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Artemisinin emulgel ameliorates cartilage degradation in knee osteoarthritis: in vitro and in vivo studies. 青蒿素凝胶改善膝关节骨关节炎软骨退化:体外和体内研究
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-11-06 DOI: 10.1080/20415990.2024.2418281
Samiksha Thote, Atul Mourya, Shristi Arya, Hoshiyar Singh, Prashanth Kumar, Santosh Kumar Guru, Jitender Madan

Aim: Laboratory scale-up of artemisinin-loaded emulgel (ART-emulgel) was carried out and characterized for therapeutic performance in osteoarthritis (OA).Materials & methods: The solubility of ART in various oils, surfactants and co-surfactants were screened for construction of pseudo ternary phase diagram (TPD), followed by scale-up of artemisinin loaded nanoemulsion (ART-NE). ART-NE was amalgamated with Carbopol Ultrez 10-NF to prepare ART-emulgel that was later characterized in vitro and in vivo to analyze therapeutic efficacy in monosodium-iodoacetate (MIA) induced knee OA.Results: The droplet diameter of ART-NE was estimated to be 104.3 ± 2.593 nm with a polydispersity index of 0.245 ± 0.019 in addition to ζ-potential of 0.434 ± 0.028 mV. Steady-state flux and permeability coefficient for ART-emulgel were estimated to be 0.651 ± 0.031 µg.cm2/h and 0.245 ± 0.011 cm/h, respectively. ART-emulgel demonstrated 43.18% reduction in COX-2 level; 52.28% drop in IL-1β, and 88.78% alleviation of Tumor Necrosis Factor-α (TNF-α) level when compared with monosodium-iodoacetate induced OA rats. ART-emulgel and injectable ART (intra-articular; I.A) portrayed minor synovial erosion compared with blank and diclofenac emulgel. Histopathological evidences indicated restoration of cartilage integrity followed by reduction of OARSI scores in ART-emulgel when compared with disease control animals.Conclusion: ART-emulgel is a potential dosage form for translating into a clinically viable product for the management of OA.

目的:对青蒿素载体凝胶(ART-emulgel)进行实验室放大,并对其在骨关节炎(OA)中的治疗性能进行表征:筛选了青蒿素在各种油类、表面活性剂和辅助表面活性剂中的溶解度,构建了伪三元相图(TPD),随后对青蒿素负载纳米乳液(ART-NE)进行了放大。ART-NE与Carbopol Ultrez 10-NF混合制备成ART-emulgel,然后对其进行体外和体内表征,分析其对碘乙酸钠(MIA)诱导的膝关节OA的疗效:ART-NE 的液滴直径估计为 104.3 ± 2.593 nm,多分散指数为 0.245 ± 0.019,ζ电位为 0.434 ± 0.028 mV。估计 ART-emulgel 的稳态通量和渗透系数分别为 0.651 ± 0.031 µg.cm2/h 和 0.245 ± 0.011 cm/h。与碘乙酸钠诱导的 OA 大鼠相比,ART 胶体可降低 COX-2 水平 43.18%;IL-1β 降低 52.28%;肿瘤坏死因子-α(TNF-α)水平降低 88.78%。与空白和双氯芬酸凝胶相比,ART凝胶和注射用ART(关节内;I.A)的滑膜侵蚀程度较轻。组织病理学证据表明,与疾病对照组动物相比,ART-栓剂恢复了软骨的完整性,OARSI评分也随之降低:ART-emulgel 是一种潜在的剂型,可转化为临床上可行的产品用于治疗 OA。
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引用次数: 0
Sodium alginate/carboxymethylcellulose gel formulations containing Capparis sepieria plant extract for wound healing. 海藻酸钠/羧甲基纤维素凝胶配方,含用于伤口愈合的蓝花楹植物提取物。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-11-12 DOI: 10.1080/20415990.2024.2418800
Sindi P Ndlovu, Shirley C M Motaung, Samson A Adeyemi, Philemon Ubanako, Lindokuhle M Ngema, Thierry Youmbi Fonkui, Derek Tantoh Ndinteh, Pradeep Kumar, Yahya E Choonara, Blessing A Aderibigbe

