2019 Fiscal Year Final Research Report
Development of brain drug delivery system for the treatment of autism spectrum disorder -Transnasal delivery of oxytocin to the brain-
| Project/Area Number |
19K21236
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| Project/Area Number (Other) |
18H06118 (2018)
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| Research Category |
Grant-in-Aid for Research Activity Start-up
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| Allocation Type | Multi-year Fund (2019)
Single-year Grants (2018) |
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| Review Section |
0801:Pharmaceutical sciences and related fields
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| Research Institution | Kobe Pharmaceutical University |
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Principal Investigator |
Tanaka Akiko 神戸薬科大学, 薬学部, 特任助教 (30824320)
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| Project Period (FY) |
2018-08-24 – 2020-03-31
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| Keywords | 鼻腔内投与 / 脳内送達 / オキシトシン / 自閉症治療 / 自閉症スペクトラム障害 / 中枢神経系疾患 / 脳内動態 |
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| Outline of Final Research Achievements |
The aim of this study was to develop brain delivery system of oxytocin (OXT) after intranasal administration. To improve brain delivery efficacy of OXT, OXT was conjugated with fatty acids. However, fatty acid-modification decreased the water-solubility of OXT, and hardly affected the brain delivery efficacy of OXT after intranasal administration in mice. These results indicate that the balance between the solubility and the permeability should be optimized for the efficient brain delivery of OXT after intranasal administration. In contrast, we examined the effects of N-acyl taurates, anionic surfactants, to the brain delivery efficacy of OXT. We demonstrated that the brain delivery efficacy of OXT was significantly improved by co-administration of N-acyl taurates. These results indicate that N-acyl taurates are promising additives for the efficient brain delivery of OXT and the treatment of autism spectrum disorder.
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| Free Research Field |
生物薬剤学
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| Academic Significance and Societal Importance of the Research Achievements |
本研究では、鼻腔内投与後のOXT の脳移行性を改善するための DDS 開発を目的として、化学修飾または製剤添加物の併用による OXT の脳移行性改善を試みた。なかでも N-アシルタウリン酸塩は、鼻腔内投与後の OXT の脳移行性を著しく改善した。これらの知見は、N-アシルタウリン酸塩が OXT などの様々な中分子医薬の脳移行性を改善する可能性を示すものである。したがって、本研究で得られた知見は、ASD 治療法の開発にとどまらず、アルツハイマー病、パーキンソン病などの神経変性疾患などの脳疾患を対象とした中分子医薬による新規治療法の開発に展開できる可能性が高く、社会的意義が大きいと考えられる。
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