Silica-Lipid Hybrid (SLH) Versus Non-lipid Formulations for Optimising the Dose-Dependent Oral Absorption of Celecoxib

Tan, Angel; Davey, Andrew K.; Prestidge, Clive A.

doi:10.1007/s11095-011-0458-x

Cited by 45 publications

(30 citation statements)

References 34 publications

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“…Celecoxib (pK a = 11.1, log P = 3.5) has poor water solubility and is almost insoluble in gastrointestinal fluid (pH range of 1-7) [2]. To enhance the dissolution and solubility of celecoxib, different formulation strategies, such as silica-lipid hybrid microcapsules [3,4], self-microemulsifying drug delivery systems [5,6], and nanoparticles [7,8], have been reported.…”

Section: Introductionmentioning

confidence: 99%

Fabrication and evaluation of celecoxib microparticle surface modified by hydrophilic cellulose and surfactant

Noh

et al. 2015

International Journal of Biological Macromolecules

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Section: Introductionmentioning

confidence: 99%

Fabrication and evaluation of celecoxib microparticle surface modified by hydrophilic cellulose and surfactant

Noh

et al. 2015

International Journal of Biological Macromolecules

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“…and thus required three first order rate constants to precisely describe the data 22. Digestion kinetics were enhanced in SLH microparticles compared to a submicron emulsion due to the increased surface area of lipid and the hydrophilic silica matrix facilitating the interfacial activation of lipase.…”

mentioning

confidence: 99%

Bioactive Hybrid Particles from Poly(d,l-lactide-co-glycolide) Nanoparticle Stabilized Lipid Droplets

Joyce

Whitby

Prestidge

2015

ACS Appl. Mater. Interfaces

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Biodegradable and bioactive hybrid particles composed of poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles and medium-chain triglycerides were prepared by spray drying lipid-in-water emulsions stabilized by PLGA nanoparticles, to form PLGA-lipid hybrid (PLH) microparticles approximately 5 μm in mean diameter. The nanoparticle stabilizer was varied and mannitol was also incorporated during the preparation to investigate the effect of stabilizer charge and cryoprotectant content on the particle microstructure. An in vitro lipolysis model was used to demonstrate the particles' bioactivity by manipulating the digestion kinetics of encapsulated lipid by pancreatic lipase in simulated gastrointestinal fluid. Lipid digestion kinetics were enhanced in PLH and PLGA-lipid-mannitol hybrid (PLMH) microparticles for both stabilizers, compared to a coarse emulsion, in biorelevant media. An optimal digestion rate was observed for the negatively charged PLMH system, evidenced by a 2-fold increase in the pseudo-first-order rate constant compared to a coarse emulsion. Improved microparticle redispersion, probed by dual dye confocal fluorescence microscopy, increased the available surface area of lipid for lipase adsorption, enhancing digestion kinetics. Thereby, lipase action was controlled in hybrid microparticles by altering the surface charge and carbohydrate content. Our results demonstrate that bioactive microparticles composed of versatile and biodegradable polymeric particles and oil droplets have great potential for use in smart food and nutrient delivery, as well as safer and more efficacious oral delivery of drugs and drug combinations.

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“…It is also a weak acid with pKa ≈ 11. 18 Celecoxib selectively inhibits the cyclooxygenase-2 enzyme. Cyclooxygenase (COX) is an enzyme that is responsible for converting arachidonic acid to the prostanoids that result in pain and inflammation.…”

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confidence: 99%

Improvement of solubility of celecoxib by inclusion in MCM-41 mesoporous silica: drug loading and release

Günaydin¹,

Yılmaz²

2015

Turk J Chem

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Abstract:Celecoxib is a poorly water-soluble nonsteroidal anti-inflammatory drug. Here we report four ordered mesoporous silica MCM-41 supports with different particle size, pore volume, and surface properties to investigate their loading capacity with celecoxib and their release abilities. Spherical MCM-41 mesoporous supports less than 50 nm in diameter were prepared and to compare the effect of the template removal process on morphology of samples, acid extraction and calcination methods were used. Moreover, nearly 500 nm sized rod-shaped MCM-41 mesoporous silica was obtained by changing the template concentration in preparation. Boron doping was performed to determine the effect of a heteroatom on the surface of mesoporous silica and adsorbance of drug molecules and release. In order to investigate the effect of polarity of solvent during drug loading, two different solvents were used: ethanol as polar solvent and hexane as nonpolar solvent. All bare and drug-loaded samples' physicochemical characterizations were performed.The release experiments were conducted in phosphate buffer solution of pH 7.4 at 37• C. Celecoxib solubility was highly improved compared to the pure drug. The morphology and surface property differences of MCM-41 and the solvent effect in adsorption of celecoxib have been discussed, including its delivery.

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Silica-Lipid Hybrid (SLH) Versus Non-lipid Formulations for Optimising the Dose-Dependent Oral Absorption of Celecoxib

Abstract: Collectively, the results highlight the potential of the SLH microparticles in enhancing the bioavailability of CEL in a dose-linear manner as facilitated by supersaturated solubilisation of CEL in the intestinal milieu.

Cited by 45 publications

References 34 publications

Fabrication and evaluation of celecoxib microparticle surface modified by hydrophilic cellulose and surfactant

Fabrication and evaluation of celecoxib microparticle surface modified by hydrophilic cellulose and surfactant

Bioactive Hybrid Particles from Poly(d,l-lactide-co-glycolide) Nanoparticle Stabilized Lipid Droplets

Improvement of solubility of celecoxib by inclusion in MCM-41 mesoporous silica: drug loading and release

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