Pharmacokinetics and tissue distribution of furanodiene W/O/W multiple emulsions in rats by a fast and sensitive HPLC–APCI–MS/MS method

Author： Zhang Li-Feng Lu Tao-Tao Zhang Shu-Qiu Lin Wen-Han Li Qing-Shan

Publisher： Informa Healthcare

ISSN： 1366-5928

Source： Xenobiotica, Vol.43, Iss.12, 2013-12, pp. : 1095-1102

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Abstract

Abstract1. A sensitive and specific HPLC--APCI--MS/MS method was developed and validated for the quantification of furanodiene, a natural antitumor compound in rat plasma and tissues. W/O/W multiple emulsions of furanodiene, identified through microscope-observation and eosin staining method, were prepared with a two-step-procedure. Pharmacokinetics and tissue distribution were studied in rats after oral, intraperitoneal and intravenous injection with the dose of 5, 10 and 50 mg/kg, respectively.2. The assay achieved a good sensitivity and specificity for the determination of furanodiene in biological samples. The results showed that the concentration–time curves of furanodiene in rats after intravenous injection were fitted to a two-compartment model and the linear pharmacokinetic characteristic. The highest concentration in rat tissue was observed in the spleen, followed by heart, liver, lung, kidney, small intestine and brain.3. Comparing with the low concentration in plasma, furanodiene could be detected in various tissue samples after oral or intraperitoneal injection which indicated furanodiene had good and rapid tissue uptake.4. The results suggested that the wide tissue distribution of furanodiene could conduce to the therapeutic effects, but the short biological half-life limited its further application as an antitumor agent. The results are helpful for the structure modification of furanodiene as an antitumor candidate.