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Effect of unsaturated fatty acids on the topical delivery of caspofungin ufasomes: In vitro/ Ex vivo evaluation and anti-fungal study against Candida albicans 不饱和脂肪酸对caspofunins ufasomes局部递送的影响:体外/体外评估和抗白色念珠菌的研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-07-01 Epub Date: 2025-06-25 DOI: 10.1016/j.onano.2025.100250
Sumayah Al-Mahmood , Nawal Ayash Rajab
Cutaneous candidiasis presents a considerable challenge in today’s medical landscape, particularly for patients with weakened immune systems or chronic illnesses. As antifungal resistance continues to rise, the development of new topical therapies has become increasingly urgent. Caspofungin (CSP), an echinocandin antifungal, exhibits fungicidal activity against Candida species by inhibiting β-1,3-d-glucan synthase, a key enzyme in fungal cell wall synthesis. However, its poor stability and requirement for intravenous administration limit its clinical application. To address these limitations, novel formulations such as ufasomes (unsaturated fatty acid vesicles) have been developed to enhance caspofungin's stability and skin penetration. In this study, ufasomes were prepared using three oils: oleic acid, linoleic acid, and palmitoleic acid, along with caspofungin and cholesterol, using the thin-film method. Among the formulations, F34, composed of 500 mg palmitoleic acid and 10 mg cholesterol, exhibited promising results. It demonstrated a particle size (PS) of 87.65± 2.65 nm, a polydispersity index (PDI) of 0.22 ± 0.00, a zeta potential (ZP) of -7.46± 0.4 mV, a drug content of 97 ± 1.34 %, and an encapsulation efficiency (EE %) of 92 ± 0.82 %. Furthermore, the optimized formulation F34 showed a sustained drug release of 81.5 ± 0.4 over 600 min (10 h) compared to 100 %±0.01 of caspofungin. The permeation of F34 in 600 min (10 h) was 94 %±0.81 compared to the caspofungin 87.85 %±0.85. The antifungal activity showed that the inhibition zone diameter, MIC and MBC for caspofungin-loaded ufasomes was 29 mm±0.8, 0.153 μg/mL±0.01, 0.283 μg/mL±0.02 compared to 25 mm±0.8, 0.214 μg/mL±0.01, 0.409±0.01 for pure caspofungin. The histopathological study revealed a positive response towards the optimized formulation. In conclusion, this optimized formulation holds potential as a novel therapeutic approach for treating topical fungal infections.
皮肤念珠菌病在当今的医疗领域提出了相当大的挑战,特别是对于免疫系统较弱或慢性疾病的患者。随着抗真菌耐药性的持续上升,开发新的局部治疗方法变得越来越紧迫。Caspofungin (CSP)是一种棘白菌素抗真菌药物,通过抑制真菌细胞壁合成的关键酶β-1,3-葡聚糖合成酶,对念珠菌具有杀真菌活性。但其稳定性差,需要静脉给药,限制了其临床应用。为了解决这些限制,新的配方如不饱和脂肪酸囊泡(不饱和脂肪酸囊泡)已经被开发出来,以提高caspofunins的稳定性和皮肤渗透性。本研究以油酸、亚油酸、棕榈油酸三种油类为原料,与caspofunins、胆固醇为原料,采用薄膜法制备ufasomes。其中,由500 mg棕榈油酸和10 mg胆固醇组成的F34具有良好的效果。其粒径(PS)为87.65±2.65 nm,多分散指数(PDI)为0.22±0.00,ζ电位(ZP)为-7.46±0.4 mV,药含量为97±1.34%,包封率(EE %)为92±0.82%。优化后的F34在600 min (10 h)内的缓释量为81.5±0.4,而卡泊芬素的缓释量为100%±0.01。F34在600 min (10 h)内的通透率为94%±0.81,而caspofungin为87.85%±0.85。抑菌活性表明,载caspofunins的抑菌带直径、MIC和MBC分别为29 mm±0.8、0.153 μg/mL±0.01、0.283 μg/mL±0.02,而纯caspofunins的抑菌带直径、MIC和MBC分别为25 mm±0.8、0.214 μg/mL±0.01、0.409±0.01。组织病理学研究显示了对优化配方的积极反应。总之,这个优化的配方具有潜力作为治疗局部真菌感染的一种新的治疗方法。
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引用次数: 0
Evaluation of Chitosan-Encapsulated Lemongrass (Cymbopogon citratus) Essential Oil Nanoemulsion for Fruit Edible Coating 壳聚糖包封柠檬草精油纳米乳用于水果食用包衣的研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-07-01 Epub Date: 2025-05-02 DOI: 10.1016/j.onano.2025.100246
Panji Setya Utama Putra , Damar Rastri Adhika , Gita Genecya , Muhammad Samman Al Madanie , Lia Amelia Tresna Wulan Asri
