Pharmaceutical Research 1987-08-01

N-Mannich-base prodrugs of 5-iodo-2'-deoxycytidine as topical delivery enhancers.

S A Koch, K B Sloan

文献索引：Pharm. Res. 4(4) , 317-20, (1987)

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摘要

Two Mannich-base prodrugs of 5-iodo-2'-deoxycytidine (5-IDC) have been synthesized. The prodrugs exhibit increased lipid solubility compared to 5-IDC and rapidly revert to 5-IDC in buffer. One of the prodrugs delivered about twice as much 5-IDC from isopropyl myristate (IPM) through hairless mouse skin in diffusion-cell experiments as did 5-IDC from IPM. Subsequent applications of theophylline/propylene glycol onto the diffusion cells to determine the effect of prodrug/IPM, 5-IDC/IPM, or IPM on the resistance of the skins to subsequent applications showed that the prodrug/IPM had no more effect than IPM itself.