Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Molecules. 2018 Mar 28;23(4):784. doi: 10.3390/molecules23040784.
The aim of this article was to study the trans-epithelial absorption to reach the blood and to target the brain by axonal transport using nasal formulations with nanonized meloxicam (nano MEL spray) and its salt form known as meloxicam potassium monohydrate (MELP spray). The physicochemical properties and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out. These forms were first investigated in "nose-to-brain" relation. It was found that the in vitro study and in vivo study did not show any significant correlation. In vitro experiments demonstrated faster dissolution rate and higher diffusion of MELP from the spray compared with the nano MEL spray. The administration of the nano MEL spray resulted in faster absorption and constant plasma concentration of the drug after five minutes of administration as compared to MELP. The axonal transport of the drug was justified. MEL appeared in the brain tissues after the first five minutes of administration in the case of both spray forms, but its amount was too small in comparison with the total plasma concentration. The application of the nano MEL spray resulted in the same AUC in the brain as the intravenous injection. The "nose-to-blood" results predicted the nasal applicability of MEL and MELP in pain management. The "nose-to-brain" pathway requires further study.
本文旨在研究经鼻制剂纳米化美洛昔康（纳米 MEL 喷雾）及其盐形式美洛昔康钾一水合物（MELP 喷雾）的跨上皮吸收到达血液并通过轴突运输靶向大脑的情况。控制了鼻用制剂的物理化学性质和黏膜黏附性。进行了体外和体内研究。首先研究了这些形式的“鼻-脑”关系。结果发现，体外研究和体内研究之间没有显著相关性。与纳米 MEL 喷雾相比，体外实验表明 MELP 喷雾具有更快的溶解速率和更高的扩散性。与 MELP 相比，纳米 MEL 喷雾给药后五分钟内药物吸收更快，血浆浓度保持稳定。药物的轴突运输得到了证明。在两种喷雾形式中，药物在给药后 5 分钟内就出现在脑组织中，但与总血浆浓度相比，其数量太少。纳米 MEL 喷雾的应用使脑内 AUC 与静脉注射相同。“鼻-血”结果预测了 MEL 和 MELP 在疼痛管理中的鼻用适用性。“鼻-脑”途径需要进一步研究。
