueous suspension. The thermal stabilities and flammability behaviors of the samples were evaluated by thermogravimetric analysis (TGA), limiting oxygen index (LOI), and vertical burning test, respectively. Both thermal decomposition temperature and LOI value of coating composites gradually increased with the increment of IPPP@SiO2-n (n = 10, 30, 50, 70), attaching to the synchronous advancement in stretching property. Furthermore, coatings were thickened by degrees from 0.4 to 4 mm, based on knife coating in multi-stage layer-by-layer mode, to build an ordered porous structure with the assisted adhesion of PVA. The following sintering preserved the close packing of silica aerogel particles and facilitated the formation of a coherent porous monolithic material with excellent thermal insulation performance.

Graphical abstract

通过两亲性聚合物(Ph8-PEG6-PEOS)的自组装及其在碱性环境中的瞬时水解和缩合,合成了亲水性介孔二氧化硅气凝胶颗粒。与此同时,阻燃剂(IPPP)和油溶性染料的捕获和封装也在上述两个过程中相继完成。通过热场扫描电子显微镜(TFESEM)观察,气凝胶颗粒的平均直径约为 10 微米。BET 表面积分析表明,油相成分(IPPP)的存在会导致孔径扩大,并促进中孔向大孔演化。然后,通过在水悬浮液中采用开发的刀涂程序,利用 IPPP@SiO2 气凝胶颗粒提高了聚乙烯醇(PVA)涂层在棉纱上的阻燃性。样品的热稳定性和可燃性分别通过热重分析(TGA)、极限氧指数(LOI)和垂直燃烧试验进行了评估。涂层复合材料的热分解温度和 LOI 值都随着 IPPP@SiO2-n (n = 10、30、50、70)的增加而逐渐升高,这与拉伸性能的同步提高有关。此外,基于多级逐层模式的刀涂,涂层厚度从 0.4 毫米到 4 毫米不等,在 PVA 的辅助粘附下建立了有序的多孔结构。随后的烧结保留了二氧化硅气凝胶颗粒的紧密堆积,促进了具有优异隔热性能的多孔整体材料的形成。
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引用次数: 0
Exploring the potential of surface-active copolymers on P123 micelles for drug solubility enhancement and in vitro cytotoxicity assay 探索 P123 胶束表面活性共聚物在提高药物溶解度和体外细胞毒性测定方面的潜力
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-09 DOI: 10.1007/s00396-024-05293-4
Nitumani Tripathi, Payal Vaswani, Dhiraj Bhatia, Ketan Kuperkar, Pratap Bahadur

This study presents the self-assembly of polyethylene oxide (PEO)-block-polypropylene oxide (PPO)-block-polyethylene oxide (PEO)-based block copolymer (BCP) commercially known as Pluronic® P123 in water and in the presence of different copolymeric surfactants (L61, L62, L64, and F68) with varying degree of hydrophilicity, i.e., %EO content. The clouding behavior demonstrates the varied phase transition ranging from solution, blue point (BP), and cloud point (CP). The characteristics of the micelles in the single and mix system are characterized utilizing dynamic light scattering (DLS) and small-angle neutron scattering (SANS) techniques at different temperatures. These scattering approaches provide an insightful information on the micelle size and shape. The size variations in self-assembled micelles designated the micelles to undergo growth/transition in shape from spherical to elongated ellipsoidal as function of temperature. Additionally, the application of these nanoscale micellar aggregates as carriers for delivering the anticancer drug Quercetin (QCT) was undertaken by a thorough quantitative and qualitative analysis to gain valuable insights into the effectiveness of the mix-micellar system as an ideal platform for drug delivery. A comprehensive investigation of drug release kinetics is presented using various kinetic models. The MTT (cytotoxicity assay) assay is used to gauge the effectiveness of the QCT-loaded copolymeric micelles.