Aim: Using appropriate wound dressings is crucial when treating burn wounds to promote accelerated healing.Materials & methods: Sodium alginate (SA)-based gels containing Carboxymethyl cellulose (CMC) and Pluronic F127 were prepared. The formulations. SA/CMC/Carbopol and SA/CMC/PluronicF127 were loaded with aqueous root extract of Capparis sepiaria. The formulations were characterized using appropriate techniques.Results: The gels' viscosity was in the range of 676.33 ± 121.76 to 20.00 ± 9.78 cP and in vitro whole blood kinetics showed their capability to induce a faster clotting rate. They also supported high cell viability of 80% with cellular migration and proliferation. Their antibacterial activity was significant against most bacteria strains used in the study.Conclusion: The gels' distinct features reveal their potential application as wound dressings for burn wounds.

目的:在治疗烧伤伤口时,使用适当的伤口敷料对促进伤口加速愈合至关重要:制备了含有羧甲基纤维素(CMC)和Pluronic F127的海藻酸钠(SA)凝胶。配方。在 SA/CMC/Carbopol 和 SA/CMC/PluronicF127 中添加了蓝花楹(Capparis sepiaria)的水性根提取物。采用适当的技术对配方进行了表征:凝胶的粘度在 676.33 ± 121.76 到 20.00 ± 9.78 cP 之间,体外全血动力学显示它们能够加快凝血速度。它们还支持高达 80% 的细胞存活率以及细胞迁移和增殖。它们对研究中使用的大多数细菌菌株都有显著的抗菌活性:凝胶的独特特性揭示了其作为烧伤伤口敷料的潜在应用。
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引用次数: 0
Exploring delivery systems for targeted nanotechnology-based gene therapy in the inner ear. 探索基于纳米技术的内耳靶向基因治疗输送系统。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-26 DOI: 10.1080/20415990.2024.2389032
Thomas Foster, Patrick Lim, Corina Mihaela Ionescu, Susbin Raj Wagle, Bozica Kovacevic, Armin Mooranian, Hani Al-Salami

Hearing loss places a significant burden on our aging population. However, there has only been limited progress in developing therapeutic techniques to effectively mediate this condition. This review will outline several of the most commonly utilized practices for the treatment of sensorineural hearing loss before exploring more novel techniques currently being investigated via both in vitro and in vivo research. This review will place particular emphasis on novel gene-delivery technologies. Primarily, it will focus on techniques used to deliver genes that have been shown to encourage the proliferation and differentiation of sensory cells within the inner ear and how these technologies may be translated into providing clinically useful results for patients.

听力损失给我们的老龄人口带来了沉重的负担。然而,在开发有效调解这种情况的治疗技术方面进展有限。本综述将概述治疗感音神经性听力损失最常用的几种方法,然后探讨目前通过体外和体内研究正在研究的更多新技术。本综述将特别强调新型基因递送技术。它将主要关注用于传递基因的技术,这些基因已被证明能促进内耳感觉细胞的增殖和分化,以及如何将这些技术转化为对患者临床有用的结果。
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引用次数: 0
Enhancing Rose Bengal penetration in ex vivo human corneas using iontophoresis. 利用离子透入技术提高罗斯孟加拉红在体外人类角膜中的渗透率。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-07-18 DOI: 10.1080/20415990.2024.2371778
James M Lai, Justin Chen, Juan Carlos Navia, Heather Durkee, Alex Gonzalez, Cornelis Rowaan, Timothy Arcari, Mariela C Aguilar, Katrina Llanes, Noel Ziebarth, Jaime D Martinez, Darlene Miller, Harry W Flynn, Guillermo Amescua, Jean-Marie Parel

Aim: Rose Bengal photodynamic antimicrobial therapy (RB-PDAT) has poor corneal penetration, limiting its efficacy against acanthamoeba keratitis (AK). Iontophoresis enhances corneal permeation of charged molecules, piquing interest in its effects on RB in ex vivo human corneas.Methods: Five donor whole globes each underwent iontophoresis with RB, soaking in RB, or were soaked in normal saline (controls). RB penetration and corneal thickness was assessed using confocal microscopy.Results: Iontophoresis increased RB penetration compared with soaking (177 ± 9.5 μm vs. 100 ± 5.7 μm, p < 0.001), with no significant differences in corneal thickness between groups (460 ± 87 μm vs. 407 ± 69 μm, p = 0.432).Conclusion: Iontophoresis significantly improves RB penetration and its use in PDAT could offer a novel therapy for acanthamoeba keratitis. Further studies are needed to validate clinical efficacy.

