How relevant are assembled equilibrium samples in understanding structure formation during lipid digestion?

Stephanie Phan, Stefan Johannes Salentinig, Adrian Hawley, Benjamin James Boyd

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Abstract

Lipid-based formulations are gaining interest for use as drug delivery systems for poorly water-soluble drug compounds. During digestion, the lipolysis products self-assemble with endogenous surfactants in the gastrointestinal tract to form colloidal structures, enabling enhanced drug solubilisation. Although earlier studies in the literature focus on assembled equilibrium systems, little is known about structure formation under dynamic lipolysis conditions. The purpose of this study was to investigate the likely colloidal structure formation in the small intestine after the ingestion of lipids, under equilibrium and dynamic conditions. The structural aspects were studied using small angle X-ray scattering and dynamic light scattering, and were found to depend on lipid composition, lipid chain length, prandial state and emulsification. Incorporation of phospholipids and lipolysis products into bile salt micelles resulted in swelling of the structure. At insufficient bile salt concentrations, a co-existing lamellar phase was observed, due to a reduction in the solubilisation capacity for lipolysis products. Emulsification accelerated the rate of lipolysis and structure formation.
Original languageEnglish
Pages (from-to)117 - 124
Number of pages8
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume96
DOIs
Publication statusPublished - 2015

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