Graphical abstract

Micellar transition of 5% w/v P123 in water and in the presence of copolymeric surfactants as additives at 0.2% weight fraction (fix) at different temperatures

本研究介绍了聚环氧乙烷(PEO)-嵌段-聚环氧丙烷(PPO)-嵌段-聚环氧乙烷(PEO)-基嵌段共聚物(BCP)在水中的自组装情况,以及在不同的共聚表面活性剂(L61、L62、L64 和 F68)存在下的自组装情况。混浊行为显示了从溶液、蓝点(BP)到浊点(CP)的不同相变。在不同温度下,利用动态光散射(DLS)和小角中子散射(SANS)技术对单一和混合体系中胶束的特性进行了表征。这些散射方法提供了有关胶束大小和形状的深刻信息。自组装胶束的尺寸变化表明,随着温度的变化,胶束的形状会发生从球形到细长椭圆形的增长/转变。此外,还通过全面的定量和定性分析,对这些纳米级胶束聚集体作为载体输送抗癌药物槲皮素(QCT)的应用进行了深入研究,从而对混合胶束系统作为理想的药物输送平台的有效性获得了宝贵的见解。使用各种动力学模型对药物释放动力学进行了全面研究。图解摘要5% w/v P123 在水中的胶束转变,以及共聚表面活性剂作为添加剂在不同温度下 0.2% 重量分数(固定值)的胶束转变。
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引用次数: 0
A versatile method for facile and reliable synthesis of colloidal particles with a size and composition gradient 便捷可靠地合成具有尺寸和成分梯度的胶体颗粒的多功能方法
IF 2.4 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-08 DOI: 10.1007/s00396-024-05282-7
Alexander Berger, Maximilian Theis, Henrike von Wedel, Tamino Rößler, Georg Papastavrou, Jürgen Senker, Markus Retsch

Abstract

Colloidal particles play a pivotal role in numerous applications across various disciplines, many of which necessitate precise control over particle size and size distribution. Seeded growth reactions have been established as effective methods for reproducibly accessing tailor-made particles. However, conventional batch-wise syntheses only yield discrete particle sizes. With the increasing focus on complex structures in current research, there is a demand for innovative and adaptable techniques to produce colloidal particles with precise sizes and size distributions. The Controlled Emulsion Extraction Process (CrEEP) is capable of addressing this challenge. Here, we present in detail how this synthesis works and demonstrate its reliability and versatility. Our approach exploits the time-dependent particle growth and enables accessing dispersions of controlled particle size distributions. We highlight these possibilities through a variation of the monomer feed and feed composition, resulting in gradual changes in both size and glass transition temperature, respectively. Beyond its application to polymer particles, CrEEP can be seamlessly extended to other seeded-growth mechanisms, such as the silica Stöber synthesis. Consequently, the Controlled Extraction Stöber Process (CrESP) similarly yields a size gradient, showcasing the generality of this synthetic advancement.

Graphical abstract

摘要胶体粒子在各学科的众多应用中发挥着关键作用,其中许多应用都需要精确控制粒度和粒度分布。种子生长反应已成为可重复获得定制颗粒的有效方法。然而,传统的批量合成只能获得离散的颗粒尺寸。目前的研究越来越关注复杂结构,因此需要创新和适应性强的技术来生产具有精确尺寸和尺寸分布的胶体粒子。可控乳液萃取工艺(CrEEP)能够应对这一挑战。在此,我们将详细介绍这种合成方法的工作原理,并展示其可靠性和多功能性。我们的方法利用了随时间变化的颗粒生长,并能获得粒度分布可控的分散体。我们通过改变单体进料和进料成分,使粒度和玻璃化转变温度分别发生渐变,从而突出了这些可能性。除了应用于聚合物颗粒之外,CrEEP 还可以无缝扩展到其他种子生长机制,如二氧化硅斯托伯合成。因此,受控萃取斯托伯工艺(CrESP)也能产生类似的尺寸梯度,从而展示了这一合成技术进步的通用性。
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引用次数: 0
Box-Behnken design based optimization of polyvinylpyrrolidone stabilized valproic acid nanoemulsion and evaluation of its anticancer potential 基于盒-贝肯设计的聚乙烯吡咯烷酮稳定丙戊酸纳米乳液优化及其抗癌潜力评估
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-06 DOI: 10.1007/s00396-024-05283-6
Namita Hegde, Kapil Juvale, Sachin Puri, Aditi Chavan, Shivani Shah

