Abstract
The 3-alkylcarbonyloxymethyl-5-fluorouracil (3-ACOM-5-FU) prodrugs have been characterized by their solubilities in isopropyl myristate (SIPM) and partition coefficients between IPM and pH 4.0 buffer (KIPM:AQ). Estimated SAQ values have been obtained from SAQ=SIPM/KIPM:AQ. The abilities of the prodrugs to deliver total 5-FU species from IPM suspensions through hairless mouse skin (Ji) have been evaluated in diffusion cell experiments. All of the prodrugs were much more soluble in IPM than 5-FU, and the propionyloxymethyl (C2) member of the series was almost twice as soluble in pH 4.0 buffer. Except for the acetyloxymethyl (C1) member of the series, the 3-ACOM-5-FU prodrugs exhibited greater SIPM and SAQ values than the corresponding 1-alkylcarbonyloxymethyl (1-ACOM-5-FU) prodrugs. The 3-ACOM-5-FU prodrugs that exhibited greater SIPM and SAQ values than the 1-ACOM-5-FU prodrugs also exhibited greater Ji values, except for the C2 member. The C2 member also gave the largest error in predicting Ji using the transformed Potts-Guy equation. All of the 3-ACOM-5-FU prodrugs delivered more 5-FU as a percentage of Ji than the 1-ACOM-5-FU prodrugs but were not more effective as a series at targeting dermal as opposed to transdermal delivery.
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