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Drug loading comparison of commercial ibuprofen on magnetite nanoparticles surface by UV–Vis spectrophotometry and acid-alkali titration by a factorial design of experiments 用紫外可见分光光度法和酸碱滴定法比较商品布洛芬在磁铁矿纳米颗粒表面的载药量
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-21 DOI: 10.1016/j.onano.2023.100193
Felipe Ocampo Osorio , Esteban Noé Villanueva Badillo , Dariana Geraldine Erazo Rondón , Erika Tatiana Muñoz Arango , Abilo Andrés Velásquez Salazar , Alvaro Andrés Velasquez Torres , Oscar Moscoso Londoño , Elisabeth Restrepo Parra , César Leandro Londoño Calderón

The drug efficacy for the pathologies treatments depends on several physicochemical properties of the drug. Among these, solubility is one of the most important and is directly related to the bioavailability of the drug. Ibuprofen is a popular drug used for the treatment of different diseases. However, its dissolution rate in aqueous media is limited, which causes undesirable adverse effects on the patient. One of the possibilities to solve this challenge is loading ibuprofen on the surface of the nanoparticles for drug delivery. However, some challenges related to complicated experimental procedures, expensive chemical precursors, the techniques for ibuprofen quantification, and the loading efficiency continue to be a problem. This work reports the synthesis of magnetite nanoparticles and the straightforward loading with commercial ibuprofen in a mixed ethanol/water solution without intermediate surfactants, stabilizers, or linkers. XRD, SEM, FT-IR, Magnetometry, UV–Vis Spectrophotometry, and DLS techniques allowed for determining the samples' structure, morphology, functional groups, magnetism, and agglomerate size. A complete factorial Design of Experiments allowed for comparing the encapsulation efficiency for two exposure and centrifugation times (20 and 40 min) by UV–VIS and Acid-alkali titration. The results suggest that the magnetic separation and centrifugation (< 2000 RPM) were inappropriate for nanoparticle decantation. This produces an underestimation of the ibuprofen adsorbed by the nanoparticles. Under our experimental conditions, 20 min is enough to achieve maximum encapsulation efficiency (14%) without surfactants or binders.

病理治疗的药物疗效取决于药物的几个物理化学性质。其中,溶解度是最重要的,直接关系到药物的生物利用度。布洛芬是一种流行的药物,用于治疗不同的疾病。然而,它在水性介质中的溶解速率是有限的,这对患者造成了不希望的不良影响。解决这一挑战的可能性之一是将布洛芬负载在纳米颗粒表面用于药物递送。然而,与复杂的实验程序、昂贵的化学前体、布洛芬定量技术和负载效率有关的一些挑战仍然是一个问题。这项工作报道了磁铁矿纳米颗粒的合成以及在不含中间表面活性剂、稳定剂或连接体的混合乙醇/水溶液中直接负载商业布洛芬。XRD、SEM、FT-IR、磁强计、UV–Vis分光光度法和DLS技术可用于测定样品的结构、形态、官能团、磁性和团聚体尺寸。完全析因实验设计允许通过紫外-可见光谱和酸碱滴定比较两次暴露和离心时间(20和40分钟)的包封效率。结果表明,磁性分离和离心(<;2000RPM)不适于纳米粒子倾析。这就低估了纳米颗粒吸附的布洛芬。在我们的实验条件下,在没有表面活性剂或粘合剂的情况下,20分钟足以实现最大封装效率(14%)。
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引用次数: 0
Nanotoxicity induced by nanomaterials: A review of factors affecting nanotoxicity and possible adaptations 纳米材料诱导的纳米毒性:影响纳米毒性的因素和可能的适应性的综述
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-13 DOI: 10.1016/j.onano.2023.100190
Hnin Ei Thu , Mohamed Haider , Shahzeb Khan , Mohammad Sohail , Zahid Hussain

