Tan Sim Ling, Stanslas Johnson, Basri Mahiran, Abedi Karjiban R A, Kirby Brian P, Sani Dahiru, Basri Hamidon Bin
Department of Medicine, Faculty of Medicine and Health Sciences, University Putra Malaysia, 43400 Serdang, Selangor, Malaysia.
Curr Drug Deliv. 2015;12(6):795-804. doi: 10.2174/1567201812666150901112544.
Carbamzepine (CBZ) was encapsulated in a parenteral oil-in-water nanoemulsion, in an attempt to improve its bioavailability. The particle size, polydispersity index and zeta potential were measured using dynamic light scattering. Other parameters such as pH, osmolality, viscosity, drug loading efficiency and entrapment efficiency were also recorded. Transmission electron microscopy revealed that emulsion droplets were almost spherical in shape and in the nano-range. The in vitro release profile was best characterized by Higuchi's equation. The parenteral nanoemulsion of CBZ showed significantly higher AUC0→5, AUC0→∞, AUMC0→5, AUMC0→∞, Cmax and lower clearance than that of CBZ solution in plasma. Additionally, parenteral nanoemulsion of CBZ showed significantly higher AUC0→∞, AUMC0→∞ and Cmaxthan that of CBZ solution in brain. The parenteral nanoemulsion of CBZ could therefore use as a carrier, worth exploring further for brain targeting.
卡马西平（CBZ）被包裹于一种肠胃外水包油纳米乳剂中，旨在提高其生物利用度。使用动态光散射法测量粒径、多分散指数和zeta电位。还记录了其他参数，如pH值、渗透压、粘度、载药效率和包封率。透射电子显微镜显示乳剂液滴几乎呈球形且处于纳米范围。体外释放曲线最适合用Higuchi方程来描述。与血浆中的CBZ溶液相比，CBZ肠胃外纳米乳剂的AUC0→5、AUC0→∞、AUMC0→5、AUMC0→∞、Cmax显著更高，清除率更低。此外，与脑中的CBZ溶液相比，CBZ肠胃外纳米乳剂的AUC0→∞、AUMC0→∞和Cmax显著更高。因此，CBZ肠胃外纳米乳剂可作为一种载体，值得进一步探索其脑靶向作用。