Agricultural and fishery products generally have a limited shelf life since these products are at high risk of experiencing changes in sensory properties in a fairly short time due to oxidation, enzymatic reactions, and microbial activity. Therefore, a food preservation system is needed to maintain its quality for longer. One preservation method for post-harvest products such as fruits and vegetables is edible coating. Edible coatings can be developed using biodegradable polymers derived from polysaccharides, proteins, fats, and their derivatives. Chitosan is a type of biopolymer that is commonly derived from the exoskeletons of marine animals such as shrimp and it possesses good antimicrobial properties. In addition, the development of food packaging technology. This study aims to develop and evaluate edible coatings that contain nano-chitosan and lemongrass essential oil nanoemulsions as antioxidant and antimicrobial agents for fruit packaging. The synthesized lemongrass essential oil nanoemulsion size was less than 100 nm and had good stability with a below 10% size change during 56 days of storage. Lemongrass essential oil nanoemulsion had a high antioxidant activity, as indicated by the low IC50 value in the DPPH reagent test. The combination of lemongrass essential oil nanoemulsion and chitosan as an edible coating had high antimicrobial activity, as indicated by the large inhibition zone in Bacillus cereus and Escherichia coli bacteria. Edible coating implementation on unpeeled banana fruit was evaluated through various tests such as pH, hardness, weight loss, and color changes. These tests showed some improvement in fruit preservation using nanoemulsion-based edible coatings treatment. The bananas were observed for 11 days and showed that the edible coating made from the combination of chitosan and lemongrass essential oil nanoemulsion can delay the ripening process of fruits, maintain firmness, and reduce weight loss. The best results for unpeeled banana preservation were obtained from edible coating with variations of lemongrass essential oil nanoemulsion and chitosan with a ratio of 2:1.
农业和渔业产品通常具有有限的保质期,因为这些产品在相当短的时间内由于氧化,酶反应和微生物活动而经历感官特性变化的风险很高。因此,需要一种食品保鲜系统来长期保持其品质。水果和蔬菜等收获后产品的一种保存方法是可食用涂层。可食用涂料可以使用从多糖、蛋白质、脂肪及其衍生物中提取的可生物降解聚合物来开发。壳聚糖是一种生物聚合物,通常从虾等海洋动物的外骨骼中提取,具有良好的抗菌性能。此外,食品包装技术的发展。本研究旨在开发和评价含有纳米壳聚糖和柠檬草精油纳米乳液作为水果包装抗氧化和抗菌剂的食用涂料。合成的香茅精油纳米乳粒径小于100 nm,稳定性好,在56 d的贮存时间内粒径变化小于10%。在DPPH试剂测试中,柠檬草精油纳米乳的IC50值较低,具有较高的抗氧化活性。香茅精油纳米乳液与壳聚糖复合作为可食用涂层,对蜡样芽孢杆菌和大肠杆菌具有较大的抑菌带,抗菌活性较高。通过pH值、硬度、失重和颜色变化等测试,对未剥皮香蕉果实的可食用涂层实施情况进行了评价。这些试验表明,纳米乳化剂可食用涂层处理对水果保鲜有一定的改善。对香蕉进行了11天的观察,结果表明,壳聚糖和柠檬草精油纳米乳复合制成的可食用包衣可以延缓香蕉的成熟过程,保持香蕉的紧致度,减少香蕉的体重。以香茅精油纳米乳液与壳聚糖的比例为2:1的可食用包衣法保存未去皮香蕉的效果最好。
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引用次数: 0
Entrapment efficiency methodology for lipid nanoparticles – a literature review 脂质纳米颗粒的捕集效率方法-文献综述
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-07-01 Epub Date: 2025-06-25 DOI: 10.1016/j.onano.2025.100251
Niklas Baltz , Regina Scherließ
Lipid nanoparticles have been used for decades to deliver lipophilic drugs. The success of particle formation and drug loading is determined by excipient selection and the production process. Entrapment efficiency (EE) as a measure for process effectiveness and drug load are critical quality attributes of lipid nanoparticles. To determine EE, the nanodispersion must be separated to determine the amount of drug inside the nanoparticles or to measure the amount of un-encapsulated drug in the medium. This review systematically analyses opportunities and challenges of different EE methods. 109 studies were included. The methodology used for EE appears to be chosen on a case-by-case basis and is often reported without a thorough method description. 78 studies (72 %) reported the EE method with enough detail to readily attempt experimental reproduction. This review underlines the need for thorough reporting of the principles and method used to determine entrapment efficiency to allow data interpretation.
