Dinc Essiz

New perspective for the treatment of Alzheimer diseases: Liposomal rivastigmine formulations

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.

Prophylactic effect of N-acetylcysteine against sodium fluoride-induced blood oxidative stress in mice.

Ninety female Balb/c mice were used. The animals were allocated to evenly six groups. While the first group was maintained as control, Groups 3, 4, 5, and 6 were administered 750 ppm, 1500 ppm, 3000 ppm, and 6000 ppm of N-acetylcysteine, respectively, for a period of 15 days. After day 15, Groups 2-6 were administered sodium fluoride, containing 100 ppm fluoride in drinking water, for another 15 days. Plasma malondialdehyde (MDA) levels and erythrocyte superoksid dismutase (SOD) and catalase (CAT) activities were determined at the beginning of the trial and on days 15 and 30. According to the data obtained in the present study, N-acetylcysteine, when administered at the indicated doses, did not produce a significant alteration in any of the three parameters investigated. On the other hand, while the plasma MDA level was determined to have increased significantly, erythrocyte SOD and CAT activities were ascertained to have decreased significantly in the group, which was administered sodium fluoride alone on day 30. In the groups, which were administered N-acetylcysteine prior to sodium fluoride, however, it was observed that, after sodium fluoride administration, plasma MDA levels and erythrocyte SOD and CAT activities drew closer to the values of the control group.