Liposomes as oral delivery systems for poorly soluble compounds: behavior during digestion and absorption processes

People involved

Dr. Loes Duivenvoorde (Postdoc fellow sponsored by the PRC) – Wageningen University & Research, the Netherlands

Abstract

Liposomes have been evolving as unique drug carriers for realizing enhanced efficacy and/or reduced toxicity.1) Currently, several liposomal drug delivery systems are on the market, and practically all of them are administered parenterally. Liposomes are also investigated for oral delivery, especially for active ingredients with extremely low oral bioavailability, such as poorly soluble compounds. The aim of this project is to study the mechanisms underlying the bioavailability improvement of poorly soluble compounds entrapped in liposomes as oral drug delivery systems. We will start by studying the mechanisms of liposome digestion and drug solubilization and the efficiency of subsequent association of the entrapped compounds into mixed micelles, using a highly relevant in vitro human digestion model and dedicated analysis methods.2)3)4) In the second part of the project, we will study the permeability of the compounds after in vitro digestion, using an in vitro permeability model consisting of a co-culture of Caco-2 and HT29-MTX cells.

We aim to gain important knowledge and insights to improve oral delivery systems for the delivery of poorly soluble compounds in the future, but we also aim to develop a robust in vitro strategy that will aid in testing or monitoring claims for liposomal formulations for oral delivery as an alternative method for animal testing.

Benefit for the community

An improved understanding of the underlying mechanisms of transfer of compounds with lipophilic properties from liposomes to mixed micelles during human in vitro digestion and subsequent absorption of the compounds over the intestinal barrier allows for the development of improved liposomal drug delivery systems for oral administration. Furthermore, the robust test strategy that will be developed in this project will aid in testing or monitoring claims made for liposomal formulations for oral delivery as an alternative method for animal testing.

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