几十年来,脂质纳米颗粒一直被用于输送亲脂性药物。颗粒形成和药物装载的成功与否取决于辅料的选择和生产工艺。包封效率(EE)作为衡量工艺有效性和药物负荷的指标是脂质纳米颗粒的关键质量属性。为了确定EE,必须分离纳米分散体以确定纳米颗粒内的药物量或测量介质中未封装药物的量。本文系统分析了不同的情感表达方法所面临的机遇和挑战。纳入109项研究。用于情感表达的方法似乎是根据具体情况选择的,并且经常在没有详细方法描述的情况下进行报道。78项研究(72%)报告了EE方法的足够细节,可以随时尝试实验复制。这项审查强调需要全面报告用于确定捕获效率的原则和方法,以便对数据进行解释。
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引用次数: 0
Sunlight-active Bi2O2(OH)(NO3)-AgBr photocatalyst for degradation of Rhodamine B (RhB) dye and disinfection of E. coli bacteria 光活性Bi2O2(OH)(NO3)-AgBr光催化剂对罗丹明B (RhB)染料的降解及对大肠杆菌的消毒
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-07-01 Epub Date: 2025-06-12 DOI: 10.1016/j.onano.2025.100249
Ruethaithip Dulyasucharit , Laksanawadee Saikhao , Sutthidech Preecharram , Nutthachai Prongmanee , Wipada Chaiyachet , Orapan Intharaksa , Suwat Nanan
A sunlight-driven Bi2O2(OH)(NO3)-AgBr heterostructure photocatalyst (denoted as BiON-AgBr) was synthesized by a two-step route combining hydrothermal and chemical precipitation methods. Firstly, the pristine BiON was prepared, via two types of solvent, by using a hydrothermal method. In the case that water was used as a solvent, the BiON.W photocatalyst with a pine-like structure was obtained. However, by using mixed solvent (comprising ethanol: water of 20:80), the BiON.M photocatalyst with a flower-like morphology was achieved. Secondly, the binary BiON-AgBr heterostructure was then constructed using a chemical precipitation technique. Accordingly, the photocatalytic performance of the prepared BiON-AgBr photocatalyst was evaluated through the photodegradation of Rhodamine B (RhB) dye under natural sunlight irradiation. The synthesized BiON-AgBr photocatalyst still exhibits high photocatalytic efficiency, even after three consecutive cycles of use. Trapping experiment revealed that the superoxide anion radicals (O₂⁻) play the most important role in RhB removal. The result suggested a Z-scheme mechanism based on AgBr/Ag/BiON. The formation of metallic silver (Ag0), upon sunlight illumination, was proved as the evidence shown in the XRD pattern of the used photocatalyst. The synergistic effect of the Z-scheme heterojunction and the surface plasmon resonance (SPR) of silver metal results in the considerable enhancement of the sunlight-driven photodegradation of RhB dye and the remarkable improvement of the disinfection of E. coli bacteria.
采用水热法和化学沉淀法相结合的两步法合成了一种光能驱动Bi2O2(OH)(NO3)-AgBr异质结构光催化剂(BiON-AgBr)。首先,采用水热法制备了两种溶剂的原始BiON。在水被用作溶剂的情况下,BiON。得到了具有松状结构的W光催化剂。然而,通过使用混合溶剂(包括乙醇:水20:80),BiON。获得了具有花状形貌的M型光催化剂。其次,利用化学沉淀法构建BiON-AgBr二元异质结构。因此,通过在自然日光照射下光降解罗丹明B (Rhodamine B, RhB)染料来评价所制备的BiON-AgBr光催化剂的光催化性能。合成的BiON-AgBr光催化剂在连续使用三次后仍具有较高的光催化效率。诱捕实验表明,超氧阴离子自由基(•O₂⁻)在RhB的清除中起着最重要的作用。结果提示了一种基于AgBr/Ag/BiON的Z-scheme机制。在阳光照射下,金属银(Ag0)的形成在所用光催化剂的XRD图中得到了证明。由于金属银的z型异质结与表面等离子体共振(SPR)的协同作用,使得RhB染料在日光下的光降解能力显著增强,对大肠杆菌的消毒效果显著提高。
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引用次数: 0
Green biogenic fabrication of AgNPs derived from Pulicaria jaubertii leaf extract: Investigation of antimicrobial and cytotoxic properties 黄芍叶提取物AgNPs的绿色生物制备:抗菌和细胞毒性研究
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-07-01 Epub Date: 2025-05-30 DOI: 10.1016/j.onano.2025.100248
Ansam Wadia Alshameri , Bilal Abdualgalil , Mahdi Mutahar