Owing to their unique characteristic features (e.g., nano-scaled dimensions, surface charge, surface chemistry, thermodynamics, morphology, etc.), diversity of functionalization, and great penetrability to body tissues, nanomaterials have been widely employed in various fields including medical and health sciences. The feasibility and significance of nanomaterials has been well-explored as drug delivery devices, diagnostic tools, vaccination, prognostic agents, and gene therapy; however, substantial evidence on safety of these nanomaterials is lacking. The aim of this study was critical evaluation of available literature on the safety concerns of various nanomaterials and conceptualization of vital factors which might help in mitigating the toxicity caused by these nanomaterials. It has been established that various factors such as particle size, dosage regimen, route of exposure, surface chemistry, degree of aggregation, transmembrane diffusivity, excretion pathway, and immunogenicity play key role in inducing the nanotoxicity. By controlling these factors, interaction of nanomaterials with biological tissues, their penetrability, diffusivity, absorption, distribution, recognition by the immune players, duration of deposition into various body tissues, and clearance from the body can be controlled to avert unintended nanotoxicity. Furthermore, it has been identified that surface functionalization of nanomaterials with diverse moieties such as sodium citrate, polyvinylpyrrolidone (PVP) and/or surfactants could significantly downregulate their nanotoxicity potential and improve their safety profile. Factually, nanotoxicity is a grave concern which should be consider while designing of any nanomaterials to circumvent their detrimental interactions with various biological tissues.

由于其独特的特征(例如,纳米尺度的尺寸、表面电荷、表面化学、热力学、形态等)、功能化的多样性和对身体组织的巨大渗透性,纳米材料已被广泛应用于包括医学和健康科学在内的各个领域。纳米材料作为药物递送装置、诊断工具、疫苗接种、预后剂和基因治疗的可行性和重要性已经得到了很好的探索;然而,缺乏关于这些纳米材料安全性的实质性证据。本研究的目的是对各种纳米材料的安全问题的现有文献进行批判性评估,并对可能有助于减轻这些纳米材料引起的毒性的重要因素进行概念化。已经证实,粒径、给药方案、暴露途径、表面化学、聚集程度、跨膜扩散率、排泄途径和免疫原性等多种因素在诱导纳米毒性中起着关键作用。通过控制这些因素,可以控制纳米材料与生物组织的相互作用、它们的穿透性、扩散性、吸收、分布、免疫参与者的识别、沉积到各种身体组织中的持续时间以及从体内清除,以避免意外的纳米毒性。此外,已经确定,具有不同部分(如柠檬酸钠、聚乙烯吡咯烷酮(PVP)和/或表面活性剂)的纳米材料的表面功能化可以显著下调其纳米毒性潜力并提高其安全性。事实上,纳米毒性是一个严重的问题,在设计任何纳米材料以避免其与各种生物组织的有害相互作用时,都应该考虑到这一点。
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引用次数: 1
Phyto-derived metal nanoparticles: Prominent tool for biomedical applications 植物衍生的金属纳米颗粒:生物医学应用的重要工具
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-13 DOI: 10.1016/j.onano.2023.100192
P.R. Bhilkar , A.S. Bodhne , S.T. Yerpude , R.S. Madankar , S.R. Somkuwar , A.R. Daddemal-Chaudhary , A.P. Lambat , M. Desimone , Rohit Sharma , R.G. Chaudhary

Nanoparticles (NPs), despite of very small in size have extraordinary power and functional ability, forms the backbone of nanomaterials science, and utilizes it in diverse fields. Many conventional methods can be employed for the fabrication of NPs, but it required either high energy with producing toxic byproducts that degrades an environment. Therefore, a green approach is needed to save an environment. Green methods provide the simple, straightforward, cost-effective and environmentally-safe approach for the NPs synthesis. Plant derived NPs, is one of the best and supreme methods with green and sustainable routes for preparation of NPs. As plant derived metal NPs gains the more attention due to their green synthesis approach and significant for biomedical appliances. In the present review, we concentrated on synthesis of plant derived metal NPs (Ag, Au, Cu, Ni, Zn and Ti) with their morphologies and biomedical applications. Also discussed the therapeutic applications and future perspective of plant derived metal NPs.

