1. Synthesis and in vitro antitumor effect of diclofenac and fenoprofen thiolated and nonthiolated polyaspartamide-drug conjugates
- Author
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Barbarić, M., Kralj, M., Marjanović, M., Husnjak, I., Pavelić, K., Filipović-Grčić, J., Zorc, D., and Zorc, B.
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POLYMERS , *DICLOFENAC , *ANTINEOPLASTIC agents , *ANTI-inflammatory agents , *CANCER cells , *MACROMOLECULES , *DRUGS , *CELL culture - Abstract
Abstract: This paper reports the synthesis and antiproliferative effects of new thiomer–diclofenac and fenoprofen conjugates, hydrophilic, bioadhesive, polymeric prodrugs, as well as antiproliferative effects of diclofenac, fenoprofen and a series of previously described polymer–fenoprofen conjugates on five tumor cell lines. Thiolated and nonthiolated polyaspartamides were the chosen polymeric components. Drug-loading ranged from 5.6 to 22.4%, and the amount of SH groups ranged from 6.9 to 45.6μmolg−1. Tensile studies demonstrated a clear correlation between the amount of thiol and the mucoadhesive properties of the conjugates. The growth-inhibitory activity of the tested polymer–drug conjugates demonstrates that polyaspartamide-type polymers, especially thiolated polymers, enable inhibition of tumor cell growth with significantly lower doses of the active substance. [Copyright &y& Elsevier]
- Published
- 2007
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