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Recent updates of carotenoid encapsulation by spray-drying technique. 利用喷雾干燥技术封装类胡萝卜素的最新进展。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-23 DOI: 10.1080/02652048.2024.2430643
Patrícia Griep, Luana Gayeski, Rosicler Colet, Jamile Zeni, Eunice Valduga

Carotenoids are compounds sensitive to environmental factors such as light, heat, and oxygen, which can result in the loss of their properties due to isomerisation and oxidation. To overcome this problem, spray drying encapsulation has been widely used as a method to protect and stabilise carotenoids in different wall materials. This article summarises the findings and research on spray drying encapsulation of carotenoids over the past 15 years, with an emphasis on the importance of controlling the operational conditions of the drying process and the association of different wall materials (proteins and polysaccharides), promising to increase encapsulation efficiency and stabilise carotenoids, with perspectives and trends in applications. The use of spray drying for carotenoid microencapsulation can open up new opportunities for controlled delivery of beneficial compounds. Based on the study, it is expected to provide information for researchers, professionals, and companies interested in the development of functional food products.

类胡萝卜素是一种对光、热和氧等环境因素非常敏感的化合物,这些因素会导致类胡萝卜素的特性因异构化和氧化而丧失。为克服这一问题,喷雾干燥封装技术已被广泛应用于保护和稳定不同壁材中的类胡萝卜素。本文总结了过去 15 年来在类胡萝卜素喷雾干燥封装方面的发现和研究,强调了控制干燥过程操作条件和不同壁材(蛋白质和多糖)结合的重要性,有望提高封装效率和稳定类胡萝卜素,并展望了应用前景和趋势。使用喷雾干燥法进行类胡萝卜素微胶囊封装可为控制有益化合物的输送带来新的机遇。本研究有望为研究人员、专业人士和对开发功能性食品感兴趣的公司提供信息。
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引用次数: 0
Physicochemical stability and controlled release of vitamin D3-loaded emulsions stabilised by whey protein isolate-basil seed gum conjugates. 用乳清蛋白分离物-巴西杉籽胶共轭物稳定的维生素 D3 负载乳剂的理化稳定性和控释。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-20 DOI: 10.1080/02652048.2024.2418615
Farzaneh Kouravand, Fakhri Shahidi, Milad Fathi, Arash Koocheki, Sahar Roshanak

Aim: The present study was conducted to produce a new carrier containing whey protein isolate-basil seed gum (WPI-BSG) conjugate to achieve superior physicochemical stability of emulsions containing vitamin D3 (Vit-D3).

Methods: Zeta-potential and particle size analysis, spectrophotometric method, encapsulation efficiency, loading capacity and dialysis bag method were used to examined physicochemical stability and Vit-D3 release from the emulsions.

Results: The conjugate-stabilised emulsion showed maximum encapsulation efficiency (87.05 ± 3.37% (w/w)) and loading capacity (5.43 ± 0.08% (w/w)) at the Vit-D3 concentration of 200 and 300 mg/kg. This emulsion also demonstrated good physical stability after 30 days of storage with the zeta potential and mean droplet size of -79.60 ± 0.62 mV and 1346.82 ± 5.95 nm, respectively. Additionally, the conjugate-stabilised emulsion had a maximum Vit-D3 retention (chemical stability) of 72.79 ± 3.58% after a 15-day storage period.

Conclusion: Our findings suggest that the conjugate-stabilised emulsion has a good stabilising capacity as a carrier for hydrophobic compounds such as Vit-D3.

目的:本研究旨在生产一种含有乳清蛋白分离物-巴西杉种子胶(WPI-BSG)共轭物的新型载体,以实现含有维生素 D3(Vit-D3)的乳剂的卓越理化稳定性:方法:采用 Zeta 电位和粒度分析法、分光光度法、包封效率、负载能力和透析袋法检测乳剂的理化稳定性和维生素 D3 的释放:共轭稳定乳剂在 Vit-D3 浓度为 200 和 300 毫克/千克时显示出最高的包封效率(87.05 ± 3.37%(重量比))和负载能力(5.43 ± 0.08%(重量比))。这种乳剂在储存 30 天后也表现出良好的物理稳定性,zeta 电位和平均液滴大小分别为 -79.60 ± 0.62 mV 和 1346.82 ± 5.95 nm。此外,共轭稳定乳剂在储存 15 天后,Vit-D3 的最大保留率(化学稳定性)为 72.79 ± 3.58%:我们的研究结果表明,共轭稳定乳液作为疏水性化合物(如 Vit-D3)的载体具有良好的稳定能力。
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引用次数: 0
Spray-dried chitosan oligosaccharide microparticles with polyvinyl alcohol-based dispersions for improved gefitinib solubility. 喷雾干燥壳聚糖寡糖微颗粒与聚乙烯醇基分散体可提高吉非替尼的溶解度。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-20 DOI: 10.1080/02652048.2024.2428359
Shubham B Ahir, Bhaskar Vallamkonda, Ranadheer Reddy Challa, Nishant Chopade, Prashant K Deshmukh, Mahesh P More