纳米颗粒(NP)虽然体积很小,但具有非凡的力量和功能,构成了纳米材料科学的支柱,并在不同领域中加以利用。许多传统方法可以用于制造NP,但它需要高能量,产生降解环境的有毒副产品。因此,需要一种绿色的方法来拯救环境。绿色方法为NPs的合成提供了简单、直接、成本效益高和环境安全的方法。植物衍生的纳米颗粒,是制备纳米颗粒的最佳和最高的方法之一,具有绿色和可持续的路线。作为植物衍生的金属纳米粒子,由于其绿色合成方法和在生物医学应用中的重要意义而受到越来越多的关注。在本综述中,我们重点研究了植物衍生金属纳米颗粒(Ag、Au、Cu、Ni、Zn和Ti)的合成及其形貌和生物医学应用。还讨论了植物衍生金属纳米粒子的治疗应用和未来前景。
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引用次数: 1
Fabrication and evaluation of poly(ε-caprolactone) based nanofibrous scaffolds loaded with homoeopathic mother tincture of Syzygium cumini for wound healing applications 聚ε-己内酯纳米纤维支架的制备及其在伤口愈合中的应用
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-12 DOI: 10.1016/j.onano.2023.100189
Deiviga Murugan , Ankitha Suresh , Goutam Thakur , Bhisham Narayan Singh

Traditional wound healing substitutes loaded with bioactive molecules such as drugs, growth factors, and so on have been extensively researched in order to promote better wound healing and restore normal tissue function. The use of nanofibrous scaffolds has enhanced the biomaterial performance, thereby offering a promising solution as wound dressings in the field of skin tissue engineering. In the present study, the homoeopathic mother tincture extract of Syzygium cumini incorporated in poly(ε-caprolactone) nanofibrous scaffolds were fabricated in the concentration range of 5 %–20 % (w/w) and its various physicochemical and biological properties were evaluated. The fabricated nanofibers structurally mimicked the extracellular matrix, with enhanced hydrophilicity for better cellular attachment and proliferation. These scaffolds also showed anti-biofilm activity against P. aeruginosa and S. aureus and exhibited superior anti-oxidant activity. Furthermore, the extract incorporation was observed to be beneficial in cell adhesion, viability, growth and proliferation. This novel poly(ε-caprolactone) nanofibrous scaffold loaded with homoeopathic mother tincture  extract of Syzygium cumini might be a suitable biomaterial for clinical management of wounds and reconstruction of damaged/diseased skin tissues.

传统的含有药物、生长因子等生物活性分子的伤口愈合替代品已被广泛研究,以促进更好的伤口愈合和恢复正常组织功能。纳米纤维支架的使用增强了生物材料的性能,从而在皮肤组织工程领域提供了一种很有前途的伤口敷料解决方案。在本研究中,在5%-20%(w/w)的浓度范围内,制备了掺入聚(ε-己内酯)纳米纤维支架的孜然同源性母酊提取物,并对其各种理化和生物学特性进行了评价。所制备的纳米纤维在结构上模拟了细胞外基质,具有增强的亲水性,以更好地附着和增殖细胞。这些支架还表现出对铜绿假单胞菌和金黄色葡萄球菌的抗生物膜活性,并表现出优异的抗氧化活性。此外,观察到提取物掺入对细胞粘附、活力、生长和增殖有益。这种新型的聚(ε-己内酯)纳米纤维支架负载了Syzygium cumini的顺势疗法母酊提取物,可能是一种适合临床治疗伤口和重建受损/患病皮肤组织的生物材料。
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引用次数: 0
Modeling the particle size of nanomaterials synthesized in a planetary ball mill 行星球磨机合成纳米材料的粒径模拟
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-10-09 DOI: 10.1016/j.onano.2023.100191
Chwadaka Pohshna, Damodhara Rao Mailapalli

