In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs

Bukara, Katarina; Schueller, Laurent; Rosier, Jan; Daems, Tinne; Verheyden, Loes; Eelen, Siemon; Martens, Johan A.; Mooter, Guy Van den; Bugarski, Branko; Kiekens, Filip

doi:10.1016/j.xphs.2016.05.019

Cited by 22 publications

(17 citation statements)

References 15 publications

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“…FNB is virtually insoluble in water and physiological fluids. 28 We utilized the mesoporous structure of MSn to increase the dissolution rate of FNB, and through in vitro drug release and in vivo pharmacokinetic study we verified that MSn was suitable as a carrier for the oral administration of poorly soluble drugs.…”

Section: Introductionmentioning

confidence: 85%

Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate

Bai

et al. 2018

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BackgroundBiopharmaceutics classification system class II drugs have low solubility, which limits their extent and speed of absorption after oral administration. Over the years, mesoporous materials have been widely used to increase the dissolution rate and oral relative bioavailability of poorly water-soluble drugs.ObjectivesIn order to improve the dissolution rate and increase oral relative bioavailability of the poorly water-soluble drugs, a tin oxide carrier (MSn) with a mesoporous structure was successfully synthesized.MethodsIn this study, MSn was synthesized using mesoporous silica material (SBA-15) as the template. Fenofibrate (FNB) was adsorbed into the channels of MSn by an adsorption method. Characterizations of the pure FNB, MSn, physical mixture of the drug and MSn (PM; 1:1) and FNB-loaded MSn (FNB-MSn) samples were carried out by the scanning electron microscopy (SEM), transmission electron microscopy (TEM), N2 adsorption/desorption, powder X-ray diffractometer (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) spectroscopy. Cytotoxicity assay (MTT) was used to evaluate the cytotoxicity of MSn. In vitro dissolution studies were performed to investigate the dissolution rate of FNB-MSn. In vivo pharmacokinetic studies were used to investigate the changes of plasma drug concentrations of FNB-MSn tablets and commercial FNB tablets in rabbits.ResultsDetailed characterization showed that FNB in the channels of MSn was present in an amorphous state. The in vitro release tests demonstrated that MSn with a good biocompatibility could effectively enhance the dissolution rate of FNB. Pharmacokinetic results indicated that MSn significantly increased the oral relative bioavailability of FNB.ConclusionMSn can be regarded as a promising carrier for an oral drug delivery system.

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Section: Introductionmentioning

confidence: 85%

Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate

Bai

et al. 2018

DDDT

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“…A study wherein the potential of ordered mesoporous silica nanoparticles (OMS) in enhancing the bioavailability of fenofibrate in man was conducted by Bukara and collaborators which can be considered as another breakthrough step acting as a trigger in evoking interest among the researchers for the use of MSNs for biomedical applications. Promising results obtained by them in their preclinical studies [ 274 ] prompted them to complement those results with clinical studies. Fenofibrate was loaded into OMS and these were subsequently enclosed within capsules.…”

Section: Biodistribution and Biocompatibility Of Msnsmentioning

confidence: 99%

Mesoporous Silica Nanoparticles: A Comprehensive Review on Synthesis and Recent Advances

et al. 2018

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Recent advancements in drug delivery technologies utilizing a variety of carriers have resulted in a path-breaking revolution in the approach towards diagnosis and therapy alike in the current times. Need for materials with high thermal, chemical and mechanical properties have led to the development of mesoporous silica nanoparticles (MSNs). These ordered porous materials have garnered immense attention as drug carriers owing to their distinctive features over the others. They can be synthesized using a relatively simple process, thus making it cost effective. Moreover, by controlling the parameters during the synthesis; the morphology, pore size and volume and particle size can be transformed accordingly. Over the last few years, a rapid increase in research on MSNs as drug carriers for the treatment of various diseases has been observed indicating its potential benefits in drug delivery. Their widespread application for the loading of small molecules as well as macromolecules such as proteins, siRNA and so forth, has made it a versatile carrier. In the recent times, researchers have sorted to several modifications in the framework of MSNs to explore its potential in drug resistant chemotherapy, antimicrobial therapy. In this review, we have discussed the synthesis of these multitalented nanoparticles and the factors influencing the size and morphology of this wonder carrier. The second part of this review emphasizes on the applications and the advances made in the MSNs to broaden the spectrum of its use especially in the field of biomedicine. We have also touched upon the lacunae in the thorough understanding of its interaction with a biological system which poses a major hurdle in the passage of this carrier to the clinical level. In the final part of this review, we have discussed some of the major patents filed in the field of MSNs for therapeutic purpose.

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“…In particular, MCM-41 exhibits a hexagonal structure, with the pore width ranging between~1.5 and 10 nm, depending on the synthesis parameters [9][10][11][12]. MCM-41 has been shown to be able to stabilize drugs in the amorphous form without recrystallization for a significantly long period of time [13,14]. It has been widely studied as a carrier for drug delivery applications, either as synthesized [15][16][17], or following post-synthetic modification [18][19][20][21].…”

Section: Introductionmentioning

confidence: 99%

3D-Printed Mesoporous Carrier System for Delivery of Poorly Soluble Drugs

et al. 2021

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Fused deposition modelling (FDM) is the most extensively employed 3D-printing technique used in pharmaceutical applications, and offers fast and facile formulation development of personalized dosage forms. In the present study, mesoporous materials were incorporated into a thermoplastic filament produced via hot-melt extrusion and used to produce oral dosage forms via FDM. Mesoporous materials are known to be highly effective for the amorphization and stabilization of poorly soluble drugs, and were therefore studied in order to determine their ability to enhance the drug-release properties in 3D-printed tablets. Celecoxib was selected as the model poorly soluble drug, and was loaded into mesoporous silica (MCM-41) or mesoporous magnesium carbonate. In vitro drug release tests showed that the printed tablets produced up to 3.6 and 1.5 times higher drug concentrations, and up to 4.4 and 1.9 times higher release percentages, compared to the crystalline drug or the corresponding plain drug-loaded mesoporous materials, respectively. This novel approach utilizing drug-loaded mesoporous materials in a printed tablet via FDM shows great promise in achieving personalized oral dosage forms for poorly soluble drugs.

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In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs

Cited by 22 publications

References 15 publications

Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate

Development of a tin oxide carrier with mesoporous structure for improving the dissolution rate and oral relative bioavailability of fenofibrate

Mesoporous Silica Nanoparticles: A Comprehensive Review on Synthesis and Recent Advances

3D-Printed Mesoporous Carrier System for Delivery of Poorly Soluble Drugs

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