开发一种新的卡维地洛和姜黄素胶束制剂,以增强自发性高血压大鼠模型的降压效果。

IF 3.1 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Yanina Alejandra Santander Plantamura, Miguel Allo, Jennifer Riedel, Pedro Fuentes, Ana Sol Riesco, Ezequiel Bernabeu, Mariana Garcés, Pablo Evelson, Susana Gorzalczany, Andrea Carranza, Christian Höcht, Diego Chiappetta
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引用次数: 0

摘要

心血管疾病仍然是全球发病率和死亡率的主要原因,需要创新的治疗策略。该项目以卡维地洛和姜黄素为重点,探索了一种提高心血管药物疗效的纳米制药方法。这些药物因其潜在的心血管疗效而闻名,它们被封装在 Soluplus® 胶束中,形成了一种新型的给药系统。这种配方的新颖之处在于它能够显著提高卡维地洛和姜黄素的溶解度,而传统上这两种药物的溶解度一直受到疏水性的限制。通过利用 Soluplus® 胶束,我们开发出了一种独特的给药系统,可优化这两种药物的治疗潜力。我们对纳米胶束的载药量、粒度分布和形态特征进行了细致的表征。对卡维地洛和姜黄素的释放模式进行了研究,发现了持续和可控的释放曲线。此外,还对胶束制剂的抗氧化能力进行了评估,结果表明它保留了姜黄素的抗氧化特性。使用自发性高血压雄性大鼠进行的体内研究探讨了纳米胶束系统的药代动力学和血液动力学效应。这些结果表明,这两种药物都被成功封装,且不会改变其血浆特征。此外,与单独给药相比,服用卡维地洛和姜黄素胶束能更显著地降低平均动脉压,这表明它们具有潜在的协同效应。总之,这种纳米制药方法为心血管治疗提供了一个前景广阔的途径,为联合给药和潜在的协同效应提供了一个平台。经过优化的配方可以改善患者的治疗效果,提高心血管健康水平。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development of a new micellar formulation of carvedilol and curcumin to enhance blood pressure reduction in a spontaneously hypertensive rat model.

Cardiovascular diseases remain a leading cause of morbidity and mortality worldwide, requiring innovative therapeutic strategies. This project explores a nano-pharmaceutical approach to enhance the efficacy of cardiovascular drugs, focusing on carvedilol and curcumin. These agents, known for their potential cardiovascular benefits, are encapsulated within Soluplus® micelles to form a novel drug delivery system. The novelty of this formulation lies in its ability to significantly improve the solubility of both carvedilol and curcumin, which have traditionally been limited by their hydrophobic nature. By utilizing Soluplus® micelles, we have developed a unique delivery system that optimizes the therapeutic potential of both drugs. The nanomicelles were meticulously characterized for drug loading, size distribution, and morphological features. The carvedilol and curcumin release patterns were investigated, revealing sustained and controlled release profiles. Additionally, the antioxidant capacity of the micellar formulation was evaluated, demonstrating the preservation of curcumin's antioxidative properties. In vivo studies using spontaneously hypertensive male rats explored the pharmacokinetics and hemodynamic effects of the nanomicellar system. These results indicated successful encapsulation of both drugs without altering their plasma profiles. Furthermore, the administration of carvedilol and curcumin micelles exhibited a more significant reduction in mean arterial pressure compared to individual drug administration, suggesting a potential synergistic effect. In conclusion, this nano-pharmaceutical approach offers a promising avenue for cardiovascular therapy, providing a platform for combined drug delivery and potential synergistic effects. The optimized formulation could lead to improved patient outcomes and enhanced cardiovascular health.

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来源期刊
CiteScore
6.20
自引率
5.60%
发文量
142
审稿时长
4-8 weeks
期刊介绍: Naunyn-Schmiedeberg''s Archives of Pharmacology was founded in 1873 by B. Naunyn, O. Schmiedeberg and E. Klebs as Archiv für experimentelle Pathologie und Pharmakologie, is the offical journal of the German Society of Experimental and Clinical Pharmacology and Toxicology (Deutsche Gesellschaft für experimentelle und klinische Pharmakologie und Toxikologie, DGPT) and the Sphingolipid Club. The journal publishes invited reviews, original articles, short communications and meeting reports and appears monthly. Naunyn-Schmiedeberg''s Archives of Pharmacology welcomes manuscripts for consideration of publication that report new and significant information on drug action and toxicity of chemical compounds. Thus, its scope covers all fields of experimental and clinical pharmacology as well as toxicology and includes studies in the fields of neuropharmacology and cardiovascular pharmacology as well as those describing drug actions at the cellular, biochemical and molecular levels. Moreover, submission of clinical trials with healthy volunteers or patients is encouraged. Short communications provide a means for rapid publication of significant findings of current interest that represent a conceptual advance in the field.
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