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橙皮苷和橙皮素的纳米植物脂质体:制备、表征及体内评价。

Nanophytosomes of hesperidin and of hesperetin: Preparation, characterization, and in vivo evaluation.

作者信息

Omidfar Fatemeh, Gheybi Fatemeh, Davoodi Javid, Amirinejad Mostafa, Badiee Ali

机构信息

Department of Biotechnology, Faculty of Advanced Science and Technology, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran.

Department of Medical Biotechnology and Nanotechnology, Faculty of Medicine, Mashhad University of Medical Sciences, Mashhad, Iran.

出版信息

Biotechnol Appl Biochem. 2023 Apr;70(2):846-856. doi: 10.1002/bab.2404. Epub 2022 Oct 17.

Abstract

Hesperidin and hesperetin are two important plant flavanones abundantly found in citrus fruit. They have discovered many biological activities to treat diseases, including cancer, diabetes, and Alzheimer's disease. Despite their various benefits, they have poor solubility, which reduces their bioavailability and absorption. In this study, nanophytosomes have been utilized to improve their payload's solubility and bioavailability. In the current study, hesperetin or hesperidin was complexed with Phospholipon 90G with a 2:1 or 3:1 molar ratio, respectively. The formation of associations between active compounds and phospholipid were confirmed by X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), and nuclear magnetic resonance (NMR) techniques. Dynamic light scattering data show that the prepared associations in the presence of body fluids can make nanoparticles in the range of 200-250 nm. In addition, oral administration demonstrated that C of hesperidin and hesperetin was increased (up to four times) after complexation with the lipid. It is concluded that phospholipid association may be used as a suitable and straightforward strategy to improve therapeutic activities of hesperidin and hesperetin by increasing their solubility and bioavailability.

摘要

橙皮苷和橙皮素是柑橘类水果中大量存在的两种重要植物黄烷酮。它们已被发现具有多种治疗疾病的生物活性,包括癌症、糖尿病和阿尔茨海默病。尽管它们有诸多益处,但溶解度较差,这降低了它们的生物利用度和吸收率。在本研究中,纳米植物脂质体已被用于提高其有效载荷的溶解度和生物利用度。在当前研究中,橙皮素或橙皮苷分别与磷脂90G以2:1或3:1的摩尔比络合。通过X射线衍射(XRD)、傅里叶变换红外光谱(FTIR)和核磁共振(NMR)技术证实了活性化合物与磷脂之间缔合物的形成。动态光散射数据表明,在体液存在下制备的缔合物可形成200 - 250纳米范围内的纳米颗粒。此外,口服给药表明,橙皮苷和橙皮素与脂质络合后,其生物利用度提高(高达四倍)。结论是,磷脂缔合可作为一种合适且直接的策略,通过提高橙皮苷和橙皮素的溶解度和生物利用度来改善它们的治疗活性。

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