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Statements

Subject Item
n2:RIV%2F00216275%3A25310%2F11%3A39892210%21RIV12-GA0-25310___
rdf:type
n14:Vysledek skos:Concept
dcterms:description
The acylation of prednisolone 20-hydrazone with star poly(ethylene glycol) tetracarboxylic acid (M = 20,000) has been used to prepare the corresponding pH-sensitive conjugate. With alpha-cyclodextrin, this conjugate forms a polypseudorotaxane, which was characterised by means of (1)H NMR spectra, powder X-ray diffraction patterns and STM microscopy. The rate of acid-catalysed hydrolysis of the conjugate was studied under in vitro conditions in model media of hydrochloric acid solutions, phosphate and acetate buffers (pH 2-5.8). The acid-catalysed hydrolysis (at pH 2) of the polypseudorotaxane was ca 3.5 times slower than that of the original conjugate. After 1 h in this medium, 86% of the covalently attached prednisolone remained unchanged. The prepared polypseudorotaxane represents a promising peroral transport system of prednisolone with a pH-sensitive linker with delayed acid-catalysed hydrolysis thanks to protection at the molecular level using alpha-cyclodextrin. The acylation of prednisolone 20-hydrazone with star poly(ethylene glycol) tetracarboxylic acid (M = 20,000) has been used to prepare the corresponding pH-sensitive conjugate. With alpha-cyclodextrin, this conjugate forms a polypseudorotaxane, which was characterised by means of (1)H NMR spectra, powder X-ray diffraction patterns and STM microscopy. The rate of acid-catalysed hydrolysis of the conjugate was studied under in vitro conditions in model media of hydrochloric acid solutions, phosphate and acetate buffers (pH 2-5.8). The acid-catalysed hydrolysis (at pH 2) of the polypseudorotaxane was ca 3.5 times slower than that of the original conjugate. After 1 h in this medium, 86% of the covalently attached prednisolone remained unchanged. The prepared polypseudorotaxane represents a promising peroral transport system of prednisolone with a pH-sensitive linker with delayed acid-catalysed hydrolysis thanks to protection at the molecular level using alpha-cyclodextrin.
dcterms:title
Prednisolone-alpha-cyclodextrin-star poly(ethylene glycol) polypseudorotaxane with delayed pH-sensitivity as a targeted drug delivery system Prednisolone-alpha-cyclodextrin-star poly(ethylene glycol) polypseudorotaxane with delayed pH-sensitivity as a targeted drug delivery system
skos:prefLabel
Prednisolone-alpha-cyclodextrin-star poly(ethylene glycol) polypseudorotaxane with delayed pH-sensitivity as a targeted drug delivery system Prednisolone-alpha-cyclodextrin-star poly(ethylene glycol) polypseudorotaxane with delayed pH-sensitivity as a targeted drug delivery system
skos:notation
RIV/00216275:25310/11:39892210!RIV12-GA0-25310___
n14:predkladatel
n15:orjk%3A25310
n3:aktivita
n13:P n13:Z
n3:aktivity
P(GAP106/11/0058), Z(MSM0021627501)
n3:cisloPeriodika
1-2
n3:dodaniDat
n5:2012
n3:domaciTvurceVysledku
n11:4978684 n11:7138512 n11:3603024 n11:8605270 n11:5655730 n11:6796834
n3:druhVysledku
n8:J
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n9:predkladatel
n3:idSjednocenehoVysledku
222832
n3:idVysledku
RIV/00216275:25310/11:39892210
n3:jazykVysledku
n21:eng
n3:klicovaSlova
Prednisolone; Polypseudorotaxane; PEG; Pro-drugs; pH-sensitivity
n3:klicoveSlovo
n16:Pro-drugs n16:pH-sensitivity n16:PEG n16:Polypseudorotaxane n16:Prednisolone
n3:kodStatuVydavatele
NL - Nizozemsko
n3:kontrolniKodProRIV
[1A83CB8C74A3]
n3:nazevZdroje
International Journal of Pharmaceutics
n3:obor
n20:FR
n3:pocetDomacichTvurcuVysledku
6
n3:pocetTvurcuVysledku
6
n3:projekt
n4:GAP106%2F11%2F0058
n3:rokUplatneniVysledku
n5:2011
n3:svazekPeriodika
414
n3:tvurceVysledku
Knotek, Petr Bílková, Eliška Imramovský, Aleš Beneš, Ludvík Sedlák, Miloš Chárová, Petra
n3:wos
000292795500006
n3:zamer
n18:MSM0021627501
s:issn
0378-5173
s:numberOfPages
6
n12:doi
10.1016/j.ijpharm.2011.04.060
n19:organizacniJednotka
25310