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Resveratrol loaded glycyrrhizic acid-conjugated human serum albumin nanoparticles for tail vein injection II: pharmacokinetics, tissue distribution and bioavailability.
Drug Delivery ( IF 6 ) Pub Date : 2019-12-20 , DOI: 10.1080/10717544.2019.1704944
Mingfang Wu 1, 2 , Chen Zhong 3 , Yiping Deng 1, 2 , Qian Zhang 1, 2 , Xiaoxue Zhang 1, 2 , Xiuhua Zhao 1, 2
Affiliation  

There are many kinds of biological activities of resveratrol itself, but its clinical application is limited by its poor solubility in water and low bioavailability. Therefore, we have prepared glycyrrhizic acid-conjugated human serum albumin nanoparticles wrapping resveratrol nanoparticles (GL-HSA-RESNPs). The purpose of this study was to investigate the bioavailability, pharmacokinetics and tissue distribution of resveratrol in rats after single-dose tail vein injection administration of GL-HSA-RESNPs. A sensitive and reliable high performance liquid chromatography (HPLC) method was established to verify the content of resveratrol in rat plasma and organs. The Cmax value after GL-HSA-RESNPs administration was significantly higher than that of resveratrol suspension (933 ± 76.64 ng/mL vs. 618 ± 42.54 ng/mL, p < .01). The Tmax value obtained after GL-HSA-RESNPs administration was significantly shorter than that after resveratrol suspension administration (0.17 ± 0.01 h vs. 0.25 ± 0.01 h, p < .001). The bioavailability of GL-HSA-RESNPs was 4.25 times higher than that of the pure resveratrol. The concentration of resveratrol in the main organs of rats treated with the GL-HSA-RESNPs was higher than that in rats treated with the pure resveratrol. Rats treated with GL-HSA-RESNPs had the highest concentration of resveratrol in their liver. It is indicated that GL-HSA-RESNPs is a promising liver-targeted delivery system that improves the in vivo bioavailability of resveratrol.

中文翻译:

白藜芦醇负载的甘草酸缀合的人血清白蛋白纳米粒子用于尾静脉注射II:药代动力学,组织分布和生物利用度。

白藜芦醇本身具有多种生物活性,但由于其在水中的溶解性差和生物利用度低,其临床应用受到了限制。因此,我们制备了包裹了白藜芦醇纳米颗粒(GL-HSA-RESNPs)的甘草酸偶联的人血清白蛋白纳米颗粒。这项研究的目的是研究白藜芦醇在大鼠单剂量尾静脉注射GL-HSA-RESNPs后的生物利用度,药代动力学和组织分布。建立了灵敏可靠的高效液相色谱(HPLC)方法,以验证大鼠血浆和器官中白藜芦醇的含量。GL-HSA-RESNPs给药后的Cmax值显着高于白藜芦醇悬液的Cmax值(933±76.64 ng / mL与618±42.54 ng / mL,p <0.01)。GL-HSA-RESNPs给药后获得的Tmax值明显短于白藜芦醇悬液给药后的Tmax值(0.17±0.01 h对0.25±0.01 h,p <.001)。GL-HSA-RESNPs的生物利用度是纯白藜芦醇的4.25倍。GL-HSA-RESNPs处理的大鼠主要器官中白藜芦醇的浓度高于纯白藜芦醇处理的大鼠中白藜芦醇的浓度。用GL-HSA-RESNPs治疗的大鼠肝脏中白藜芦醇的浓度最高。表明GL-HSA-RESNPs是有希望的肝靶向递送系统,其改善了白藜芦醇的体内生物利用度。GL-HSA-RESNPs的生物利用度是纯白藜芦醇的4.25倍。GL-HSA-RESNPs处理的大鼠主要器官中白藜芦醇的浓度高于纯白藜芦醇处理的大鼠中白藜芦醇的浓度。用GL-HSA-RESNPs治疗的大鼠肝脏中白藜芦醇的浓度最高。表明GL-HSA-RESNPs是有希望的肝靶向递送系统,其改善了白藜芦醇的体内生物利用度。GL-HSA-RESNPs的生物利用度是纯白藜芦醇的4.25倍。GL-HSA-RESNPs处理的大鼠主要器官中白藜芦醇的浓度高于纯白藜芦醇处理的大鼠中白藜芦醇的浓度。用GL-HSA-RESNPs治疗的大鼠肝脏中白藜芦醇的浓度最高。表明GL-HSA-RESNPs是有希望的肝靶向递送系统,其改善了白藜芦醇的体内生物利用度。
更新日期:2020-04-20
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