title: 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.
abstract: 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.
authors.affiliation: Department of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education; Department of Pharmaceutics, School of Pharmacy.
authors.forename: Xiangrong
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Department of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education.
authors.forename: Yi
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Biomedical Science, School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning, People's Republic of China.
authors.forename: Shuang
authors.initials: S
authors.lastname: Guo
authors.affiliation: Department of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education.
authors.forename: Feifei
authors.initials: F
authors.lastname: Bai
authors.affiliation: Department of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education.
authors.forename: Tong
authors.initials: T
authors.lastname: Wu
authors.affiliation: Department of Traditional Chinese Materia Medica, Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education.
authors.forename: Yuqing
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D036145:Ginsenosides; D057927:Hydrophobic and Hydrophilic Interactions; D010743:Phospholipids / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility / Q000187:drug effects*; D014315:Triterpenes / Q000737:chemistry / Q000493:pharmacokinetics*; D000097669:Dammaranes
chemical_list: D036145:Ginsenosides; D010743:Phospholipids; D014315:Triterpenes; D000097669:Dammaranes; C582879:20(R)-25-methoxyldammarane-3beta,12beta,20-triol
keywords: 25-OCH3-PPD; LC–MS/MS; bioavailability; phospholipid complex; solubility