Permeapad™ for investigation of passive drug permeability: The effect of surfactants, co-solvents and simulated intestinal fluids (FaSSIF and FeSSIF)

Bibi, Hanady Ajine; Cagno, Massimiliano Pio di; Holm, René; Bauer‐Brandl, Annette

doi:10.1016/j.ijpharm.2015.07.028

Cited by 45 publications

(17 citation statements)

References 24 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The calcein P app in the presence of the superSNEDDS solution was significantly higher when compared the calcein P app from the present control study, which might indicate that the permeation barrier in these studies was disrupted to some degree. However, because all values were lower than the calcein P app of 1.65 ± 0.1 × 10 −5 cm/s previously reported for the PermeaPad ® barrier with no lipid barrier layer [49], it was concluded that some barrier function was retained throughout the study. This was additionally based on the observation that the higher calcein P app did not affect the permeation of cinnarizine (Section 3.3).…”

Section: Permeation Barrier Integritycontrasting

confidence: 54%

Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method

2021

View full text Add to dashboard Cite

The aim of this study was to design an in vitro lipolysis-permeation method to estimate drug absorption following the oral administration of self-nanoemulsifying drug delivery systems (SNEDDSs). The method was evaluated by testing five oral formulations containing cinnarizine (four SNEDDSs and one aqueous suspension) from a previously published pharmacokinetic study in rats. In that study, the pharmacokinetic profiles of the five formulations did not correlate with the drug solubilization profiles obtained during in vitro intestinal lipolysis. Using the designed lipolysis-permeation method, in vitro lipolysis of the five formulations was followed by in vitro drug permeation in Franz diffusion cells equipped with PermeaPad® barriers. A linear in vivo–in vitro correlation was obtained when comparing the area under the in vitro drug permeation–time curve (AUC0–3h), to the AUC0–3h of the plasma concentration–time profile obtained from the in vivo study. Based on these results, the evaluated lipolysis-permeation method was found to be a promising tool for estimating the in vivo performance of SNEDDSs, but more studies are needed to evaluate the method further.

show abstract

Section: Permeation Barrier Integritycontrasting

confidence: 54%

Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method

2021

View full text Add to dashboard Cite

show abstract

“…[10][11][12] Donor solutions were prepared with calcein and Lucifer Yellow CH at a final concentration of 500 µM in 0.1 M phosphate buffer (pH 6.5) containing 0-3% (vol) polysorbate 80. The fluorescence of the receiver solutions was measured after 16 h incubation at 25°C with a Gemini EM Microplate Reader (Molecular Devices, Sunnyvale, CA, U.S.A.); the respective excitation and emission wavelengths were 445 and 512 nm for calcein, and 435 and 485 nm for Lucifer Yellow CH.…”

Section: Lc-ms/ms Analytical Methodsmentioning

confidence: 99%

Development of Cassette PAMPA for Permeability Screening

Lee

et al. 2017

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

The parallel artificial membrane permeability assay (PAMPA) is widely used in early-stage drug discovery to discriminate compounds by intestinal permeability. The purpose of the current study was to establish a cassette (n-in-1) PAMPA to enable permeability screening of lipophilic compounds. A double-sink PAMPA consisting of a pH gradient (i.e., pH 6.5 and 7.4 for the donor and receiver compartments, respectively) and a lipophilic sink (i.e., a surfactant in the receiver solution) was utilized with cassette incubation of 10 reference compounds. Sample analysis was conducted using selected reaction monitoring (SRM) with a triple quadrupole LC-MS/MS system. Correlation between PAMPA permeability and human intestinal absorption (HIA) of the reference compounds yielded two false negatives, namely propranolol (PPN) and verapamil (VER); these two compounds showed a substantially lower recovery (ca. 10%) than other reference compounds (>69%). This cassette PAMPA was repeated subsequently with polysorbate 80 added to the donor compartments, which resulted in a significant increase in both the recovery and the permeability of the false negatives. Accordingly, the permeability class of all reference compounds could be unambiguously differentiated using this cassette PAMPA. Also, a strong linear correlation (r 0.9845) was observed between the cassette and discrete permeability of all reference compounds.

show abstract

“…The authors calculated that it would take an area to volume ratio of 5.9 cm 2 /ml to achieve a 90% permeation of hydrocortisone into the acceptor chamber within 4 h. The inter‐laboratory variability of these biomimetic membranes needs to be further investigated. The compatibility of the Permeapad ® membrane with surfactants, co‐solvents and biorelevant media, and ability to be used over a long duration, up to 94.5 h in the experiment, are advantages compared with cellular membranes, such as Caco‐2. To evaluate this setup's usefulness in assessing drug precipitation in the upper fasted small intestine, further studies must be carried out incorporating a pH shift from gastric to intestinal media.…”

Section: Small‐scale Methods To Assess Drug Precipitationmentioning

confidence: 99%

“…surfactants) and some media (e.g. Level II FeSSIF) also further limit the use of Caco‐2 cell monolayers as intestinal barriers in studies examining intestinal precipitation …”

Section: Compartmental Methods Using Cellular Membranesmentioning

confidence: 99%

In vitro methods to assess drug precipitation in the fasted small intestine – a PEARRL review

O’Dwyer

Litou

Box

et al. 2019

Journal of Pharmacy and Pharmacology

View full text Add to dashboard Cite

Despite the progress from compendial quality control dissolution methods, further work is required to validate the usefulness of proposed setups and to increase their biorelevance, particularly in simulating the absorption of drug along the intestinal lumen. Coupling results from in vitro testing with physiologically based pharmacokinetic modelling holds significant promise and requires further evaluation.

show abstract

Permeapad™ for investigation of passive drug permeability: The effect of surfactants, co-solvents and simulated intestinal fluids (FaSSIF and FeSSIF)

Cited by 45 publications

References 24 publications

Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method

Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method

Development of Cassette PAMPA for Permeability Screening

In vitro methods to assess drug precipitation in the fasted small intestine – a PEARRL review

Contact Info

Product

Resources

About