Synthesis and in vitro antitumor effect of diclofenac and fenoprofen thiolated and nonthiolated polyaspartamide-drug conjugates (CROSBI ID 128951)
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Podaci o odgovornosti
Barbarić, Monika ; Kralj, Marijeta ; Marjanović, Marko ; Husnjak, Ivana ; Pavelić, Krešimir ; Filipović-Grčić, Jelena ; Zorc, Davor ; Zorc, Branka
engleski
Synthesis and in vitro antitumor effect of diclofenac and fenoprofen thiolated and nonthiolated polyaspartamide-drug conjugates
The paper reports the synthesis and the antiproliferative effect of new thiomer-diclofenac and fenoprofen conjugates, hydrophilic, bioadhesive, polymeric prodrugs, as well as antiproliferative effect of diclofenac, fenoprofen and a series of previously described polymer-fenoprofen conjugates on five tumor cell lines. Thiolated and nonthiolated polyaspartamides were chosen as polymeric components. The drug loading ranged from 5.6 to 22.4%, and amount of SH groups from 6.9 to 45.6 mu mol g-1. Tensile studies demonstrated a clear correlation between the thiol amount and mucoadhesive properties of the conjugates. The growth inhibitory activity of the tested polymer-drug conjugates clearly demonstrates that polyaspartamide-type polymers, especially thiolated polymers, enable the inhibition of tumor cells' growth with significantly lower doses of the active substance.
diclofenac; fenoprofen; polyaspartamide; thiomer; polymer-drug conjugate; human tumor cell lines; antiproliferative effect
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Podaci o izdanju
Povezanost rada
Kemija, Temeljne medicinske znanosti, Farmacija