Preparation and Evaluation of Lipid-Based Liquid Crystalline Formulation of Fenofibrate

非诺贝特脂质基液晶制剂的制备与评价

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Abstract

BACKGROUND: Many drugs have poor water solubility and so the oral delivery of such drugs is usually associated with limitation of low bioavailability and lack of dose proportionality. Lipid-based liquid crystal (LC) systems are excellent potential formulations for increasing dissolution and bioavailability of drugs. The aim of the present study was to formulate lipid-based LC containing fenofibrate (FFB) as a hydrophobic drug. MATERIALS AND METHODS: The studied variables included lipid and stabilizer concentrations and the type of stabilizer. The LC formation was identified by the polarized optical microscopic method. The effects of variables on formulation characteristics such as particle size, drug release, and rheological behavior were evaluated. RESULTS: The results showed that the prepared formulations had the particle size between 42 and 503 nm. The drug release profiles showed that FFB had the continuous release from the formulations and the highest dissolution efficiency was seen in formulation prepared by 1.5% of glyceryl monostearate and 0.5% of Pluronic F127 as the stabilizer. The change of stabilizer type from colloidal silica to Pluronic F127 increased the drug release, significantly. CONCLUSIONS: In the most formulations of FFB LCs, the DE% was more than the pure drug, and therefore, it seems that the liquid crystalline formulations can be effective for enhancing drug release. Furthermore, drug release rate depended on the stabilizer type so that the presence of colloidal silica caused slower drug release compared to Pluronic F127.

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