Acta Pharmaceutica, Vol. 61 No. 4, 2011.
Kratko priopćenje
https://doi.org/10.2478/v10007-011-0039-x
Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer
MARIJANA ZOVKO KONČIĆ
; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
BRANKA ZORC
orcid.org/0000-0003-4355-8816
; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
PREDRAG NOVAK
; University of Zagreb, Faculty of Science, Department of Chemistry, Zagreb, Croatia
Sažetak
Two hydrosoluble conjugates of 17β-estradiol (ED) and estradiol-17β-valerate (EV) with polyaspartamide polymer were prepared and characterized. ED and EV were first chemically modified and bound to poly,-(N-2-hydroxyethyl-DL-aspartamide)-poly,-(N-2-aminoethyl-DL-aspartamide) (PAHA), a hydrosoluble polyaspartamide-type copolymer bearing both hydroxyl and amino groups. ED was first converted to 17-hemisuccinate (EDS) and then bound to PAHA. In the resulting conjugate PAHA-EDS, the estradiol moiety was linked to the polymer through a 2-aminoethylhemisuccinamide spacer. On the other hand, EV was first converted to estradiol-17-valerate-3-(benzotriazole-1-carboxylate), which readily reacted with amino groups in PAHA affording the polymer-drug conjugate PAHA-EV. In the prepared conjugate PAHA-EV, the estradiol moiety was covalently bound to the polyaspartamide backbone by carbamate linkage, through an ethylenediamine spacer. The polymer-drug conjugates were designed and prepared with the aim to increase water-solubility, bioavailability and to improve drug delivery of the lipophilic estrogen hormone.
Ključne riječi
estradiol; polyaspartamide; poly,-(N-2-hydroxyethyl-DL-aspartamide)-poly,-(N-2-aminoethyl-DL-aspartamide); polymer-drug conjugate
Hrčak ID:
71385
URI
Datum izdavanja:
31.12.2011.
Posjeta: 1.625 *