Anticancer drug delivery systems: multi-loaded N4-acyl poly(ethylene glycol) prodrugs of ara-C. II. Efficacy in ascites and solid tumors. |
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| Authors: | Yun H Choe Charles D Conover Dechun Wu Maksim Royzen Yoany Gervacio Virna Borowski Mary Mehlig Richard B Greenwald |
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| Affiliation: | Enzon, Inc., 20 Kingsbridge Road, Piscataway, NJ 08854-3969, USA. |
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| Abstract: | The synthesis of branched PEG (40,000) acids has been achieved using aspartic acid (Asp) and AspAsp dendrons. Complete conjugation of these dendritic acids with cytosine arabinoside (ara-C) was achieved by the use of spacers that allowed a greater separation of the branches to accommodate several large ara-C molecules in proximity to each other. The tetrameric and octameric PEG-ara-C amide prodrugs were much more effective in the treatment of solid and ascites tumors compared to the native drug. The greater loading of the PEG backbone appears to have achieved a minimum threshold concentration for the therapeutic delivery of ara-C. |
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