Enhancing intestinal drug solubilisation using lipid-based delivery systems

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Lipid-based delivery systems are finding increasing application in the oral delivery of poorly water-soluble, lipophilic drugs. Whilst lipidic dose forms may improve oral bioavailability via several mechanisms, enhancement of gastrointestinal solubilisation remians arguably the most important method of absorption enhancement. This review firstly describes the mechanistic rationale which underpins the use of lipid-based delivery systems to enhance drug solubilisation and briefly reviews the available literature describing increases in oral bioavilability after the administration of lipid solution, suspension and self-emulsifying formulations. The use of in vitro mthods including dispersion tests and more complex models of in vitro lipolysis as indicators of potential in vivo performance are subsequently described, with particular focus on recent data which suggests that the digestion of surfactants present in lipid-based formulations may impact on formulation performance. Finally, a series of seven guiding principles for formulation design of lipid-based delivery systmes are suggested based on an analysis of recent data generated in our laboratories and elsewhere.
Original languageEnglish
Pages (from-to)673 - 691
Number of pages19
JournalAdvanced Drug Delivery Reviews
Issue number6
Publication statusPublished - 2008

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