Abstract
Gelucire<sup>®<sup/> 44/14, a lauroyl polyoxylglycerides obtained by polyglycolysis of hydrogenated coconut oil with PEG-32, is used to increase the oral bioavailability of poorly-water soluble drugs. It is a solid dispersion composed of a PEG ester fraction under a lamellar phase of 120 Å with a helical conformation and an acylglycerol fraction under a hexagonal packing. This excipient spontaneously evolves to its most stable phase of 120 Å after storage at 25 °C for 21 hours leading to physically stable formulations. Gelucire<sup>®<sup/> 44/14 is a hydrophilic system that hydrates and swells in contact with water and forms cubic mesophases before complete erosion/emulsification. It is also lipolyzed by various enzymes such as gastric lipase or carboxyl ester hydrolase. After an in vitro gastrointestinal lipolysis simulation, the main components remaining are mono and diesters of PEG-32. These amphiphilic metabolites can explain the beneficial role of Gelucire<sup>®<sup/> 44/14 on the solubility of poorly-water soluble drugs such as cinnarizine even after partial lipolysis of the lipid-based system. Finally that excipient can also increase the bioavailability of active substances by interacting with enterocyte-based proteins like P-glycoprotein or cytochromes P450.
Highlights
Most of the new chemical entities developed by the pharmaceutical industry are practically insoluble in water and possess a low oral bioavailability [1]
In order to efficiently formulate these active substances for the oral route, formulators should either increase the dissolution of the drug in the gastro-intestinal tract or predissolve the drug into the formulation and avoid its precipitation when in contact with the biological fluids
The combined use of X-Ray Diffraction (XRD) and Differential Scanning Calorimetry (DSC) allows the detection of all polymorphs formed after various thermal treatments ranging from quenching into liquid nitrogen to slow crystallization
Summary
Most of the new chemical entities developed by the pharmaceutical industry are practically insoluble in water and possess a low oral bioavailability [1] These poorly-water soluble molecules are classified in the class 2 and 4 of the Biopharmaceutics Classification System [2]. A classification of these lipid-based systems was introduced and characterized [3] and in addition, many formulation techniques have been developed to produce solid or semi-solid systems [4]. Among these self-emulsifying systems Gelucire® 44/14, a PEG-32 lauroyl polyoxylglycerides (Gattefossé SAS, Saint-Priest, France), is obtained by polyglycolysis of hydrogenated coconut oil (medium and long chain triacylglycerols) and PEG-32. The aim of this paper is to present the physical and biopharmaceutical characterizations needed to develop a successful formulation with Gelucire® 44/14
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