Ex vivo permeability study of poorly soluble drugs across gastrointestinal membranes: acceptor compartment media composition

Andrejs Sitovs; Valentyn Mohylyuk

doi:10.1016/j.drudis.2024.104214

Ex vivo permeability study of poorly soluble drugs across gastrointestinal membranes: acceptor compartment media composition

Andrejs Sitovs, Valentyn Mohylyuk (Corresponding Author)

Research output: Contribution to journal › Article › peer-review

2 Citations (Scopus)

Abstract

Ex vivo drug permeability testing across gastrointestinal (GI) membranes is crucial in drug discovery and oral drug delivery. It is a reliable method for drugs with good solubility, but it poses challenges for poorly soluble drugs, which are common in development pipelines today. Although enabling formulations increase the apparent solubility in the GI compartment (dissolution vessel or permeation chamber’s donor compartment), maintaining solubilized drug in the acceptor compartment during ex vivo testing remains largely unresolved. This review compiles and critically evaluates the diverse compositions of acceptor media used in ex vivo permeability studies for poorly soluble drugs, highlighting this significant yet underexplored aspect of pharmaceutical science. An algorithm is proposed for selecting solubility-enhancing additives for the acceptor media in ex vivo permeability studies of poorly soluble drugs.

Original language	English
Article number	104214
Journal	Drug Discovery Today
Volume	29
Issue number	12
DOIs	https://doi.org/10.1016/j.drudis.2024.104214
Publication status	Published - Dec 2024

Keywords*

ex vivo
permeability
poorly soluble drugs
Ussing chamber
acceptor

Field of Science*

3.1 Basic medicine

Publication Type*

1.1. Scientific article indexed in Web of Science and/or Scopus database

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/j.drudis.2024.104214Licence: CC BY

Cite this

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title = "Ex vivo permeability study of poorly soluble drugs across gastrointestinal membranes: acceptor compartment media composition",

abstract = "Ex vivo drug permeability testing across gastrointestinal (GI) membranes is crucial in drug discovery and oral drug delivery. It is a reliable method for drugs with good solubility, but it poses challenges for poorly soluble drugs, which are common in development pipelines today. Although enabling formulations increase the apparent solubility in the GI compartment (dissolution vessel or permeation chamber{\textquoteright}s donor compartment), maintaining solubilized drug in the acceptor compartment during ex vivo testing remains largely unresolved. This review compiles and critically evaluates the diverse compositions of acceptor media used in ex vivo permeability studies for poorly soluble drugs, highlighting this significant yet underexplored aspect of pharmaceutical science. An algorithm is proposed for selecting solubility-enhancing additives for the acceptor media in ex vivo permeability studies of poorly soluble drugs.",

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author = "Andrejs Sitovs and Valentyn Mohylyuk",

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doi = "10.1016/j.drudis.2024.104214",

language = "English",

volume = "29",

journal = "Drug Discovery Today",

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TY - JOUR

T1 - Ex vivo permeability study of poorly soluble drugs across gastrointestinal membranes: acceptor compartment media composition

AU - Sitovs, Andrejs

AU - Mohylyuk, Valentyn

PY - 2024/12

Y1 - 2024/12

N2 - Ex vivo drug permeability testing across gastrointestinal (GI) membranes is crucial in drug discovery and oral drug delivery. It is a reliable method for drugs with good solubility, but it poses challenges for poorly soluble drugs, which are common in development pipelines today. Although enabling formulations increase the apparent solubility in the GI compartment (dissolution vessel or permeation chamber’s donor compartment), maintaining solubilized drug in the acceptor compartment during ex vivo testing remains largely unresolved. This review compiles and critically evaluates the diverse compositions of acceptor media used in ex vivo permeability studies for poorly soluble drugs, highlighting this significant yet underexplored aspect of pharmaceutical science. An algorithm is proposed for selecting solubility-enhancing additives for the acceptor media in ex vivo permeability studies of poorly soluble drugs.

AB - Ex vivo drug permeability testing across gastrointestinal (GI) membranes is crucial in drug discovery and oral drug delivery. It is a reliable method for drugs with good solubility, but it poses challenges for poorly soluble drugs, which are common in development pipelines today. Although enabling formulations increase the apparent solubility in the GI compartment (dissolution vessel or permeation chamber’s donor compartment), maintaining solubilized drug in the acceptor compartment during ex vivo testing remains largely unresolved. This review compiles and critically evaluates the diverse compositions of acceptor media used in ex vivo permeability studies for poorly soluble drugs, highlighting this significant yet underexplored aspect of pharmaceutical science. An algorithm is proposed for selecting solubility-enhancing additives for the acceptor media in ex vivo permeability studies of poorly soluble drugs.

KW - ex vivo

KW - permeability

KW - poorly soluble drugs

KW - Ussing chamber

KW - acceptor

UR - https://www-webofscience-com.db.rsu.lv/wos/alldb/full-record/MEDLINE:39428083

UR - http://www.scopus.com/inward/record.url?scp=85208459257&partnerID=8YFLogxK

U2 - 10.1016/j.drudis.2024.104214

DO - 10.1016/j.drudis.2024.104214

M3 - Article

SN - 1359-6446

VL - 29

JO - Drug Discovery Today

JF - Drug Discovery Today

IS - 12

M1 - 104214

ER -

Ex vivo permeability study of poorly soluble drugs across gastrointestinal membranes: acceptor compartment media composition

Abstract

Keywords*

Field of Science*

Publication Type*

UN SDGs

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