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

Autori
Barbarić, Monika ; Kralj, Marijeta ; Marjanović, Marko ; Husnjak, Ivana ; Pavelić, Krešimir ; Filipović-Grčić, Jelena ; Zorc, Davor ; Zorc, Branka

Izvornik
European Journal of Medicinal Chemistry (0223-5234) 42 (2007), 1; 20-29

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
diclofenac; fenoprofen; polyaspartamide; thiomer; polymer-drug conjugate; human tumor cell lines; antiproliferative effect

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija

POVEZANOST RADA