Anticancer drug delivery systems: multi-loaded N4-acyl poly(ethylene glycol) prodrugs of ara-C.II. Efficacy in ascites and solid tumors
| Autor: | Yun H. Choe, Dechun Wu, Yoany Gervacio, Charles D. Conover, Maksim Royzen, Virna Borowski, Richard B. Greenwald, Mary Mehlig |
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| Rok vydání: | 2002 |
| Předmět: |
Antimetabolites
Antineoplastic Stereochemistry Mice Nude Pharmaceutical Science macromolecular substances Chemical synthesis Dosage form Polyethylene Glycols Mice chemistry.chemical_compound Drug Delivery Systems In vivo Amide Aspartic acid PEG ratio Tumor Cells Cultured Animals Humans Prodrugs Carcinoma Ehrlich Tumor Leukemia P388 Chemistry Cytarabine food and beverages biochemical phenomena metabolism and nutrition Prodrug Xenograft Model Antitumor Assays carbohydrates (lipids) Solvents Female Drug Screening Assays Antitumor Drug carrier |
| Zdroj: | Journal of Controlled Release. 79:55-70 |
| ISSN: | 0168-3659 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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