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

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method. / Klitgaard, Mette; Mullertz, Anette; Berthelsen, Ragna.

In: Pharmaceutics, Vol. 13, No. 4, 489, 2021.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Klitgaard, M, Mullertz, A & Berthelsen, R 2021, 'Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method', Pharmaceutics, vol. 13, no. 4, 489. https://doi.org/10.3390/pharmaceutics13040489

APA

Klitgaard, M., Mullertz, A., & Berthelsen, R. (2021). Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method. Pharmaceutics, 13(4), [489]. https://doi.org/10.3390/pharmaceutics13040489

Vancouver

Klitgaard M, Mullertz A, Berthelsen R. Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method. Pharmaceutics. 2021;13(4). 489. https://doi.org/10.3390/pharmaceutics13040489

Author

Klitgaard, Mette ; Mullertz, Anette ; Berthelsen, Ragna. / Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method. In: Pharmaceutics. 2021 ; Vol. 13, No. 4.

Bibtex

@article{56cda34604df49109bf07c47d7d8cb41,
title = "Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method",
abstract = "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(R) barriers. A linear in vivo-in vitro correlation was obtained when comparing the area under the in vitro drug permeation-time curve (AUC(0-3h)), to the AUC(0-3h) 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.",
keywords = "in vivo&#8211, in vitro correlation, lipolysis-permeation, lipid-based drug delivery system, PermeaPad, cinnarizine, lipolysis",
author = "Mette Klitgaard and Anette Mullertz and Ragna Berthelsen",
year = "2021",
doi = "10.3390/pharmaceutics13040489",
language = "English",
volume = "13",
journal = "Pharmaceutics",
issn = "1999-4923",
publisher = "MDPI AG",
number = "4",

}

RIS

TY - JOUR

T1 - Estimating the Oral Absorption from Self-Nanoemulsifying Drug Delivery Systems Using an In Vitro Lipolysis-Permeation Method

AU - Klitgaard, Mette

AU - Mullertz, Anette

AU - Berthelsen, Ragna

PY - 2021

Y1 - 2021

N2 - 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(R) barriers. A linear in vivo-in vitro correlation was obtained when comparing the area under the in vitro drug permeation-time curve (AUC(0-3h)), to the AUC(0-3h) 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.

AB - 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(R) barriers. A linear in vivo-in vitro correlation was obtained when comparing the area under the in vitro drug permeation-time curve (AUC(0-3h)), to the AUC(0-3h) 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.

KW - in vivo&#8211

KW - in vitro correlation

KW - lipolysis-permeation

KW - lipid-based drug delivery system

KW - PermeaPad

KW - cinnarizine

KW - lipolysis

U2 - 10.3390/pharmaceutics13040489

DO - 10.3390/pharmaceutics13040489

M3 - Journal article

C2 - 33918449

VL - 13

JO - Pharmaceutics

JF - Pharmaceutics

SN - 1999-4923

IS - 4

M1 - 489

ER -

ID: 263033903