"Plant-mediated synthesis of nanomaterials offers an eco-friendly and cost-effective alternative for biomedical applications. In this study, silver nanoparticles (AgNPs) were green-synthesized using a leaf extract of Pulicaria jaubertii, which served as both a reducing and stabilizing agent. The biophysical characterization of synthesized AgNPs confirmed their successful fabrication through Ultraviolet-Visible spectroscopy, Dynamic Light Scattering, Fourier Transform Infrared spectroscopy, Transmission Electron Microscopy, and Scanning Electron Microscope- Energy Dispersive X-ray Analysis. The synthesized AgNPs demonstrated potent antibacterial activity against gram-negative (Escherichia coli) and gram-positive (Staphylococcus aureus) pathogens, as evidenced by agar well diffusion, time-kill, and antibiofilm assays. Notably, the nanoparticles exhibited minimal cytotoxicity toward Peripheral Blood Mononuclear Cells and Human Red Blood Cells, underscoring their biocompatibility. These findings highlight the potential of Pulicaria jaubertii-derived AgNPs as promising candidates for antimicrobial therapies and biomedical applications."
“植物介导的纳米材料合成为生物医学应用提供了一种环保且具有成本效益的替代方案。在这项研究中,银纳米粒子(AgNPs)是绿色合成的,使用白芍叶提取物,作为还原剂和稳定剂。通过紫外-可见光谱、动态光散射、傅里叶变换红外光谱、透射电子显微镜和扫描电子显微镜-能量色散x射线分析,证实了合成AgNPs的生物物理特性。合成的AgNPs对革兰氏阴性(大肠杆菌)和革兰氏阳性(金黄色葡萄球菌)病原体具有有效的抗菌活性,这一点通过琼脂孔扩散、时间杀伤和抗生素膜实验得到了证明。值得注意的是,纳米颗粒对外周血单核细胞和人红细胞表现出最小的细胞毒性,强调了它们的生物相容性。这些发现突出了黄檗衍生的AgNPs作为抗菌治疗和生物医学应用的有希望的候选者的潜力。”
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引用次数: 0
Enhanced immunomodulator activity of Carthamus tinctorius (L.) extracts, a traditional medicine using nanostructured lipid carrier approach 利用纳米结构脂质载体方法增强传统药物红花提取物的免疫调节活性
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-05-01 Epub Date: 2025-03-20 DOI: 10.1016/j.onano.2025.100244
Rachmat Mauludin , Insan Nurul Padjar , Neng Fisheri Kurniati , Ratna Annisa Utami
Considering the potential of Carthamus tinctorius (L.) (CT) for therapeutic purposes mainly as immunomodulator as well as the ability of nanostructured lipid carriers (NLC) to protect phytochemicals from degradation and improving their solubility, the objective of this study was design, optimization, and characterization CT-loaded NLC (CTNLC) system as an immunomodulator. The NLCs were prepared using hot homogenization techniques, which were later subjected to ultrasonication according to the Box Behnken design. The NLCs were characterized in terms of polydispersity index (PDI), particle size (PS), zeta potential (ZP), entrapment efficiency (%EE), and surface morphologies. The immunomodulatory activity was carried out by measuring phagocytic activity using carbon clearance method, organ index, antibody titres using indirect hemagglutination test and level of interferon-gamma (IFN-γ). The CT extracts (300 mg/kg), CT-NLC (100 mg/kg and 300 mg/kg) were administered orally. Levamisole (3 mg/kg) and Methylprednisolone (16 mg/kg) was used as standard drug. The selected CTNLC displayed a spherical particle with an average of ∼199.6 nm, polydispersity index of ∼0.305 and zeta potential of ∼-27.4 mV. %EE ∼74.04 % was attained. TEM images exhibited nanoparticles to be non-aggregated and in spherical shape. CTNLC treatment significantly increased the phagocytic index, antibody titres and level of IFN-γ but did not influence organ index compared to free CT. Carthamus tinctorius (L.) was successfully encapsulated into nanostructured lipid carriers. The developed NLC exhibited desirable parameters and was found to further improve immunomodulation efficacy. NLC has the potential to significantly enhance the efficacy of CT.
