Variations in gastrointestinal lipases, pH and bile acid levels with food intake, age and diseases: Possible impact on oral lipid-based drug delivery systems

Amara, Sawsan; Bourlieu-Lacanal, Claire; Humbert, Lydie; Rainteau, Dominique; Carrière, Frédéric

doi:10.1016/j.addr.2019.03.005

Cited by 53 publications

(34 citation statements)

References 150 publications

(256 reference statements)

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“…The effects of food administration on drug absorption have been studied widely [20]. The presence of food and/or its digested products in the GIT causes slower gastric emptying, changes of GI pH, changes of GI fluid viscosity, and increased secretion of bile from the intestine that facilitates the emulsification and digestion of su-SEDDSs.…”

Section: Effect Of Food On Supersaturationmentioning

confidence: 99%

“…In a more fundamental aspect, both conventional SEDDSs and su-SEDDSs could be prone to interactions with food due to their composition and/or structure. For the conventional SEDDSs without PI, the various probabilities of the interaction between food and lipid components are well documented in detail in several papers [18][19][20]. Based on these literatures, useful information for food effect on the performance of su-SEDDS can be obtained.…”

Section: Effect Of Food On Supersaturationmentioning

confidence: 99%

“…However, food, age, diseases, such as exocrine pancreatic insufficiency (a pathological condition that can alter physiological and hydrodynamic GIT parameters including gastric and intestinal pH), digestive lipases, bile salts, emptying rate, gut transit time, and gut motility have been studied. These change in GI physiological conditions influence the supersaturation and absorption of drugs from SEDDSs [20].…”

Section: Effects Of Various Factors On Lipid Digestion and Drug Absormentioning

confidence: 99%

“…Thus, an in vitro digestion system should be established to reflect the three most important mechanisms: the increase in solubilization, the generation of supersaturation, and the inhibition of recrystallization. However, it is very difficult to consider all complex effects of various GI physiological factors in in vitro evaluations [20]. Recently, following the emphasis placed on the importance of in vitro digestion models by many research scientists, promising progress has been made in the development of a biorelevant in vitro digestion model with good IVIVC for predicting the effects of various GI factors on the performance of supersaturable drug delivery systems, including in vivo supersaturation, drug precipitation, and absorption [42,171].…”

Section: Biorelevant Supersaturation Testingmentioning

confidence: 99%

“…This aspect of SEDDS has been discussed in more detail by other authors, thus, several excellent review references are cited here to aid the reader's in-depth understanding [7,18,19].Self-emulsification depends on the nature of the oil/surfactant pair, surfactant concentration, and oil/surfactant ratio, and on the various physiological conditions, such as temperature and pH, under which self-emulsification occurs. SEDDSs differ from other oral drug delivery systems in that the excipients in the formulation are markedly altered by enzymatic digestion [20]. The lipids in the oil phase of SEDDSs are hydrolyzed by gastric and pancreatic lipases in the GIT to release more amphiphilic lipid digestion products.…”

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confidence: 99%

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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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Section: Effect Of Food On Supersaturationmentioning

confidence: 99%

Section: Effect Of Food On Supersaturationmentioning

confidence: 99%

Section: Effects Of Various Factors On Lipid Digestion and Drug Absormentioning

confidence: 99%

Section: Biorelevant Supersaturation Testingmentioning

confidence: 99%

mentioning

confidence: 99%

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Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Park

Kim

2020

Pharmaceutics

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Comparative evaluation of static and dynamic simulated digestion models

Wang

Liu

et al. 2023

J Sci Food Agric

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BACKGROUND The digestion behavior of lipids plays a crucial role in their nutritional values. Currently, the complex dynamic variations of human gastrointestinal conditions are considered in simulated digestion models. The present study compared the digestion behavior of glycerol trilaurate (GTL), glycerol tripalmitate (GTP) and glycerol tristearate (GTS) in a static in vitro digestion model and a dynamic in vitro digestion model. In the dynamic digestion model, the parameters of gastric juice secretion, the rate of gastric emptying, the secretion of intestinal juice and the pH variations were estimated. RESULTS The dynamic digestion model showed a certain extent of gastric lipase hydrolysis, while almost no lipolysis happened in the gastric phase of the static digestion model. A smoother digestive behavior was observed in the dynamic model than that in the static model. In the static model, the particle size distribution in gastric and intestinal phase changed rapidly in all triacylglycerol (TAG) groups. The change of particle size during the whole digestion period in GTL is more moderate than GTP and GTS. In addition, the final free fatty acids release degree was 58.558%, 54.36%, and 52.97% for GTL, GTP, and GTS, respectively. CONCLUSION This study illustrated the different digestion profiles of TAGs in two digestion models and the results will contribute to a better understanding of different in vitro digestion models in lipid digestion. © 2023 Society of Chemical Industry.

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One‐Step Synthesis of Hydrogen‐Bonded Microcapsules for pH‐Triggered Protein Release

et al. 2023

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One‐step microfluidic approach in which interfacial complexation of hydrogen bonding polymers is utilized to prepare pH‐responsive microcapsules is presented. Using water‐in‐oil‐in‐oil‐in‐water (W1/O1/O2/W2) triple‐emulsion droplets as templates, it is shown that polymeric microcapsules with an aqueous core and a shell that consists of two complementary hydrogen bonding polymers, poly(propylene oxide)(PPO) and poly(methacrylic acid)(PMAA), can be prepared in a robust manner. The presence of a buffer layer enables controlled interfacial complexation of PMAA and PPO at the water/oil interface, followed by spontaneous dewetting of the oil droplet to result in hydrogen‐bonded microcapsules dispersed in aqueous media. In addition, it is demonstrated that the permeability of the PPO/PMAA membrane can be readily tuned by varying the molecular weight of PMAA. Furthermore, it is shown that the resulting PPO/PMAA microcapsules are stable at a high salt concentration (>1 m NaCl) unlike analogous capsules prepared through electrostatic complexation while they release the encapsulated protein above the critical pH of which the PMAA ionizes and results in disassembly of the shell membrane.

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Variations in gastrointestinal lipases, pH and bile acid levels with food intake, age and diseases: Possible impact on oral lipid-based drug delivery systems

Cited by 53 publications

References 150 publications

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems

Comparative evaluation of static and dynamic simulated digestion models

One‐Step Synthesis of Hydrogen‐Bonded Microcapsules for pH‐Triggered Protein Release

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