Hung Chi-Feng, Fang Chia-Lang, Liao Mei-Hui, Fang Jia-You
School of Medicine, Fu-Jen Catholic University, Taipei, Taiwan.
Department of Pathology, College of Medicine, Taipei Medical University, Taipei, Taiwan.
Int J Pharm. 2007 Apr 20;335(1-2):193-202. doi: 10.1016/j.ijpharm.2006.11.016. Epub 2006 Nov 11.
An emulsion system composed of vitamin E, coconut oil, soybean phosphatidylcholine, non-ionic surfactants, and polyethylene glycol (PEG) derivatives (referred to as the tocol emulsion) was characterized in terms of its physicochemical properties, drug release, in vivo efficacy, toxicity, and stability. Systems without vitamin E (referred to as the lipid emulsion) and without any oils (referred to as the aqueous micelle system) were prepared for comparison. A lipophilic antioxidant, resveratrol, was used as the model drug for emulsion loading. The incorporation of Brij 35 and PEG derivatives reduced the vesicle diameter to <100nm. The inclusion of resveratrol into the emulsions and aqueous micelles retarded the drug release. The in vitro release rate showed a decrease in the order of aqueous micelle system>tocol emulsion>lipid emulsion. Treatment of resveratrol dramatically reduced the intimal hyperplasia of the injured vascular wall in rats. There was no significant difference in this reduction when resveratrol was delivered by either emulsion or the aqueous micelle system. The percentages of erythrocyte hemolysis by the emulsions and aqueous micelle system were approximately 0 and approximately 10%, respectively. Vitamin E prevented the aggregation of emulsion vesicles. The mean vesicle size of the tocol emulsion remained unchanged during 30 days at 37 degrees C. The lipid emulsion and aqueous micelle system, respectively, showed 11- and 16-fold increases in vesicle size after 30 days of storage.
一种由维生素E、椰子油、大豆磷脂酰胆碱、非离子表面活性剂和聚乙二醇（PEG）衍生物组成的乳液体系（称为生育酚乳液），对其物理化学性质、药物释放、体内疗效、毒性和稳定性进行了表征。制备了不含维生素E的体系（称为脂质乳液）和不含任何油的体系（称为水性胶束体系）用于比较。一种亲脂性抗氧化剂白藜芦醇用作乳液负载的模型药物。加入Brij 35和PEG衍生物可将囊泡直径减小至<100nm。将白藜芦醇包入乳液和水性胶束中可延缓药物释放。体外释放速率按水性胶束体系>生育酚乳液>脂质乳液的顺序降低。白藜芦醇治疗显著降低了大鼠受损血管壁的内膜增生。当通过乳液或水性胶束体系递送白藜芦醇时，这种降低没有显著差异。乳液和水性胶束体系引起的红细胞溶血百分比分别约为0和约10%。维生素E可防止乳液囊泡聚集。生育酚乳液的平均囊泡大小在37℃下30天内保持不变。脂质乳液和水性胶束体系在储存30天后囊泡大小分别增加了11倍和16倍。
