Pharmacokinetic study and brain tissue analysis of Zolmitriptan loaded chitosan nanoparticles in rats by LC-MS method

佐米曲普坦 药代动力学 最大值 药理学 黄芩苷 化学 药品 鼻喷雾剂 医学 鼻腔给药 色谱法 内科学 高效液相色谱法 苏马曲普坦 受体 兴奋剂
作者
Farshid Ali Naghi Zadeh Khezri,C. Lakshmi,Rama Bukka,Nidhi Malviya,Shachindra L. Nargund
出处
期刊:International Journal of Biological Macromolecules [Elsevier]
卷期号:142: 52-62 被引量:9
标识
DOI:10.1016/j.ijbiomac.2019.08.236
摘要

Migraine has recently become a major interest to the neuroscientists. Zolmitriptan is an effective medicine used in the treatment of migraine. The nasal spray was prepared from Zolmitriptan loaded chitosan nanoparticles and evaluated for pharmacokinetic properties. In this study male Wistar albino rats weighing between 200 and 250 g were taken and divided into 4 groups with 6 rats in each group. Nasal spray containing Zolmitriptan loaded Chitosan nanoparticles were administered nasally (using specific inhalation mask) at a dose of 0.5 mg/kg as a test formulation and compared with the control groups which received either water for injection or marketed standard drug (Zolmist) or standard drug solution at a same dose. The pharmacokinetic parameters such as Cmax, Tmax, and brain tissue analyses for accumulation of drug were performed for Zolmitriptan by LC-MS method. Amount of drug in the plasma from the test formulation, standard marketed drug (Zolmist) and standard drug solution was found to be 41.37 ± 2.31, 34.76 ± 4.22 and 23.74 ± 2.42 ng/ml at 10 min respectively, which indicated significantly (p < 0.05) greater amount of drug being delivered from the test formulation compared to the both standard groups. The amount of the drug (Zolmitriptan) present in brain tissue (Olfactory lobe) was found to be 15 ± 0.08, 13 ± 0.14 and 8 ± 0.13 ng/g at 60 min for test formulation, marketed standard and standard drug solution respectively which indicates significantly (p < 0.05) higher amount of drug absorption in brain tissue from the test formulation compared to both the standard groups. Pharmacokinetics studies of nasal spray containing Zolmitriptan loaded chitosan nanoparticles proved rapid onset of action in animals and is promising in treatment of migraine.
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