Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies.
Oral lipid-based drug delivery systems may include a broad range of oils, surfactants, and cosolvents. This diversity makes comparison of lipid-based formulations difficult. Although the relationship between formulation and drug absorption is understood at a conceptual level, performance in vivo cannot be predicted with confidence at present. The Lipid Formulation Classification System (LFCS) identifies the factors which are likely to affect performance in vivo. There is now a need to establish performance criteria which will facilitate in vitro-in vivo correlation studies. In this review we discuss the properties of excipients, and identify criteria for selection of excipients for lipid-based formulations. Excipients are discussed in the context of the LFCS, our existing knowledge of the fate of these materials during dispersion and digestion, and the likely consequences of their use in formulations. We outline the formulation strategies that can be used for each type of lipid formulation, and suggest a framework for the in vitro testing of each type. Finally we address the choice of lipid formulations in relation to the physicochemical properties of the drug.
Pouton
Colin W
CW
Department of Pharmaceutical Biology, Victorian College of Pharmacy, Monash University (Parkville Campus), Victoria 3052, Australia. colin.pouton@vcp.monash.edu.au
Porter
Christopher J H
CJ
D000284:Administration, Oral; D002626:Chemistry, Pharmaceutical / Q000145:classification; D005079:Excipients / Q000737:chemistry*; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D009821:Oils / Q000737:chemistry; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry
D005079:Excipients; D008055:Lipids; D009821:Oils; D004364:Pharmaceutical Preparations; D012997:Solvents; D013501:Surface-Active Agents