Planetary ball milling (PBM) synthesis of nanoparticles involves conducting several trials to obtain the desired size. Mathematical modeling of the PBM process is a tool to tackle the issue of PBM synthesis. In this study, a conceptual model was proposed by integrating the kinematics of the PBM process along with the breakage mechanism of a material to determine particle size at different milling parameters and hence be able to select appropriate milling parameters for PBM synthesis. The conceptual model was tested for hydroxyapatite, zeolite and fly ash material. The conceptual model successfully simulated the size-reduction mechanism in PBM and predicted the particle size of the tested material with good accuracy. The most sensitive milling parameters were found to be the milling speed followed by the vial volume, milling time, and ball to powder ratio. The material properties input parameters were observed to be less sensitive than the milling parameters. The PBM model may be used as a prediction tool for determining the appropriate milling parameters needed in synthesizing any nanomaterial by knowing the material properties.

行星球磨(PBM)合成纳米颗粒需要进行几次试验以获得所需的尺寸。PBM过程的数学建模是解决PBM合成问题的工具。在本研究中,通过将PBM过程的运动学与材料的破碎机制相结合,提出了一个概念模型,以确定不同研磨参数下的颗粒尺寸,从而能够为PBM合成选择合适的研磨参数。对羟基磷灰石、沸石和粉煤灰材料的概念模型进行了测试。该概念模型成功地模拟了PBM中的尺寸减小机制,并以良好的精度预测了测试材料的粒度。发现最敏感的研磨参数是研磨速度,其次是小瓶体积、研磨时间和球粉比。观察到材料特性输入参数不如铣削参数敏感。PBM模型可以用作预测工具,用于通过知道材料性质来确定合成任何纳米材料所需的适当铣削参数。
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引用次数: 0
Application of the novel Cu-resistant fungus Aspergillus niger A3 in bioremoval of Cu-NPs from its aqueous solutions 新型抗铜真菌黑曲霉A3在水中生物去除Cu-NPs中的应用
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-09-12 DOI: 10.1016/j.onano.2023.100187
Osama M. Darwesh , Marwa A. Shalaby , Mohamed M. Gharieb , Ibrahim A. Matter

Copper is an essential element for the metabolism of plants and animals, and has wide applications in the agricultural and industrial sectors. On the other hand, copper nanoparticles (Cu-NPs) have become widely used for research and application, which increases the chances of its spread and potential environmental exposure to this element. Therefore, in this study, the bioremediation bioreactor for the removing of Cu-NPs based on a fungal strain (Aspergillus niger) was introduced. A. niger isolate MR3 with accession No. OP861660.1 after molecular identification was selected as a promising isolate for copper resistance and Cu-NPs bioremoval. The impact of biomass age, pH, and contact time was investigated in order to establish the ideal biosorption conditions. The results showed a high Cu-NPs removal via two-days-old A. niger biomass, where the bioremoval percentage reached 66.8 % at pH value 7 after a contact time of 10 min. Dead biomass of A. niger achieved the highest Cu-NPs removal rate, eliminating 68.2 % compared with both living and alginate beads-immobilized biomass. Thus, bioremoval experiments using dead biomass were performed in a bioreactor for sequential removal of Cu-NPs. The bioremoval capacity reached 97 % under optimized conditions from synthetic wastewater after a contacting time of 10 min. Thus, the present work considered the first report for bioremediation of Cu-NPs into bioreactor.

铜是动植物代谢的重要元素,在农业和工业部门有着广泛的应用。另一方面,铜纳米颗粒(Cu-NPs)已被广泛用于研究和应用,这增加了其传播的机会,并增加了其潜在的环境暴露于该元素的可能性。因此,在本研究中,介绍了一种基于真菌菌株(黑曲霉)的生物修复生物反应器,用于去除Cu NPs。经分子鉴定后,黑曲霉分离物MR3(登录号OP861660.1)被选为耐铜和Cu NPs生物去除的有前途的分离物。研究了生物量年龄、pH值和接触时间的影响,以建立理想的生物吸附条件。结果表明,通过两天龄的黑曲霉生物质对Cu NPs的去除率很高,在接触时间为10分钟后,pH值为7时,生物去除率达到66.8%。黑曲霉的死生物量对Cu NPs的去除率最高,与活生物和藻酸盐珠固定化生物量相比,去除率为68.2%。因此,在生物反应器中使用死生物质进行生物去除实验,以顺序去除Cu NP。在优化的条件下,经10分钟的接触,合成废水的生物去除率达到97%。因此,本工作考虑了将Cu NPs生物修复到生物反应器中的第一份报告。
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引用次数: 0
In-vitro antioxidant, antidiabetic, anticholinergic activity of iron/copper nanoparticles synthesized using Strobilanthes cordifolia leaf extract 桔梗叶提取物合成铁/铜纳米颗粒体外抗氧化、抗糖尿病、抗胆碱能活性研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-09-12 DOI: 10.1016/j.onano.2023.100188
Dharmalingam Kirubakaran , Kuppusamy Selvam , Palanisamy Prakash , Muthugounder Subaramanian Shivakumar , Manickam Rajkumar

