Synthesis and in vitro antitumor effect of diclofenac and fenoprofen thiolated and nonthiolated polyaspartamide-drug conjugates

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 45.6 μmol g−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.

Graphical abstractThis paper reports the synthesis, characterization and in vitro antitumor effect of a series of diclofenac and fenoprofen polymer–drug conjugates. The results demonstrate that polyaspartamide-type polymers, especially thiolated polymers, enable the inhibition of tumor cell growth with significantly lower doses of the active substance.Figure optionsDownload full-size imageDownload as PowerPoint slide