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Exploring contemporary breakthroughs in utilizing vesicular nanocarriers for breast cancer therapy. 探索利用囊泡纳米载体治疗乳腺癌的当代突破。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-04-01 Epub Date: 2024-02-20 DOI: 10.4155/tde-2023-0092
Nalla Usha Kumari, Ekta Pardhi, Padakanti Sandeep Chary, Neelesh Kumar Mehra

Breast cancer (BC) is a heterogeneous disease with various morphological features, clinicopathological conditions and responses to different therapeutic options, which is responsible for high mortality and morbidity in women. The heterogeneity of BC necessitates new strategies for diagnosis and treatment, which is possible only by cautious harmonization of the advanced nanomaterials. Recent developments in vesicular nanocarrier therapy indicate a paradigm shift in breast cancer treatment by providing an integrated approach to address current issues. This review provides a detailed classification of various nanovesicles in the treatment of BC with a special emphasis on recent advances, challenges in translating nanomaterials and future potentials.

乳腺癌(BC)是一种异质性疾病,具有不同的形态特征、临床病理条件和对不同治疗方案的反应,是造成妇女高死亡率和发病率的罪魁祸首。由于乳腺癌的异质性,有必要采用新的诊断和治疗策略,而这只有通过谨慎协调先进的纳米材料才能实现。囊泡纳米载体疗法的最新发展表明,乳腺癌治疗的模式正在发生转变,它提供了一种综合方法来解决当前的问题。本综述对治疗乳腺癌的各种纳米微粒进行了详细分类,并特别强调了最新进展、纳米材料转化方面的挑战和未来潜力。
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引用次数: 0
Exploring magnesium myristate for its dual functionality as a binder and lubricant in the formulation of tablet. 探索肉豆蔻酸镁在片剂配方中作为粘合剂和润滑剂的双重功能。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-04-01 Epub Date: 2024-02-29 DOI: 10.4155/tde-2023-0101
Rachana Pockle, Rajashree Masareddy, Vijay Bambulkar, Rishabh Desai, Sai Kiran

Purpose: To explore 'magnesium myristate' for its dual functionality as a lubricant and binder in the formulation of tablets. Methods: Using (DoE), tablet formulations using magnesium myristate and conventional excipients (magnesium stearate and PVP K30) were developed by wet granulation technique. The prepared granules and formulated tablets were evaluated for pre- and post-compression parameters, respectively. Results: Magnesium myristate exhibited excellent flow properties. The optimized formulations containing magnesium myristate exhibited increased hardness and in vitro drug release in comparison to conventional excipients. f2 similarity index for in vitro drug release showed no significant variations with optimized formulations and with the marketed formulations. Conclusion: Magnesium myristate shows a promising replacement for conventional excipients as both a lubricant and binder in tablet formulation.

目的:探索 "肉豆蔻酸镁 "在片剂配方中作为润滑剂和粘合剂的双重功能。方法利用湿法制粒技术,使用肉豆蔻酸镁和传统辅料(硬脂酸镁和 PVP K30)开发了片剂配方。分别对制备的颗粒和配制的片剂进行了压缩前和压缩后参数评估。结果显示肉豆蔻酸镁具有优异的流动性。与传统辅料相比,含有肉豆蔻酸镁的优化制剂的硬度和体外药物释放量都有所提高。体外药物释放量的 f2 相似度指数显示,优化制剂与市场上的制剂没有明显差异。结论肉豆蔻酸镁作为片剂配方中的润滑剂和粘合剂,有望替代传统辅料。
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引用次数: 0
Investigating anti-cancer activity of dual-loaded liposomes with thymoquinone and vitamin C. 研究胸腺醌和维生素 C 双载脂质体的抗癌活性
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-04-01 Epub Date: 2024-03-07 DOI: 10.4155/tde-2023-0140
Ahmed Munef, Zainab Lafi, Naeem Shalan

Background: Thymoquinone (TQ) and vitamin C (Vit C) have demonstrated individual anticancer effects in various studies. TQ exhibits inhibitory properties against tumor growth, induces apoptosis, while Vit C protects against DNA damage and oxidative stress. Aim: Formulation of TQ and Vit C combination into liposomes using two methods and investigate the synergistic anticancer. Method: Liposomal preparations were characterized, and the purity of drug components was confirmed using encapsulation efficiency (EE %). Results: In vitro cell viability studies demonstrated the inhibitory effect of TQ and Vit C against colorectal (HT29, 5.5 ± 0.9 μM) and lung cancer (A549, 6.25 ± 0.9 μM) cell lines with combination index <1. Conclusion: The formulation of TQ and Vit C displayed synergistic anticancer activity.