The Strobilanthes cordifolia plant, a member of the Acanthaceae family, has been extensively studied due to its wide range of biological properties. This particular research focused on the green synthesis of FeNPs/CuNPs and evaluated the effectiveness of the experiment through various characterization techniques, including UV, FTIR, XRD, and SEM with EDAX. The UV analysis provided valuable insights, showing that the synthesized nanoparticles had the highest absorption values at 462nm for FeNPs and 438nm for CuNPs. FTIR analysis confirmed the presence of different functional groups, while XRD measurements validated their crystalline nature. SEM data revealed the diverse shapes of the nanoparticles, including rods and spherical shapes. Additionally, EDAX analysis confirmed the presence of Fe and Cu elements in the biosynthesized nanoparticles. The antibacterial activity of FeNPs and CuNPs against Staphylococcus aureus and Escherichia coli showed significant inhibition. Moreover, the nanoparticles demonstrated strong antioxidant activity, as evidenced by their effective inhibition in DPPH and ABTS assays. Their potential as anti-diabetic agents was also explored, with assessments of their inhibitory effects on α-Amylase and α-Glucosidase enzymes. Additionally, the nanoparticles displayed inhibitory effects on anti-cholinergic enzymes such as AChE and BChE. Furthermore, comprehensive toxicological studies revealed a higher level of mosquito larvicidal activity against Aedes aegypti, Anopheles stephensi, and Culex quinquefasciatus. Among these, the FeNPs exhibited a larval mortality rate of 95% in Cx. Quinquefasciatus, while the CuNPs showed a rate of 93%. In conclusion, this study demonstrated that FeNPs/CuNPs possess favorable characteristics and significant potential for various biomedical applications.

心叶牛膝属无患子科植物,由于其广泛的生物学特性,已被广泛研究。这项特别的研究集中在FeNPs/CuNPs的绿色合成上,并通过各种表征技术评估了实验的有效性,包括UV、FTIR、XRD和EDAX的SEM。UV分析提供了有价值的见解,表明合成的纳米颗粒在462nm处对FeNPs和438nm处对CuNPs具有最高的吸收值。FTIR分析证实了不同官能团的存在,而XRD测量验证了它们的结晶性质。SEM数据揭示了纳米颗粒的不同形状,包括棒状和球形。此外,EDAX分析证实了在生物合成的纳米颗粒中存在Fe和Cu元素。FeNPs和CuNPs对金黄色葡萄球菌和大肠杆菌的抗菌活性显示出显著的抑制作用。此外,纳米颗粒表现出强大的抗氧化活性,这在DPPH和ABTS测定中得到了有效的抑制。还探讨了它们作为抗糖尿病药物的潜力,并评估了它们对α-淀粉酶和α-葡萄糖苷酶的抑制作用。此外,纳米颗粒对抗胆碱能酶如AChE和BChE表现出抑制作用。此外,全面的毒理学研究表明,蚊子对埃及伊蚊、斯氏按蚊和致倦库蚊具有更高水平的杀幼虫活性。其中,FeNPs在Quinquefasciatus中的幼虫死亡率为95%,而CuNPs的死亡率为93%。总之,本研究表明,FeNPs/CuNPs具有良好的特性,在各种生物医学应用中具有巨大的潜力。
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引用次数: 1
Pulmonary delivery of siRNA-loaded lipid-polymer hybrid nanoparticles: Effect of nanoparticle size sirna负载的脂质-聚合物混合纳米颗粒的肺递送:纳米颗粒大小的影响
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-09-01 DOI: 10.1016/j.onano.2023.100180
Abishek Wadhwa , Thomas R. Bobak , Lennart Bohrmann , Reka Geczy , Sathiya Sekar , Gowtham Sathyanarayanan , Jörg P. Kutter , Henrik Franzyk , Camilla Foged , Katayoun Saatchi , Urs O. Häfeli

