HU Hai-yan1��2��LIN Yun-zhu1��GONG Tao1��ZHANG Zhi-rong1
1.Key Lab of Drug Targeting of Miuistry of Eduction��Sichuan University��Chengdu 610041��China�� 2.School of Pharmaceutical Sciences��Sun Yat-sen University��Guangzhou 510080��China
Abstract��
OBJECTIVE To study in vivo distribution of penciclovir-loaded microemulsion (PCV-ME) after I.v. administration and to estimate its targeting performance. METHODS Penciclovir solution,penciclovir micelle and PCV-ME (25 mg��kg-1) were administrated by caudal vein to mice. Penciclovir concentration in tissue and plasma was determined by HPLC method. Overall targeting efficiency (TE),targeting Index (TI) and relative overall targeting efficiency (RTE) of drug in tissue including brain were calculated by AUC0��9 h .RESULTS 0��9 h after I.v. administration,PCV-ME showed higher AUCs in plasma,brain,heart,liver,spleen and muscle than that of penciclovir solution and micelle,but similar AUC in kidney and lower AUC in lung.The higher concentrations,with two peaks (tmax 0.33 and 1.0 h),were observed in the concentration-time curve of PCV-ME in brain,compared with the administration of micelle and solution. As a result,high TI and RTE of brain were obtained by 1.65 and 0.369 and PCV-ME showed a quick and short-life brain accumulation after I.v. administration.CONCLUSION The results indicate that penciclovir-loaded microemulsion can alter the penciclovir in vivo distribution in mice and have the tendency of brain targeting in vivo.
2007, Vol. 42 