考虑到红花(Carthamus tinctorius, L.) (CT)主要作为免疫调节剂用于治疗目的的潜力,以及纳米结构脂质载体(NLC)保护植物化学物质免受降解和提高其溶解度的能力,本研究的目的是设计、优化和表征CT负载的NLC (CTNLC)作为免疫调节剂的系统。采用热均质技术制备NLCs,然后根据Box Behnken设计对其进行超声处理。用多分散性指数(PDI)、粒径(PS)、ζ电位(ZP)、捕获效率(%EE)和表面形貌对nlc进行了表征。通过碳清除法测定吞噬活性、器官指数、间接血凝试验测定抗体滴度和干扰素γ (IFN-γ)水平测定免疫调节活性。CT提取物(300 mg/kg)、CT- nlc (100 mg/kg、300 mg/kg)口服。左旋咪唑(3mg /kg)和甲基强的松龙(16mg /kg)作为标准药物。所选择的CTNLC显示出平均为~ 199.6 nm的球形颗粒,多分散性指数为~ 0.305,zeta电位为~ -27.4 mV。获得了%EE ~ 74.04%。TEM图像显示纳米颗粒呈非聚集球形。与游离CT相比,CTNLC治疗显著提高了吞噬指数、抗体滴度和IFN-γ水平,但对器官指数没有影响。红花(Carthamus tinctorius, L.)被成功包裹成纳米结构的脂质载体。开发的NLC具有理想的参数,并被发现进一步提高免疫调节功效。NLC具有显著提高CT疗效的潜力。
{"title":"Enhanced immunomodulator activity of Carthamus tinctorius (L.) extracts, a traditional medicine using nanostructured lipid carrier approach","authors":"Rachmat Mauludin ,&nbsp;Insan Nurul Padjar ,&nbsp;Neng Fisheri Kurniati ,&nbsp;Ratna Annisa Utami","doi":"10.1016/j.onano.2025.100244","DOIUrl":"10.1016/j.onano.2025.100244","url":null,"abstract":"<div><div>Considering the potential of <em>Carthamus tinctorius (</em>L.<em>)</em> (CT) for therapeutic purposes mainly as immunomodulator as well as the ability of nanostructured lipid carriers (NLC) to protect phytochemicals from degradation and improving their solubility, the objective of this study was design, optimization, and characterization CT-loaded NLC (CT<img>NLC) system as an immunomodulator. The NLCs were prepared using hot homogenization techniques, which were later subjected to ultrasonication according to the Box Behnken design. The NLCs were characterized in terms of polydispersity index (PDI), particle size (PS), zeta potential (ZP), entrapment efficiency (%EE), and surface morphologies. The immunomodulatory activity was carried out by measuring phagocytic activity using carbon clearance method, organ index, antibody titres using indirect hemagglutination test and level of interferon-gamma (IFN-γ). The CT extracts (300 mg/kg), CT-NLC (100 mg/kg and 300 mg/kg) were administered orally. Levamisole (3 mg/kg) and Methylprednisolone (16 mg/kg) was used as standard drug. The selected CT<img>NLC displayed a spherical particle with an average of ∼199.6 nm, polydispersity index of ∼0.305 and zeta potential of ∼-27.4 mV. %EE ∼74.04 % was attained. TEM images exhibited nanoparticles to be non-aggregated and in spherical shape. CTNLC treatment significantly increased the phagocytic index, antibody titres and level of IFN-γ but did not influence organ index compared to free CT. <em>Carthamus tinctorius (</em>L.<em>)</em> was successfully encapsulated into nanostructured lipid carriers. The developed NLC exhibited desirable parameters and was found to further improve immunomodulation efficacy. NLC has the potential to significantly enhance the efficacy of CT.</div></div>","PeriodicalId":37785,"journal":{"name":"OpenNano","volume":"23 ","pages":"Article 100244"},"PeriodicalIF":0.0,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143697055","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Microbicidal mechanisms for light-activated molecular nanomachines in Mycobacterium smegmatis: A model for pathogenic bacteria 耻垢分枝杆菌中光激活分子纳米机器的杀微生物机制:一种致病菌模型
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-05-01 Epub Date: 2025-02-25 DOI: 10.1016/j.onano.2025.100240
Thushara Galbadage , Dongdong Liu , James M. Tour , Jeffrey D. Cirillo , Richard S. Gunasekera
There is a global health crisis of antimicrobial resistance, responsible for over a million deaths annually. Mycobacterial infections are a major contributor to this crisis, causing more deaths than any other single infectious agent. Notably, the rise of multidrug-resistant (MDR), extensively drug-resistant (XDR), and totally drug-resistant (TDR) strains of Mycobacterium tuberculosis has led to higher mortality rates and challenge all existing antibiotic regimens. Light-activated molecular nanomachines (MNMs) represent a promising class of broad-spectrum antimicrobial agents that could help counter this rise in antimicrobial resistance. Addressing a key knowledge gap, this study explores the mechanisms of action for MNMs in Mycobacterium smegmatis, a surrogate model for pathogenic mycobacteria. We show that fast-rotor MNMs significantly reduce bacterial viability, achieving up to 97 % reduction in M. smegmatis with 30 minutes of light activation when compared to non-activated MNM 1 (p < 0.0001, t = 24.55), as determined by an unpaired t-test. Using fluorescence and confocal microscopy, we also show the colocalization of MNM 1 with M. smegmatis as part of their mechanism of action. The ability to translate these observations to pathogenic mycobacteria was demonstrated by the ability of MNM 1 to kill 93.5 % of M. tuberculosis with 5 minutes of light activation when compared to non-activated MNM 1 (p < 0.0001, t = 19.24). These findings suggest that MNMs have the potential to be innovative and sustainable antimicrobial agents for the treatment of pathogenic mycobacterial infections.
