Biorelevant Media Simulating Fed State Intestinal Fluids: Colloid Phase Characterization and Impact on Solubilization Capacity

Kleberg, Karen; Jacobsen, Freja Aksel; Fatouros, D.G.; Müllertz, Anette

doi:10.1002/jps.22122

Cited by 82 publications

(93 citation statements)

References 25 publications

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“…In the current study, BS and BS/PL systems representing the gastrointestinal environment prior to lipid digestion revealed the presence of micelles only, which is consistent with previous observations [4,5,9]. The DLS measurements revealed a larger hydrodynamic radius for the fasted BS/PL micelles, compared to the fed BS and BS/PL micelles, and fasted BS micelles.…”

Section: Similarities and Differences Between Equilibrium And Dynamicsupporting

confidence: 94%

“…Past work in examining phase behaviour in digesting lipid systems has involved the mixing of medium-and long-chain lipid digestion products and endogenous amphiphilic molecules with water and bile salts to form equilibrium systems [1][2][3][4][5][6]. These studies vary in the composition of guest molecules, osmotic pressure and pH conditions to simulate conditions in the small intestine.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

How relevant are assembled equilibrium samples in understanding structure formation during lipid digestion?

Phan

Salentinig

Hawley

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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Section: Similarities and Differences Between Equilibrium And Dynamicsupporting

confidence: 94%

Section: Introductionmentioning

confidence: 99%

How relevant are assembled equilibrium samples in understanding structure formation during lipid digestion?

Phan

Salentinig

Hawley

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…That is to say, the poor water interactions of some molecules are improved through wetting and solubilisation by additives such as surfactants and/or lipids [77]. Other media developed and used include the Copenhagen fasted and fed media in which the pH is kept constant and the male-ate is used as a buffering component (Table 1) [78][79][80]. Studying the dissolution rate in different BDM and using the different experimental results obtained to select compounds to advance further development is one way to speed up the assessment of in vivo performance.…”

Section: Dissolution Mediamentioning

confidence: 99%

Drug release from matrix tablets: physiological parameters and the effect of food

Nokhodchi

Asare-Addo

2014

Expert Opinion on Drug Delivery

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Introduction: As dissolution plays an important and vital role in the drug-delivery process of oral solid dosage forms, it is, therefore, essential to critically evaluate the parameters that can affect this process. Areas covered:The consumption of food as well as the physiological environment and properties of the gastrointestinal tract, such as its volume and composition of fluid, the fluid hydrodynamics, properties of the intestinal membrane, drug dose and solubility, pK a , diffusion coefficient, permeability and particle size, all affect drug dissolution and absorption rate. There are several dissolution approaches that have been developed to address the conditions as experienced in the in vivo environment, as the traditional dissolution being a quality control method is not biorelevant and as such do not always produce meaningful data. This review also describes the development of a systematic way that differentiates between robust and non-robust formulations by varying the effects of agitation and ionic strength through the use of the automated United States Pharmacopeia type III Bio-Dis apparatus. Expert opinion:With the improved understanding of the physiological parameters that can affect the oral bioperformance of dosage forms, strides have, therefore, been made in making dissolution testing methods more bio-logically based with the view of obtaining more in vitro--in vivo correlations.Keywords: agitation rate, biodissolution, drug release, effect of food, hydrophilic matrices, ionic strength Highlights -Understanding all the physiological parameters can serve as a basis for designing dissolution testing methods and systems that can more fully represent the gastrointestinal (GI) tract in humans and allow more in vitro-in vivo (IVIVC) correlations to be obtained thereby improving the oral bioperformance of dosage forms.-Simulation of GI conditions is essential to adequately predict the in vivo behaviour of drug formulations.-The choice of appropriate media for in vitro tests is crucial to their ability to correctly forecast the food effect in pharmacokinetic studies.-Several methods of dissolution testing have been conducted and are still ongoing that seek to further understand and develop media and dissolution methods to better represent the in vivo conditions and to aid in the better prediction of in vivo drug release.-Systematic change of agitation method and ionic strength evaluation may be used as additional tools in allowing for the identification of potential fed and fasted effects on drug release from hydrophilic matrices in the drive for developing dissolution methodologies that are more relevant in helping to achieve more IVIVC.

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“…During the last decades, the thorough physicochemical characterisation of human gastrointestinal fluids allowed the development of biorelevant media closer matching the in vivo conditions compared with the rather simple compendial media (43)(44)(45). The proposed biorelevant media contain physiological relevant amounts of buffer, lecithin and bile salts mimicking either the fasted or fed state (Table I) and have been subject of recent reviews (46,47).…”

Section: Dispersion Testing Of Lbddsmentioning

confidence: 99%

“…While the concentration of bile is similar (5-30 mM) throughout the employed lipolysis models, some groups utilise pure taurocholic acid (51,52,71) or taurodeoxycholic acid (57,58,72), whereas others employ a crude (porcine) bile extract (47,73,56). The utilisation of pure bile acids renders the composition of the lipolysis medium more reproducible compared with the more variable crude extract, but lacks the complex composition of human bile (63).…”

Section: In Vitro Lipolysismentioning

confidence: 99%

Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development

Thomas

Holm

Rades

2012

AAPS J

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Abstract. Facing the increasing number of poorly water-soluble drugs, pharmaceutical scientists are required to break new grounds for the delivery of these pharmaceutically problematic drugs. Lipid-based drug delivery systems (LBDDS) have received increased interest as a novel drug delivery platform during the last decades and several successfully marketed products have shown the potential for LBDDS. However, there exists a discrepancy between the clear need for innovative delivery forms and their rational design. In the case of LBDDS, this can be attributed to the complexity of LBDDS after administration. Unlike conventional formulations, LBDDS are susceptible to digestion in the gastrointestinal tract, the interplay of delivery system, drug and physiology ultimately effecting drug disposition. In vitro lipolysis has become an important technique to mimic the enzymatic degradation. For the better understanding of how LBDDS promote drug delivery, in vitro lipolysis requires advanced characterisation methods. In this review, the physiological background of lipid digestion is followed by a thorough summary of the techniques that are currently used to characterise in vitro lipolysis. It would be desirable that the increasing knowledge about LBDDS will foster their rationale development thereby increasing their broader application.KEY WORDS: in vitro digestion; in vitro lipolysis models; lipid-based drug delivery systems; poorly soluble drugs; self-nanoemulsifying drug delivery systems (SNEDDS).

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Biorelevant Media Simulating Fed State Intestinal Fluids: Colloid Phase Characterization and Impact on Solubilization Capacity

Cited by 82 publications

References 25 publications

How relevant are assembled equilibrium samples in understanding structure formation during lipid digestion?

How relevant are assembled equilibrium samples in understanding structure formation during lipid digestion?

Drug release from matrix tablets: physiological parameters and the effect of food

Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development

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