Hung Chi-Feng, Chen Jan-Kan, Liao Mei-Hui, Lo Huey-Ming, Fang Jia-You
School of Medicine, Fu Jen Catholic University, Taipei, Taiwan.
J Nanosci Nanotechnol. 2006 Sep-Oct;6(9-10):2950-8. doi: 10.1166/jnn.2006.420.
Nano- and submicron-sized vesicles are beneficial for the controlled delivery of drugs. Resveratrol, the main active polyphenol in red wine, was incorporated into various combinations of emulsions and liposomes to examine its physicochemical characteristics and cardiovascular protection. The blends of emulsion-liposome were composed of coconut oil, soybean lecithin, glycerol formal, and non-ionic surfactants. Multiple systems were assessed by evaluating the droplet size, surface charge, drug encapsulation, release rate, and stability. The vesicle diameter of the systems ranged from 114 to 195 nm. The liposomal vesicles in the systems had smaller diameters (of 43 approximately 56 nm) (F6 and F7). Drug encapsulation of approximately 70% were achieved by the vesicles. The inclusion of resveratrol in these systems retarded the drug release in both the presence and absence of plasma in vitro. The emulsion-liposome blends which incorporated Brij 98 (F5) exhibited the slowest release at zero-order for resveratrol delivery. Treatment using resveratrol in the blended formulations dramatically inhibited vascular intimal thickening, which was tested in an experimental model in which endothelial injury was produced in normal rat carotid arteries. Intraperitoneal injection of the multiple systems was associated with no or negligible liver and kidney toxicity. We concluded that encapsulation by the emulsion-liposome blends is a potent way to enhance the preventative and therapeutic benefits of resveratrol.
纳米和亚微米级囊泡有利于药物的控释。白藜芦醇是红酒中的主要活性多酚，被纳入乳液和脂质体的各种组合中，以研究其理化特性和心血管保护作用。乳液 - 脂质体混合物由椰子油、大豆卵磷脂、甘油甲醛和非离子表面活性剂组成。通过评估液滴大小、表面电荷、药物包封、释放速率和稳定性来评估多种体系。这些体系的囊泡直径范围为114至195纳米。体系中的脂质体囊泡直径较小（约43至56纳米）（F6和F7）。囊泡实现了约70%的药物包封。在这些体系中加入白藜芦醇在体外有血浆和无血浆存在的情况下均延缓了药物释放。含有Brij 98（F5）的乳液 - 脂质体混合物在白藜芦醇递送方面表现出最慢的零级释放。在正常大鼠颈动脉产生内皮损伤的实验模型中测试发现，使用混合制剂中的白藜芦醇进行治疗可显著抑制血管内膜增厚。腹腔注射多种体系与无肝脏和肾脏毒性或毒性可忽略不计相关。我们得出结论，乳液 - 脂质体混合物包封是增强白藜芦醇预防和治疗益处的有效方法。
