Simultaneous lipolysis/permeation in vitro model, for the estimation of bioavailability of lipid based drug delivery systems

Hanady Ajine Bibi, René Holm, Annette Bauer-Brandl*

*Kontaktforfatter for dette arbejde

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Resumé

The simultaneous processes of lipid digestion and absorption together determine the oral bioavailability of drugs incorporated into lipid based drug delivery systems (LBDDS). A number of slightly different protocols for in vitro lipolysis are widely accepted; however, the permeation process has so far not been included into the models due to the harsh conditions of lipid digestion compromising permeation barriers. The present study for the first time combines biomimetic permeation and lipolysis of LBDDS. The focus of the current work was on the functional stability of the barrier - Permeapad® during lipid digestion. Using calcein as a marker molecule the investigations demonstrated that the barrier was able to maintain its permeation properties in the presence of the SNEDDS (self-emulsifying drug delivery system) formulation, the lipolysis medium, and the lipolysis medium while digesting the SNEDDS. Furthermore, the permeation of cinnarizine (CINN) from SNEDDS was demonstrated to be lower, if the formulation as such was applied as compared to the digested formulation. This support the general perception that meaningful in vitro evaluation of lipid based formulations requires consideration of both, the digestion and absorption, i.e. lipolysis and permeation.

OriginalsprogEngelsk
TidsskriftEuropean Journal of Pharmaceutics and Biopharmaceutics
Vol/bind117
Sider (fra-til)300-307
ISSN0939-6411
DOI
StatusUdgivet - 2017

Fingeraftryk

Lipids
Cinnarizine
In Vitro Techniques
Pharmaceutical Preparations

Citer dette

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title = "Simultaneous lipolysis/permeation in vitro model, for the estimation of bioavailability of lipid based drug delivery systems",
abstract = "The simultaneous processes of lipid digestion and absorption together determine the oral bioavailability of drugs incorporated into lipid based drug delivery systems (LBDDS). A number of slightly different protocols for in vitro lipolysis are widely accepted; however, the permeation process has so far not been included into the models due to the harsh conditions of lipid digestion compromising permeation barriers. The present study for the first time combines biomimetic permeation and lipolysis of LBDDS. The focus of the current work was on the functional stability of the barrier - Permeapad{\circledR} during lipid digestion. Using calcein as a marker molecule the investigations demonstrated that the barrier was able to maintain its permeation properties in the presence of the SNEDDS (self-emulsifying drug delivery system) formulation, the lipolysis medium, and the lipolysis medium while digesting the SNEDDS. Furthermore, the permeation of cinnarizine (CINN) from SNEDDS was demonstrated to be lower, if the formulation as such was applied as compared to the digested formulation. This support the general perception that meaningful in vitro evaluation of lipid based formulations requires consideration of both, the digestion and absorption, i.e. lipolysis and permeation.",
keywords = "Cinnarizine, In vitro, Lipid based formulations, Lipolysis, Permeability, Permeapad{\circledR}, SNEDDS",
author = "Bibi, {Hanady Ajine} and Ren{\'e} Holm and Annette Bauer-Brandl",
year = "2017",
doi = "10.1016/j.ejpb.2017.05.001",
language = "English",
volume = "117",
pages = "300--307",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",

}

Simultaneous lipolysis/permeation in vitro model, for the estimation of bioavailability of lipid based drug delivery systems. / Bibi, Hanady Ajine; Holm, René; Bauer-Brandl, Annette.

I: European Journal of Pharmaceutics and Biopharmaceutics, Bind 117, 2017, s. 300-307.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

TY - JOUR

T1 - Simultaneous lipolysis/permeation in vitro model, for the estimation of bioavailability of lipid based drug delivery systems

AU - Bibi, Hanady Ajine

AU - Holm, René

AU - Bauer-Brandl, Annette

PY - 2017

Y1 - 2017

N2 - The simultaneous processes of lipid digestion and absorption together determine the oral bioavailability of drugs incorporated into lipid based drug delivery systems (LBDDS). A number of slightly different protocols for in vitro lipolysis are widely accepted; however, the permeation process has so far not been included into the models due to the harsh conditions of lipid digestion compromising permeation barriers. The present study for the first time combines biomimetic permeation and lipolysis of LBDDS. The focus of the current work was on the functional stability of the barrier - Permeapad® during lipid digestion. Using calcein as a marker molecule the investigations demonstrated that the barrier was able to maintain its permeation properties in the presence of the SNEDDS (self-emulsifying drug delivery system) formulation, the lipolysis medium, and the lipolysis medium while digesting the SNEDDS. Furthermore, the permeation of cinnarizine (CINN) from SNEDDS was demonstrated to be lower, if the formulation as such was applied as compared to the digested formulation. This support the general perception that meaningful in vitro evaluation of lipid based formulations requires consideration of both, the digestion and absorption, i.e. lipolysis and permeation.

AB - The simultaneous processes of lipid digestion and absorption together determine the oral bioavailability of drugs incorporated into lipid based drug delivery systems (LBDDS). A number of slightly different protocols for in vitro lipolysis are widely accepted; however, the permeation process has so far not been included into the models due to the harsh conditions of lipid digestion compromising permeation barriers. The present study for the first time combines biomimetic permeation and lipolysis of LBDDS. The focus of the current work was on the functional stability of the barrier - Permeapad® during lipid digestion. Using calcein as a marker molecule the investigations demonstrated that the barrier was able to maintain its permeation properties in the presence of the SNEDDS (self-emulsifying drug delivery system) formulation, the lipolysis medium, and the lipolysis medium while digesting the SNEDDS. Furthermore, the permeation of cinnarizine (CINN) from SNEDDS was demonstrated to be lower, if the formulation as such was applied as compared to the digested formulation. This support the general perception that meaningful in vitro evaluation of lipid based formulations requires consideration of both, the digestion and absorption, i.e. lipolysis and permeation.

KW - Cinnarizine

KW - In vitro

KW - Lipid based formulations

KW - Lipolysis

KW - Permeability

KW - Permeapad®

KW - SNEDDS

U2 - 10.1016/j.ejpb.2017.05.001

DO - 10.1016/j.ejpb.2017.05.001

M3 - Journal article

VL - 117

SP - 300

EP - 307

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

ER -