Department of Pharmaceutical Technology, Gazi University Faculty of Pharmacy, Ankara.
Drug Dev Ind Pharm. 2011 Jul;37(7):775-89. doi: 10.3109/03639045.2010.541262. Epub 2011 Jan 14.
The aim of this study was to determine the transportations of rivastigmine containing from various liposome formulations through Madin Darby Canine Kidney (MDCK) cells monolayer and to compare the in vitro test results with in vivo. There is no other liposome formulation of rivastigmine and the transportations of rivastigmine through MDCK cell monolayers or related study available in the literature. Cytotoxicity (MTT) test was used to determine cell viabilities. The effect of sodium-taurocholate or dimethyl-beta-cyclodextrine as penetration enhancer was also investigated. Characterization and stability studies for liposome formulations were performed. Permeation experiments of rivastigmine were performed through MDCK cells and dialysis membrane. The kinetic of release from liposomes was also investigated. The highest apparent permeability coefficient (log. values) was obtained with sodium-taurocholate liposomes for -1.15 ± 0.16 for MDCK cell. Rivastigmine liposomes and solutions were also administered to mice orally and intraperitonally. Acetylcholinesterase (AChE) activity was determined by Ellman method. AChE% inhibition values were calculated for both blood and brain after administration of rivastigmine solution and liposomes. The highest AChE inhibition was observed for rivastigmine-sodium-taurocholate liposomes. Histological observations of the mice' brains were performed under transmission electron microscope (TEM). The histological results were also indicated and supported all these findings.
本研究旨在确定不同脂质体配方中含有利伐斯的明的转运情况，通过 Madin Darby 犬肾 (MDCK) 细胞单层，并将体外试验结果与体内进行比较。目前尚无其他利伐斯的明脂质体配方，也没有文献报道利伐斯的明通过 MDCK 细胞单层的转运或相关研究。细胞毒性 (MTT) 试验用于测定细胞活力。还研究了牛磺胆酸钠或二甲基-β-环糊精作为渗透增强剂的作用。对脂质体配方进行了特性和稳定性研究。通过 MDCK 细胞和透析膜进行了利伐斯的明渗透实验。还研究了从脂质体中释放的动力学。对于 MDCK 细胞，牛磺胆酸钠脂质体的表观渗透系数 (log 值) 最高，为 -1.15 ± 0.16。还通过口服和腹腔内给药将利伐斯的明脂质体和溶液施用于小鼠。乙酰胆碱酯酶 (AChE) 活性通过 Ellman 法测定。给药后，计算了血液和大脑中的 AChE%抑制值利伐斯的明溶液和脂质体。牛磺胆酸钠脂质体观察到最高的 AChE 抑制。在透射电子显微镜 (TEM) 下对小鼠大脑进行了组织学观察。组织学结果也表明并支持了所有这些发现。