Nanomedicines based on nanoparticles rely both on the potency of the drug as well as the efficiency of the delivery system, for which particle size plays a crucial role. For the intracellular delivery of small interference RNA (siRNA), lipid-polymer nanoparticle (LPN) hybrid systems constitute a safe and highly effective class of delivery systems. In the present study, we employ a microfluidics method for the manufacturing of spherical siRNA-loaded LPNs for pulmonary delivery with distinct size distributions with average diameters of approximately 70, 110, and 220 nm. We designed an optically clear, inexpensive thiol-ene polymeric microfluidic chip prototype that is compatible with standard ‘soft-lithography’ techniques, allows for replica molding, and is resistant to harsh solvents. By using SPECT/CT in vivo imaging, we show comparable pulmonary clearance patterns of all three differently sized LPN formulations following intratracheal administration. Also, negligible accumulation in the liver was observed.

基于纳米颗粒的纳米药物既依赖于药物的效力,也依赖于输送系统的效率,其中颗粒大小起着至关重要的作用。对于小干扰RNA (siRNA)的细胞内递送,脂质-聚合物纳米颗粒(LPN)混合系统构成了一种安全高效的递送系统。在本研究中,我们采用微流体方法制造了用于肺输送的球形sirna负载lpn,其平均直径约为70、110和220 nm。我们设计了一种光学清晰,廉价的巯基聚合物微流控芯片原型,它与标准的“软光刻”技术兼容,允许复制成型,并且耐苛刻的溶剂。通过使用SPECT/CT体内成像,我们显示了气管内给药后所有三种不同大小的LPN制剂的可比较的肺清除率模式。此外,在肝脏中观察到可忽略不计的积累。
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引用次数: 0
Carotenoid containing cationic nanoparticles for effective therapy for suppressing oxidative stress: An intranasal approach 含类胡萝卜素阳离子纳米颗粒有效治疗氧化应激:经鼻途径
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-09-01 DOI: 10.1016/j.onano.2023.100172
Namdev Dhas , Atul Garkal , Ritu Kudarha , Srinivas Hebbar , Srinivas Mutalik , Tejal Mehta

Alzheimer's disease is the most common type of dementia. Oxidative stress is involved in the progression of aging and Alzheimer's disease. It is known that lutein is a carotenoid having antioxidant properties. The present research explores Lutein loaded chitosan nanoparticles for Suppressing Oxidative Stress in the treatment of Alzheimer's. The developed nanoparticles are administered through the nose to target brain via nose-to-brain pathway. For optimization of formulation a systematic QbD approach was used. The developed nanoparticles further characterized for Physicochemical parameters, Morphology, In-vitro drug releases, Ex-vivo diffusion, In-vitro Cell viability, cellular uptake, In-vitro BBB Permeation, antioxidant properties, In-vivo biodistribution, and stability study. The developed nanoparticles' surface morphology suggested homogeneously dispersed spherical nanoparticles having < 200 nm size. The drug release study demonstrate the controlled release of lutein for more than 96 h while less than 50% lutein was released after 24 h in an ex-vivo diffusion study. The cell cytotoxicity assay confirms the nontoxicity of l-CNPs. The cellular uptake study shows enhanced internalization of l-CNPs through the caveolae-mediated endocytosis pathway. The ROS generation confirmed the absence of any significant ROS generation nanoparticles. The antioxidant assay shows significant ROS scavenging activity of l-CNPs. In-vitro BBB permeation demonstrates the efficient passage of l-CNPs through BBB compared to pure lutein. This was further supported by bio-distribution demonstrating the deposition of nanoparticles in the brain through nasal administration. The acquired outcomes prove the possible activities of lutein-loaded l-CNPs for reducing oxidative stress in the brain for Alzheimer's treatment.