目的:玫瑰红光动力抗菌疗法(RB-PDAT)的角膜渗透性较差,限制了其对阿卡巴氏角膜炎(AK)的疗效。电离子透入疗法可增强带电分子在角膜上的渗透性,这引起了人们对电离子透入疗法在体外人类角膜上对 RB 的影响的兴趣。方法:五个供体全球分别接受 RB 离子透入、RB 浸泡或正常生理盐水浸泡(对照组)。使用共聚焦显微镜评估 RB 的渗透性和角膜厚度。结果与浸泡相比,离子透入法增加了 RB 穿透力(177 ± 9.5 μm vs. 100 ± 5.7 μm,P = 0.432)。结论离子透入疗法能明显提高 RB 的穿透力,在 PDAT 中使用这种疗法可为棘阿米巴角膜炎提供一种新的疗法。临床疗效还需进一步研究验证。
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引用次数: 0
Localized tacrolimus therapy: innovations in peripheral nerve regeneration through advanced drug delivery systems. 局部他克莫司疗法:通过先进的给药系统实现周围神经再生的创新。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-04 DOI: 10.1080/20415990.2024.2392481
Elena Millesi, Flavia Millesi, Julian S Rechberger, David J Daniels, Christine Radtke, Samir Mardini
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引用次数: 0
Synthesis and characterization of fullerene-based nanocarrier for targeted delivery of quercetin to the brain. 用于向大脑定向输送槲皮素的富勒烯基纳米载体的合成与表征。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-05 DOI: 10.1080/20415990.2024.2365620
Amit Kumar Palai, Amit Kumar, Farhan Mazahir, Ankita Sharma, Awesh K Yadav

Aim: Preparation of quercetin fullerene conjugate (QFC) for nose-to-brain delivery and their in vitro and ex vivo characterizations.Methods: Carboxylated fullerene was converted into acetylated fullerene and quercetin was conjugated and physically adsorbed on acetylated fullerene.Results: The particle size and zeta potential of QFC and chitosan-coated QFC (CC-QFC) were found to be 179.2 ± 1.10, 293.4 ± 2.757, -5.28 ± 1.43 and 11.6 ± 0.4 respectively. The entrapment efficiency, loading efficiency of QFC were found to be 85.55% and 42.77%. The MTT assay revealed 80.69% SH-SY5Y cell viability at a concentration of 50 μg/ml. CC-QFC showed remarkable (89.20%) ex vivo mucoadhesive properties compared with QFC (66.67%). Further study showed no significant ciliotoxicity by CC-QFC.Conclusion: The obtained results suggested the potential of CC-QFC for treatment in Alzheimer's disease.

目的:制备用于鼻脑给药的槲皮素富勒烯共轭物(QFC)及其体内外表征:方法:将羧化富勒烯转化为乙酰化富勒烯,将槲皮素共轭并物理吸附在乙酰化富勒烯上:QFC和壳聚糖包覆QFC(CC-QFC)的粒度和ZETA电位分别为179.2 ± 1.10、293.4 ± 2.757、-5.28 ± 1.43和11.6 ± 0.4。QFC 的夹带效率和负载效率分别为 85.55% 和 42.77%。MTT 检测显示,浓度为 50 μg/ml 的 SH-SY5Y 细胞存活率为 80.69%。与 QFC(66.67%)相比,CC-QFC 的体外粘附性更强(89.20%)。进一步研究表明,CC-QFC 没有明显的纤毛毒性:结论:研究结果表明,CC-QFC 具有治疗阿尔茨海默病的潜力。
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引用次数: 0
Targeting superficial cancers with gold nanoparticles: a review of current research. 用金纳米粒子靶向浅表癌症:当前研究综述。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-24 DOI: 10.1080/20415990.2024.2395249
Susana M Gomes, Maria Manuela Gaspar, João Mp Coelho, Catarina Pinto Reis