Marketed valproic acid formulations use its solid salt forms, which are hygroscopic and difficult to handle. The current study focuses on developing valproic acid nanoemulsion using the physically most stable liquid form of the drug and evaluating its anticancer potential. Valproic acid is a histone deacetylase inhibitor having anticancer potential.The valproic acid nanoemulsion was formulated using a facile and scalable homogenization process. The emulsion stabilization was achieved through viscosity-enhancing polymer polyvinylpyrrolidone K-30 and tween 80. The formulation was optimized using the Box-Behnken model of design of experiments and was evaluated for efficacy and safety in cancer and fibroblast cell lines, respectively.The optimized emulsion showed particle size below 150 nm, polydispersity index below 0.3, zeta potential near − 8.5 mV, density 0.9923 g/cm3, viscosity 2.06 poise, creaming index below 20, drug content 100.37%w/v and acceptable stability at accelerated environmental conditions. Overall, under all the studied conditions of in vitro dissolution and ex vivo permeability, drug release from emulsion was found better than the free drug and comparable to the marketed solution of sodium valproate. The cytotoxicity studies demonstrated improved IC50 values for breast and lung cancer cell lines, with selectivity for cancer cells.The valproic acid nanoemulsion was prepared using its physically stable liquid form. The combination of polymer polyvinylpyrrolidone K-30 and tween 80 demonstrated the desired stabilization of the dispersed phase of the emulsion. The formulated nanoemulsion effectively potentiated valproic acid’s anticancer activity in cell culture assays.

Graphical Abstract

市场上销售的丙戊酸制剂使用的是固体盐形式,具有吸湿性且难以处理。目前的研究重点是利用物理上最稳定的液态药物开发丙戊酸纳米乳剂,并评估其抗癌潜力。丙戊酸是一种组蛋白去乙酰化酶抑制剂,具有抗癌潜力。通过增粘聚合物聚乙烯吡咯烷酮 K-30 和吐温 80 实现了乳液稳定。优化后的乳剂粒径小于 150 nm,多分散指数小于 0.3,zeta 电位接近 - 8.5 mV,密度为 0.9923 g/cm3,粘度为 2.06 poise,起皱指数小于 20,药物含量为 100.37%w/v,在加速环境条件下具有可接受的稳定性。总之,在体外溶解度和体内渗透性的所有研究条件下,乳剂的药物释放均优于游离药物,与丙戊酸钠的市售溶液相当。细胞毒性研究表明,对乳腺癌和肺癌细胞株的 IC50 值有所提高,对癌细胞具有选择性。聚合物聚乙烯吡咯烷酮 K-30 和吐温 80 的组合为乳液的分散相提供了所需的稳定性。配制的纳米乳液在细胞培养试验中有效地增强了丙戊酸的抗癌活性。
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引用次数: 0
Oral linalool-based nanoemulsion of acalabrutinib for ameliorating its oral bioavailability and in vitro anticancer potential in T lymphoblast cell lines 基于芳樟醇的阿卡布替尼口服纳米乳液可改善其口服生物利用度和在 T 淋巴母细胞系中的体外抗癌潜力
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-04 DOI: 10.1007/s00396-024-05290-7
Arti Shettiwar, Ujala Gupta, Essha Chatterjee, Bhagyashree Patra, Mayur Aalhate, Srushti Mahajan, Indrani Maji, Neelesh Kumar Mehra, Santosh Kumar Guru, Pankaj Kumar Singh

Acalabrutinib (ACL) was approved in the United States in the year of 2017 and 2019 for the treatment of chronic lymphocytic leukemia (CLL) and relapsed mantle cell lymphoma (MCL). Low-energy method was employed to curate nanoemulsion (NE) for which various components were screened through solubility study and optimization was done through a pseudo-ternary phase diagram. The NE was evaluated for its droplet size, polydispersity index (PDI), transmittance, morphology, rheology, robustness to dilution, the effect of pH, storage stability, and ex vivo permeation study. The optimized ACL-NE demonstrated an appropriate droplet size (94.35 ± 0.3 nm), PDI (0.27 ± 0.03), and an entrapment efficiency of 67.38 ± 2.69%. It showed non-Newtonian (shear thinning behavior) due to reduced viscosity with an increasing shear rate. The apparent permeability was 3.09-fold higher for ACL-NE than ACL suspension. An in vitro drug release study depicted a higher release of ACL (71.10 ± 10.99%) from the optimized NE in a sustained fashion than the suspension (49.01 ± 1.65%). A dose-dependent cytotoxicity was observed in MOLT-4 and HH-cell lines where the IC50 values of ACL were 5.62- and 16.49-fold reduced when encapsulated in oil globules for the respective cell lines. Blank-NE did cause a reduction in cellular toxicity at higher doses. A 7.31- and 5.1-fold increase in Cmax and bioavailability was noted between ACL suspension and ACL-NE.

