Lee Dong-Hwan, Sim Gwan-Sub, Kim Jin-Hwa, Lee Geun-Soo, Pyo Hyeong-Bae, Lee Bum-Chun
R & D Center, Hanbul Cosmetics Co., 72-7, Yongsung-ri, Samsung-myun, Umsung-kun, Chungbuk 369-834, Republic of Korea.
J Pharm Pharmacol. 2007 Dec;59(12):1611-20. doi: 10.1211/jpp.59.12.0002.
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 microm to 2.39+/-0.42 microm, 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.
黄酮类化合物及相关化合物具有广泛的有益药理特性,但在常用溶剂中的稳定性和溶解性方面存在挑战。在本研究中,采用一种新型的多元醇包油型多元醇(P/O/P)乳液溶剂蒸发法制备聚甲基丙烯酸甲酯(PMMA)微胶囊,以槲皮素作为黄酮类药物模型来稳定黄酮类化合物。使用扫描电子显微镜对微胶囊的形态进行评估,结果显示其呈表面光滑的球形。在内层多元醇相中使用两亲聚合物制备的PMMA微胶囊的横截面图像表明,微胶囊内部填充有几个亚微米级的微球。平均直径在1.03±0.12微米至2.39±0.42微米之间,包封率在12.7%至26.9%之间。当游离槲皮素在42℃下储存时,由于氧化作用,28天内槲皮素残留量逐渐降至18%。然而,当将其包封于内层多元醇相中含有两亲聚合物的PMMA微胶囊时,槲皮素残留量仅降至82%。体外释放研究表明,在整个36小时的研究过程中呈现出持续释放模式。含有两亲聚合物的微胶囊的释放动力学遵循扩散控制机制,而不含两亲聚合物的微胶囊则呈现出异常扩散行为。本研究表明,新型的P/O/P乳液溶剂蒸发法可应用于黄酮类化合物的包封。