Enhanced release of itraconazole from ordered mesoporous SBA-15 silica materials

Mellaerts, Randy; Aerts, C.; Humbeeck, Jan Van; Augustijns, Patrick; Mooter, Guy Van den; Martens, Johan A.

doi:10.1039/b616746b

Cited by 207 publications

(141 citation statements)

References 17 publications

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“…Finally, the synthesized products were washed with demineralized water three times, dried, and calcined at 600°C with a heating rate of 1°C/min for 6 hours in a muffle furnace to obtain SBA15 powder. 27 Preparation of sF solution SF solution was prepared as previously described. 28,29 Briefly, Bombyx mori silkworm cocoons were cut into small pieces and boiled for 30 minutes in a solution of 0.5 wt% Na 2 CO 3 .…”

Section: Synergy Of Ic and Bmp2mentioning

confidence: 99%

Evaluation of synergistic osteogenesis between icariin and BMP2 through a micro/meso hierarchical porous delivery system

Wang¹,

Cao²,

Liu³

et al. 2017

IJN

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BMP2 is well known as an outstanding growth factor for inducing new bone formation. However, improvements are still required to use BMP2 effectively and expand its clinical application due to the potential side effects at high doses. In this study, icariin (IC), a type of traditional Chinese medicine, was originally proposed to be a cooperative factor for BMP2. An alkaline phosphatase (ALP) activity assay showed that IC promoted BMP2 osteogenesis in a concentration-dependent manner with significant enhancement at 38.4 µM versus that for BMP2 at 0.8 µg/mL. Furthermore, we developed a composite hierarchical porous scaffold (SF/SBA15; composed of micropores of silk fibroin [SF] scaffold and mesopores of SBA15) for the controlled delivery of BMP2 and IC. This composite scaffold was investigated by a series of physical characterizations and displayed good in vitro cell biocompatibility. In addition, the composite scaffold also showed the degradation rate of 12% dry weight loss and a slight change in the microstructures within 10 days. Moreover, BMP2 and IC were loaded into the SF and SBA15 structures, respectively, of the SF/SBA15 scaffold. This protein/drug loading system (SF BMP2 /SBA15 IC ) provided delivery of BMP2 with an initial burst release of 60.9%±0.9% in the first 24 hours and a gradual release over the subsequent 6 days to 97.9%±0.8%, whereas IC exhibited a burst release of 64.2%±0.7% in the first 24 hours, followed by a sustained release to 92.4%±0.8% over 10 days. With the prolonged local retention and interaction duration of BMP2 and IC, the SF BMP2 /SBA15 IC scaffold provided better osteogenic differentiation than other groups with different loading modes of BMP2 or IC, as determined by ALP staining and quantitation and Alizarin red staining. Finally, the results of quantitative real-time polymerase chain reaction analysis indicated that the SF BMP2 /SBA15 IC scaffold induced a significantly higher increase in the RUNX2, ALP, COL I , and OCN expression levels of cocultured bone marrow mesenchymal stem cells than other payload composite scaffolds. This study suggests that a micro/meso hierarchical porous delivery system of BMP2 and IC ensures osteogenic synergy and demonstrates promise for bone tissue engineering.

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Section: Synergy Of Ic and Bmp2mentioning

confidence: 99%

Evaluation of synergistic osteogenesis between icariin and BMP2 through a micro/meso hierarchical porous delivery system

Wang¹,

Cao²,

Liu³

et al. 2017

IJN

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“…This type of regulation is common for drug release from functionalized mesoporous silicates, which will be presented in the last paragraph. Although there are many studies of mesoporous silicates as drug-delivery systems, there are still many open questions associated with the drug release mechanisms either from non-functionalized (26) or functionalized frameworks (27,28). In the literature there are only a few studies of the actual physical state of drugs confined in mesoscopic dimensions, which are mostly limited to very specific examples (26,29), whereas general knowledge about the physical form of the drug incorporated into mesopores and about the mechanism of drug release and its relation to structural properties of the mesoporous framework are still missing.…”

Section: Controlled Drug Release From Ordered Mesoporous Matricesmentioning

confidence: 99%

“…Although there are many studies of mesoporous silicates as drug-delivery systems, there are still many open questions associated with the drug release mechanisms either from non-functionalized (26) or functionalized frameworks (27,28). In the literature there are only a few studies of the actual physical state of drugs confined in mesoscopic dimensions, which are mostly limited to very specific examples (26,29), whereas general knowledge about the physical form of the drug incorporated into mesopores and about the mechanism of drug release and its relation to structural properties of the mesoporous framework are still missing. One can even find examples where the release studies of structurally very similar molecules from equivalent mesoporous carriers lead to equal drug-release profiles, which are explained by entirely different or even opposing mechanisms (11,26).…”

