科研之友
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Objective: The deeper research of N-octyl-N-arginine chitosan (OACS) as intravenous delivery was characterized, cell uptake study, pharmacokinetics, and biodistribution of OACS micelles (GA-OACS) were investigated. @@@ Significance: Gambogic acid (GA) can inhibit the growth of various cancer cells. However, the short elimination half-life time and treatment without targeting limits its application. OACS was synthesized as delivery carrier for GA by us, but the deeper characterization of OACS, such as molecular modeling, pharmacokinetics, and biodistribution were not investigated. @@@ Methods: Gambogic acid loaded OACS micelles (GA-OACS) were evaluated by the molecular modeling, characterized by TEM, DLS, IR, (HNMR)-H-1, XRD. Confocal laser scanning microscope and flow cytometry were analyzed for cell uptake study. Imaging analysis was used to show the distribution of OACS in vivo directly, pharmacokinetics and biodistribution were also investigated. @@@ Results: The molecular modeling result showed that GA could encapsulated stably in the core of OACS micelles. TEM, IR, (HNMR)-H-1, and XRD also suggested that GA was encapsulated in amorphous form in the core of OACS micelles. AUC and elimination half-life of GA-OACS were all increased by 1.5-fold and 2.0-fold compared with GA-ARG in rat, respectively. Biodistribution study indicated that GA-OACS was distributed mainly in the liver. GA amount in the kidney and heart was greatly reduced in the GA-OACS group. From the imaging analysis, OACS distribution in the liver was the most. @@@ Conclusions: OACS was an excellent carrier for GA intravenous delivery to prolong half-life. Moreover, OACS targeted on liver.