The aim of research is to enhance the solubility of crystalline gefitinib (GF), a poorly water-soluble drug, by developing drug delivery systems using chitosan oligosaccharide (COS) particle engineering. Fabrication utilizes ionic gelation followed by spray drying. The preliminary evaluations such as Uv-Vis, FTIR, DSC followed by advanced techniques like SEM and invitro drug release characteristics was performed along with solubility study. The spray-dried particles measured a mean diameter of 3.18 ± 0.5 microns, %EE as well as load w/w improved from 63.25 ± 2.1% and 37.98 ± 1.5% w/w (COS nanoparticles) to 78.15 ± 2.6% and 45.34 ± 1.6% w/w (engineered microparticles), respectively. The zeta potential and in vitro studies demonstrated 41 ± 3.5 mV and 92 ± 2.1% (w/w) release suggest long-term stability and prolonged release. This novel engineering approach effectively enhances GF solubility and surface characteristics, offering promising potential for improving delivery characteristics.

本研究的目的是利用壳聚糖寡糖(COS)颗粒工程开发给药系统,从而提高结晶吉非替尼(GF)这种水溶性较差药物的溶解度。制造方法是先离子凝胶化,然后喷雾干燥。在进行了 Uv-Vis、FTIR、DSC 等初步评估后,又采用了 SEM、体外药物释放特性和溶解度研究等先进技术。喷雾干燥颗粒的平均直径为 3.18 ± 0.5 微米,EE%和负载(湿重)分别从 63.25 ± 2.1%(COS 纳米颗粒)和 37.98 ± 1.5%(湿重)提高到 78.15 ± 2.6%(工程微粒)和 45.34 ± 1.6%(湿重)。zeta电位和体外研究表明,其释放率分别为41 ± 3.5 mV和92 ± 2.1%(重量比),这表明其具有长期稳定性和延长释放时间的特点。这种新颖的工程方法有效地提高了 GF 的溶解度和表面特性,为改善给药特性提供了广阔的前景。
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引用次数: 0
Development, QbD-based optimisation, in-vivo pharmacokinetics, and ex-vivo evaluation of Eudragit® RS 100 loaded flurbiprofen nanoparticles for oral drug delivery. 用于口服给药的 Eudragit® RS 100 负载氟比洛芬纳米颗粒的开发、基于 QbD 的优化、体内药代动力学和体外评估。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-16 DOI: 10.1080/02652048.2024.2427294
Shilpa Mandpe, Eknath Kole, Vishal Parate, Aniruddha Chatterjee, Arun Mujumdar, Jitendra Naik

This study aims to develop and evaluate flurbiprofen-loaded polymeric nanoparticles to achieve sustained drug release, enhancing therapeutic efficacy and minimising dosing frequency for improved patient outcomes. Flurbiprofen-loaded polymeric nanoparticles were prepared using a tubular microreactor and spray drying, optimised via Box-Behnken Design. Characterisation included particle size, encapsulation efficiency, in vitro and in vivo drug release, and techniques like FTIR, DSC, XRD, and SEM. Statistical analysis ensured robust formulation optimisation and evaluation of performance. The optimised batch of flurbiprofen-loaded polymeric nanoparticles was characterised for mean diameter, PDI, zeta potential, drug release, and EE% were found to be 306.1 ± 6.00 nm, 0.184 ± 0.02 Mw, -23.6 ± 1.51 mV, 85.46 ± 0.53% and 92.31 ± 0.84 (% w/w) respectively. Pharmacokinetic analysis further confirmed the sustained release, extending up to 12 hours and enhancing permeation compared to the pure flurbiprofen. Sustained release of flurbiprofen-loaded polymeric nanoparticles significantly enhances therapeutic effectiveness for inflammatory conditions.

