Chinese Journal of Tissue Engineering Research ›› 2016, Vol. 20 ›› Issue (5): 688-693.doi: 10.3969/j.issn.2095-4344.2016.05.014

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Feasibility of nasal brain targeted drug delivery through the nose-brain channel in the nasal olfactory region using cimicifugoside H-1

Wu Mi-shan1, Zhao Su-zhi2, Gao Wei-juan3, Wang Ru1, Han Hong-wei1, Shi Xu-liang1   

  1. 1Department of Formulaology, Basic Medicine College, Hebei University of Chinese Medicine, Shijiazhuang 050200, Hebei Province, China; 2Changan District Shengbei Community Health Center of Shijiazhuang, Shijiazhuang 050041, Hebei Province, China; 3Hebei Key Laboratory of Chinese Medicine Research on Cardio-Cerebrovascular Disease, Shijiazhuang 050091, Hebei Province, China
  • Received:2015-11-07 Online:2016-01-29 Published:2016-01-29
  • About author:Wu Mi-shan, M.D., Professor, Doctoral supervisor, Department of Formulaology, Basic Medicine College, Hebei University of Chinese Medicine, Shijiazhuang 050200, Hebei Province, China
  • Supported by:

    the National Natural Science Foundation of China, No. 81073074, 30472200; the Natural Science Foundation of Hebei Province, No. H2013206005; the Major Scientific Research Project of Hebei Provincial Higher Education Schools, No. ZD2015053; the High-Level Personnel of Institutions of Higher Learning in Hebei Province (Scientific Research Project) No. GCC2014013

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Abstract:

BACKGROUND: Recent studies have suggested that intranasal administration is one of the ways to target drug 
delivery, and can effectively make the drug that cannot pass through the blood brain barrier by other pathways to bypass the blood brain barrier, resulting in targeted delivery to the brain. It provides a promising route for the treatment of central nervous system diseases.
OBJECTIVE: To study the pharmacokinetic and brain-targeted channel-tropism tissue distribution character of cimicifugoside H-1 after nasal and intravenous administration in plasma and tissues in rats, in order to evaluate the feasibility of developing brain-targeted nasal delivery system of cimicifugoside H-1 by the passage between nose and brain in nasal olfactory area.
METHODS: After intravenous injection and nasal administration of cimicifugoside H-1, the drug concentrations of plasma and channel-tropism organs (lung, spleen, stomach, large intestine, liver, kidney, brain, brain, cerebellum, cerebrospinal fluid, olfactory bulb and olfactory region) were detected. Drug-time curve was drawn. DAS program was used to select apartment model and pharmacokinetics parameters.
RESULTS AND CONCLUSION: (1) The pharmacokinetics characters of cimicifugoside H-1 are rapidly absorbed and extensively distribution. Among major channel-tropism organs, drug concentrations were higher in the lung and brain than in the other organs. (2) Cimicifugoside H-1 could be straightly transported into brain by the intranasal administration. The molecule through olfactory mucosa in nasal cavity entered into olfactory bulb in arachno-hypostegal cavity, and then entered into olfactory region, cerebrospinal fluid, cerebrum and cerebellum gradually. Olfactory bulb was the only way for drug molecule to go through nasal cavity into brain. (3) Compared with the intravenous injection, cimicifugoside H-1 through the intranasal administration has a significant channel-tropism of lung and brain targeting.