prikaz prve stranice dokumenta Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer
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Scientific paper - Preliminary note / Short communication
Makromolekulski prolijekovi. XIII. Vodotopljivi konjugati 17β-estradiola i estradiol-17β-valerata s poliaspartamidnim polimerom
Acta Pharmaceutica, 61 (2011), 4; 465-472. https://doi.org/10.2478/v10007-011-0039-x
Zovko Končić, Marijana; Zorc, Branka; Novak, Predrag

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Zovko Končić, M., Zorc, B. & Novak, P. (2011). Makromolekulski prolijekovi. XIII. Vodotopljivi konjugati 17β-estradiola i estradiol-17β-valerata s poliaspartamidnim polimerom. Acta Pharmaceutica, 61. (4), 465-472. doi: 10.2478/v10007-011-0039-x

Zovko Končić, Marijana, et al. "Makromolekulski prolijekovi. XIII. Vodotopljivi konjugati 17β-estradiola i estradiol-17β-valerata s poliaspartamidnim polimerom." Acta Pharmaceutica, vol. 61, no. 4, 2011, pp. 465-472. https://doi.org/10.2478/v10007-011-0039-x

Zovko Končić, Marijana, Branka Zorc and Predrag Novak. "Makromolekulski prolijekovi. XIII. Vodotopljivi konjugati 17β-estradiola i estradiol-17β-valerata s poliaspartamidnim polimerom." Acta Pharmaceutica 61, no. 4 (2011): 465-472. https://doi.org/10.2478/v10007-011-0039-x

Zovko Končić, M., Zorc, B. and Novak, P. (2011) 'Makromolekulski prolijekovi. XIII. Vodotopljivi konjugati 17β-estradiola i estradiol-17β-valerata s poliaspartamidnim polimerom', Acta Pharmaceutica, 61(4), pp. 465-472. doi: 10.2478/v10007-011-0039-x

Zovko Končić M, Zorc B, Novak P. Makromolekulski prolijekovi. XIII. Vodotopljivi konjugati 17β-estradiola i estradiol-17β-valerata s poliaspartamidnim polimerom. Acta Pharmaceutica [Internet]. 2011 December 31 [cited 2024 December 23];61(4):465-472. doi: 10.2478/v10007-011-0039-x

M. Zovko Končić, B. Zorc and P. Novak, "Makromolekulski prolijekovi. XIII. Vodotopljivi konjugati 17β-estradiola i estradiol-17β-valerata s poliaspartamidnim polimerom", Acta Pharmaceutica, vol. 61, no. 4, pp. 465-472, December 2011. [Online]. Available at: https://urn.nsk.hr/urn:nbn:hr:163:867852. [Accessed: 23 December 2024]

Metadata
Title (croatian)Makromolekulski prolijekovi. XIII. Vodotopljivi konjugati 17β-estradiola i estradiol-17β-valerata s poliaspartamidnim polimerom
Title (english)Macromolecular prodrugs. XIII. Hydrosoluble conjugates of 17β-estradiol and estradiol-17β-valerate with polyaspartamide polymer
AuthorMarijana Zovko Končić
AuthorBranka Zorc
AuthorPredrag Novak
Author's institutionUniversity of Zagreb
Faculty of Pharmacy and Biochemistry
(Department of medicinal chemistry)
Author's institutionUniversity of Zagreb
Faculty of Pharmacy and Biochemistry
(Department of pharmacology)
Scientific / art field,
discipline and subdiscipline		BIOMEDICINE AND HEALTHCARE
Pharmacy
Pharmacy
Abstract (croatian)
U radu je opisana priprava i karakterizacija dvaju vodotopljivih polimer-lijek konjugata 17β-estradiola (ED) i estradiol-17β-valerata (EV) s poliaspartamidnim polimerom. ED i EV su prvo kemijski modificirani i vezani na poli,-(N-2-hidroksietil-DL-aspartamid)-poli,-(N-2-aminoetil-DL-aspartamid) (PAHA), vodotopljivi poliaspartamidni kopolimer s hidroksi i amino skupinama. ED je prvo preveden u 17-hemisukcinat (EDS), a zatim vezan na PAHA. U nastalom konjugatu PAHA-EDS estradiolska komponenta vezana je na polimer preko 2-aminoetilhemisukcinatne razmaknice. S druge strane, EV je prvo preveden u estradiol-17-valerat-3-(benzotriazol-1-karboksilat), koji reagira s amino skupinama u PAHA dajući polimer-lijek konjugat PAHA-EV. U tom je konjugatu estradiolska komponenta kovalentno vezana na poliaspartamidnu okosnicu karbamatnom vezom, preko etilenediaminske razmaknice. Polimer-lijek konjugati estradiola dizajnirani su i pripravljeni sa ciljem da se poveća topljivost i bioraspoloživost te isporuka tog lipofilnog estrogenog hormona.
Abstract (english)
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.
Keywords (croatian)
Keywords (english)
Languageenglish
Publication typeScientific paper - Preliminary note / Short communication
Publication statusPublished
Peer reviewPeer review
Publication versionPublished version
Journal titleActa Pharmaceutica
Numberingvol. 61, no. 4, pp. 465-472
p-ISSN1330-0075
e-ISSN1846-9558
DOIhttps://doi.org/10.2478/v10007-011-0039-x
URN:NBNurn:nbn:hr:163:867852
Publication2011-12-31
Document URLhttp://hrcak.srce.hr/71385
Type of resourceText
Access conditionsOpen access
Terms of useLicence In copyright icon
Created on2017-06-14 15:34:12