23–24 Sept 2021
Europe/Lisbon timezone

Membrane-water partitioning to screen drug candidates: towards a high-throughput microfluidic platform

24 Sept 2021, 13:30
1h 30m
Poster Materials and Technologies for Health and Environment Materials and technologies for Health and Environment (Posters)

Speaker

Eduarda Fernandes (CF-UM-UP)

Description

In a rational drug design, the modulation of the chemical structure based on drug’s pharmacokinetic profile can be the solution to improve drug development efficiency. Significant correlations between lipophilicity and membrane permeation have been established [1]. Further, anisotropic membrane-like systems, such as membranes/water (M/W) partitioning systems, are described as a more accurate alternative to octanol/water for the estimation of pharmacokinetic behavior [2]. In the present study, derivative spectroscopy was used to calculate M/W partition coefficient of two model drugs and to predict several parameters of their pharmacokinetic profile using lipid nanosystems of different constitution as biomembrane mimetic models (Fig. 1A) [3,4]. The obtained results highlight the relevance of using biomimetic models to determine the logM/W to obtain reliable information in the early stages of drug development. Notwithstanding, this methodology is being restricted mainly to the academic research. Their large-scale use at industrial level has been hindered mostly by its low throughput. The work presented here also considers the development of a microfluidic platform in which microchannels are coated with supported lipid bilayers that enable the assessment of the logM/W partitioning of drugs (Fig. 1B). This microfluidic platform constitutes a promising high-throughput technology to screen drug candidates at a large scale fulfilling the requirements from pharmaceutical and cosmetic industries.

Primary authors

Eduarda Fernandes (CF-UM-UP) Marlene Lúcio (CF-UM-UP, Universidade do Minho, Campus de Gualtar, 4710-057 Braga, Portugal) Senentxu Lanceros-Méndez (CF-UM-UP, Universidade do Minho, Campus de Gualtar, 4710-057 Braga, Portugal; BCMaterials, UPV/EHU Science Park, 48940 Leioa, Spain; IKERBASQUE, Basque Foundation for Science, 48009 Bilbao, Spain) Vanessa F. Cardoso (CMEMS-UMinho, Universidade do Minho, Campus de Azurém, 4800-058 Guimarães, Portugal)

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