本研究旨在开发和评估负载氟比洛芬的聚合物纳米粒子,以实现药物的持续释放,提高疗效并减少给药次数,从而改善患者的治疗效果。采用管式微反应器和喷雾干燥法制备了氟比洛芬负载聚合物纳米粒子,并通过盒式贝肯设计进行了优化。表征包括粒度、封装效率、体外和体内药物释放,以及傅立叶变换红外光谱(FTIR)、电子稳定性扫描(DSC)、X射线衍射(XRD)和扫描电子显微镜(SEM)等技术。统计分析确保了配方优化和性能评估的稳健性。优化后的氟比洛芬负载聚合物纳米颗粒的平均直径、PDI、zeta 电位、药物释放和 EE% 分别为 306.1 ± 6.00 nm、0.184 ± 0.02 Mw、-23.6 ± 1.51 mV、85.46 ± 0.53% 和 92.31 ± 0.84(% w/w)。药代动力学分析进一步证实,与纯氟比洛芬相比,该药物的持续释放时间可延长至 12 小时,且渗透性更强。负载氟比洛芬的聚合物纳米粒子的持续释放大大提高了对炎症的治疗效果。
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引用次数: 0
Paliperidone-loaded nose to brain targeted NLCS: optimisation, evaluation, histopathology and pharmacokinetic estimation for schizophernia. 帕潘立酮(Paliperidone-loaded)鼻脑靶向 NLCS:用于精神分裂症的优化、评估、组织病理学和药代动力学估算。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-16 DOI: 10.1080/02652048.2024.2426545
Manish Ashok Khedkar, Vipin Sharma, Meraj Anjum, Sanjay Singh, Kamal Shah, Perwez Alam, Hitesh Kumar Dewangan

Study was to develop a nanostructured-lipid-careers (NLCs) of paliperidone (PLP) for nose-to-brain targeting. NLCs was prepared by sonication, high-shear homogenisation method, and characterised their mean diameter, PDI, zeta-potential, morphology (by SEM, TEM and AFM), entrapment efficiency, drug loading, in vitro release, interaction study (by FTIR), and stability. Further, ex vivo permeation and ciliotoxicity performed in sheep nasal mucosa, and in vivo biodistribution/pharmacokinetic was performed in rats for schizophernia. Developed NLCs showed spherical and clearly 3-dimentinal structure with 129 ± 2.7 nm mean diameter, 0.304 ± 0.003 PDI, -7.61 ± 0.56 mV zeta-potential, 58.16 ± 0.17% entrapment efficiency, 65.8 ± 2% drug loading and 74.32 ± 0.003% release in 12 h, followed by Higuchi model. Ex vivo study showed NLCs have three times higher permeation, compare to pure drug (around 71.50.32% in 6 h) and 3.98 g/cm2/h steady sate flux. The blood/brain ratio given by intranasally have higher compare to IV route, and 94.53 ± 21.45% drug targeting efficiency in brain. In conclusion, NLCs have easily crossed BBB, higher drug delivery and effective for schizophrenia in given by intranasal.

本研究旨在开发一种用于鼻脑靶向的帕利哌酮(PLP)纳米结构脂护理剂(NLCs)。研究采用超声和高剪切均质法制备了 NLCs,并对其平均直径、PDI、zeta 电位、形态(通过 SEM、TEM 和 AFM)、包埋效率、药物负载、体外释放、相互作用研究(通过 FTIR)和稳定性进行了表征。此外,还在绵羊鼻粘膜上进行了体外渗透和纤毛毒性研究,并在治疗精神分裂症的大鼠身上进行了体内生物分布/药代动力学研究。根据樋口模型,所开发的 NLC 呈球形,具有清晰的 3 层结构,平均直径为 129 ± 2.7 nm,PDI 为 0.304 ± 0.003,zeta 电位为 -7.61 ± 0.56 mV,夹带效率为 58.16 ± 0.17%,载药量为 65.8 ± 2%,12 小时释放率为 74.32 ± 0.003%。体内外研究表明,与纯药物相比,NLCs 的渗透率高三倍(6 小时内约为 71.50.32%),稳态通量为 3.98 g/cm2/h。与静脉注射途径相比,鼻内给药的血脑比例更高,药物在脑内的靶向效率为 94.53 ± 21.45%。总之,NLCs 很容易穿过 BBB,具有较高的给药效率,通过鼻内给药可有效治疗精神分裂症。
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引用次数: 0
Synthesis of cefixime loaded PCL/HPMC blend nanoparticles: a controlled release study and in vitro anti-bacterial evaluation. 合成负载头孢克肟的 PCL/HPMC 混合纳米颗粒:控释研究和体外抗菌评估。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-12 DOI: 10.1080/02652048.2024.2427292
Yashvi Naik, Hem N Naik, Jay Rai, Rushabh Shah, Smita Jauhari, Anand J Patel

