Laboratoire d'Automatique et de Génie des Procédés, UMR-CNRS 5007, Université Claude Bernard Lyon 1, CPE Lyon, Bat 308 G, 43 Boulevard du 11 Novembre 1918, F-69622 Villeurbanne Cedex, France.
Int J Pharm. 2011 Aug 30;415(1-2):53-61. doi: 10.1016/j.ijpharm.2011.05.034. Epub 2011 May 27.
In this study, we present a novel liposome preparation technique suitable for the entrapment of pharmaceutical and cosmetic agents. This new method uses a membrane contactor in a hollow fiber configuration. In order to investigate the process, key parameters influence on the liposome characteristics was studied. It has been established that the vesicle size distribution decreased with the organic phase pressure decrease, the phospholipid concentration decreases and the aqueous to organic phase volume ratio increases. Liposomes were filled with a hydrophobic drug model, spironolactone that could be used for a paediatric medication. The mean size of drug-free and drug-loaded liposomes was, respectively, 113 ± 4 nm and 123 ± 3 nm. The zeta potential of drug-free and drug-loaded liposomes was, respectively, -43 ± 0.7 mV and -23 ± 0.6 mV. High entrapment efficiency values were successfully achieved (93 ± 1.12%). Transmission electron microscopy images revealed nanometric sized and spherical shaped oligo-lamellar vesicles. The release profile showed a rapid and complete release within about 5h. Additionally, special attention was paid on process reproducibility and long term lipid vesicles stability. Results confirmed the robustness of the hollow fiber module based technique. Moreover, the technique is simple, fast and has a potential for continuous production of nanosized liposome suspensions at large scale.
在这项研究中,我们提出了一种适用于包封药物和化妆品的新型脂质体制备技术。这种新方法使用中空纤维构型的膜接触器。为了研究该工艺,研究了关键参数对脂质体特性的影响。结果表明,随着有机相压力的降低、磷脂浓度的降低和水相/有机相体积比的增加,囊泡的粒径分布减小。脂质体中填充了一种疏水性药物模型螺内酯,可用于儿科药物。载药和非载药脂质体的平均粒径分别为 113 ± 4nm 和 123 ± 3nm。载药和非载药脂质体的 zeta 电位分别为-43 ± 0.7mV 和-23 ± 0.6mV。成功实现了高包封效率(93 ± 1.12%)。透射电子显微镜图像显示了纳米级和球形的寡层囊泡。释放曲线表明,约 5 小时内迅速完全释放。此外,还特别注意了工艺重现性和长脂质体稳定性。结果证实了基于中空纤维模块的技术的稳健性。此外,该技术简单、快速,具有在大规模生产纳米脂质体悬浮液的连续生产潜力。