Kumar Mukesh, Misra Ambikanandan, Mishra A K, Mishra Pushpa, Pathak Kamla
Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura, India.
J Drug Target. 2008 Dec;16(10):806-14. doi: 10.1080/10611860802476504.
The objective of the present study was to optimize olanzapine nanoemulsion (ONE), for nose-to-brain delivery. The nanoemulsions and olanzapine mucoadhesive nanoemulsions (OMNEs) were prepared using water titration method and characterized for technical and electrokinetic properties. Biodistribution of nanoemulsions and olanzapine solution (OS) in the brain and blood of rats following intranasal (intranasal) and intravenous (intravenous) administrations were examined using optimized technetium-labeled ((99m)Tc-labeled) olanzapine formulations. The brain/blood uptake ratios of 0.45, 0.88, 0.80, and 0.04 of OS (intranasal), ONE (intranasal), OMNE (intranasal), ONE (intravenous), respectively, at 0.5 h are indicative of direct nose-to-brain transport (DTP). Higher % drug targeting efficiency (%DTE) and %DTP for mucoadhesive nanoemulsions indicated effective brain targeting of olanzapine among the prepared nanoemulsions. Gamma scintigraphy imaging of the rat brain conclusively demonstrated rapid and larger extent of transport of olanzapine by OMNE (intranasal), when compared with OS (intranasal), ONE (intranasal), and ONE (intravenous), into the rat brain.
本研究的目的是优化奥氮平纳米乳（ONE）用于鼻脑给药。采用水滴定法制备纳米乳和奥氮平黏膜黏附纳米乳（OMNE），并对其技术和电动性质进行表征。使用优化的锝标记（（99m）Tc标记）奥氮平制剂，研究纳米乳和奥氮平溶液（OS）经鼻内（鼻内）和静脉内（静脉内）给药后在大鼠脑和血液中的生物分布。在0.5小时时，OS（鼻内）、ONE（鼻内）、OMNE（鼻内）、ONE（静脉内）的脑/血摄取率分别为0.45、0.88、0.80和0.04，表明存在直接鼻脑转运（DTP）。黏膜黏附纳米乳的较高药物靶向效率（%DTE）和%DTP表明在制备的纳米乳中奥氮平对脑具有有效的靶向作用。与OS（鼻内）、ONE（鼻内）和ONE（静脉内）相比，大鼠脑的γ闪烁显像最终证实OMNE（鼻内）能使奥氮平更快且更大程度地转运至大鼠脑内。
