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Statements

Subject Item
n2:RIV%2F61989592%3A15310%2F12%3A33141479%21RIV13-MSM-15310___
rdf:type
n13:Vysledek skos:Concept
dcterms:description
The pharmaceutical use of some 3-hydroxyquinolinone derivatives with high cytotoxic and cytostatic activities (under in vitro conditions) as well as potential immunosuppressive properties is seriously limited by their low solubility in water accompanied by instability in oxidative environment, like physiological fluids. In an attempt to improve the bioavailability and the stability of four of these derivatives, we propose here two different approaches: complexation with beta-cyclodextrin derivatives and incorporation of these substances inside antioxidant micelles. The comparison of the two different methods is the focus of this work, as well as the investigation of some physicochemical properties of the micellar aqueous dispersions. Antioxidant micellar dispersions appear to be suitable for increasing the apparent solubility and stability for all the compounds studied, most probably because of the antioxidant activity of the specific surfactant used, combined with the low amount of water present in the center of the micelles. On this regard, 1H NMR and UV-vis spectroscopy result as efficient tools to verify that the drug molecules are indeed placed in the core of the micelles. Moreover, freeze-drying provides a very easy and powerful technique to obtain solid formulations starting from micellar dispersions. On the contrary, cyclodextrins could potentially be used as solubilizing agents, but the drawback connected to degradation in aqueous media could not be overcome with this type of solubilizer. The pharmaceutical use of some 3-hydroxyquinolinone derivatives with high cytotoxic and cytostatic activities (under in vitro conditions) as well as potential immunosuppressive properties is seriously limited by their low solubility in water accompanied by instability in oxidative environment, like physiological fluids. In an attempt to improve the bioavailability and the stability of four of these derivatives, we propose here two different approaches: complexation with beta-cyclodextrin derivatives and incorporation of these substances inside antioxidant micelles. The comparison of the two different methods is the focus of this work, as well as the investigation of some physicochemical properties of the micellar aqueous dispersions. Antioxidant micellar dispersions appear to be suitable for increasing the apparent solubility and stability for all the compounds studied, most probably because of the antioxidant activity of the specific surfactant used, combined with the low amount of water present in the center of the micelles. On this regard, 1H NMR and UV-vis spectroscopy result as efficient tools to verify that the drug molecules are indeed placed in the core of the micelles. Moreover, freeze-drying provides a very easy and powerful technique to obtain solid formulations starting from micellar dispersions. On the contrary, cyclodextrins could potentially be used as solubilizing agents, but the drawback connected to degradation in aqueous media could not be overcome with this type of solubilizer.
dcterms:title
Overcoming instability and low solubility of new cytostatic compounds: A comparsion of two approaches Overcoming instability and low solubility of new cytostatic compounds: A comparsion of two approaches
skos:prefLabel
Overcoming instability and low solubility of new cytostatic compounds: A comparsion of two approaches Overcoming instability and low solubility of new cytostatic compounds: A comparsion of two approaches
skos:notation
RIV/61989592:15310/12:33141479!RIV13-MSM-15310___
n13:predkladatel
n20:orjk%3A15310
n3:aktivita
n11:Z
n3:aktivity
Z(MSM6198959216)
n3:cisloPeriodika
3
n3:dodaniDat
n5:2013
n3:domaciTvurceVysledku
n17:6013449 n17:5110386
n3:druhVysledku
n15:J
n3:duvernostUdaju
n7:S
n3:entitaPredkladatele
n18:predkladatel
n3:idSjednocenehoVysledku
157381
n3:idVysledku
RIV/61989592:15310/12:33141479
n3:jazykVysledku
n14:eng
n3:klicovaSlova
TPGS micelles, Cyclodextrins, Quinolinone derivatives, Solubilization
n3:klicoveSlovo
n8:TPGS%20micelles n8:Quinolinone%20derivatives n8:Cyclodextrins n8:Solubilization
n3:kodStatuVydavatele
NL - Nizozemsko
n3:kontrolniKodProRIV
[E18DF3B74D9E]
n3:nazevZdroje
European Journal of Pharmaceutics and Biopharmaceutics
n3:obor
n19:FR
n3:pocetDomacichTvurcuVysledku
2
n3:pocetTvurcuVysledku
6
n3:rokUplatneniVysledku
n5:2012
n3:svazekPeriodika
80
n3:tvurceVysledku
Cagno, M. Hlaváč, Jan Stein, P. C. Brauer-Brandl, A. Skalko-Basnet, N. Stýskala, Jakub
n3:wos
000302930200022
n3:zamer
n12:MSM6198959216
s:issn
0939-6411
s:numberOfPages
6
n16:doi
10.1016/j.ejpb.2011.11.016
n9:organizacniJednotka
15310