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OBJECTIVE To evaluate the difference of pharmacokinetics and tissue distribution of folate-modified cantharidin/baicalin liposomes(FA-Can&Bai@Lips) in normal and tumor-bearing rats. METHODS HepG2 cell suspension was inoculated into the right armpit of rat to induce tumor bearing animal models. After tail vein injection of FA-Can&Bai@Lips, plasma and tissues(heart, liver, spleen, lung and kidney) were collected at different time points. The concentrations of cantharidin and baicalin in plasma and tissues were determined by ultra high performance liquid chromatography-mass spectrometry(UPLC-MS/MS). The pharmacokinetic parameters were calculated by Phoenix WinNonlin software, and the pharmacokinetic and tissue distribution differences of FA-Can&Bai@Lips in normal and tumor-bearing rats were analyzed and compared. RESULTS The UPLC-MS/MS method for simultaneous determination of cantharidin and baicalin has a good linear relationship. The specificity, accuracy and precision, extraction recovery rate and matrix effect, residual effect and stability meet the requirements of biological sample detection. The pharmacokinetic parameters showed that the area under the curve(AUC0-t,AUC0-∞), the mean residence time(MRT0-t, MRT0-∞) of cantharidin and baicalin in plasma of tumor-bearing rats were significantly higher than those in normal rats(P<0.05), which increased by 55.68%, 72.50%, 43.10%, 45.95% and 15.10%, 42.54%, 9.09%, 10.53% respectively. The half-life(t1/2) of cantharidin was slightly shortened in tumor-bearing rats with no significant difference, while the t1/2 of baicalin was significantly prolonged(P<0.05). The apparent volume of distribution(Vd) and clearance(CL) of cantharidin and BA were significantly decreased. The results of tissue distribution showed that the concentrations of cantharidin and BA in the liver of tumor-bearing rats were significantly higher than those of normal rats, and the other tissues were significantly lower(P<0.01). CONCLUSION The UPLC-MS/MS method is rapid, simple, specific and sensitive, and can be used for the determination of cantharidin and baicalin in plasma and tissues of rats. It is confirmed that the tumor-bearing status can significantly affect the pharmacokinetics and tissue distribution of FA-Can&Bai@Lips in vivo.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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