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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 : 2025-01-01 Epub 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
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 : 2025-01-01 Epub 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
Lipid nanocarrier-based bigel of Piper betel oil for analgesic and anti-inflammatory applications. 基于脂质纳米载体的胡椒槟榔油镇痛消炎应用。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2025-01-01 Epub Date: 2024-11-25 DOI: 10.1080/02652048.2024.2430651
Bhabani Sankar Satapathy, Abhishek Mishra, Kritika Mohanty, Snigdha Pattnaik, Shyamalendu Tripathy, Biswabhusan Biswal

Present study reports analgesic and anti-inflammatory potential of Piper betel (L.) leaf oil loaded lipid nanocarrier (BLNs)-embedded bigel. BLNs were developed by solvent evaporation technique and were characterised by FESEM, Cryo-TEM, mean diameter, zeta potential, loading efficiency, etc. BLNs embedded bigel (BLNs-G) was evaluated for analgesic and anti-inflammatory efficacy in rat model. Data showed spherical BLNs with intact lamellarity, 138.2 ± 1.08 nm mean diameter, 0.182 PDI, -46.6 ± 0.61 mV zeta potential, 76.2 ± 2.1% (w/w) loading efficiency and a sustained release in vitro. BLNs-G was homogenous with satisfied viscosity (40 734 ± 1.7 cps), spreadability (8.3 ± 1.5 g.cm sec-1), extrudability (91.33 ± 1.3% w/w) along with a sustained permeation ex vivo. Significant analgesic and anti-inflammatory action were depicted by BLNs-G (1% w/w) in rat model (p ˂ 0.05) within 30 minutes post topical application. In silico docking study revealed high affinity of major phytoactive components with key analgesic/inflammatory mediators. Further pre-clinical investigations are warranted for futuristic clinical application of BLNs-G.

本研究报告了含槟榔叶脂质纳米载体(BLNs)的槟榔叶镇痛和抗炎潜力。BLNs 采用溶剂蒸发技术开发,并通过 FESEM、Cryo-TEM、平均直径、Zeta 电位、负载效率等进行表征。在大鼠模型中评估了嵌入 bigel 的 BLNs(BLNs-G)的镇痛和抗炎功效。数据显示,BLNs-G 为球形,具有完整的层状结构,平均直径为 138.2 ± 1.08 nm,PDI 为 0.182,Zeta 电位为 -46.6 ± 0.61 mV,负载效率为 76.2 ± 2.1%(w/w),体外可持续释放。BLNs-G 具有均匀的粘度(40 734 ± 1.7 cps)、铺展性(8.3 ± 1.5 g.cm sec-1)和挤出性(91.33 ± 1.3% w/w),并具有体内持续渗透性。在大鼠模型中,BLNs-G(1% w/w)在局部使用后 30 分钟内具有显著的镇痛和抗炎作用(p ˂ 0.05)。硅学对接研究显示,主要植物活性成分与关键的镇痛/炎症介质具有很高的亲和力。有必要对 BLNs-G 的未来临床应用进行进一步的临床前研究。
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引用次数: 0
Harnessing the power of novel drug delivery systems for effective delivery of apigenin: an updated review. 利用新型药物输送系统的力量有效输送芹菜素:最新综述。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2025-01-01 Epub Date: 2024-12-13 DOI: 10.1080/02652048.2024.2437375
Vanshita, Tanu Rawal, Hemant Bhati, Keshav Bansal

Phytochemicals as dietary components are being extensively explored in order to prevent and treat a wide range of diseases. Apigenin is among the most studied flavonoids found in significant amount in fruits (oranges), vegetables (celery, parsley, onions), plant-based beverages (beer, tea, wine) and herbs (thyme, chamomile, basil, oregano) that has recently gained interest due to its promising pharmacological effects. However, the poor solubility and extended first pass metabolism of apigenin limits its clinical use. Various advantages have been demonstrated by nanocarrier-based platforms in the delivery of hydrophobic drugs like apigenin to diseased tissues. Apigenin nanoformulations have been reported to have better stability, high encapsulation efficiency, prolonged circulation time, sustained release, enhanced accumulation at targeted sites and better therapeutic efficacy. An overview of the major nanocarriers based delivery including liposomes, niosomes, solid lipid nanoparticles, micelles, dendrimers etc., is described. This review sheds insight into the therapeutic effects and advanced drug delivery strategies for the delivery of apigenin.

