Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, N.P. Marg, Matunga, Mumbai, 400 019, India.
Pharm Res. 2010 Apr;27(4):655-64. doi: 10.1007/s11095-009-0041-x. Epub 2010 Feb 12.
The investigation was aimed at developing micellar nanocarriers for nose-to-brain delivery of zolmitriptan with the objective to investigate the pathway involved in the drug transport.
The micellar nanocarrier was successfully formulated and characterized for particle size and shape by multi-angle dynamic light scattering, small angle neutron scattering and cryo-transmission electron microscopy. Toxicity and biodistribution studies were carried out in rat. The distribution of the nasally administered labeled micellar nanocarrier in various regions of the rat brain was determined using the brain localization and autoradiography studies.
Micellar nanocarrier of zolmitriptan, with size of around 23 nm, was successfully formulated. The spherical nature of the nanocarrier was confirmed using DLS, SANS and cryo-TEM. Toxicity studies indicated the safety for administration in the nasal cavity. In vivo biodistribution studies indicated the superiority of the developed nanocarrier for brain targeting when compared with the intravenous and nasal solutions of the drug. Brain localization and autoradiography studies illustrated the distribution of the drug in various regions of the brain and revealed a possible nose-to-brain transport pathway for the labeled drug.
The investigation indicated the potential of the developed nanocarrier as an effective new-generation vehicle for brain targeting of zolmitriptan.
本研究旨在开发米库利坦纳米载体，用于佐米曲普坦的脑内递药，旨在研究药物转运途径。
通过多角度动态光散射、小角中子散射和冷冻传输电子显微镜成功地对米库利坦纳米载体进行了粒径和形态的配方和表征。在大鼠中进行了毒性和体内分布研究。采用脑定位和放射自显影研究，确定了鼻腔给予标记的米库利坦纳米载体在大鼠脑内各区域的分布。
成功地制备了佐米曲普坦的纳米载体，粒径约为 23nm。DLS、SANS 和冷冻-TEM 证实了纳米载体的球形性质。毒性研究表明，鼻腔给药是安全的。体内分布研究表明，与药物的静脉和鼻腔溶液相比，开发的纳米载体具有更好的脑靶向优势。脑定位和放射自显影研究说明了药物在大脑各个区域的分布，并揭示了标记药物可能的经鼻脑内转运途径。
本研究表明，所开发的纳米载体有潜力成为佐米曲普坦脑靶向的新一代有效载体。
