KLEU College of Pharmacy , Belgaum, Karnataka , India and.
Drug Deliv. 2015;22(5):647-51. doi: 10.3109/10717544.2013.860502. Epub 2013 Nov 27.
Gemcitabine-loaded solid lipid nanoparticles (SLNs) were produced by double emulsification technique using stearic acid as lipid, soy lecithin as surfactant and sodium taurocholate as cosurfactant. Prepared nanoparticles are characterized for particle size and surface morphology using scanning electron microscopy (SEM). Particle yield, entrapment efficiency and zeta potential were also determined. In-vitro release studies were performed in phosphate-buffered saline (PBS) pH 7.4 using metabolic shaker. The formulation F6 with maximum entrapment efficiency 72.42% and satisfactory in-vitro release was selected. In-vivo tissue distribution to liver, spleen, lung, heart and kidneys of optimized formulation followed by stability study under specific conditions were also determined. This investigation has shown preferential drug targeting to liver followed by spleen, lungs, kidneys and heart. Stability studies showed no significant change in the particle size followed with very slight decrease in entrapment efficiency at 25 ± 2 °C/60 ± 5% RH over a period of three months.
载盐酸吉西他滨固体脂质纳米粒（SLNs）采用双重乳化技术，以硬脂酸为脂质，大豆卵磷脂为表面活性剂，牛磺胆酸钠为助表面活性剂制备而成。采用扫描电子显微镜（SEM）对纳米粒的粒径和表面形态进行了表征。还测定了载药纳米粒的得率、包封率和 Zeta 电位。在 pH7.4 的磷酸盐缓冲液（PBS）中采用代谢摇床进行体外释放研究。选择包封率最高（72.42%）、体外释放效果满意的 F6 制剂。还对优化后的制剂进行了体内组织分布（肝脏、脾脏、肺、心脏和肾脏）及特定条件下的稳定性研究。研究表明，药物具有向肝脏和脾脏的优先靶向性，随后是肺部、肾脏和心脏。稳定性研究表明，在三个月的时间内，载药纳米粒的粒径没有明显变化，包封率略有下降。
