LC-UV Determination of Baicalin in Rabbit Plasma and Tissues for Application in Pharmacokinetics and Tissue Distribution Studies of Baicalin after Intravenous Administration of Liposomal and Injectable Formulations.
A simple and sensitive LC-UV method to investigate the pharmacokinetics and biodistribution pattern of baicalin in rabbits was established and validated. Baicalin and the internal standard, rutin, were extracted from biosamples using acetonitrile as protein precipitation after pretreated with ammonium acetate buffer (pH 3.5; 1 M) to obtain a pure chromatographic peak and high extraction recovery. Chromatographic separation was achieved on a reverse-phase C18 column with a gradient elution at flow rate of 1.0 mL/min. UV absorption was set at 278 nm. Chromatographic response was linear over the ranges of 0.05-10.00 μg/mL in plasma and 0.05-300.00 μg/g in tissues with the limits of quantification of 50.0 ng/mL in plasma and tissues, and the limit of detection of baicalin in bio-samples of 15 ng/mL. The RSD of intra-and inter-day for the biosamples were from 4.19% to 10.84% and from 4.37% to 10.93%, respectively. The accuracy of plasma and tissue samples ranged from 81.6% to 95.2% and 80.8% to 98.4%, respectively. The extraction recoveries ranged from 81.5% to 88.3% for plasma, from 73.1% to 93.2% for tissues, respectively. Baicalin was stable in rabbit biosamples. The validated method was successfully applied to the study of the pharmacokinetics and tissue distribution of baicalin after intravenous administration of liposomal and injectable formulations to rabbits. Compared to baicalin injection, the pharmacokinetics and biodistribution behavior of baicalin was altered significantly in rabbits treated with its liposomes and drug concentration in the lungs was greatly increased.
Department of Pharmaceutical Sciences, School of Pharmacy, Southwest Medical University, No. 3-319, Zhongshan Road, Jiangyang District, Luzhou 646000, China. weiyumeng-268@163.com.
Yumeng
Y
Wei
Department of Pharmaceutical Sciences, School of Pharmacy, Southwest Medical University, No. 3-319, Zhongshan Road, Jiangyang District, Luzhou 646000, China. pichao2016@sina.com.
Chao
C
Pi
Department of Chemistry, the Institute of Basic Medical Sciences, Southwest Medical University, No. 3-319, Zhongshan Road, Jiangyang District, Luzhou 646000, China. gangy405@163.com.
Gang
G
Yang
Department of Pathology, the Affiliated Hospital of Southwest Medical University, No. 25, Taiping Street, Luzhou 646000, China. zl2006998@sina.com.
Xiaoming
X
Xiong
Department of Radiology, the Affiliated Hospital of Southwest Medical University, No. 25, Taiping Street, Luzhou 646000, China. LYBLUE2008@aliyun.com.
Yongshu
Y
Lan
Department of Oncology, the Affiliated Hospital of Southwest Medical University, No. 25, Taiping Street, Luzhou 646000, China. yanghr2015@sina.com.
Hongru
H
Yang
Department of Pharmaceutical Sciences, School of Pharmacy, Southwest Medical University, No. 3-319, Zhongshan Road, Jiangyang District, Luzhou 646000, China. zhouyg2014@sina.com.
Yang
Y
Zhou
Department of Pharmaceutical Sciences, School of Pharmacy, Southwest Medical University, No. 3-319, Zhongshan Road, Jiangyang District, Luzhou 646000, China. zl2006998@126.com.|Department of Pharmacy, the Affiliated Hospital of Southwest Medical University, No. 25, Taiping Street, Luzhou 646000, China. zl2006998@126.com.
Yun
Y
Ye
Department of Orthopedics, the Affiliated Hospital of Traditional Chinese Medicine of Southwest Medical University, No. 16, Chunhui Road, Longma Tan District, Luzhou 646000, China. zouyg2015@sina.com.
Yonggen
Y
Zou
Department of Cardiovascular Medicine, The Affiliated Hospital of Southwest Medical University, No. 25, Taiping Street, Luzhou 646000, China. weilivipcqmc@163.com.
Wenwu
W
Zheng
Department of Pharmaceutical Sciences, School of Pharmacy, Southwest Medical University, No. 3-319, Zhongshan Road, Jiangyang District, Luzhou 646000, China. zhaoling-998@163.com.
Ling
L
Zhao
D061605:Administration, Intravenous; D000818:Animals; D002853:Chromatography, Liquid / Q000379:methods*; D004355:Drug Stability; D005419:Flavonoids / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D007267:Injections; D008081:Liposomes / Q000737:chemistry; D008168:Lung / Q000737:chemistry; D010949:Plasma / Q000737:chemistry; D011817:Rabbits; D014018:Tissue Distribution
D005419:Flavonoids; D008081:Liposomes; C038044:baicalin
LC-UV; baicalin; lung targeting; pharmacokinetics; tissue distribution