Deng Yun, Xu Jinku, Li Xinsong
Biomaterials and Drug Delivery Laboratories, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China.
Zhongguo Zhong Yao Za Zhi. 2010 Feb;35(3):301-4.
To prepare eye drops of puerarin liposomes and investigate its lacrimal pharmacokinetics in rabbit tears.
Puerarin liposomes were prepared by reverse phase evaporation technique. The liposomes and free puerarin were separated by SephadexG-50 chromatography and then encapsulation ratio of liposomes was determined in detail. Micromorphology of liposome particles was observed by electronic transmission microscope and the size distribution of the liposomes was analyzed by laser particle size analyzer. The concentration of puerarin in rabbit's tears was determined by HPLC after ocular administration of 50 microL puerarin liposomes while puerarin eye drops was chosen as control with the same puerarin concentration. The pharmacokinetic parameters were calculated by software program 3P97 according to one-compartment mode.
Global liposome nanoparticles with diameter of about 195.7 nm were prepared successfully. The encapsulation ratio of puerarin in the liposomes was 48.3%. The mean residence time (MRT) value and the area under concentration (AUC) of puerarin in liposome were 3.89 and 3.06 times more than those of puerarin eye drops.
Liposomes as a drug carrier can greatly increase the concentration of puerarin in tears, enhance the pre-ocular retention time than that of eye drops.
制备葛根素脂质体滴眼液并研究其在兔泪液中的泪液药代动力学。
采用逆相蒸发法制备葛根素脂质体。通过葡聚糖凝胶G - 50柱色谱法分离脂质体和游离葛根素，然后详细测定脂质体的包封率。用电子透射显微镜观察脂质体颗粒的微观形态，并用激光粒度分析仪分析脂质体的粒径分布。眼部滴注50 μL葛根素脂质体后，用高效液相色谱法测定兔泪液中葛根素的浓度，同时选用相同葛根素浓度的葛根素滴眼液作为对照。根据一室模型，用软件程序3P97计算药代动力学参数。
成功制备出粒径约为195.7 nm的球形脂质体纳米粒。葛根素在脂质体中的包封率为48.3%。脂质体中葛根素的平均驻留时间（MRT）值和浓度 - 时间曲线下面积（AUC）分别是葛根素滴眼液的3.89倍和3.06倍。
脂质体作为药物载体可显著提高泪液中葛根素的浓度，比滴眼液延长眼表滞留时间。
