Preparation and characterization of quercetin-loaded polymethyl methacrylate microcapsules using a polyol-in-oil-in-polyol emulsion solvent evaporation method

被引:26
|
作者
Lee, Dong-Hwan [2 ]
Sim, Gwan-Sub [2 ]
Kim, Jin-Hwa [2 ]
Lee, Geun-Soo [2 ]
Pyo, Hyeong-Bae [2 ]
Lee, Bum-Chun [1 ]
机构
[1] Dalhousie Univ, Fac Med, Dept Biochem & Mol Biol, Halifax, NS B3H 1X5, Canada
[2] Hanbul Cosmet Co, R&D Ctr, Chungbuk 369834, South Korea
关键词
D O I
10.1211/jpp.59.12.0002
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Flavonoids and related compounds exhibit a wide range of useful pharmacological properties but present challenges related to their stability and solubility in commonly available solvents. In this study, polymethyl methacrylate (PMMA) microcapsules were prepared using a novel polyol-in-oil-in-polyol (P/O/P) emulsion solvent evaporation method as a means of stabilizing the flavonoids, using quercetin as a model flavonoid drug. The morphology of the microcapsules was evaluated using a scanning electron microscope, revealing a spherical shape with a smooth surface. The cross-section image of the PMMA microcapsules prepared with an amphiphilic polymer in the inner polyol phase showed that the microcapsule was filled with several submicron microspheres. The mean diameter varied from 1.03 +/- 0.12 mu m to 2.39 +/- 0.42 mu m, and the encapsulation efficiency ranged from 12.7% to 26.9%. When free quercetin was stored at 42 degrees C, the residual quercetin content gradually decreased to 18% over 28 days as a result of oxidation. However, when encapsulated in PMMA microcapsules with an amphiphilic polymer in the inner polyol phase, the residual quercetin content decreased to just 82%. In-vitro release studies indicated a sustained release pattern throughout the 36-h study. The release kinetics of the microcapsules with an amphiphilic polymer followed a diffusion-controlled mechanism and the microcapsule without amphiphilic polymer followed an anomalous diffusion behaviour. This study suggests that the novel P/O/P emulsion solvent evaporation method can be applied to the encapsulation of flavonoids.
引用
收藏
页码:1611 / 1620
页数:10
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