A comparison between conventional liposome and drug-cyclodextrin complex in liposome system.

A drug-cyclodextrin complex in liposome system was prepared in order to make a comparison with conventional risperidone-loaded liposome. Thin film hydration, reverse phase evaporation and ethanol injection methods were taken as preparation means to obtain the two types of liposome. Differential thermal analysis (DTA) and transmission electron microscopy (TEM) were used to investigate the thermal characters of inclusion complexes and morphology of liposome, respectively. Particle size, zeta potential and encapsulation efficiency were studied by light scattering analysis and ultrafiltration. In vitro release was carried out in the pH 7.4 phosphate buffer solution and samples were collected at the certain time. As a result, drug-cyclodextrin complex in liposome prepared by various methods displayed lower encapsulation efficiency than conventional liposome. However, size was larger and its stability was better than the latter. The second release phase of novel delivery system was slightly slower after initial burst release at the first phase, while the conventional liposome displayed a more regular trait. Thus, the novel liposome have potential to be developed as co-administration formulation with long-acting injection.

Efficient delivery of Notch1 siRNA to SKOV3 cells by cationic cholesterol derivative-based liposome.

A novel cationic cholesterol derivative-based small interfering RNA (siRNA) interference strategy was suggested to inhibit Notch1 activation in SKOV3 cells for the gene therapy of ovarian cancer. The cationic cholesterol derivative, N-(cholesterylhemisuccinoyl-amino-3-propyl)-N, N-dimethylamine (DMAPA-chems) liposome, was incubated with siRNA at different nitrogen-to-phosphate ratios to form stabilized, near-spherical siRNA/DMAPA-chems nanoparticles with sizes of 100-200 nm and zeta potentials of 40-50 mV. The siRNA/DMAPA-chems nanoparticles protected siRNA from nuclease degradation in 25% fetal bovine serum. The nanoparticles exhibited high cell uptake and Notch1 gene knockdown efficiency in SKOV3 cells at an nitrogen-to-phosphate ratio of 100 and an siRNA concentration of 50 nM. They also inhibited the growth and promoted the apoptosis of SKOV3 cells. These results may provide the potential for using cationic cholesterol derivatives as efficient nonviral siRNA carriers for the suppression of Notch1 activation in ovarian cancer cells.