Oral absorption in rats and tissue distribution in mice of raloxifene nanoemulsion after oral administration
ZHANG Ying-feng
ZHENG Yu-rong
LIU Chang-shun
LU Yao-wen
YANG Sheng-yun
LI Li
HUANG Chuan-li
LONG Xiao-ying
Abstract:Objective:To investigate the oral absorption in rats and tissue distribution in mice of raloxifene (RAL) nanoemulsion (NE) and raloxifenen suspension after oral administration.Methods:The plasma and tissue samples were collected from rats or mice at different time points post-dose for oral studies (a single dose of 60 mg·kg 1) or intravenous injection studies (a single dose of 10 mg·kg-1).An HPLC method was established to determine the concentrations of RAL in plasma of rats and tissues of mice then the characteristics of oral absorption and tissue distribution were compared.Results:In the oral absorption studies in rats and mice,the main oral absorption parameters such as the AUC and Cmax of RAL-NE were significantly increased compared with the suspension.In the tissue distribution studies,the distribution of RAL was highest in the lungs for both nanoemulsion and suspension;the AUC and C of RAL in the spleen were increased significantly,but they were almost the same in the liver compared with the suspension.Conclusion:Compared with RAL suspension,RAL-NE was able to improve the oral bioavailability of RAL to a certain extent.The targeting property of RAL loaded in nanoemulsion was changed,which was obviously targeted to spleen.
Keywords:raloxifenenanoemulsionoral absorptiontissue distributionbioavailability
Publication Date:2017-01-01
Online Publishing Date:2026-08-14(First online date of this platform, not the publication date of the document)
Pages:7( 923-929 )