为了预防和治疗多种疾病,人们正在广泛探索将植物化学物质作为膳食成分。芹菜素是研究最多的类黄酮之一,在水果(橙子)、蔬菜(芹菜、欧芹、洋葱)、植物性饮料(啤酒、茶、葡萄酒)和草药(百里香、洋甘菊、罗勒、牛至)中发现了大量的芹菜素,最近由于其有希望的药理作用而引起了人们的兴趣。然而,芹菜素的溶解度差和第一次代谢延长限制了其临床应用。基于纳米载体的平台在将疏水药物(如芹菜素)递送到病变组织方面已经证明了各种优势。芹菜素纳米制剂具有稳定性好、包封效率高、循环时间长、缓释、靶向蓄积增强、治疗效果好等优点。概述了主要的基于纳米载体的递送,包括脂质体、乳质体、固体脂质纳米颗粒、胶束、树状大分子等。本文综述了芹菜素的治疗效果和先进的给药策略。
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引用次数: 0
Preparation and optimisation of solid lipid nanoparticles of rivaroxaban using artificial neural networks and response surface method. 利用人工神经网络和响应面法制备利伐沙班固体脂质纳米颗粒并进行优化。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2025-01-01 Epub Date: 2025-01-05 DOI: 10.1080/02652048.2024.2437362
Fatemeh Ghorbannejad Nashli, Sareh Aghajanpour, Ali Farmoudeh, Seyed Sajad Hosseini Balef, Meshkat Torkamanian, Alireza Razavi, Hamid Irannejad, Pedram Ebrahimnejad

Aims: This study aimed to improve rivaroxaban delivery by optimising solid lipid nanoparticles (SLN) for minimal mean diameter and maximal entrapment efficiency (EE), enhancing solubility, bioavailability, and the ability to cross the blood-brain barrier.

Methods: A central composite design was employed to synthesise 32 SLN formulations. Response surface methodology (RSM) and artificial neural networks (ANN) models predicted mean diameter and EE based on five independent variables.

Results: The optimised SLN formulation achieved a mean particle diameter of 159.8 ± 15.2 nm, with a Polydispersity index of 0.46, a zeta potential of -28.8 mV, and an EE of 74.3% ± 5.6%. The ANN model showed superior accuracy for both mean diameter and EE, outperforming the RSM model. Structural integrity and stability were confirmed by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier-transform infrared spectroscopy (FTIR).

Conclusion: The high accuracy of the ANN model highlights its potential in optimising pharmaceutical formulations and improving SLN-based drug delivery systems.

目的:本研究旨在通过优化固体脂质纳米颗粒(SLN)以实现最小平均直径和最大包裹效率(EE)、提高溶解度、生物利用度和穿越血脑屏障的能力来改善利伐沙班的递送。方法:采用中心复合设计,合成32个SLN配方。响应面法(RSM)和人工神经网络(ANN)模型基于5个自变量预测了平均直径和EE。结果:优化后的SLN平均粒径为159.8±15.2 nm,多分散性指数为0.46,zeta电位为-28.8 mV, EE为74.3%±5.6%。人工神经网络模型在平均直径和EE上都表现出更高的精度,优于RSM模型。通过扫描电镜(SEM)、差示扫描量热法(DSC)和傅里叶变换红外光谱(FTIR)证实了结构的完整性和稳定性。结论:人工神经网络模型的高准确性突出了其在优化药物配方和改进基于sln的给药系统方面的潜力。
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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 : 2025-01-01 Epub 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。
{"title":"Spray-dried chitosan oligosaccharide microparticles with polyvinyl alcohol-based dispersions for improved gefitinib solubility.","authors":"Shubham B Ahir, Bhaskar Vallamkonda, Ranadheer Reddy Challa, Nishant Chopade, Prashant K Deshmukh, Mahesh P More","doi":"10.1080/02652048.2024.2428359","DOIUrl":"10.1080/02652048.2024.2428359","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":16391,"journal":{"name":"Journal of microencapsulation","volume":" ","pages":"14-25"},"PeriodicalIF":3.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142675971","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
Advancements in microneedle technology: current status and next-generation innovations. 微针技术的进步:现状与下一代创新。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-12-01 Epub Date: 2024-10-30 DOI: 10.1080/02652048.2024.2418613
Siddhant Kumar, Rahul Shukla

Microneedle technology is a pivotal component of third-generation transdermal drug delivery systems featuring tiny needles that create temporary microscopic channels in the stratum corneum which facilitate drug penetration in the dermis. This review offers a detailed examination of the current types of microneedles, including solid, coated, dissolving, hollow, and swelling microneedles, along with their preparation techniques as well as their benefits and challenges. Use of 3D printing technology is especially gaining significant attention due to its ability to achieve the high dimensional accuracy required for precise fabrication. Additionally, its customisability presents significant potential for exploring new designs and creating personalised microneedles products. Furthermore, this review explores next generation microneedles, especially stimuli-responsive microneedle, bioinspired microneedle and microneedles combined with other transdermal technology like sonophoresis, electroporation and iontophoresis. Regulatory aspects, characterisation techniques, safety considerations, and cost factors have also been addressed which are crucial for translation from lab to the market.

