Development of long acting therapeutic system for arthritis by using prodrug contained in nanoparicle
| Project/Area Number |
24590660
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Applied pharmacology
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| Research Institution | Kumamoto University |
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Principal Investigator |
IMAI TERUKO 熊本大学, 薬学部, 教授 (70176478)
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2012: ¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
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| Keywords | プロドラッグ / 変形性膝関節症 / ブチリルコリンエステラーゼ / 滑膜細胞 / パラオクソナーゼ / ドラッグデリバリーシステム / 関節液 / エステラーゼ / 関節 / 加水分解 / ソフトドラッグ |
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| Outline of Final Research Achievements |
Aim of this study is a design of long acting therapeutic system for arthritis or osteoarthritis. Our strategy is followed; a prodrug is sustainedly released from nanoparticle with long retention into articular cavity and then prodrug taken up into synovial cells is converted to active drug that is locked in synovial cells to show its pharmacological effect.
It was expected that more than 100nm of size was required for retention of a nanoparticle into articular cavity because paraoxonase associated with high-density lipoprotein (diameter: about 10nm) presented in human synovial fluid. Also, butyrylcholinesterase was detected as a dimer and a monomer as well as a tetramer. In analysis of esterases in synoviocytes using native PAGE, human and rabbit synoviocytes showed two major esterase with different mobility of their plasma esterases. The different expression of esterase between synovial fluid and synoviocytes facilitates the development of prodrugs.
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Report
(4 results)
Research Products
(6 results)