全球存在抗微生物药物耐药性的健康危机,每年造成100多万人死亡。分枝杆菌感染是造成这一危机的一个主要因素,它造成的死亡人数超过任何其他单一传染因子。值得注意的是,耐多药(MDR)、广泛耐药(XDR)和完全耐药(TDR)结核分枝杆菌菌株的增加导致了更高的死亡率,并对所有现有的抗生素治疗方案构成了挑战。光激活分子纳米机器(MNMs)代表了一类有前途的广谱抗菌剂,可以帮助对抗这种抗菌素耐药性的上升。为了解决一个关键的知识缺口,本研究探讨了MNMs在耻垢分枝杆菌(致病性分枝杆菌的替代模型)中的作用机制。我们发现,快速转子MNMs显著降低了细菌活力,与未激活的MNM 1相比,在30分钟的光激活下,耻垢分枝杆菌的活性降低了97% (p <;0.0001, t = 24.55),由非配对t检验确定。利用荧光和共聚焦显微镜,我们还发现MNM - 1与耻垢分枝杆菌的共定位是其作用机制的一部分。与未激活的MNM 1相比,MNM 1在5分钟的光激活下杀死93.5%的结核分枝杆菌,证明了将这些观察结果转化为致病性分枝杆菌的能力(p <;0.0001, t = 19.24)。这些发现表明,MNMs有潜力成为治疗致病性分枝杆菌感染的创新和可持续的抗菌药物。
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引用次数: 0
Development and evaluation of drug-loaded niosomes fabricated by flow chemistry: A novel vortex tube reactor approach 流动化学制备载药小体的研究与评价:一种新型涡流管反应器方法
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-05-01 Epub Date: 2025-03-19 DOI: 10.1016/j.onano.2025.100243
Kampanart Huanbutta , Kittipat Suwanpitak , Possawee Ponlakorn , Phatsawi Sonkongdang , Isariya Kongklai , Kunlathida Luangpraditkun , Tistaya Semangoen , Tanikan Sangnim
Continuous flow technology has been increasingly applied in the fabrication of nanoparticle drug delivery systems due to its ability to provide enhanced process control, scalability, and improved uniformity in particle size. Therefore, this study aims to utilize a newly designed flow chemistry vortex tube reactor for the preparation of ketoconazole-loaded niosomes, with the goal of enhancing mixing efficiency and increasing production rates. The experiment was designed using a central composite design to investigate the effects of key preparation parameters, including total flow rate, surfactant concentration, and cholesterol content, on particle size, size distribution, zeta potential, entrapment efficiency, and drug loading percentage. The optimized formulation (Span 80 = 25 mg, Cholesterol = 50 mg) was achieved using a total flow rate of 20 mL/min. The resulting niosomes exhibited a particle size of 212.3 nm, a zeta potential of 40.2 mV, a polydispersity index of 0.282, an entrapment efficiency of 50.84 %, a drug loading of 0.58 %, and a productivity of 70.67 mg/min. Moreover, ketoconazole-loaded niosomes prepared using the newly designed flow chemistry vortex tube reactor demonstrated prolonged inhibition of Candida albicans growth compared to ketoconazole solution. A comparison with batch synthesis revealed that flow chemistry produces smaller particles with a narrower size distribution and significantly improved productivity. These findings indicate the potential for further development of the vortex reactor for industrial-scale production of nanovesicular drug delivery systems.
