title: Ordered mesoporous silica material SBA-15: a broad-spectrum formulation platform for poorly soluble drugs.
abstract: Encapsulating poorly soluble drugs in mesoporous silicates is an emerging strategy to improve drug dissolution. This study evaluates the applicability of the ordered mesoporous silicate SBA-15 as an excipient to enhance dissolution, for a test series of 10 poorly soluble compounds with a high degree of physicochemical diversity (carbamazepine, cinnarizine, danazol, diazepam, fenofibrate, griseofulvin, indomethacin, ketoconazole, nifedipine, and phenylbutazone). A generic solvent impregnation method was used to load all model compounds. The target drug content was 20%. The physical nature of the formulations was investigated using differential scanning calorimetry (DSC) and the pharmaceutical performance evaluated by means of in vitro dissolution. Aliquots of each formulation were stored at 25 degrees C/52% RH for 6 months, and again subjected to DSC and in vitro dissolution. The target drug content of 20% was attained in all cases. DSC data evidenced the noncrystalline state of the confined drugs. All SBA-15 formulations exhibited an enhanced dissolution as compared to their corresponding crystalline materials, and the high pharmaceutical performance of all formulations was retained during the 6 months storage period. The results of this study suggest that encapsulation in SBA-15 can be applied as a dissolution-enhancing formulation approach for a very wide variety of poorly soluble drugs.
authors.affiliation: Laboratory for Pharmacotechnology and Biopharmacy, K.U. Leuven, Belgium.
authors.forename: Michiel
authors.initials: M
authors.lastname: Van Speybroeck
authors.forename: Valéry
authors.initials: V
authors.lastname: Barillaro
authors.forename: Thao Do
authors.initials: TD
authors.lastname: Thi
authors.forename: Randy
authors.initials: R
authors.lastname: Mellaerts
authors.forename: Johan
authors.initials: J
authors.lastname: Martens
authors.forename: Jan
authors.initials: J
authors.lastname: Van Humbeeck
authors.forename: Jan
authors.initials: J
authors.lastname: Vermant
authors.forename: Pieter
authors.initials: P
authors.lastname: Annaert
authors.forename: Guy
authors.initials: G
authors.lastname: Van den Mooter
authors.forename: Patrick
authors.initials: P
authors.lastname: Augustijns
mesh_terms: D002626:Chemistry, Pharmaceutical; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000378:metabolism; D016062:Porosity; D012822:Silicon Dioxide / Q000737:chemistry* / Q000378:metabolism*; D012995:Solubility
chemical_list: D004364:Pharmaceutical Preparations; C509969:SBA-15; D012822:Silicon Dioxide