阿尔茨海默病是最常见的痴呆症。氧化应激与衰老和阿尔茨海默病的进展有关。众所周知,叶黄素是一种具有抗氧化特性的类胡萝卜素。本研究探讨了负载叶黄素的壳聚糖纳米颗粒在阿尔茨海默病治疗中的氧化应激抑制作用。所研制的纳米颗粒通过鼻子到大脑的途径进入目标大脑。为了优化配方,采用了系统的QbD方法。进一步表征了纳米颗粒的理化参数、形态、体外药物释放、体外扩散、体外细胞活力、细胞摄取、体外血脑屏障渗透、抗氧化性能、体内生物分布和稳定性研究。发育的纳米颗粒的表面形貌表明,均匀分散的球形纳米颗粒具有<200nm尺寸。药物释放研究表明,叶黄素的控释时间超过96 h,而体外扩散研究表明,24 h后叶黄素的释放量不到50%。细胞毒性实验证实了l-CNPs的无毒性。细胞摄取研究表明,通过小泡介导的内吞途径增强了l-CNPs的内在化。ROS生成证实没有任何显著的ROS生成纳米颗粒。抗氧化实验表明,l-CNPs具有明显的ROS清除活性。与纯叶黄素相比,体外血脑屏障渗透证明了l-CNPs通过血脑屏障的有效通道。这进一步得到了生物分布的支持,证明纳米颗粒通过鼻腔给药在大脑中沉积。获得的结果证明了叶黄素负载的l-CNPs可能具有降低大脑氧化应激的活性,从而治疗阿尔茨海默病。
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引用次数: 0
Dendrimer-based nanocomposites for the production of RNA delivery systems 用于RNA递送系统的树突基纳米复合材料
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-09-01 DOI: 10.1016/j.onano.2023.100173
Chiou Chyi Lim, Le Yi Chia, Palanirajan Vijayaraj Kumar

A novel approach to treating cancer has been revealed to be effective cancer vaccination. It has also been demonstrated that nucleic acid therapies such as mRNA and siRNA are very efficient in the treatment of cancer. However, the instability of mRNA makes a delivery system necessary to reach the target sites. Dendrimers have emerged as being of important interest in healthcare due to their ideal characteristic of having a very strong drug delivery capacity to become carriers. The dendrimer's center can be loaded with specific pharmaceutical active ingredients, or they can be bonded to the surface. RNA delivery systems that transport siRNA, mRNA, and other forms of RNA can be made using dendrimers. This review article focuses on several dendrimer-based RNA delivery systems, such as dendrimers modified with PEG, mannosylated dendrimers, dendrisomes, amphiphilic dendrimer vectors, magnetic nanoparticles modified with dendrimers, peptide dendrimers, and gold nanoparticles coated with dendrimers.

一种治疗癌症的新方法是有效的癌症疫苗接种。研究还表明,mRNA和siRNA等核酸疗法在治疗癌症方面非常有效。然而,mRNA的不稳定性使得递送系统必须到达目标位点。由于树突状分子具有很强的药物输送能力成为载体的理想特性,因此树突状分子在医疗保健领域具有重要的兴趣。树状大分子的中心可以装载特定的药物活性成分,或者它们可以与表面结合。利用树突大分子可以制造出运输siRNA、mRNA和其他形式RNA的RNA传递系统。本文综述了几种基于树状大分子的RNA递送系统,如聚乙二醇修饰的树状大分子、甘露糖基树状大分子、树状小体、两亲性树状大分子载体、用树状大分子修饰的磁性纳米粒子、肽树状大分子和涂覆树状大分子的金纳米粒子。
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引用次数: 2
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