Preparation, Characterization, and Hepatoprotective Activity Evaluation of Quercetin-loaded Pluronic® F127/Chitosan-Myristic Acid Mixed Micelles.

Darshan R Telange, Seema Kamdi, Atul T Hemke, Anil M Pethe, Vijay B Lambole, Umesh B Telrandhe
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Abstract

Background: Quercetin (QTN) is a flavonol antioxidant found in foods, medicinal plants, fruits, vegetables, and beverages. QTN oral consumption produces several biological effects, including antioxidant, cardioprotective, anti-apoptotic, anti-cancer, neuroprotection, anti-hypertensive, and chemo preventive.

Objective: The study aimed to prepare Pluronic®F127/chitosan-myristic acid copolymer (PF127/C-MAc)-based mixed micelles (QTN MM) to improve the biopharmaceutical and hepatoprotective potential of QTN.

Methods: QTN MM was developed employing thin-film hydration and optimized using full factorial design (FFD). Optimized QTN MM was analyzed using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR), powder x-ray diffractometry (PXRD), in vitro dissolution, ex vivo permeation, and in vivo antioxidant activity in carbon tetrachloride (CCL4)-induced albino rats.

Results: PF127/C-MAc ratio (1:1) with CMC value ~ 5 μg/mL showed the suitability for MM. Characterization supported the formation of MM. QTN MM revealed prominent encapsulation efficiency and drug loading of about ~ 95.10% and ~ 12.28% w/w, respectively. MM spherical shape of QTN with a smaller particle size of ~ 34.08 nm and a higher zeta potential of ~ 36.24 nm indicated excellent physical stability. Dissolution and ex vivo permeation results revealed higher dissolution and permeation of QTN MM compared to QTN and PM. In vivo antioxidant activity suggested that QTN MM at (~ 20 mg/kg, p.o.) restored the enhanced marker enzyme level compared to QTN.

Conclusion: The findings demonstrate that developed QTN MM could be used as an alternative nanocarrier to increase the biopharmaceutical and hepatoprotective potential of QTN and other flavonoids.

载槲皮素的 Pluronic® F127/壳聚糖-肉豆蔻酸混合胶束的制备、表征和肝保护活性评估
背景:槲皮素(QTN)是一种存在于食物、药用植物、水果、蔬菜和饮料中的黄酮醇类抗氧化剂。口服槲皮素可产生多种生物效应,包括抗氧化、保护心脏、抗细胞凋亡、抗癌、神经保护、抗高血压和预防化疗:本研究旨在制备基于 Pluronic®F127/ 壳聚糖-肉豆蔻酸共聚物(PF127/C-MAc)的混合胶束(QTN MM),以提高 QTN 的生物制药和保肝潜力:方法:采用薄膜水合技术开发了 QTN MM,并利用全因子设计(FFD)对其进行了优化。采用扫描电子显微镜(SEM)、差示扫描量热仪(DSC)、傅立叶变换红外光谱(FT-IR)、粉末 X 射线衍射仪(PXRD)对优化后的 QTN MM 进行了分析,并对四氯化碳(CCL4)诱导的白化大鼠进行了体外溶解、体内渗透和体内抗氧化活性分析:结果表明:PF127/C-MAc 的比例为 1:1,CMC 值约为 5 μg/mL,适用于 MM。表征支持 MM 的形成。QTN MM 的包封效率和载药量分别约为 95.10%和 12.28%(重量百分比)。QTN MM 呈球形,粒径较小,约为 34.08 nm,zeta 电位较高,约为 36.24 nm,这表明其具有良好的物理稳定性。溶解和体内渗透结果表明,与 QTN 和 PM 相比,QTN MM 的溶解度和渗透度更高。体内抗氧化活性表明,与 QTN 相比,QTN MM(~ 20 mg/kg,p.o.)可恢复增强的标记酶水平:研究结果表明,开发的 QTN MM 可用作替代纳米载体,以提高 QTN 和其他黄酮类化合物的生物制药和保肝潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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