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Polymeric prodrug of gemfibrozil

Gemfibrozil (5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid, Gem), a known lipid regulating agent, was bond to poly[a,b-(N-2-hydroxyethyl)-DL-aspartamide] (PHEA) in order to prepare hydrophilic polymeric prodrug. Gemfibrozil (1) was first chemically modified to 2-aminoethyl amide 4 which was allowed to react with poly(2,5)-dioxo-1,3-pyrolidinediyl) (PSI, 5) in the molar ratio of 4 and succinimide units 1:3. The aminolysis was completed with 2-aminoethanol to give water soluble PHEA-Gem conjugate (6) with drug load of 12 %. The conjugate 6 contained gemfibrozil covalently bond by amide link, through nontoxic ethylenediamine spacer. schema

gemfibrozil; polymeric prodrug; poly[a;b-(N-2-hydroxyethyl)-DL-aspartamide] (PHEA)

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