Superficial cancers typically refer to cancers confined to the surface layers of tissue. Low-targeting therapies or side effects prompt exploration of novel therapeutic approaches. Gold nanoparticles (AuNPs), due to their unique optical properties, serve as effective photosensitizers, enabling tumor ablation through photothermal therapy (PTT). PTT induced by AuNPs can be achieved through light sources externally applied to the skin. Near-infrared radiation is the main light candidate due to its deep tissue penetration capability. This review explores recent advancements in AuNP-based PTT for superficial cancers, specifically breast, head and neck, thyroid, bladder and prostate cancers. Additionally, challenges and future directions in utilizing AuNPs for cancer treatment are discussed, emphasizing the importance of balancing efficacy with safety in clinical applications.

表层癌症通常指局限于组织表层的癌症。低靶向性疗法或副作用促使人们探索新的治疗方法。金纳米粒子(AuNPs)具有独特的光学特性,可作为有效的光敏剂,通过光热疗法(PTT)消融肿瘤。AuNPs诱导的PTT可通过外部照射皮肤的光源来实现。近红外辐射具有深层组织穿透能力,是主要的候选光源。本综述探讨了基于 AuNP 的浅表癌症 PTT 的最新进展,特别是乳腺癌、头颈癌、甲状腺癌、膀胱癌和前列腺癌。此外,还讨论了利用 AuNPs 治疗癌症的挑战和未来方向,强调了在临床应用中平衡疗效和安全性的重要性。
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引用次数: 0
Nanotechnology-driven therapies for neurodegenerative diseases: a comprehensive review. 神经退行性疾病的纳米技术驱动疗法:综述。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-19 DOI: 10.1080/20415990.2024.2401307
Jessica López-Espinosa, Peter Park, Morgan Holcomb, Biana Godin, Sonia Villapol

Neurological diseases, characterized by neuroinflammation and neurodegeneration, impose a significant global burden, contributing to substantial morbidity, disability and mortality. A common feature of these disorders, including stroke, traumatic brain injury and Alzheimer's disease, is the impairment of the blood-brain barrier (BBB), a critical structure for maintaining brain homeostasis. The compromised BBB in neurodegenerative conditions poses a significant challenge for effective treatment, as it allows harmful substances to accumulate in the brain. Nanomedicine offers a promising approach to overcoming this barrier, with nanoparticles (NPs) engineered to deliver therapeutic agents directly to affected brain regions. This review explores the classification and design of NPs, divided into organic and inorganic categories and further categorized based on their chemical and physical properties. These characteristics influence the ability of NPs to carry and release therapeutic agents, target specific tissues and ensure appropriate clearance from the body. The review emphasizes the potential of NPs to enhance the diagnosis and treatment of neurodegenerative diseases through targeted delivery, improved drug bioavailability and real-time therapeutic efficacy monitoring. By addressing the challenges of the compromised BBB and targeting inflammatory biomarkers, NPs represent a cutting-edge strategy in managing neurological disorders, promising better patient outcomes.

以神经炎症和神经变性为特征的神经系统疾病给全球造成了沉重负担,导致大量患者发病、残疾和死亡。这些疾病(包括中风、脑外伤和阿尔茨海默病)的一个共同特征是血脑屏障(BBB)受损,而血脑屏障是维持大脑平衡的关键结构。神经退行性疾病中受损的血脑屏障会使有害物质在大脑中积聚,从而对有效治疗构成重大挑战。纳米医学为克服这一障碍提供了一种前景广阔的方法,通过对纳米粒子(NPs)进行设计,可将治疗药物直接输送到受影响的脑区。本综述探讨了 NPs 的分类和设计,分为有机和无机两类,并根据其化学和物理特性作了进一步分类。这些特性影响着 NPs 携带和释放治疗剂、靶向特定组织以及确保适当清除体外的能力。综述强调了 NPs 通过靶向递送、改善药物生物利用度和实时疗效监测来提高神经退行性疾病诊断和治疗水平的潜力。通过应对BBB受损和靶向炎症生物标志物的挑战,NPs代表了一种治疗神经系统疾病的前沿策略,有望为患者带来更好的治疗效果。
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引用次数: 0
Enhancing therapy with nano-based delivery systems: exploring the bioactive properties and effects of apigenin. 利用纳米给药系统增强治疗效果:探索芹菜素的生物活性特性和作用。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-11 DOI: 10.1080/20415990.2024.2386928
Girish Kumar, Pushpika Jain, Tarun Virmani, Ashwani Sharma, Md Sayeed Akhtar, Saad A Aldosari, Mohd Faiyaz Khan, Sofia O D Duarte, Pedro Fonte