Aim: To enhance cefixime's effectiveness and address drug delivery challenges like concentration at the site, dose, and time, present study investigated the impact of polymer blends on cefixime's in vitro release profile.

Methods: Cefixime-loaded nanoparticles were prepared via a modified solvent evaporation method, forming a W/O/W double emulsion. Characterisation included FT-IR, zeta potential, TGA, TEM, and XRD, with in vitro studies and kinetic models used to analyse the release mechanism.

Results: The PH-4 nanoparticle formulation (80:20 PCL/HPMC, 0.5% PVA) achieved an 81% loading rate, no adverse effects, and a controlled release of 84.66%±2.53 over 30 days. It showed stable physicochemical properties, with in vitro antibacterial tests revealing inhibition zones of 27.4 ± 2.12 mm for E. coli and 17.2 ± 2.23 mm for S. aureus at 12 hours.

Conclusion: Based on the findings, developed nanoparticulate system containing PCL/HPMC demonstrates its efficacy and safety as a controlled drug delivery method for antibiotics like cefixime.

目的:为提高头孢克肟的疗效,解决给药部位浓度、剂量和时间等难题,本研究探讨了聚合物混合物对头孢克肟体外释放曲线的影响:方法:采用改良溶剂蒸发法制备头孢克肟负载纳米粒子,形成 W/O/W 双乳液。表征包括傅立叶变换红外光谱、ZETA电位、TGA、TEM和XRD,体外研究和动力学模型用于分析释放机制:结果:PH-4 纳米粒子配方(80:20 PCL/HPMC,0.5% PVA)的负载率达到 81%,无不良反应,30 天内的控释率为 84.66%±2.53。其理化性质稳定,体外抗菌测试显示,12 小时内对大肠杆菌的抑菌区为 27.4 ± 2.12 mm,对金黄色葡萄球菌的抑菌区为 17.2 ± 2.23 mm:根据研究结果,所开发的含有 PCL/HPMC 的纳米颗粒系统证明了其作为头孢克肟等抗生素的控制给药方法的有效性和安全性。
{"title":"Synthesis of cefixime loaded PCL/HPMC blend nanoparticles: a controlled release study and <i>in vitro</i> anti-bacterial evaluation.","authors":"Yashvi Naik, Hem N Naik, Jay Rai, Rushabh Shah, Smita Jauhari, Anand J Patel","doi":"10.1080/02652048.2024.2427292","DOIUrl":"https://doi.org/10.1080/02652048.2024.2427292","url":null,"abstract":"<p><strong>Aim: </strong>To enhance cefixime's effectiveness and address drug delivery challenges like concentration at the site, dose, and time, present study investigated the impact of polymer blends on cefixime's <i>in vitro</i> release profile.</p><p><strong>Methods: </strong>Cefixime-loaded nanoparticles were prepared via a modified solvent evaporation method, forming a W/O/W double emulsion. Characterisation included FT-IR, zeta potential, TGA, TEM, and XRD, with in vitro studies and kinetic models used to analyse the release mechanism.</p><p><strong>Results: </strong>The PH-4 nanoparticle formulation (80:20 PCL/HPMC, 0.5% PVA) achieved an 81% loading rate, no adverse effects, and a controlled release of 84.66%±2.53 over 30 days. It showed stable physicochemical properties, with <i>in vitro</i> antibacterial tests revealing inhibition zones of 27.4 ± 2.12 mm for <i>E. coli</i> and 17.2 ± 2.23 mm for <i>S. aureus</i> at 12 hours.</p><p><strong>Conclusion: </strong>Based on the findings, developed nanoparticulate system containing PCL/HPMC demonstrates its efficacy and safety as a controlled drug delivery method for antibiotics like cefixime.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"1-12"},"PeriodicalIF":3.0,"publicationDate":"2024-11-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142622161","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Dermal drug delivery via bilosomes: a synergistic integration for better therapeutic outcomes. 通过双糖体进行皮肤给药:协同整合,提高疗效。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-07 DOI: 10.1080/02652048.2024.2423618
Kartik Aralelimath, Jagannath Sahoo, Sarika Wairkar

