Nanostructuring Biomaterials with Specific Activities towards Digestive Enzymes for Controlled Gastrointestinal Absorption of Lipophilic Bioactive Molecules

Joyce, Paul; Whitby, Catherine P.; Prestidge, Clive A.

doi:10.1016/j.cis.2016.10.003

Cited by 37 publications

(27 citation statements)

References 226 publications

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“…Since then, the interest of emulsion as carrier or delivery systems for nutrients, lipophilic bioactive compounds or drugs is booming (Velikov and Pelan, 2008;Raynal-Ljutovac et al, 2011;Yao et al, 2014;Livney, 2015;Mao and Miao, 2015;Norton et al, 2015;Singh et al, 2015;Joyce et al, 2016;Zhang et al, 2016). Some schematic structures of these delivery structures are presented in Figure 3.…”

Section: Supramolecular Structure Of Dietary Lipidsmentioning

confidence: 99%

“…We have already mentioned that the interface composition influences lipase absorption and lipid digestibility. Two main mechanisms were involved: (i) alteration of the colloidal stability of the lipid droplets in the stomach and intestine impacts the rate and extent of droplet coalescence or destabilization, (ii) alteration of gastric and pancreatic lipase affinity for the substrate and thereby, the rate of enzyme adsorption to the lipid surface (Joyce et al, 2016). Double emulsions have found great application in the encapsulation of hydrophilic and hydrophobic compounds, respectively, in the internal and external droplets or encapsulation of compounds with unpleasant taste or flavor.…”

Section: Supramolecular Structure Of Dietary Lipidsmentioning

confidence: 99%

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Molecular and structural organization of lipids in foods: their fate during digestion and impact in nutrition

Meynier

Génot

2017

OCL

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-Lipids are basic constituents of our diet. They play an active part in the acceptability, flavour and perception of our foods. At the same time, they are also regarded as beneficial for health or as sources to various pathologies. Until now, the nutritional impact of the various dietary lipid structures beyond the amounts of ingested lipids and selected fatty acids has been marginally taken into account in nutritional studies and thus in food application. This review gathers first our current knowledge on the diversity of molecular and supramolecular structures of dietary lipids, and then based on the scientific studies carried out on the human model, tempts to sum up the current knowledge and the latest hypotheses concerning the metabolic and nutritional effects of these multiscale structures. It is shown that the perception of lipids in the mouth during oral processing modulates the production of digestive fluids and food intake. Then, during the stomach and intestine phases of lipid digestion, the kinetics of release of the fatty acids are modulated by the multiscale structures of lipids influencing the fatty acid bioaccessibility and rate of absorption. In turn this may impair the postabsorption metabolism and nutritional effects. Future trends of research are evoked as concluding remarks.Keywords: dietary lipids / molecular and supramolecular structures / absorption / digestion / nutrition Résumé -Structures moléculaires et supramoléculaires des lipides dans les aliments : leur devenir au cours de la digestion et impact potentiel en nutrition. Les lipides prennent une part active dans l'acceptabilité et la perception de nos aliments, mais sont perçus à la fois comme vecteurs de tous les maux et sources de bienfaits. Au-delà de la quantité de lipides et d'acides gras ingérés, l'impact de leurs structures au sein des aliments reste encore mal appréhendé dans les études nutritionnelles. Cette revue, basée sur les travaux réalisés sur le modèle humain, fait le point des connaissances actuelles et des dernières hypothèses concernant les effets métaboliques et nutritionnels liés à la structuration aux échelles moléculaires et supramoléculaires des lipides alimentaires. Il apparaît que la perception des lipides commence dès la mise en bouche de l'aliment et module la prise alimentaire. Puis lors des phases stomacales et intestinales de la digestion, les nutriments lipidiques absorbables sont libérés des structures avec des cinétiques différentes, déterminant leur bioaccessibilité et influant leur vitesse d'absorption. Ces différences pourraient impacter le métabolisme post absorption et les effets nutritionnels. Des pistes de recherches possibles sont évoquées en perspectives.

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Section: Supramolecular Structure Of Dietary Lipidsmentioning

confidence: 99%

Section: Supramolecular Structure Of Dietary Lipidsmentioning

confidence: 99%

Molecular and structural organization of lipids in foods: their fate during digestion and impact in nutrition

Meynier

Génot

2017

OCL

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“…It can be supposed that the lipase activity can be altered by formulation of lipids using PIs with varying physicochemical properties because PIs can influence on the lipid-water interface, hence, affecting interfacial activation mechanism of lipase [132][133][134]. For this reason, PIs can manipulate GI lipolysis via interactions between PIs and lipids, lipases, and lipid digested products.…”

Section: Effects Of Lipid-pi Interactions On Lipid Digestionmentioning

confidence: 99%

“…These lipid digestion products can be adsorbed onto the interface of lipid-water via their surface-active by amphiphilic nature, leading to a reduction in lipid bioaccessibility and digestion kinetics [145][146][147]. Recently, it was reported that variation of molecular or surface charge of some excipients can control the rate and extent of lipolysis product partitioning toward the aqueous phase through electrostatic and agglomeration interactions [133]. These interactions can facilitate expulsion of fatty acids into the aqueous phase and thus reduced the interference of digestion products at the lipid-water interface [148].…”

