Modification of glycyrrhetinic acid derivatives NCTD liposomal targeting in the liver of mice.doc

 PAGE \* MERGEFORMAT 11 Modification of glycyrrhetinic acid derivatives NCTD liposomal targeting in the liver of mice [Abstract] Objective To study the glycyrrhetinic acid derivatives (glycyrrhetinic acid stearyl ester-3-O-galactoside, Gal-GAOSt cantharidin modified to a liposome (Gal-GAOStNC-LP) in mice Distribution of liver targeting. Methods prepared by film dispersion of glycyrrhetinic acid derivatives modified norcantharidin liposomal, after tail vein injection, using a HPLC assay to cantharidin in the mouse liver and kidney concentration over time, and to a solution of cantharidin were compared, and targeting index TI = (AUCNC-SOL / (AUCGal-GAOStNC-LP to determine the Gal-GAOStNC-LP targeting the major organs. Results Gal-GAOStNC-LP set in the liver tissue was significantly higher than that of NC-SOL group, the liver targeting index greater than 1, while the kidney targeting index of less than 1. Conclusions of glycyrrhetinic acid derivatives to a modification of cantharidin liver targeting liposome, can improve drug efficacy, reduced side effects. [Keywords:] glycyrrhetinic acid, to a cantharidin, liposomes, targeted, tissue distribution Abstract: Objective To study the distribution and liver targeting of glycyrrhetinic acid derivatives (stearin glycyrrhetinic acid ester-3-O-galactosidase, Gal-GAOSt) modifying norcantharidin liposomes (Gal-GAOStNC-LP) in rats. Methods Making use of film decentralization to prepare glycyrrhetinic acid derivatives modifying norcantharidin liposomes, and then injecting it to the tail vein of rats. Making use of HPLC to detect the change of norcantharidin concentration in the rats’ liver and kidney over time and compared it with norcantharidin solution group and targeting index TI = (AUC) NC-SOL / (AUC) Gal-GAOStNC-LP to determine the targeting of Gal-GAOStNC-LP to the main organs. Results Organization concentration of Gal-GAOStNC-LP group in the liver was significantly higher than NC- SOL group, the liver targeting