The dermal route is commonly used to deliver the drugs at the targeted site and achieve maximum therapeutic efficacy. The stratum corneum, the uppermost layer of the skin, presents a significant diffusional barrier for most drugs. Various nanoformulations face challenges such as limited drug absorption and inadequate retention at the targeted site, frequently hindering therapeutic efficacy. Researchers are increasingly exploring innovative strategies that leverage nanotechnology and specialized carriers to address these challenges and enhance the outcomes of dermal medications. A novel drug delivery system, bilosomes, has been designed as a potential vesicular carrier system for the dermal route. Bilosomes are colloidal, lipid-based vesicles stabilized with bile salts, offering greater stability during storage and transportation. The lipid bilayer of bilosomes imparts ultra-flexibility, facilitating penetration through the stratum corneum. This review explores the use of bilosomes in dermal formulations for treating diverse diseases, their developmental techniques, and characterization, and it sheds light on their advantages over traditional lipid nanocarriers.

为了将药物输送到目标部位并取得最大疗效,通常采用皮肤途径。角质层是皮肤的最上层,对大多数药物来说都是一个重要的扩散屏障。各种纳米制剂都面临着药物吸收受限和在目标部位滞留不足等挑战,常常妨碍疗效。研究人员正越来越多地探索利用纳米技术和专用载体的创新策略,以应对这些挑战并提高皮肤药物的疗效。我们设计了一种新型给药系统--双糖体,作为皮肤途径的潜在囊泡载体系统。双糖体是一种以胆汁盐为稳定剂的脂基胶体囊泡,在储存和运输过程中具有更高的稳定性。双糖体的脂质双分子层具有超强的柔韧性,有利于穿透角质层。本综述探讨了双糖体在治疗各种疾病的皮肤制剂中的应用、其开发技术和特性,并阐明了其与传统脂质纳米载体相比的优势。
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引用次数: 0
A comparative analysis of PLA and PCL microparticles for hydrophilic and hydrophobic drugs. 聚乳酸(PLA)和聚苯乙烯(PCL)微颗粒用于亲水性和疏水性药物的比较分析。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-05 DOI: 10.1080/02652048.2024.2423631
Subrat Kumar Panigrahi, Sougat Das, Saptarshi Majumdar

This study aims to investigate Polylactic Acid (PLA) and Polycaprolactone (PCL) polymers for microencapsulation of hydrophilic and hydrophobic anti-glaucoma drugs using an emulsion-based solvent evaporation technique. Microparticle size was analysed using optical microscopy, while drug-polymer interactions through Dynamic-Light-Scattering (DLS) and Fourier-Transform-Infra-red/Attenuated-Total-Reflection spectroscopy (FTIR/ATR). In vitro, drug release studies were performed to investigate drug encapsulation and release profiles. Spherical microparticles, with particle size 94 ± 6.9 μm for PCL-based and 100 ± 3.74 μm for PLA-based formulation, were obtained. Drug release studies showed 100% release over about 32 days, with encapsulation efficiency (%EE) and drug loading (%w/w) reaching up to 95 and 2.84% for PLA-based and 97 and 2.91% for PCL-based microparticles, respectively. DLS studies reveal an increase in hydrodynamic radius (RH), which correlates to enhanced drug encapsulation. So, the nature of the drug and polymer significantly impacts drug encapsulation and release, with drug-polymer interactions playing a crucial role alongside experimental parameters.