背景:在多项研究中,胸腺醌(TQ)和维生素 C(Vit C)都显示出各自的抗癌作用。胸腺醌具有抑制肿瘤生长、诱导细胞凋亡的作用,而维生素 C 则能防止 DNA 损伤和氧化应激。目的:用两种方法将 TQ 和维生素 C 组合配制成脂质体,并研究其协同抗癌作用。方法:对脂质体制剂进行表征:对脂质体制剂进行表征,并用包封效率(EE %)确认药物成分的纯度。结果体外细胞活力研究表明,TQ 和维生素 C 对结直肠癌细胞株(HT29,5.5 ± 0.9 μM)和肺癌细胞株(A549,6.25 ± 0.9 μM)具有抑制作用,且具有联合指数:TQ和维生素C制剂具有协同抗癌活性。
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引用次数: 0
Are mathematical equations important for improving drug-delivery devices performances? 数学公式对提高给药装置的性能重要吗?
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-04-01 Epub Date: 2024-02-15 DOI: 10.4155/tde-2023-0125
Fabio Pizzetti, Giuseppe Perale, Maurizio Masi, Filippo Rossi
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引用次数: 0
Probucol-bile acid based nanoparticles protect auditory cells from oxidative stress: an in vitro study. 基于丙三醇胆酸的纳米颗粒保护听觉细胞免受氧化应激:一项体外研究。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-04-01 Epub Date: 2024-03-12 DOI: 10.4155/tde-2023-0099
Susbin Raj Wagle, Bozica Kovacevic, Corina Mihaela Ionescu, Thomas Foster, Melissa Jones, Momir Mikov, Andrew Wise, Armin Mooranian, Hani Al-Salami

Aim: Excessive free radicals contribute to oxidative stress and mitochondrial dysfunction in sensorineural hearing loss (SNHL). The antioxidant probucol holds promise, but its limited bioavailability and inner ear barriers hinder effective SNHL treatment. Methodology: We addressed this by developing probucol-loaded nanoparticles with polymers and lithocholic acid and tested them on House Ear Institute-Organ of Corti cells. Results: Probucol-based nanoparticles effectively reduced oxidative stress-induced apoptosis, enhanced cellular viability, improved probucol uptake and promoted mitochondrial function. Additionally, they demonstrated the capacity to reduce reactive oxygen species through the nuclear factor erythroid 2-related factor 2/heme oxygenase-1 pathway. Conclusion: This innovative nanoparticle system holds the potential to prevent oxidative stress-related hearing impairment, providing an effective solution for SNHL.

目的:过多的自由基会导致感音神经性听力损失(SNHL)的氧化应激和线粒体功能障碍。抗氧化剂普布洛尔具有良好的前景,但其有限的生物利用度和内耳屏障阻碍了对感音神经性听力损失的有效治疗。方法:为了解决这一问题,我们开发了含有聚合物和石胆酸的普布酚载纳米颗粒,并在豪斯耳研究所-科蒂细胞器官上进行了测试。结果基于普罗布考的纳米颗粒有效减少了氧化应激诱导的细胞凋亡,提高了细胞活力,改善了普罗布考的吸收并促进了线粒体功能。此外,它们还能通过红细胞核因子 2 相关因子 2/血红素加氧酶 1 途径减少活性氧。结论这种创新的纳米粒子系统具有预防氧化应激相关听力损伤的潜力,为治疗急性咽喉炎提供了有效的解决方案。
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引用次数: 0
Synthesis and evaluation of amylose-mefenamic acid conjugates as colon-targeting prodrugs. 作为结肠靶向原药的直链淀粉-甲灭酸共轭物的合成与评估。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-03-18 DOI: 10.4155/tde-2023-0106
Shraddha Chugh, Mousmee Sharma, Harish Mudila, Parteek Prasher

Aim: Amide-linked amylose-based prodrugs were developed for colon-targeted release of mefenamic acid. Materials & methods: Activation of prodrug was studied spectrophotometrically, enzyme-linked immunosorbent assay appraised cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibition at different concentrations of the prodrug, the behavior of prodrug under physiological conditions was monitored by scanning electron microscopy. Results: Prodrug was poorly activated in the enzyme-free simulated gastric media and simulated intestinal media (SIM) but preincubation in pancreatin followed by treatment in aminopeptidase containing SIM led to a significant activation of prodrug. Conclusion: Amide-linked amylose-mefenamic acid conjugates showed a slow release in simulated gastric media and a controlled release in SIM with pancreatin playing an important role in drug release.

