Improved oral bioavailability of 20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol using nanoemulsion based on phospholipid complex: design, characterization, and in vivo pharmacokinetics in rats

被引：16
|
作者：
Zhang, Xiangrong [1 ,2 ]
Zhang, Yi [1 ]
Guo, Shuang [3 ]
Bai, Feifei [1 ]
Wu, Tong [1 ]
Zhao, Yuqing [1 ]
机构：
[1] Shenyang Pharmaceut Univ, Dept Tradit Chinese Mat Med, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Rd, Shenyang 110016, Liaoning, Peoples R China
[2] Shenyang Pharmaceut Univ, Sch Pharm, Dept Pharmaceut, Shenyang, Liaoning, Peoples R China
[3] Shenyang Pharmaceut Univ, Sch Life Sci & Biopharmaceut, Dept Biomed Sci, Shenyang, Liaoning, Peoples R China
来源：
DRUG DESIGN DEVELOPMENT AND THERAPY | 2016年 / 10卷
基金：
美国国家科学基金会;
关键词：
25-OCH3-PPD; phospholipid complex; solubility; bioavailability; LC-MS/MS; PROBUCOL; GINSENG; DRUG; 20(S)-25-METHOXYL-DAMMARANE-3-BETA; NANOPARTICLES; DELIVERY; SYSTEMS;
D O I：
10.2147/DDDT.S114374
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The aim of the study was to improve the oral absorption of the compound 25-OCH3-PPD with poor hydrophilicity and lipophilicity. 25-OCH3-PPD-phospholipid complex was prepared by solvent evaporation, then characterized by differential scanning calorimetry, scanning electron microscopy, and infrared absorption spectroscopy. The aqueous solubility and oil-water partition coefficient were compared with the free compound. A nanoemulsion loaded with 25-OCH3-PPD-phospholipid complex was developed by dissolving the complex in water in the presence of hydrophilic surfactant under sonication. After oral administration of the nanoemulsion and the suspension of 25-OCH3-PPD in rats, the concentrations of 25-OCH3-PPD in plasma were determined by high-performance liquid chromatography-tandem mass spectrometry method. The results showed that the solubility of the complex in water and n-octanol was enhanced. The oil-water partition coefficient improved 1.7 times. Peak plasma concentration and area under the curve((0-24 h)) of the nanoemulsion of 25-OCH3-PPD-phospholipid complex were higher than that of free compound by 3.9- and 3.5-folds.
引用
收藏
页码：3707 / 3716
页数：10
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