Pharmaceutical Nanotechnology
Enzymatic characterization of lipid-based drug delivery systems

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Abstract

The present work introduces a simple and robust in vitro method for enzymatic characterisation of surface properties of lipid dispersions in aqueous media. The initial lipolysis rate in biorelevant media, using pancreatic lipase and a self-microemulsifying formulation (SMEDDS) containing digestible lipids as substrate, was determined. The impact of incorporating two sparingly water soluble model drugs, probucol and halofantrine, into the SMEDDS was studied. It was found that both model drugs reduced the initial rate of lipolysis compared with the vehicle, probucol having a larger effect than halofantrine. The reduction of initial lipolysis rate indicates that probucol and halofantrine are bound in the water/emulsion interface limiting the substrate availability.

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Acknowledgements

VINNOVA in Sweden and Erhvervsfremme Styrelsen in Denmark are gratefully acknowledged for financial support to the Øresund contracts. Halofantrine was kindly donated by GlaxoSmithKline (West Sussex, UK).

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