Section: Interactions Between Pis and Digested Productsmentioning

confidence: 99%

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Park

Kim

2020

Pharmaceutics

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Self-emulsifying drug delivery systems (SEDDSs) are a vital strategy to enhance the bioavailability (BA) of formulations of poorly water-soluble compounds. However, these formulations have certain limitations, including in vivo drug precipitation, poor in vitro in vivo correlation due to a lack of predictive in vitro tests, issues in handling of liquid formulation, and physico-chemical instability of drug and/or vehicle components. To overcome these limitations, which restrict the potential usage of such systems, the supersaturable SEDDSs (su-SEDDSs) have gained attention based on the fact that the inclusion of precipitation inhibitors (PIs) within SEDDSs helps maintain drug supersaturation after dispersion and digestion in the gastrointestinal tract. This improves the BA of drugs and reduces the variability of exposure. In addition, the formulation of solid su-SEDDSs has helped to overcome disadvantages of liquid or capsule dosage form. This review article discusses, in detail, the current status of su-SEDDSs that overcome the limitations of conventional SEDDSs. It discusses the definition and range of su-SEDDSs, the principle mechanisms underlying precipitation inhibition and enhanced in vivo absorption, drug application cases, biorelevance in vitro digestion models, and the development of liquid su-SEDDSs to solid dosage forms. This review also describes the effects of various physiological factors and the potential interactions between PIs and lipid, lipase or lipid digested products on the in vivo performance of su-SEDDSs. In particular, several considerations relating to the properties of PIs are discussed from various perspectives.Pharmaceutics 2020, 12, 365 2 of 57 intraluminal supersaturation and the biorelevance of supersaturation assays will be addressed. Finally, we will make suggestions for the successful development of su-SEDDs.There are many review articles that give useful information about the nature and application of supersaturable drug delivery systems or conventional SEDDSs. However, these reviews cover only a limited range of su-SEDDSs. Therefore, this review, which includes the current status of technology focused only on su-SEDDSs, is a valuable addition to the previous review literature because no review article currently covers such a wide range of su-SEDDSs. Conventional Solubilized SEDDSsThere has been a steady increase in the number of new drug candidates (almost 40%) that are highly hydrophobic and poorly water-soluble. The oral bioavailability of poorly water-soluble drugs is hindered by low solubility and slow dissolution in the aqueous environment of the GIT. Thus, it is a great challenge for pharmaceutical scientists to overcome the inherent slow dissolution and poor oral absorption of hydrophobic drugs [1][2][3][4]. SEDDSs have emerged as a promising approach to improving the biopharmaceutical performance of hydrophobic drugs by enhancing their bioavailability [5,6].An SEDDS is a pre-concentrate composed of a drug, oils, surfactants, and sometimes co-solvents and/or co-surfactan...

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“…The ability to develop lipid‐based delivery vehicles that control lipase activity has received considerable interest in recent years . However, the mechanism of lipase action is a complex process, by which a protective α‐helical loop covers the catalytic domains when in its inactive conformation, but opens upon interaction with an interface, exposing the active site to the bulk aqueous phase .…”

Section: Introductionmentioning

confidence: 99%

Modulating the Lipase‐Mediated Bioactivity of Particle‐Lipid Conjugates Through Changes in Nanostructure and Surface Chemistry

Joyce

Dening

Gustafsson

et al. 2017

Euro J Lipid Sci & Tech

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The lipase‐mediated hydrolysis of triglycerides can be controlled by confining lipid droplets within highly porous nanostructured particle matrices. Novel hybrid materials with varying bioactivities toward lipase have been developed by spray drying particle‐stabilized emulsions to form highly organized three‐dimensional architectures. In this study, the particle size, nanostructure, and surface chemistry of hybrid particles are tailored to systematically investigate the influence of material characteristics on lipase activity. This is achieved by varying (i) the spray drying process and (ii) the structure and composition of particulate colloids employed to stabilize the precursor emulsions. In all cases, the colloidal self‐assembly of particles and droplets into nanostructured conjugates during the water removal process facilitated enhanced lipase activity compared to submicron triglyceride emulsions, with lipolysis kinetics increasing in the following order: polymer‐lipid hybrid (PLH) < silica‐lipid hybrid (SLH) ≤ clay‐lipid hybrid (CLH). Lipase activity increased as a function of increasing interfacial surface area of the lipid substrate and increasing hydrophilicity of the solid matrix support. The novel insights into the role of hybrid particle nanostructure and surface chemistry on the mechanism of lipase action can be harnessed for the intelligent design of new and improved lipid‐based drug delivery vehicles and functional foods. Practical Applications: Understanding and controlling the interaction between triglyceride molecules and pancreatic lipase is of fundamental importance for the rational design of new functional foods and drug formulations. Lipid digestion in the body facilitates the delivery of fat and encapsulated bioactive compounds from the gastrointestinal tract (GIT) to the blood and surrounding tissues. Hence, the bioavailability of poorly soluble compounds can be controlled by engineering lipid‐based systems that regulate lipase activity. In this study, three novel solid‐state systems have been designed that finely control the catalytic activity of lipase, and therefore, demonstrate high commercial potential within the pharmaceutical and biotechnology industries. The lipase‐mediated hydrolysis of triglycerides is controlled by designing novel solid‐state particle‐lipid conjugates with unique nanostructures and surface chemistries. The hybrid materials are prepared by spray‐drying particle‐stabilized lipid droplets, which induced the forced agglomeration of particles and droplets into micron‐sized particles with distinctive three‐dimensional architectures. The ability to modulate lipase activity through material design presented novel insights into the mechanism of digestive enzyme action, which is of fundamental importance for the rational design of new functional foods and drug formulations.

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Nanostructuring Biomaterials with Specific Activities towards Digestive Enzymes for Controlled Gastrointestinal Absorption of Lipophilic Bioactive Molecules

Cited by 37 publications

References 226 publications

Molecular and structural organization of lipids in foods: their fate during digestion and impact in nutrition

Molecular and structural organization of lipids in foods: their fate during digestion and impact in nutrition

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Modulating the Lipase‐Mediated Bioactivity of Particle‐Lipid Conjugates Through Changes in Nanostructure and Surface Chemistry

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