Graphical abstract

阿卡布替尼(ACL)于2017年和2019年在美国获批用于治疗慢性淋巴细胞白血病(CLL)和复发套细胞淋巴瘤(MCL)。研究人员采用低能法制备了纳米乳液(NE),通过溶解度研究筛选了其中的各种成分,并通过伪三元相图进行了优化。对纳米乳液的液滴大小、多分散指数(PDI)、透光率、形态、流变性、对稀释的稳定性、pH 值的影响、储存稳定性和体内外渗透研究进行了评估。优化后的 ACL-NE 显示出适当的液滴大小(94.35 ± 0.3 nm)、PDI(0.27 ± 0.03)和 67.38 ± 2.69% 的夹带效率。由于粘度随剪切速率的增加而降低,它呈现出非牛顿性(剪切稀化行为)。ACL-NE 的表观渗透性比 ACL 悬浮液高 3.09 倍。体外药物释放研究表明,从优化的 NE 中持续释放的 ACL(71.10 ± 10.99%)高于悬浮液(49.01 ± 1.65%)。在 MOLT-4 和 HH 细胞系中观察到了剂量依赖性细胞毒性,当 ACL 被包裹在油球中时,其 IC50 值分别降低了 5.62 倍和 16.49 倍。在较高剂量下,Blank-NE 确实会降低细胞毒性。ACL 悬浮液和 ACL-NE 的 Cmax 和生物利用度分别增加了 7.31 倍和 5.1 倍。
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引用次数: 0
Visible light-responsive all-organic polyurethane antibacterial coatings using a polythiophene derivative 使用聚噻吩衍生物的可见光响应型全有机聚氨酯抗菌涂层
IF 2.2 4区 化学 Q3 CHEMISTRY, PHYSICAL Pub Date : 2024-07-04 DOI: 10.1007/s00396-024-05280-9
Chunbo Liu, Xiaohuan Li, Paul A. Charpentier, William Z. Xu, Haiyong Guo

Visible light-responsive antimicrobial coatings are of importance for antibacterial applications owing to widespread multidrug-resistant infections. Herein, the photocatalytic disinfection performance of an all-organic poly[2,11′-thiophene-ethylene-thiophene-alt-(2,5-(3-carboxyl)-thiophene] (PTET-T-COOH)/polyurethane (PU) coating was synthesized and evaluated. The coating consists of both a protective PU layer and a photoactive layer (PTET-T-COOH), which was prepared using isocyanate groups as linkers, then fabricated by drop-casting. The chemical linkage between PTET-T-COOH and NCO-terminated PU was researched based on ATR-FTIR and XPS analyses. The developed coating demonstrated good photocatalytic bactericidal performance on S. aureus under visible-light irradiation for 6 h. This study provided an effective platform for fabricating environmental-friendly and cheap antimicrobial surfaces.

由于耐多药感染的广泛存在,可见光响应抗菌涂层在抗菌应用中具有重要意义。本文合成并评估了一种全有机聚[2,11′-噻吩-乙烯-噻吩-alt-(2,5-(3-羧基)-噻吩](PTET-T-COOH)/聚氨酯(PU)涂层的光催化消毒性能。该涂层由聚氨酯保护层和光活性层(PTET-T-COOH)组成,使用异氰酸酯基团作为连接剂制备,然后通过滴注法制造。根据 ATR-FTIR 和 XPS 分析研究了 PTET-T-COOH 与 NCO 端聚氨酯之间的化学联系。该研究为制备环保、廉价的抗菌表面提供了一个有效的平台。
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引用次数: 0
期刊
Colloid and Polymer Science
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