Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development
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Review Article Theme: Develop Enabling Technologies for Delivering Poorly Water Soluble Drugs: Current Status and Future Perspectives Guest Editors: Ping Gao and Lawrence Yu
Characterising Lipid Lipolysis and Its Implication in Lipid-Based Formulation Development Nicky Thomas,1 René Holm,2 Thomas Rades,1,3 and Anette Müllertz3,4,5
Received 17 June 2012; accepted 30 July 2012; published online 7 September 2012 Abstract. Facing the increasing number of poorly water-soluble drugs, pharmaceutical scientists are required to break new grounds for the delivery of these pharmaceutically problematic drugs. Lipid-based drug delivery systems (LBDDS) have received increased interest as a novel drug delivery platform during the last decades and several successfully marketed products have shown the potential for LBDDS. However, there exists a discrepancy between the clear need for innovative delivery forms and their rational design. In the case of LBDDS, this can be attributed to the complexity of LBDDS after administration. Unlike conventional formulations, LBDDS are susceptible to digestion in the gastrointestinal tract, the interplay of delivery system, drug and physiology ultimately effecting drug disposition. In vitro lipolysis has become an important technique to mimic the enzymatic degradation. For the better understanding of how LBDDS promote drug delivery, in vitro lipolysis requires advanced characterisation methods. In this review, the physiological background of lipid digestion is followed by a thorough summary of the techniques that are currently used to characterise in vitro lipolysis. It would be desirable that the increasing knowledge about LBDDS will foster their rationale development thereby increasing their broader application. KEY WORDS: in vitro digestion; in vitro lipolysis models; lipid-based drug delivery systems; poorly soluble drugs; self-nanoemulsifying drug delivery systems (SNEDDS).
INTRODUCTION It has long been observed that the intake of food, notably lipids, can have profound effects on the absorption and bioavailability of drugs (1). In particular, the bioavailability of poorly water-soluble, lipophilic drugs has been shown to benefit from the concomitant ingestion of lipids, sparking the interest in the use of lipids as potential drug delivery systems (2,3). As a result some compounds formulated as lipid-based drug delivery systems (LBDDS) have entered the market successfully (4). However, there appears some reluctance in the broader utilisation of LBDDS, indicated by the stilllimited number of products commercially available (4,5). This might be attributed to the intricate interplay of LBDDS and the digestive system. After administration, LBDDS are
processed in a complex physiological sequence which is not completely understood. It is this inherent alteration of the drug carrier during its transit through the gastrointestinal tract (GIT) which distinguishes LBDDS from conventional formulations such as tablets. Consequently this attribute asks for protocols capable of assessing and predicting
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