Section: Controlled Drug Release From Ordered Mesoporous Matricesmentioning

confidence: 99%

“…In the literature there are only a few studies of the actual physical state of drugs confined in mesoscopic dimensions, which are mostly limited to very specific examples (26,29), whereas general knowledge about the physical form of the drug incorporated into mesopores and about the mechanism of drug release and its relation to structural properties of the mesoporous framework are still missing. One can even find examples where the release studies of structurally very similar molecules from equivalent mesoporous carriers lead to equal drug-release profiles, which are explained by entirely different or even opposing mechanisms (11,26). The model most commonly used to describe the kinetics of drug release is the Korsmeyer-Peppas (power law) model (30), which is successfully fitted to experimental results but does not give any information about the underlying mechanism of drug release.…”

Section: Controlled Drug Release From Ordered Mesoporous Matricesmentioning

confidence: 99%

“…As mentioned before, the release of the drug is usually controlled by diffusion and so the release profile can be easily modified by changing the material properties such as, for example, pore diameter (23,25,43). In the case of hydrophobic and poorly water soluble itraconazole, the authors found that the release of the drug from the ordered mesoporous SBA-15 silica matrix was enhanced compared to the dissolution of crystalline itraconazole itself (26). They synthesized four different SBA-15 silicates with pore diameters ranging from 4.5 to 9.0 nm and pore volume varying from 0.42 to 0.80 cm 3 g -1 .…”

Section: Non-functionalized Sba-15 Matrixmentioning

confidence: 99%

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Ordered mesoporous silicates as matrices for controlled release of drugs

Ukmar

Planinšek

2010

Acta Pharmaceutica

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According to the International Union of Pure and Applied Chemistry (IUPAC), porous materials are classified into three categories: microporous with pore diameters less than 2 nm, mesoporous having pore diameters between 2 and 50 nm, and macroporous with pore sizes larger than 50 nm. Highly ordered mesoporous silicates such as MCM (Mobil Composition of Matter No. 41, 48,...) and SBA (Santa Barbara Amorphous material No. 1, 3, 15,...) have been long recognized as very promising materials with a rich variety of possible applications (1). The various types of MCM and SBA silicates can be distinguished by the number after the acronym. The three most important MCM materials are: MCM-41 (hexagonal), MCM-48 (cubic) and MCM-50 (lamellar). Also a wide variety of SBA materials has been prepared, such as SBA-1 (cubic), SBA-11 (cubic), SBA-12 (3D hexagonal network), SBA-14 (lamellar), SBA-15 (2D hexagonal) and SBA-16 (cubic cage-structured). They show ordered arrangements of channels and cavities of different geometry confined between walls built up from SiO 2 units. Among all numerous applications of mesoporous materials, ranging from separation technology, catalysis, hydrogen Interest in and thereby also development of ordered mesoporous silicates as drug delivery devices have grown immensely over the past few years. On hand selected cases from the literature, the power of such systems as delivery devices has been established. Specifically, it is shown how it is possible to enhance the release kinetics of poorly soluble drugs by embedding them in mesoporous silicates. Further critical factors governing the structure and release of the model drug itraconazole incorporated in an SBA-15 matrix are briefly reviewed. The possibility of functionalizing the surface of mesoporous matrices also under harsher conditions offers a broad platform for the design of stimuli-responsive drug release, including pH responsive systems and systems which respond to the presence of specific ions, reducing agents, magnetic field or UV light, whose efficiency and biocompatibility has been established in vitro.

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Preclinical and Clinical Studies

Brewster¹,

Verreck²,

Bevernage³

et al. 2015

Pharmaceutical Sciences Encyclopedia

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Contemporary drug pipelines are increasingly populated with difficult‐to‐formulate drug substances. Amorphous solid dispersions can increase drug dissolution rate by reducing the effective drug particle size through its dispersion in the matrix. Based on the theorized way of working of amorphous solid dispersions, one of the most important design elements is their ability to dissolve and supersaturate. This is initially assessed in vitro through the use of dissolution protocols especially set up for that purpose. A number of in vivo assessments of the potential utility of amorphous solid dispersions have been completed using various animal models. Clinical assessments to investigate itraconazole supersaturation (indirectly) have also been completed. Itraconazole is a widely studied compound in this context with numerous in vitro , in vivo , and clinical evaluations completed. Useful preclinical and clinical models for assessing solid dispersion fitness will contribute to the drug development process.

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Enhanced release of itraconazole from ordered mesoporous SBA-15 silica materials

Abstract: This in vitro study reports on the enhanced release of the hydrophobic drug itraconazole from the ordered mesoporous SBA-15 silica material and on the existence of a critical mesopore diameter for enhancing release.

Cited by 207 publications

References 17 publications

Evaluation of synergistic osteogenesis between icariin and BMP2 through a micro/meso hierarchical porous delivery system

Evaluation of synergistic osteogenesis between icariin and BMP2 through a micro/meso hierarchical porous delivery system

Ordered mesoporous silicates as matrices for controlled release of drugs

Preclinical and Clinical Studies

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