Wu Yu, Chen Jun, Fang Yun, Dong Jie
Drum Tower Clinical College of Integrative Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210008, China.
Pharmaceutical Research Laboratory, College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Zhongguo Zhong Yao Za Zhi. 2016 Aug;41(16):3009-3015. doi: 10.4268/cjcmm20161611.
To prepare the liposomes and transfersomes of brucine, characterize their pharmaceutical properties, and compare their in vitro transdermal permeation properties. The liposomes and transfersomes of brucine were prepared by ammonium sulfate gradient method to investigate their pharmaceutical properties such as the particle size, encapsulation efficiency and deformation. The transdermal permeation properties in vitro of liposome and transfersomes from different prescriptions were compared by using modified Franz-diffustion cells with rat skin as the transdermal barrier. The results showed that the particle size of liposomes and transfersomes for brucine ranged from 100 nm to 150 nm, with even distribution for particle size. As compared with the soybean phosphatidylcholine (SPC) transfersomes, the encapsulation efficiency of complex phospholipid transfersomes was significantly improved. The deformation index of complex phospholipid transfersomes in brucine was 2.09 times and 1.76 times as much as SPC liposomes and SPC transfersomes respectively. The steady state flux of complex phospholipid transfersomes was 3.43 times and 1.41 times as much as SPC liposomes and SPC transfersomes. The steady state flux of the physical mixture of brucine and blank complex phospholipid transfersomes was 2.20 times as much as brucine solution. The concentration of complex phospholipid had effect on transdermal permeation of blank transfersomes. In conclusion, as compared with liposomes, the permeation behavior of transfersomes was significantly improved; complex phospholipid technology can improve the membrane phase behavior of transfersomes, and further improve the deformation index and transdermal flux of transfersomes; in addition, blank transfersomes have promoting effect on transdermal absorption of brucine.
制备马钱子碱脂质体和传递体,表征其药学性质,并比较它们的体外透皮渗透性质。采用硫酸铵梯度法制备马钱子碱脂质体和传递体,考察其粒径、包封率和变形性等药学性质。以大鼠皮肤为透皮屏障,采用改良的Franz扩散池比较不同处方脂质体和传递体的体外透皮渗透性质。结果表明,马钱子碱脂质体和传递体的粒径范围为100 nm至150 nm,粒径分布均匀。与大豆磷脂酰胆碱(SPC)传递体相比,复合磷脂传递体的包封率显著提高。马钱子碱中复合磷脂传递体的变形指数分别是SPC脂质体和SPC传递体的2.09倍和1.76倍。复合磷脂传递体的稳态通量分别是SPC脂质体和SPC传递体的3.43倍和1.41倍。马钱子碱与空白复合磷脂传递体物理混合物的稳态通量是马钱子碱溶液的2.20倍。复合磷脂浓度对空白传递体的透皮渗透有影响。综上所述,与脂质体相比,传递体的渗透行为显著改善;复合磷脂技术可改善传递体的膜相行为,进一步提高传递体的变形指数和透皮通量;此外,空白传递体对马钱子碱的透皮吸收有促进作用。