本研究旨在利用基于乳液的溶剂蒸发技术,研究聚乳酸(PLA)和聚己内酯(PCL)聚合物用于亲水性和疏水性抗青光眼药物的微囊化。使用光学显微镜分析了微粒的大小,并通过动态光散射(DLS)和傅立叶变换红外/衰减全反射光谱(FTIR/ATR)分析了药物与聚合物之间的相互作用。体外进行了药物释放研究,以调查药物的封装和释放情况。获得的球形微粒粒径为:基于 PCL 的配方为 94 ± 6.9 μm,基于 PLA 的配方为 100 ± 3.74 μm。药物释放研究表明,在大约 32 天的时间里,药物释放率达到 100%,聚乳酸基微粒的封装效率(%EE)和载药量(%w/w)分别达到 95%和 2.84%,聚CL 基微粒的封装效率和载药量分别达到 97%和 2.91%。DLS 研究显示,流体力学半径(RH)增加,这与药物包囊能力增强有关。因此,药物和聚合物的性质对药物的封装和释放有重大影响,药物与聚合物之间的相互作用与实验参数一起发挥着至关重要的作用。
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引用次数: 0
Nano-emulsion based on Santolina chamaecyparissus essential oil potentiates the cytotoxic and apoptotic effects of Doxorubicin: an in vitro study. 基于山苍子精油的纳米乳液可增强多柔比星的细胞毒性和凋亡效应:一项体外研究。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-01 Epub Date: 2024-08-02 DOI: 10.1080/02652048.2024.2386287
Sahar M AlMotwaa, Waad A Al-Otaibi

Aim: This study was aimed at investigating the cytotoxic effect of a novel combination of doxorubicin (DOX) and nano-formulation of Santolina chamaecyparissus L. essential oil (SCEO-NANO) on hepatic (HepG2) and colon (HT29) cancer cell lines.

Methods: A nano-emulsion was prepared by high-pressure homogenisation, then analysed by zetasizer and Fourier transform infrared spectroscopy. HepG2 and HT29 cells were used in in vitro tests for apoptosis detection.

Results: Formulated droplet size increased in DOX@SCEO-NANO/DOX to 11.54 ± 0.02 with uniform distribution (PDI = 0.13 ± 0.01), when compared with SCEO-NANO (size: 8.91 ± 0.02 nm; PDI = 0.1 ± 0.02). In both cells, DOX@SCEO-NANO/DOX led to a considerable reduction in colony formation. Compared to DOX, apoprotein proteins were overexpressed in HepG2 cells, showing increases of 8.66-fold for caspase-3 and 4.24-fold for the Bax/Bcl-2 ratio. In HT29 cells, ROS-dependent necrosis and apoptosis were seen. Comparing DOX@SCEO-NANO/DOX versus DOX, greater levels of caspase-3 and the Bax/Bcl-2 ratio were observed.

Conclusion: The DOX@SCEO-NANO/DOX formulation showed potential for targeted eradication of colon adenocarcinoma and hepatocellular carcinoma cells.

目的:本研究旨在探讨多柔比星(DOX)与山茱萸精油纳米制剂(SCEO-NANO)的新型组合对肝癌(HepG2)和结肠癌(HT29)细胞株的细胞毒作用:方法:通过高压均质法制备纳米乳液,然后用zetasizer和傅立叶变换红外光谱进行分析。在体外试验中使用 HepG2 和 HT29 细胞进行细胞凋亡检测:结果:与SCEO-NANO(尺寸:8.91 ± 0.02 nm;PDI = 0.1 ± 0.02)相比,DOX@SCEO-NANO/DOX的配方液滴尺寸增加到11.54 ± 0.02,分布均匀(PDI = 0.13 ± 0.01)。在这两种细胞中,DOX@SCEO-NANO/DOX 可显著减少菌落的形成。与 DOX 相比,apoprotein 蛋白在 HepG2 细胞中过度表达,Caspase-3 增加了 8.66 倍,Bax/Bcl-2 比率增加了 4.24 倍。在 HT29 细胞中,出现了 ROS 依赖性坏死和凋亡。DOX@SCEO-NANO/DOX与DOX相比,Caspase-3和Bax/Bcl-2比率的水平更高:结论:DOX@SCEO-NANO/DOX制剂具有靶向消灭结肠腺癌和肝癌细胞的潜力。
{"title":"Nano-emulsion based on <i>Santolina chamaecyparissus</i> essential oil potentiates the cytotoxic and apoptotic effects of Doxorubicin: an <i>in vitro</i> study.","authors":"Sahar M AlMotwaa, Waad A Al-Otaibi","doi":"10.1080/02652048.2024.2386287","DOIUrl":"10.1080/02652048.2024.2386287","url":null,"abstract":"<p><strong>Aim: </strong>This study was aimed at investigating the cytotoxic effect of a novel combination of doxorubicin (DOX) and nano-formulation of <i>Santolina chamaecyparissus</i> L. essential oil (SCEO-NANO) on hepatic (HepG2) and colon (HT29) cancer cell lines.</p><p><strong>Methods: </strong>A nano-emulsion was prepared by high-pressure homogenisation, then analysed by zetasizer and Fourier transform infrared spectroscopy. HepG2 and HT29 cells were used in <i>in vitro</i> tests for apoptosis detection.</p><p><strong>Results: </strong>Formulated droplet size increased in DOX@SCEO-NANO/DOX to 11.54 ± 0.02 with uniform distribution (PDI = 0.13 ± 0.01), when compared with SCEO-NANO (size: 8.91 ± 0.02 nm; PDI = 0.1 ± 0.02). In both cells, DOX@SCEO-NANO/DOX led to a considerable reduction in colony formation. Compared to DOX, apoprotein proteins were overexpressed in HepG2 cells, showing increases of 8.66-fold for caspase-3 and 4.24-fold for the Bax/Bcl-2 ratio. In HT29 cells, ROS-dependent necrosis and apoptosis were seen. Comparing DOX@SCEO-NANO/DOX versus DOX, greater levels of caspase-3 and the Bax/Bcl-2 ratio were observed.</p><p><strong>Conclusion: </strong>The DOX@SCEO-NANO/DOX formulation showed potential for targeted eradication of colon adenocarcinoma and hepatocellular carcinoma cells.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"503-518"},"PeriodicalIF":3.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141875115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The assessment of pharmacokinetics and neuroprotective effect of berberine hydrochloride-embedded albumin nanoparticles via various administration routes: comparative in-vivo studies in rats. 通过不同给药途径评估盐酸小檗碱嵌入白蛋白纳米颗粒的药代动力学和神经保护作用:大鼠体内对比研究。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-11-01 Epub Date: 2024-09-04 DOI: 10.1080/02652048.2024.2395976
Hany G Attia, Maha E Elmataeeshy, Mohamed Aleraky, Samar R Saleh, Doaa A Ghareeb, Maha A El Demellawy, Hanan M El-Nahas, Tarek M Ibrahim

