Kinetic model for membrane transport. III. Solute transport through an asymmetrical membrane

Makino, Kimiko; Ohshima, Hiroyuki; Kondo, Tamotsu

doi:10.1016/0301-4622(92)80045-7

Cited by 6 publications

(6 citation statements)

References 7 publications

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“…This asymmetry in the membrane transport process is discussed in detail by Makino et al, and Kocherginsky and Zhang, with the development of mathematical models. 56,57 The presence of a solubilizing agent would lead to enhanced partitioning of the drug into the receiver compartment, as well as an almost negligible free drug concentration in the receiver, further enhancing the concentration gradient. The asymmetry will also change the membrane selectivity as the overall partitioning coefficient is no longer K (k 1 =k 2 Þ, but rather logarithmic mean of K d (on the donor) and K r (on the receiver).…”

Section: Influence Of Receiver Sink On Mass Flow Rate Of Supersaturat...mentioning

confidence: 99%

A Mechanistic Study of Drug Mass Transport from Supersaturated Solutions Across PAMPA Membranes

Hate

Mosquera-Giraldo

Taylor

2022

Journal of Pharmaceutical Sciences

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Section: Influence Of Receiver Sink On Mass Flow Rate Of Supersaturat...mentioning

confidence: 99%

A Mechanistic Study of Drug Mass Transport from Supersaturated Solutions Across PAMPA Membranes

Hate

Mosquera-Giraldo

Taylor

2022

Journal of Pharmaceutical Sciences

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“…Given the high experimental errors obtained (Figure A) as well as contradicting results seen at different stirring rates for atazanavir, we performed mass transport simulations using the Makino model , to assess the impact of different receiver solubilization capacity on the particle drifting effect. The results are shown in Figure and Figure S3 (Supporting Information).…”

Section: Resultsmentioning

confidence: 99%

“…The kinetic model developed by Makino et al 51 ( Figure S1 ) was used to analyze the impact of membrane asymmetry on the particle drifting effect. Calculation details and results are provided in the Supporting Information .…”

Section: Methodsmentioning

confidence: 99%

Mechanisms and Extent of Enhanced Passive Permeation by Colloidal Drug Particles

Narula

Sabra

2022

Mol. Pharmaceutics

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Formulations containing nanosized drug particles such as nanocrystals and nanosized amorphous drug aggregates recently came into light as promising strategies to improve the bioavailability of poorly soluble drugs. However, the increased solubility due to the reduction in particle size cannot adequately explain the enhanced bioavailability. In this study, the mechanisms and extent of enhanced passive permeation by drug particles were investigated using atazanavir, lopinavir, and clotrimazole as model drugs. Franz diffusion cells with lipid-infused membranes were utilized to evaluate transmembrane flux. The impact of stirring rate, receiver buffer condition, and particle size was investigated, and mass transport analyses were conducted to calculate transmembrane flux. Flux enhancement by particles was found to be dependent on particle size as well as the partitioning behavior of the drug between the receiver solution and the membrane, which is determined by both the drug and buffer used. A flux plateau was observed at high particle concentrations above amorphous solubility, confirming that mass transfer of amorphous drug particles from the aqueous solution to the membrane occurs only through the molecularly dissolved drug. Mass transport models were used to calculate flux enhancement by particles for various drugs at different conditions. Good agreements were obtained between experimental and predicted values. These results should contribute to improved bioavailability prediction of nanosized drug particles and better design of formulations containing colloidal drug particles.

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“…Tissue-based models, including intestinal sacs, Ussing chamber, and in situ perfusion experiments, most closely mimic the in vivo permeation and absorption process. However, the extent of flux enhancement by drug nanoparticles is dependent on factors such as membrane hydrophobicity and membrane asymmetry (media composition), , which may differ greatly among different models. ,− Currently, little is known about the impact of model selection on flux enhancement by drug particles, and whether artificial membranes and cell monolayers are appropriate models in place of biological tissues in the evaluation of the particle drifting effect.…”

Section: Introductionmentioning

confidence: 99%

Comparisons of in Vitro Models to Evaluate the Membrane Permeability of Amorphous Drug Nanoparticles

et al. 2022

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The spontaneous formation of amorphous drug nanoparticles following the release of a drug from a supersaturating formulation is gaining increasing attention due to their potential contribution to increased oral bioavailability. The formation of nanosized drug particles also has considerable implications for the interpretation of in vitro and in vivo data. However, the membrane transport properties of these drug particles remain less well understood. Herein, the membrane permeation of nanosized amorphous drug particles of a model drug atazanavir was evaluated using different artificial membrane-based, cell-based, and animal tissue-based models. Results showed that flux enhancement by particles was different for the various systems used. Generally, good agreement was obtained among experiments performed using the same apparatus with different model membranes, with the exception of the Madin-Darby canine kidney cell monolayer and the Long-Evans rat intestine tissue, which showed lower flux enhancements. Franz cell-based models showed slightly higher flux enhancements by particles compared to Transwell and intestinal tissue sac models. Mass transport analysis suggested that the extent of flux enhancement by particles is dependent on the geometry of the apparatus as well as the properties of the membrane and buffer used, whereas the flux plateau concentration is dependent on the unstirred water later (UWL) asymmetry. These results highlight the complexity in characterizing the permeability advantage of these nonmembrane permeable drug particles and suggest that caution should be used in selecting the appropriate in vitro model to evaluate the overall permeability of colloidal drug particles.

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Kinetic model for membrane transport. III. Solute transport through an asymmetrical membrane

Cited by 6 publications

References 7 publications

A Mechanistic Study of Drug Mass Transport from Supersaturated Solutions Across PAMPA Membranes

A Mechanistic Study of Drug Mass Transport from Supersaturated Solutions Across PAMPA Membranes

Mechanisms and Extent of Enhanced Passive Permeation by Colloidal Drug Particles

Comparisons of in Vitro Models to Evaluate the Membrane Permeability of Amorphous Drug Nanoparticles

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