目的:开发酰胺连接的淀粉基原药,用于结肠靶向释放甲灭酸。材料与方法:用分光光度法研究原药的活化,用酶联免疫吸附试验评估不同浓度原药对环氧化酶-1(COX-1)和环氧化酶-2(COX-2)的抑制作用,用扫描电子显微镜监测原药在生理条件下的行为。结果显示原药在无酶模拟胃培养基和模拟肠培养基(SIM)中的活化程度较低,但在胰蛋白酶中预培养后在含有氨基肽酶的 SIM 中处理会显著活化原药。结论酰胺连接的淀粉-甲灭酸共轭物在模拟胃介质中显示出缓慢释放,而在模拟肠介质中显示出控制释放,其中胰蛋白酶在药物释放中发挥了重要作用。
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引用次数: 0
Preparation, characterization and in vitro evaluation of 5-fluorouracil loaded into chitosan-acacia gum nanoparticles. 壳聚糖-金合欢胶纳米颗粒负载的 5-氟尿嘧啶的制备、表征和体外评价。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-03-12 DOI: 10.4155/tde-2023-0136
Hasan Al-Nasrawi, Naeem Shalan, Bassam M Abualsoud, Hamdi Nsairat

Aim: In this study, we prepared, characterized and in vitro evaluated a 5-fluorouracil (5-FU)-loaded chitosan-acacia gum nanoparticles. Methods: Nanoparticles were characterized for their size, charge, morphology and encapsulation efficiency (EE%) followed by cellular investigations against HT-29 colon cancer cell line. Results: The nanoparticles exhibited a spherical morphological size with 94.42% EE%. Free 5-FU showed a fast and fully cumulative release after 6 h while 5-FU loaded into CS-AG NPs showed good entrapment and slow, prolonged 5-FU release even after 24 h. Enhanced IC50 for the 5-FU loaded NPs compared with free 5-FU against HT-29 colon cancer cell line was reported with high selectivity compared with normal fibroblast cells. Conclusion: 5-FU loaded NPs is promising nano-therapy against colon cancer.

目的:本研究制备了一种载5-氟尿嘧啶(5-FU)的壳聚糖-阿拉伯胶纳米颗粒,并对其进行了表征和体外评估。制备方法对纳米颗粒的尺寸、电荷、形态和包封效率(EE%)进行表征,然后对 HT-29 结肠癌细胞系进行细胞研究。结果:纳米颗粒呈球形,EE% 为 94.42%。与游离的 5-FU 相比,负载 5-FU 的 NPs 对 HT-29 结肠癌细胞株的 IC50 值更高,与正常成纤维细胞相比具有更高的选择性。结论:负载 5-FU 的 NPs 是一种很有前景的结肠癌纳米疗法。
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引用次数: 0
Chia nanoemulsion: anti-inflammatory mechanism, biological behavior and cellular interactions. 奇异果纳米乳液:抗炎机制、生物行为和细胞相互作用。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-03-12 DOI: 10.4155/tde-2023-0088
Luana Barbosa Correa, Natália Cristina Gomes-da-Silva, Clenilton Costa Dos Santos, Luciana Magalhães Rebelo Alencar, Maria das Graças Muller de Oliveira Henriques, Prapanna Bhattarai, Lin Zhu, Pedro Filho Noronha Souza, Elaine Cruz Rosas, Ralph Santos-Oliveira

Aim: This study explores chia oil, rich in ω-3 fatty acids and nutraceutical components, as a potential remedy for diseases, especially those linked to inflammation and cancer. Methods/materials: A chia oil-based nanoemulsion, developed through single emulsification, underwent comprehensive analysis using various techniques. In vitro and in vivo assays, including macrophage polarization, nitrite and cytokine production, cellular uptake and biodistribution, were conducted to assess the anti-inflammatory efficacy. Results & conclusion: Results reveal that the chia nanoemulsion significantly inhibits inflammation, outperforming pure oil with twice the efficacy. Enhanced uptake by macrophage-like cells and substantial accumulation in key organs indicate its potential as an economical and effective anti-inflammatory nanodrug, addressing global economic and health impacts of inflammation-related diseases.

