TANG Han-xiao, ZHAO Tian-wen, HUANG Yu, et al. Pharmacokinetics and Hepatic Targeting of Trionycis Carapax Peptide Sterically Stabilized Liposomes[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(9): 68-73.
TANG Han-xiao, ZHAO Tian-wen, HUANG Yu, et al. Pharmacokinetics and Hepatic Targeting of Trionycis Carapax Peptide Sterically Stabilized Liposomes[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(9): 68-73. DOI: 10.13422/j.cnki.syfjx.2017090068.
this liposome was performed on SD rats and BALB/c nude mice for in vivo targeting studies.HGRFG-5-FAM-SSL (HFL) was preparing by SSL loading Trionycis Carapax peptide containing 5-carboxylfluorescein(5-FAM) (HGRFG-5-FAM
HF)
and to investigate pharmacokinetics of administration by HF and HFL in rats
respectively. Method: DiR-SSL and HFL were prepared by thin-film dispersion method.HF and HFL were injected into the tail vein of two groups of SD rats
respectively;the concentration and dose of HF were the same.Plasma samples were collected at different time points and analyzed by multi-function microplate detector
and pharmacokinetic parameters were calculated.DiR-SSL was injected intravenously in BALB/c nude mice
the mice were in vivo imaged respectively at 1
2
5
7
24 h
and fluorescence values were read.The normal SD rats were injected DiR-SSL intravenously
after 24 h
the heart
liver
spleen
lung and kidney were imaged in fluorescence imaging system and fluorescence values were read
frozen sections of liver tissue were taken for confocal laser scanning. Result: After HF being injected into rats
its T1/2 was only 0.826 h;at the same dose
T1/2 and AUC0-∞ of HFL were 16.253 times and 11.899 times that of HF
respectively.In vivo fluorescence imaging of BALB/c nude mice showed fluorescence was mainly in the liver position and weakened gradually over time.The fluorescence of DiR-SSL in the liver of SD rats among different organs was strongest
DiR-SSL remained in the liver tissue at 24 h after injection. Conclusion: SSL drug delivery system can significantly extend T1/2 of HF in SD rats
and this system has a liver targeting effect
suggesting that this system can be used as drug carriers to realize liver targeted drug delivery.