College of Life Science, Jilin University, Jilin, People's Republic of China.
Int J Nanomedicine. 2013;8:421-30. doi: 10.2147/IJN.S37984. Epub 2013 Jan 24.
The aim of this study was to develop an optimal niosomal system to deliver Ginkgo biloba extract (GbE) with improved oral bioavailability and to replace the conventional GbE tablets.
In this study, the film dispersion-homogenization method was used to prepare GbE niosomes. The resulting GbE niosome suspension was freeze-dried or spray-dried to improve the stability of the niosomes. GbE-loaded niosomes were formulated and characterized in terms of their morphology, particle size, zeta potential, entrapment efficiency, and angle of repose, and differential scanning calorimetry analysis was performed. In vitro release and in vivo distribution studies were also carried out.
The particle size of the optimal delivery system prepared with Tween 80, Span 80, and cholesterol was about 141 nm. There was a significant difference (P < 0.05) in drug entrapment efficiency between the spray-drying method (about 77.5%) and the freeze-drying method (about 50.1%). The stability study revealed no significant change in drug entrapment efficiency for the GbE niosomes at 4°C and 25°C after 3 months. The in vitro release study suggested that GbE niosomes can prolong the release of flavonoid glycosides in phosphate-buffered solution (pH 6.8) for up to 48 hours. The in vivo distribution study showed that the flavonoid glycoside content in the heart, lung, kidney, brain, and blood of rats treated with the GbE niosome carrier system was greater than in the rats treated with the oral GbE tablet (P < 0.01). No flavonoid glycosides were detected in the brain tissue of rats given the oral GbE tablets, but they were detected in the brain tissue of rats given the GbE niosomes.
Niosomes are a promising oral system for delivery of GbE to the brain.
本研究旨在开发一种最优的脂质体系统，以提高银杏叶提取物（GbE）的口服生物利用度，并替代传统的 GbE 片剂。
本研究采用薄膜分散-匀化法制备 GbE 脂质体。所得 GbE 脂质体混悬液经冷冻干燥或喷雾干燥，以提高脂质体的稳定性。对载 GbE 脂质体进行了形态学、粒径、Zeta 电位、包封率和休止角的评价，并进行了差示扫描量热分析。同时进行了体外释放和体内分布研究。
采用 Tween 80、Span 80 和胆固醇制备的最佳递药系统的粒径约为 141nm。喷雾干燥法（约 77.5%）和冷冻干燥法（约 50.1%）的药物包封率有显著差异（P<0.05）。稳定性研究表明，GbE 脂质体在 4°C 和 25°C 下放置 3 个月后，药物包封率无明显变化。体外释放研究表明，GbE 脂质体可将黄酮苷类在磷酸盐缓冲液（pH6.8）中的释放时间延长至 48 小时。体内分布研究表明，给予 GbE 脂质体载体系统的大鼠心脏、肺、肾、脑和血液中的黄酮苷类含量大于给予口服 GbE 片剂的大鼠（P<0.01）。给予口服 GbE 片剂的大鼠脑组织中未检测到黄酮苷类，而给予 GbE 脂质体的大鼠脑组织中则检测到。
脂质体是一种有前途的口服 GbE 递药系统，可将 GbE 递送至脑部。
