title: Preparation and evaluation of kaempferol-phospholipid complex for pharmacokinetics and bioavailability in SD rats.
abstract: As one of the dietary flavonoids, kaempferol (KP) has been well known to show strong anti-oxidative effect along with other biological properties. However, the oral bioavailability of KP is relatively low due to its poor solubility. In this study, we intended to increase the solubility and bioavailability of KP by preparing kaempferol-phospholipid complex (KP-PC). The KP-PC's physicochemical properties were characterized in terms of infrared spectroscopy (IR), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), water/n-Octanol solubility and in vitro dissolution. KP-PC exhibited higher solubility and dissolution rate than KP, indicating a significant improvement in hydrophilicity. A UPLC-ESI-MS/MS method was developed and validated for the determination of KP in Sprague-Dawley (SD) rat plasma, so as to investigate the oral bioavailability of KP-PC versus KP. Results showed that Cmax and AUC(0-48 h) of KP from the complex (Cmax: 3.94 ± 0.83 μg/mL, AUC(0-48 h): 57.81 ± 9.43 mg/Lh) were higher than that of KP (Cmax: 1.43 ± 0.21 μg/mL, AUC(0-48 h): 13.65 ± 3.12 mg/Lh). This research indicated that phospholipid complex (PC) might be one of the suitable approachs to improve the oral bioavailability of KP and other poor-solubility flavonoids.
authors.affiliation: School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Kexia
authors.initials: K
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Liqiang
authors.initials: L
authors.lastname: Gu
authors.affiliation: School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Jinpeng
authors.initials: J
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Yuanyuan
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Jiang
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Longshan
authors.initials: L
authors.lastname: Zhao
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
authors.forename: Kaishun
authors.initials: K
authors.lastname: Bi
authors.affiliation: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address: cxh_syphu@hotmail.com.
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Chen
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D002138:Calibration; D002152:Calorimetry, Differential Scanning; D044949:Kaempferols / Q000032:analysis* / Q000493:pharmacokinetics*; D057230:Limit of Detection; D000442:Octanols / Q000737:chemistry; D010743:Phospholipids / Q000032:analysis* / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012995:Solubility; D013055:Spectrophotometry, Infrared; D017550:Spectroscopy, Fourier Transform Infrared; D053719:Tandem Mass Spectrometry; D013696:Temperature; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D044949:Kaempferols; D000442:Octanols; D010743:Phospholipids; D014867:Water; C006552:kaempferol
keywords: Bioavailability; Kaempferol; Kaempferol–phospholipid complex; Pharmacokinetics