关键词: Luteolin anticancer activity bio-availability nanoformulations solubility targeting.

来  源:   DOI:10.2174/0113816128313713240628063301

Abstract:
BACKGROUND: Luteolin (LUT), a naturally occurring flavonoid found in vegetables, fruits, and herbal medicines, has been extensively studied for its pharmacological activities, including anti-proliferative and anticancer effects on various cancer lines. It also exhibits potent antioxidant properties and pro-apoptotic activities against human cancers. However, its therapeutic potential is hindered by its poor solubility in water (5 μg/ml at 45°C) and low bioavailability. This research on the development of luteolin-loaded nanocarrier aims to overcome these limitations, thereby opening up new possibilities in cancer treatment.
METHODS: This paper covers several nanoformulations studied to increase the solubility and bioavailability of LUT. The physicochemical characteristics of the nanoformulation that influence luteolin\'s solubility and bioavailability have been the subject of more in-depth investigation. Furthermore, it examines how LUT\'s anti-inflammatory and antioxidant properties aid in lessening the side effects of chemotherapy.
RESULTS: Most nanoformulations, including phytosomes, lipid nanoparticles, liposomes, protein nanoparticles, polymer micelles, nanoemulsions, and metal nanoparticles, have shown promising results in improving the solubility and bioavailability of LUT. This is a significant step forward in enhancing the therapeutic potential of LUT in cancer treatment. Furthermore, the study found that LUT\'s ability to scavenge free radicals can significantly reduce the side effects of cancer treatment, further highlighting its potential to improve patient outcomes.
CONCLUSIONS: Nanoformulations, because of their unique surface and physiochemical properties, improve the solubility and bioavailability of LUT. However, poor in-vitro and in-vivo correlation and scalability of nanoformulations need to be addressed to achieve good clinical performance of LUT in oncology.
摘要:
背景:木犀草素(LUT),一种在蔬菜中发现的天然类黄酮,水果,和草药,其药理活性已被广泛研究,包括对各种癌细胞系的抗增殖和抗癌作用。它还表现出有效的抗氧化特性和针对人类癌症的促凋亡活性。然而,其在水中的溶解性差(45°C时为5μg/ml)和生物利用度低,阻碍了其治疗潜力。本研究开发木犀草素负载纳米载体的目的是克服这些限制,从而为癌症治疗开辟了新的可能性。
方法:本文涵盖了为提高LUT的溶解度和生物利用度而研究的几种纳米制剂。纳米制剂的物理化学特性影响木犀草素的溶解度和生物利用度已成为更深入研究的主题。此外,它研究了LUT的抗炎和抗氧化特性如何帮助减轻化疗的副作用。
结果:大多数纳米配方,包括植物体,脂质纳米粒,脂质体,蛋白质纳米颗粒,聚合物胶束,纳米乳液,和金属纳米粒子,在提高LUT的溶解度和生物利用度方面显示出有希望的结果。这是提高LUT在癌症治疗中的治疗潜力的重要一步。此外,研究发现,LUT清除自由基的能力可以显著降低癌症治疗的副作用,进一步强调其改善患者预后的潜力。
结论:纳米配方,由于其独特的表面和生理化学性质,提高LUT的溶解度和生物利用度。然而,需要解决纳米制剂的弱的体外和体内相关性和可扩展性,以实现LUT在肿瘤学中的良好临床性能。
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