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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 ; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
PREDRAG NOVAK ; University of Zagreb, Faculty of Science, Department of Chemistry, Zagreb, Croatia

Puni tekst: engleski, pdf (81 KB) str. 465-472 preuzimanja: 330* citiraj
APA 6th Edition
ZOVKO KONČIĆ, M., ZORC, B. i NOVAK, P. (2011). Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer. Acta Pharmaceutica, 61 (4), 465-472. https://doi.org/10.2478/v10007-011-0039-x
MLA 8th Edition
ZOVKO KONČIĆ, MARIJANA, et al. "Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer." Acta Pharmaceutica, vol. 61, br. 4, 2011, str. 465-472. https://doi.org/10.2478/v10007-011-0039-x. Citirano 22.09.2019.
Chicago 17th Edition
ZOVKO KONČIĆ, MARIJANA, BRANKA ZORC i PREDRAG NOVAK. "Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer." Acta Pharmaceutica 61, br. 4 (2011): 465-472. https://doi.org/10.2478/v10007-011-0039-x
Harvard
ZOVKO KONČIĆ, M., ZORC, B., i NOVAK, P. (2011). 'Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer', Acta Pharmaceutica, 61(4), str. 465-472. https://doi.org/10.2478/v10007-011-0039-x
Vancouver
ZOVKO KONČIĆ M, ZORC B, NOVAK P. Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer. Acta Pharm. [Internet]. 2011 [pristupljeno 22.09.2019.];61(4):465-472. https://doi.org/10.2478/v10007-011-0039-x
IEEE
M. ZOVKO KONČIĆ, B. ZORC i P. NOVAK, "Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer", Acta Pharmaceutica, vol.61, br. 4, str. 465-472, 2011. [Online]. https://doi.org/10.2478/v10007-011-0039-x

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
https://hrcak.srce.hr/71385

[hrvatski]

Posjeta: 527 *