微针技术是第三代透皮给药系统的重要组成部分,其特点是用微小的针头在角质层建立临时的微通道,从而促进药物在真皮层的渗透。本综述详细介绍了目前的微针类型,包括实心微针、涂层微针、溶解微针、空心微针和膨胀微针,以及它们的制备技术、优点和挑战。三维打印技术能够实现精确制造所需的高尺寸精度,因此尤其受到人们的关注。此外,三维打印技术的可定制性为探索新设计和创造个性化微针产品提供了巨大潜力。此外,本综述还探讨了下一代微针,特别是刺激响应微针、生物启发微针以及与其他透皮技术(如声波电泳、电穿孔和离子电泳)相结合的微针。此外,还讨论了监管方面、表征技术、安全考虑因素和成本因素,这些因素对于从实验室到市场的转化至关重要。
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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 : 2024-12-01 Epub 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。
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引用次数: 0
Biodegradable polymeric nanocomposite containing phloretin for enhanced oral bioavailability and improved myocardial ischaemic recovery. 生物可降解聚合物纳米复合材料,含有可提高口服生物利用度和改善心肌缺血恢复的酞丁胺。
IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Pub Date : 2024-12-01 Epub Date: 2024-10-21 DOI: 10.1080/02652048.2024.2418608
Prasanti Sharma, Trishna Bal, Sandeep Kumar Singh, Neelima Sharma

Aim: The study aimed to enhance phloretin's oral absorption and systemic availability through nanoencapsulation within biodegradable polymers, improving its anti-oxidant and cardioprotective potential.

Methods: Phloretin-loaded polymeric nanocomposites were prepared using ionic gelation and optimised for yield, encapsulation, loading, particle size, PdI and zeta potential. The formulation was characterised by FTIR, XRD, FESEM and MS. In-vitro drug release, stability, pharmacokinetics, biodistribution, anti-oxidant capacity, haemolysis and both in-vitro and in-vivo assessments were conducted in an ischaemia-induced rat model.

Results: The average particle size, zeta potential, encapsulation and drug loading of the optimised nanoparticles were 105.8 ± 1.92 nm, -41.5 ± 1.10 mV, 92.36 ± 0.01% and 18.47 ± 0.38%, respectively. Nano-phloretin enhanced oral bioavailability, anti-oxidant capacity. In-vivo, it reduced myocardial infarct size by ∼46% versus ∼13% for free phloretin, showing significant cardiomyocyte protection and ROS suppression.

Conclusion: The study demonstrates polymer-based nanoparticles as effective oral drug delivery systems capable of enhancing both systemic bioavailability and therapeutic efficacy of the encapsulated drug.

目的:该研究旨在通过在生物可降解聚合物中进行纳米包囊,增强酚络汀的口服吸收和全身可用性,从而提高其抗氧化和保护心脏的潜力:方法:采用离子凝胶法制备了载药萝芙汀的聚合物纳米复合材料,并对其产量、封装、载药量、粒度、PdI 和 zeta 电位进行了优化。傅立叶变换红外光谱(FTIR)、XRD、FESEM 和 MS 对配方进行了表征。在缺血诱导的大鼠模型中进行了体外药物释放、稳定性、药代动力学、生物分布、抗氧化能力、溶血以及体内和体外评估:结果:优化纳米颗粒的平均粒径、ZETA电位、包封率和载药量分别为 105.8 ± 1.92 nm、-41.5 ± 1.10 mV、92.36 ± 0.01% 和 18.47 ± 0.38%。纳米紫檀素提高了口服生物利用度和抗氧化能力。在体内,它使心肌梗死面积缩小了 46%,而游离的小叶紫檀素则缩小了 13%,显示出显著的心肌细胞保护和 ROS 抑制作用:该研究表明,聚合物纳米颗粒是一种有效的口服给药系统,能够提高封装药物的全身生物利用度和疗效。
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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 : 2024-12-01 Epub 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
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