Potential of amorphous microporous silica for ibuprofen controlled release

Amorphous microporous silica (AMS) xerogel materials were synthesized in an acid-catalyzed sol–gel process. The porosity of AMS was adapted by varying sol–gel synthesis parameters including the molar hydrolysis ratio ( r-value), HCl:Si molar ratio, the type of silicon alkoxide source and the solvent...

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Bibliographic Details
Published in:	International journal of pharmaceutics Vol. 397; no. 1; pp. 84 - 91
Main Authors:	Aerts, C.A., Verraedt, E., Depla, A., Follens, L., Froyen, L., Van Humbeeck, J., Augustijns, P., Van den Mooter, G., Mellaerts, R., Martens, J.A.
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier B.V 15-09-2010 Elsevier
Subjects:	Biological and medical sciences Chemical Phenomena Controlled release Delayed-Action Preparations Drug Carriers - chemistry Drug Delivery Systems Drug Stability Gels General pharmacology Ibuprofen Ibuprofen - administration & dosage Ibuprofen - chemistry Medical sciences Micropore diffusion Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Porosity Silica Silicon Dioxide - chemistry Solubility Sol–gel Micropore diffusion Sol–gel Silica Controlled release Ibuprofen Prostaglandin-endoperoxide synthase Pharmaceutical technology Enzyme Controlled release form Control release polymer Sol-gel Enzyme inhibitor Non steroidal antiinflammatory agent Colloidal gel Microporosity Dosage form Arylpropionic acid derivatives Oxidoreductases Diffusion
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Summary:	Amorphous microporous silica (AMS) xerogel materials were synthesized in an acid-catalyzed sol–gel process. The porosity of AMS was adapted by varying sol–gel synthesis parameters including the molar hydrolysis ratio ( r-value), HCl:Si molar ratio, the type of silicon alkoxide source and the solvent. AMS particles of millimeter size were loaded with ibuprofen, by heat treatment and melt impregnation. In vitro release experiments were performed in simulated gastric and intestinal fluid. The release kinetics were critically depending on the AMS particle size distribution and the micropore diameter. The release was interpreted as configurational diffusion in the AMS micropores. The stability of unloaded and ibuprofen loaded AMS material upon storage was investigated using nitrogen physisorption, DSC analysis and in vitro release experiments. Ibuprofen loaded AMS formulations show remarkable stability, which can be attributed to the presence of ibuprofen molecules in the channels, functioning as scaffolds to support the pore structure.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0378-5173 1873-3476
DOI:	10.1016/j.ijpharm.2010.06.053