Hybrid Nanomaterials that Mimic the Food Effect: Controlling Enzymatic Digestion for Enhanced Oral Drug Absorption

Tan, Angel; Martin, Amanda L.; Nguyen, Tri‐Hung; Boyd, Ben J.; Prestidge, Clive A.

doi:10.1002/ange.201200409

Cited by 18 publications

(26 citation statements)

References 31 publications

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“…When aerosil or ludox are tested in presence of fat globules and a surfactant (lecithin), the silica particles locate at the interface between water and fat, coating the fat globule. This type of behavior produces a much faster and more complete hydrolysis of fats than in model systems in which the nanomaterial is not present [ 17 ]. The same authors also verified that the size of the particles, their topology, the material to fat ratio and the surface charge are factors that modify the surface properties and therefore the ability of the lipase to access the substrate and vary the hydrolysis rate [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

Use of Silica Based Materials as Modulators of the Lipase Catalyzed Hydrolysis of Fats under Simulated Duodenal Conditions

et al. 2020

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The effect of silica materials and their functionalization in the lipase catalyzed fat hydrolysis has been scarcely studied. Fifteen silica materials were prepared and their effect on the fat hydrolysis was measured, under simulated duodenal conditions, using the pH-stat method. The materials are composed of the combination of three supports (Stöber massive silica nanoparticles, Stöber mesoporous nanoparticles and UVM-7) and four surface functionalizations (methyl, trimethyl, propyl and octyl). In addition, the non-functionalized materials were tested. The functional groups were selected to offer a hydrophobic character to the material improving the interaction with the fat globules and the lipase. The materials are able to modulate the lipase activity and their effect depending on the support topology and the organic covering, being able to increase or reduce the fat hydrolysis. Depending of the material, relative fat hydrolysis rates of 75 to 140% in comparison with absence of the material were obtained. The results were analyzed by Partial Least Square Regression and suggest that the alkyl modified mesopores are able to improve the fat hydrolysis, by contrast the non-porous nanoparticles and the textural pores tend to induce inhibition. The effects are more pronounced for materials containing long alkyl chains and/or in absence of taurodeoxycholate.

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Section: Introductionmentioning

confidence: 99%

Use of Silica Based Materials as Modulators of the Lipase Catalyzed Hydrolysis of Fats under Simulated Duodenal Conditions

et al. 2020

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“…However, oil/water microemulsion was applied in the morphology control, not suitable for scalable synthesis. Spray drying, on the other hand, is a facile method for the synthesis of multi-shelled metal oxides (Zhou et al, 2013) and the assembly of colloidal silica nanoparticles into microspheres (Tan et al, 2012). When Ludox silica templates, resorcinol and formaldehyde as carbon precursors were used via the spray drying method, silica/polymer microspheres and subsequently mesoporous carbon microspheres were synthesized (Li et al, 2014), with a surface area below 1,200 m 2 g −1 .…”

Section: Introductionmentioning

confidence: 99%

Nitrogen-Doped Mesoporous Carbon Microspheres by Spray Drying-Vapor Deposition for High-Performance Supercapacitor

et al. 2020

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“…Silica-lipid hybrid (SLH) microparticles are a kind of solid system based on silica particles and oil-in-water emulsion, which were reported for the first time by Simovic et al ( 21 ) and Tan et al ( 22 ). The researches show that the SLH microparticles significantly improve the solubility and stability of the water-insoluble drugs, and also enhance the oral absorption of drugs in experimental animals by simulating food effects ( 21 - 23 ). In another study ( 24 ), researchers found that the ibuprofen in SLH microparticles prepared by spray drying has higher solubility than the control group during a two-step dissolution and its bioavailability increased nearly 1.95-fold compared to the commercial tablets in clinical trials.…”

Section: Introductionmentioning

confidence: 99%

Silica-Lipid Hybrid Microparticles as Efficient Vehicles for Enhanced Stability and Bioaccessibility of Curcumin

Wang

et al. 2019

Food technol. biotechnol. (Online)

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SUMMARYCurcumin is an active ingredient with multiple functions, but its application is often restricted due to its poor water solubility, weak stability, and consequently low bioaccessibility. Based on this, the aim of this work is to develop a new vehicle to overcome these restrictions. Here we developed a curcumin-loaded nanoemulsion and then curcumin-loaded silica-lipid hybrid microparticles through emulsification and vacuum drying, respectively. The loading of curcumin in the nanoemulsion and microparticles was (0.30±0.02) and (0.67±0.02) %, respectively. FTIR and XRD analyses of microparticles revealed that curcumin was encapsulated in porous, amorphous silica. In vitro antioxidant activities showed that the encapsulation would not affect the antioxidant activity of curcumin. In vitro simulated digestion indicated that nanoemulsion and microparticles had higher curcumin bioaccessibility than the control group. The storage stability of microparticles remained the same during 6 weeks in the dark at 4, 25 and 40 °C. Moreover, the microparticles had a better chemical stability than nanoemulsion under the light. The cell viability was over 80% when the concentration of nanocarriers was less than 45 μg/mL. Hence, the microparticles could be a promising means to load curcumin and improve its solubility, light stability and bioaccessibility.

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Hybrid Nanomaterials that Mimic the Food Effect: Controlling Enzymatic Digestion for Enhanced Oral Drug Absorption

Cited by 18 publications

References 31 publications

Use of Silica Based Materials as Modulators of the Lipase Catalyzed Hydrolysis of Fats under Simulated Duodenal Conditions

Use of Silica Based Materials as Modulators of the Lipase Catalyzed Hydrolysis of Fats under Simulated Duodenal Conditions

Nitrogen-Doped Mesoporous Carbon Microspheres by Spray Drying-Vapor Deposition for High-Performance Supercapacitor

Silica-Lipid Hybrid Microparticles as Efficient Vehicles for Enhanced Stability and Bioaccessibility of Curcumin

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