Abstract
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.
Highlights
IntroductionBaicalin (7-glucuronic acid-5,6-dihydroxy-flavone, Figure 1), as one of the main bioactive flavone compounds, was isolated from the Radix Scutellariae that is a well-known traditional Chinese medicine
Baicalin (7-glucuronic acid-5,6-dihydroxy-flavone, Figure 1), as one of the main bioactive flavone compounds, was isolated from the Radix Scutellariae that is a well-known traditional Chinese medicine used to treat diarrhea, fever, inflammatory and hepatic disease, and so on, in many countries [1].Recently, a great deal of studies regarding baicalin have presented its excellent pharmacologicalBaicalin acid-5,6-dihydroxy-flavone, Figure1), as one of the main bioactive flavone anti-inflammation [2]
Compounds, was isolated from the Radix Scutellariae that is a well-known traditional Chinese baicalin was widely used in the clinic either as a single compound such as its tablets and capsules or as medicine used to treat diarrhea, fever, inflammatory and hepatic disease, and so on, in many a main active component in morea than of preparations recorded in the its Chinese countries [1]
Summary
Baicalin (7-glucuronic acid-5,6-dihydroxy-flavone, Figure 1), as one of the main bioactive flavone compounds, was isolated from the Radix Scutellariae that is a well-known traditional Chinese medicine. Establish a simple and analytical method for the determination of baicalindrug in plasma to some extent This made it sensitive necessary for us to develop a lung-targeting delivery system and tissues to characterize its pharmacokinetics and tissue distribution patterns. In the preliminary experiments, baicalin loaded liposomes prepared by analytical methods for baicalin in plasma, serum, urine had been well developed mainly using the an effervescent technique displayed lung targeting for first time. This made it necessary techniques of LC-UV [15], LC-MS [16], LC-DAD [17],effects.
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