Apigenin, a potent natural flavonoid, has emerged as a key therapeutic agent due to its multifaceted medicinal properties in combating various diseases. However, apigenin's clinical utility is greatly limited by its poor water solubility, low bioavailability and stability issues. To address these challenges, this review paper explores the innovative field of nanotechnology-based delivery systems, which have shown significant promise in improving the delivery and effectiveness of apigenin. This paper also explores the synergistic potential of co-delivering apigenin with conventional therapeutic agents. Despite the advantageous properties of these nanoformulations, critical challenges such as scalable production, regulatory approvals and comprehensive long-term safety assessments remain key hurdles in their clinical adoption which must be addressed for commercialization of apigenin-based formulations.

芹菜素是一种有效的天然类黄酮,因其在防治各种疾病方面的多重药用特性,已成为一种重要的治疗药物。然而,芹菜素的水溶性差、生物利用率低和稳定性问题极大地限制了它的临床应用。为了应对这些挑战,本综述论文探讨了基于纳米技术的给药系统这一创新领域。本文还探讨了芹菜素与传统治疗药物联合给药的协同潜力。尽管这些纳米制剂具有优势特性,但可规模化生产、监管审批和全面的长期安全性评估等关键挑战仍然是临床应用的主要障碍,必须加以解决,才能实现芹菜素制剂的商业化。
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引用次数: 0
Enhanced bioavailability and efficacy in antimalarial treatment through QbD approach enteric encased inclusion delivery. 通过 QbD 方法肠溶包合物给药提高抗疟治疗的生物利用度和疗效。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-03 DOI: 10.1080/20415990.2024.2377948
Neha Bajwa, Preet Amol Singh, Sumant Kumar, Girish Chandra Arya, Ashish Baldi

Aim: In this study, we aimed to prepare enteric encapsulated spheroids containing inclusion complex using quality by design approach.Methods: A Box-Behnken design was employed to determine effects of variables on selected responses. Risk assessment was conducted using Ishikawa fishbone diagram. A model with a p-value was less than 0.5 for being a significant error of model was determined based on significance 'lack of fit' value. Spheroids were formulated using the extrusion spheronization technique and were characterized using analytical techniques.Results: In vitro release was performed in both acidic (pH 1.2) and simulated intestinal (pH 6.8) conditions. Permeability studies demonstrated tenfold enhancement compared with arteether. In vivo studies further validated increase of 51.8% oral bioavailability. Ex vivo studies revealed 3.4-fold enhancement in antimalarial activity compared with arteether.Conclusion: These findings highlight effectiveness of inclusion complexation technique as a viable approach to enhance solubility and bioavailability for drugs with low aqueous solubility.

目的:在本研究中,我们旨在采用质量设计法制备含有包涵复合物的肠道包裹球。方法采用方框-贝肯设计来确定变量对选定反应的影响。使用石川鱼骨图进行风险评估。根据显著性 "不拟合 "值,确定 p 值小于 0.5 的模型为显著误差模型。使用挤压球化技术配制球体,并使用分析技术对其进行表征。结果:在酸性(pH 值为 1.2)和模拟肠道(pH 值为 6.8)条件下进行了体外释放。渗透性研究表明,与蒿甲醚相比,蒿甲醚的渗透性提高了十倍。体内研究进一步验证了口服生物利用率提高了 51.8%。体内外研究表明,与蒿甲醚相比,其抗疟活性提高了 3.4 倍。结论:这些研究结果凸显了包合复合物技术的有效性,它是提高低水溶性药物的溶解度和生物利用度的一种可行方法。
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引用次数: 0
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