由于连续流技术能够提供增强的过程控制、可扩展性和颗粒尺寸的均匀性,因此它在纳米颗粒药物输送系统的制造中得到了越来越多的应用。因此,本研究旨在利用新设计的流动化学涡流管反应器制备负载酮康唑的纳米体,以提高混合效率,提高产量。本实验采用中心复合设计,考察了总流速、表面活性剂浓度和胆固醇含量等关键制备参数对样品粒径、粒径分布、zeta电位、包封效率和载药率的影响。在总流速为20 mL/min的条件下,获得最佳配方(Span 80 = 25 mg,胆固醇= 50 mg)。所得纳米粒粒径为212.3 nm, zeta电位为40.2 mV,多分散性指数为0.282,包封效率为50.84%,载药量为0.58%,产率为70.67 mg/min。此外,使用新设计的流动化学涡旋管反应器制备的负载酮康唑的ni质体与酮康唑溶液相比,对白色念珠菌的生长具有较长的抑制作用。与间歇合成的比较表明,流动化学生产的颗粒更小,粒径分布更窄,生产效率显著提高。这些发现表明涡旋反应器在工业规模生产纳米囊泡给药系统方面有进一步发展的潜力。
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引用次数: 0
Anti-cancer activity of Kaempferia galanga L.–loaded polydopamine nanoparticles against colorectal cancer 山奈高良l -负载聚多巴胺纳米颗粒对结直肠癌的抗癌作用
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-05-01 Epub Date: 2025-03-21 DOI: 10.1016/j.onano.2025.100242
Paweena Dana , Anukul Taweechaipaisankul , Yodsathorn Wongngam , Suttipun Sungsuwan , Walailuk Chonniyom , Saksorn Klibaim , Prattana Tanyapanyachon , Monthira Rattanatayarom , Onuma Phoraksa , Udom Asawapirom , Primana Punnakitikashem , Duangporn Polpanich , Nattika Saengkrit
Kaempferia galanga L. (KGL) is an aromatic ginger that has been used as a medicinal plant. Specifically, KGL possesses anti-inflammatory, antioxidant, anti-bacterial, and anti-cancer effects. However, the key component of KGL, ethyl p‑methoxy cinnamate (EPMC), is insoluble in water, resulting in low bioavailability. Hence, a nano-drug delivery system is used to enhance KGL activities. This study aimed to employ polydopamine (PDA) nanoparticles as a carrier for KGL delivery to improve its anti-cancer activity against colorectal cancer cells. PDA- and PDA nanoparticle–loaded KGL (PDA-KGL) were synthesized using a spontaneous oxidation process. The physicochemical properties of the PDA-KGL were characterized by dynamic light scattering methods. The anti-cancer activity of PDA-KGL was evaluated in HT-29, a colorectal cancer (CRC) cell line. Average hydrodynamic sizes of PDA and PDA-KGL were 236.2 ± 1.2 and 316.6 ± 2.0 nm, respectively, and the zeta potential of PDA and PDA-KGL were -23.0 ± 0.4 and -39.5 ± 0.6 mV, respectively. The morphology of PDA-KGL observed under TEM was spherical in shape. Anti-proliferative activity was monitored in HT-29 cells using MTT and 3D tumor spheroid assays. PDA-KGL strongly inhibited cell viability of HT-29 cells compared to free KGL and PDA treatments. PDA-KGL induced apoptosis in HT-29 cells as shown by an Annexin V binding assay. In addition, PDA-KGL suppressed the invasive ability of HT-29 cells compared to free KGL or PDA, which was determined by a transwell invasion assay. Taken together, it implies that PDA-KGL might be used as a nano-drug delivery approach for colorectal cancer treatment.
