Optimized self-microemulsifying drug delivery systems (SMEDDS) for enhanced oral bioavailability of astilbin.
The main purpose of this research work was to design an optimized self micro-emulsifying drug delivery system (SMEDDS) to enhance the bioavailability of the poor water soluble drug, astilbin. The solubility of astilbin was evaluated in various vehicles. Pseudoternary phase diagrams were used to select the components and their ranges by evaluating the micro-emulsification area. Central composite design was applied to optimize the properties of the formulation, including particle size, polydispersity index, drug loading capacity and effective intestinal permeability. The optimized SMEDDS characteristics were investigated including the study of factors influencing particle size and showed the stability of microemulsion when varying the pH and volume of diluents. In vitro drug release profile study was performed using the reverse dialysis method where 95% of the drug was released after 4 h. The developed astilbin SMEDDS was subjected to bioavailability studies in beagle dogs by LC-MS and showed a significant enhancement of bioavailability, indicating the possibility of using SMEDDS as possible drug carrier for astilbin.
Department of Pharmaceutics, China Pharmaceutical University, Nanjing, China. mezghrani_omar@yahoo.fr
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D000042:Absorption; D000465:Algorithms; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000032:analysis / Q000493:pharmacokinetics; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004285:Dogs; D016503:Drug Delivery Systems; D004655:Emulsions; D044948:Flavonols / Q000008:administration & dosage* / Q000032:analysis / Q000493:pharmacokinetics; D006863:Hydrogen-Ion Concentration; D008297:Male; D009821:Oils; D010316:Particle Size; D012995:Solubility; D013501:Surface-Active Agents; D013535:Suspensions
D000975:Antioxidants; D004655:Emulsions; D044948:Flavonols; D009821:Oils; D013501:Surface-Active Agents; D013535:Suspensions; C099069:astilbin