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To microemulsify the entire oil and water phases, ME requires high surfactant concentrations. The value of the particle surface charges indicates the stability of ME at the macroscopic level. However, in order to provide a very low interfacial tension (≤10 -3 mN/m), the surface charge properties are studied through the zeta potential. These characteristics seem ideal for an oral formulation of a poorly aqueous soluble drug. They are transparent, isotropic, and thermodynamically stable with a droplet size usually in the range of 20-200 nm. They are systems of water, oil, and surfactant frequently combined with a cosurfactant. Microemulsions (MEs) are a lipid-based formulation. Various formulation strategies have tried to overcome this problem such as solid dispersion, complexations with cyclodextrins, and coprecipitates. This active metabolite presents a poor bioavailability which has been considered as its main drawback. As a prodrug, fenofibrate will be rapidly converted after oral administration by hydrolysis of the ester into an active and major metabolite, the fenofibric acid.
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It is a lipid-lowering agent used to treat high levels of cholesterol and triglyceride.
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It is a class II drug according to the Biopharmaceutical Classification System (BCS) since it has a high permeability. Introductionįenofibrate is a poorly water soluble drug, and it is neutral and lipophilic (log ). Thus, this paper shows that the composition and the characteristics of ME may be explored to increase the permeability of fenofibrate across the GI membrane. The use of the excipients that inhibit GI P-glycoprotein may be a new perspective. This suggests that the carrier-mediated uptake/efflux may present the dominant transport mechanism of fenofibrate. The ex vivo technique, performed using the everted gut sac model, showed a 2.5-fold higher permeability.
#Examples of bcs class 2 drugs list free#
The passive permeability evaluated using Sartorius was 1.6 times higher than that of the free drug. The optimized ME showed a droplet size of 48.5 nm and physical stability. The classical method of ME development was coupled with the factorial design in order to minimize the droplet size using a low concentration of surfactant. A quick selection of excipients was made based on the capacity of solubilization and the value of hydrophilic-lipophilic balance. Its main drawback is the low bioavailability of the metabolite. It undergoes a nearly complete presystemic metabolism. It is a prodrug that is converted rapidly after oral administration into a major active metabolite which is the fenofibric acid. Our work is aimed at exploring the composition and the properties of microemulsion (ME), as a drug delivery system, to enhance the permeability across the gastrointestinal (GI) barrier of fenofibrate, a BCS class II drug.
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