The current study aimed to evaluate the pharmacokinetics and neuroprotective effect of well-characterised berberine-bovine serum albumin (BBR-BSA) nanoparticles. BBR-BSA nanoparticles were generated by desolvation method. Entrapment efficiency, loading capacity, particle size, polydispersity index, surface morphology, thermal stability, and in-vitro release were estimated. In-vitro pharmacokinetic and tissue distribution were conducted. Their neuroprotection was evaluated against lipopolysaccharides-induced neurodegeneration. BBR-BSA nanoparticles showed satisfactory particle size (202.60 ± 1.20 nm) and entrapment efficiency (57.00 ± 1.56%). Results confirmed the formation of spheroid-thermal stable nanoparticles with a sustained drug release over 48 h. Sublingual and intranasal routes had higher pharmacokinetic plasma profiles than other routes, with Cmax values at 0.75 h (444 ± 77.79 and 259 ± 42.41 ng/mL, respectively). BBR and its metabolite distribution in the liver and kidney were higher than in plasma. Intranasal and sublingual treatment improves antioxidants, proinflammatory, amyloidogenic biomarkers, and brain architecture, protecting the brain. In conclusion, neuroinflammation and neurodegeneration may be prevented by intranasal and sublingual BBR-BSA nanoparticles.

本研究旨在评估特征明确的小檗碱-牛血清白蛋白(BBR-BSA)纳米颗粒的药代动力学和神经保护作用。小檗碱-牛血清白蛋白(BBR-BSA)纳米颗粒由脱溶法生成。对其包封效率、负载能力、粒度、多分散指数、表面形态、热稳定性和体外释放进行了估算。还进行了体外药代动力学和组织分布研究。评估了它们对脂多糖诱导的神经变性的神经保护作用。BBR-BSA 纳米粒子的粒径(202.60 ± 1.20 nm)和包埋效率(57.00 ± 1.56%)均令人满意。舌下和鼻内途径的药代动力学血浆曲线高于其他途径,0.75 h时的Cmax值分别为(444 ± 77.79和259 ± 42.41 ng/mL)。BBR 及其代谢物在肝脏和肾脏中的分布高于在血浆中的分布。鼻内和舌下治疗可改善抗氧化剂、促炎症、淀粉样蛋白生成生物标志物和大脑结构,从而保护大脑。总之,鼻内和舌下含服 BBR-BSA 纳米粒子可预防神经炎症和神经变性。
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引用次数: 0
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Journal of microencapsulation
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