Department of Pharmaceutical Sciences & Technology Institute of Chemical Technology, N.P. Marg, Matunga, Mumbai 400 019, India.
Nanomedicine (Lond). 2010 Jun;5(4):575-87. doi: 10.2217/nnm.10.28.
The investigation was aimed at designing a micellar nanocarrier of sumatriptan for nose-to-brain delivery and to identify the probable pathway of drug transport to the brain.
MATERIALS & METHODS: Micellar nanocarriers were formulated using various safe and acceptable excipients. Optimized formulation was characterized for particle size by multiangle dynamic light scattering, small-angle neutron scattering and cryo-transmission electron microscopy. (99m)Tc was used as a radiolabeling agent to radiolabel sumatriptan for in vivo studies.
Various characterization studies demonstrated the nanometric, homogenous and spherical nature of the developed micellar nanocarrier. Biodistribution and autoradiography studies in rats showed a significantly higher brain uptake of sumatriptan micellar nanocarrier as compared with sumatriptan solution.
Preliminary investigations in rats indicated the potential of the developed micellar nanocarrier for nose-to-brain delivery of sumatriptan. These investigations in lower animals provided an excellent lead to further evaluate the formulation in higher animals and finally in clinical settings.
本研究旨在设计一种用于经鼻脑递药的舒马曲坦胶束纳米载体，并确定药物向脑内转运的可能途径。
采用多种安全且可接受的辅料制备胶束纳米载体。采用多角度动态光散射、小角中子散射和冷冻传输电子显微镜对优化后的载体制备进行粒径表征。（99m）Tc 被用作放射性标记物，对舒马曲坦进行放射性标记，用于体内研究。
各种表征研究表明，所开发的胶束纳米载体具有纳米级、均一和球形的特性。大鼠的体内分布和放射自显影研究表明，与舒马曲坦溶液相比，舒马曲坦胶束纳米载体具有更高的脑摄取。
在大鼠中的初步研究表明，所开发的胶束纳米载体具有经鼻脑递运舒马曲坦的潜力。这些在低等动物中的研究为进一步在高等动物中以及最终在临床环境中评估该制剂提供了良好的依据。
