Physical state of poorly water soluble therapeutic molecules loaded into SBA-15 ordered mesoporous silica carriers : a case study with itraconazole and ibuprofen

The ordered mesoporous silica material SBA-15 was loaded with the model drugs itraconazole and ibuprofen using three different procedures: (i) adsorption from solution, (ii) incipient wetness impregnation, and (iii) heating of a mixture of drug and SBA-15 powder. The location of the drug molecules i...

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Veröffentlicht in:Langmuir : the ACS journal of surfaces and colloids. - 1992. - 24(2008), 16 vom: 19. Aug., Seite 8651-9
1. Verfasser: Mellaerts, Randy (VerfasserIn)
Weitere Verfasser: Jammaer, Jasper A G, Van Speybroeck, Michiel, Chen, Hong, Van Humbeeck, Jan, Augustijns, Patrick, Van den Mooter, Guy, Martens, Johan A
Format: Online-Aufsatz
Sprache:English
Veröffentlicht: 2008
Zugriff auf das übergeordnete Werk:Langmuir : the ACS journal of surfaces and colloids
Schlagworte:Journal Article SBA-15 Water 059QF0KO0R Itraconazole 304NUG5GF4 Silicon Dioxide 7631-86-9 Ibuprofen WK2XYI10QM
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245 1 0 |a Physical state of poorly water soluble therapeutic molecules loaded into SBA-15 ordered mesoporous silica carriers  |b a case study with itraconazole and ibuprofen 
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520 |a The ordered mesoporous silica material SBA-15 was loaded with the model drugs itraconazole and ibuprofen using three different procedures: (i) adsorption from solution, (ii) incipient wetness impregnation, and (iii) heating of a mixture of drug and SBA-15 powder. The location of the drug molecules in the SBA-15 particles and molecular interactions were investigated using nitrogen adsorption, TGA, DSC, DRS UV-vis, and XPS. The in vitro release of hydrophobic model drugs was evaluated in an aqueous environment simulating gastric fluid. The effectiveness of the loading method was found to be strongly compound dependent. Incipient wetness impregnation using a concentrated itraconazole solution in dichloromethane followed by solvent evaporation was most efficient for dispersing itraconazole in SBA-15. The itraconazole molecules were located on the mesopore walls and inside micropores of the mesopore walls. When SBA-15 was loaded by slurrying it in a diluted itraconazole solution from which the solvent was evaporated, the itraconazole molecules ended up in the mesopores that they plugged locally. At a loading of 30 wt %, itraconazole exhibited intermolecular interactions inside the mesopores revealed by UV spectroscopy and endothermic events traced with DSC. The physical mixing of itraconazole and SBA-15 powder followed by heating above the itraconazole melting temperature resulted in formulations in which glassy itraconazole particles were deposited externally on the SBA-15 particles. Loading with ibuprofen was successful with each of the three loading procedures. Ibuprofen preferably is positioned inside the micropores. In vitro release experiments showed fast release kinetics provided the drug molecules were evenly deposited over the mesoporous surface 
650 4 |a Journal Article 
650 7 |a SBA-15  |2 NLM 
650 7 |a Water  |2 NLM 
650 7 |a 059QF0KO0R  |2 NLM 
650 7 |a Itraconazole  |2 NLM 
650 7 |a 304NUG5GF4  |2 NLM 
650 7 |a Silicon Dioxide  |2 NLM 
650 7 |a 7631-86-9  |2 NLM 
650 7 |a Ibuprofen  |2 NLM 
650 7 |a WK2XYI10QM  |2 NLM 
700 1 |a Jammaer, Jasper A G  |e verfasserin  |4 aut 
700 1 |a Van Speybroeck, Michiel  |e verfasserin  |4 aut 
700 1 |a Chen, Hong  |e verfasserin  |4 aut 
700 1 |a Van Humbeeck, Jan  |e verfasserin  |4 aut 
700 1 |a Augustijns, Patrick  |e verfasserin  |4 aut 
700 1 |a Van den Mooter, Guy  |e verfasserin  |4 aut 
700 1 |a Martens, Johan A  |e verfasserin  |4 aut 
773 0 8 |i Enthalten in  |t Langmuir : the ACS journal of surfaces and colloids  |d 1992  |g 24(2008), 16 vom: 19. Aug., Seite 8651-9  |w (DE-627)NLM098181009  |x 1520-5827  |7 nnns 
773 1 8 |g volume:24  |g year:2008  |g number:16  |g day:19  |g month:08  |g pages:8651-9 
856 4 0 |u http://dx.doi.org/10.1021/la801161g  |3 Volltext 
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