山柰属高良姜(KGL)是一种芳香姜,已被用作药用植物。具体来说,KGL具有抗炎、抗氧化、抗菌和抗癌作用。然而,KGL的关键成分对甲氧基肉桂酸乙酯(EPMC)不溶于水,导致生物利用度低。因此,纳米给药系统被用来增强KGL的活性。本研究旨在利用聚多巴胺(PDA)纳米颗粒作为KGL的载体,提高其对结直肠癌细胞的抗癌活性。采用自然氧化法合成了PDA-和PDA纳米颗粒负载的KGL (PDA-KGL)。采用动态光散射方法对聚乳酸- kgl的物理化学性质进行了表征。在结直肠癌(CRC)细胞系HT-29中评价了PDA-KGL的抗癌活性。PDA和PDA- kgl的平均水动力尺寸分别为236.2±1.2和316.6±2.0 nm, zeta电位分别为-23.0±0.4和-39.5±0.6 mV。透射电镜观察到PDA-KGL的形貌为球形。使用MTT和3D肿瘤球体测定法监测HT-29细胞的抗增殖活性。与游离KGL和PDA处理相比,PDA-KGL对HT-29细胞活力有较强的抑制作用。Annexin V结合实验显示,PDA-KGL诱导HT-29细胞凋亡。此外,与游离KGL或PDA相比,PDA-KGL抑制了HT-29细胞的侵袭能力,这是通过transwell侵袭实验确定的。综上所述,这意味着PDA-KGL可能作为一种纳米药物递送方法用于结直肠癌的治疗。
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引用次数: 0
Nanotechnology for effective bovine mastitis treatment: Applications in biosensors and vaccines 有效治疗牛乳腺炎的纳米技术:在生物传感器和疫苗中的应用
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-03-01 Epub Date: 2025-02-19 DOI: 10.1016/j.onano.2025.100238
Soheil Sadr , Babak Khoramian , Zahra Yousefsani , Ahad Jafari Rahbar Alizadeh , Abbas Rahdar , Hassan Borji
A dairy farm's most significant economic loss is caused by mastitis, one of the most common diseases in dairy cows. Mastitis occurs due to many different pathogens, such as bacteria, fungi, and algae, and antibiotics are the first line of treatment and control. Alternative methods are therefore being investigated to eradicate pathogenic microorganisms that cause mastitis. Nanotechnology is a rapidly growing field that can manufacture new materials at the nanoscale level and has tremendous potential to revolutionize the agri-food industry by offering new treatments for bovine mastitis. Considering the increasing ineffectiveness of current therapies for resistant bacteria, developing innovative products that combine nanotechnology may provide a sustainable animal health solution that can support the production of safe and high-quality food products while directly addressing a critical global problem such as antimicrobial resistance. Additionally, nanotechnology offers promising advancements in bovine mastitis research, with nanovaccines providing targeted and efficient delivery of antigens to enhance the cow's immune response and prevent the disease. On the other hand, nanobiosensors play a crucial role in the early detection of bovine mastitis, allowing for real-time monitoring of biomarkers and enabling prompt intervention, thus reducing economic losses and promoting animal welfare. Although metalic nanoparticles have the potential to offer great benefits in terms of treating bovine mastitis, there are several challenges related to their toxicity, stability, environmental safety, and production costs that need to be carefully examined and addressed in order to facilitate their use. Considering the potential of nanoparticles, these challenges can be successfully managed if applied to the right areas, which will be a new and efficient therapeutic method for improving bovine mastitis and reducing drug resistance in livestock farms, given the potential of nanoparticles. In summary, nanovaccines, nanodrugs, and nanobiosensors have great potential in managing bovine mastitis, offering targeted prevention, effective treatment, and early detection capabilities, respectively.
奶牛场最重大的经济损失是由乳腺炎造成的,乳腺炎是奶牛最常见的疾病之一。乳腺炎是由许多不同的病原体引起的,如细菌、真菌和藻类,抗生素是治疗和控制的第一线。因此,正在研究其他方法来根除引起乳腺炎的病原微生物。纳米技术是一个快速发展的领域,它可以制造纳米级的新材料,并且通过提供牛乳腺炎的新治疗方法,具有巨大的潜力来彻底改变农业食品工业。考虑到目前治疗耐药细菌的方法越来越无效,开发结合纳米技术的创新产品可能提供一种可持续的动物健康解决方案,可以支持生产安全和高质量的食品,同时直接解决诸如抗菌素耐药性等关键的全球问题。此外,纳米技术为牛乳腺炎研究提供了有希望的进展,纳米疫苗提供了有针对性和有效的抗原递送,以增强奶牛的免疫反应并预防疾病。另一方面,纳米生物传感器在牛乳腺炎的早期检测中起着至关重要的作用,可以实时监测生物标志物并进行及时干预,从而减少经济损失并促进动物福利。尽管金属纳米颗粒在治疗牛乳腺炎方面具有巨大的潜力,但在其毒性、稳定性、环境安全性和生产成本方面存在一些挑战,需要仔细检查和解决,以促进其使用。考虑到纳米颗粒的潜力,如果应用到正确的领域,这些挑战可以成功地管理,考虑到纳米颗粒的潜力,这将是改善牛乳腺炎和减少牲畜农场耐药性的一种新的有效治疗方法。总之,纳米疫苗、纳米药物和纳米生物传感器在管理牛乳腺炎方面具有巨大潜力,分别提供有针对性的预防、有效的治疗和早期发现能力。
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