目的:本研究探讨了奇异果油,它富含ω-3 脂肪酸和营养保健成分,是治疗疾病,尤其是与炎症和癌症有关的疾病的一种潜在疗法。方法/材料:利用各种技术对通过单一乳化技术开发的基于奇异果油的纳米乳液进行了综合分析。进行了体外和体内试验,包括巨噬细胞极化、亚硝酸盐和细胞因子的产生、细胞吸收和生物分布,以评估其抗炎功效。结果与结论结果显示,奇异果纳米乳液能显著抑制炎症,其功效是纯油的两倍。巨噬细胞的吸收能力增强以及在关键器官中的大量积累表明,它有潜力成为一种经济、有效的抗炎纳米药物,从而解决炎症相关疾病对全球经济和健康的影响。
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引用次数: 0
Delivery of nano-emulgel carrier: optimization, evaluation and in vivo anti-inflammation estimations for osteoarthritis. 纳米软凝胶载体的输送:骨关节炎的优化、评估和体内抗炎估计。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-03-01 Epub Date: 2024-02-15 DOI: 10.4155/tde-2023-0109
Rajni, Kamal Shah, Hitesh Kumar Dewangan

Aim: Optimization and evaluation of Aceclofenac nanoemulgel for treatment for rheumatoid arthritis and reduction of GI irritation and enhancement of bioavaibility. Materials & methods: Different batches of emulgel and selected batch was proceeded for characterization like particle size, scanning electron microscopy, drug ingredient, in vitro release, Fourier transform infrared and x-ray diffraction in vitro inflammation and gel evaluation such as (spreadability, swelling index), ex vitro permeation, skin irritation and in vivo anti-inflammatory. Result: Emulgel showed nanometri size sustained release (79.96% in 6 h), compatibility and anti-inflammatory activity compared with pure drug. Concluded that emulgels had better (nearly twice as good) anti-inflammatory action as the commercial product. Conclusion: Compared with the commercial gel, the emulgel's anti-inflammatory effect had a quicker onset and a longer duration of action.

目的:优化和评估用于治疗类风湿性关节炎的醋氯芬酸纳米凝胶,减少对胃肠道的刺激并提高其生物可溶性。材料与方法:对不同批次的凝胶进行表征,如粒度、扫描电子显微镜、药物成分、体外释放、傅立叶变换红外线和 X 射线衍射、体外炎症和凝胶评估,如(铺展性、膨胀指数)、体外渗透、皮肤刺激性和体内抗炎性。结果与纯药物相比,凝胶显示出纳米级的持续释放(6 小时内释放 79.96%)、相容性和抗炎活性。结论是,乳凝胶的抗炎作用比商用产品更好(几乎是后者的两倍)。结论与市售凝胶相比,润肤凝胶的抗炎作用起效更快,持续时间更长。
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引用次数: 0
Alopecia areata: review of epidemiology, pathophysiology, current treatments and nanoparticulate delivery system. 斑秃:流行病学、病理生理学、当前治疗方法和纳米颗粒给药系统综述。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-03-01 Epub Date: 2024-03-07 DOI: 10.4155/tde-2023-0071
Robel Singh, Pawan Kumar, Davinder Kumar, Navidha Aggarwal, Hitesh Chopra, Virender Kumar

Alopecia areata (AA) is a kind of alopecia that affects hair follicles and nails. It typically comes with round patches and is a type of nonscarring hair loss. Various therapies are accessible for the management and treatment of AA, including topical, systemic and injectable modalities. It is a very complex type of autoimmune disease and is identified as round patches of hair loss and may occur at any age. This review paper highlights the epidemiology, clinical features, pathogenesis and new treatment options for AA, with a specific emphasis on nanoparticulate drug-delivery systems. By exploring these innovative treatment approaches, researchers aim to enhance the effectiveness and targeted delivery of therapeutic agents, ultimately improving outcomes for individuals living with AA.

斑秃(AA)是一种影响毛囊和指甲的脱发症。它通常伴有圆形斑块,是一种非瘢痕性脱发。有多种疗法可用于控制和治疗 AA,包括局部、全身和注射疗法。AA 是一种非常复杂的自身免疫性疾病,表现为圆形脱发斑,可发生于任何年龄。这篇综述论文重点介绍了 AA 的流行病学、临床特征、发病机制和新的治疗方案,特别强调了纳米颗粒给药系统。通过探索这些创新的治疗方法,研究人员旨在提高治疗药物的有效性和靶向性,最终改善 AA 患者的治疗效果。
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引用次数: 0
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Therapeutic delivery
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