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Development of bifunctional colon-specific delivery system of prednisolone using chitosan capsules and inhibitors of efflux transporters

Research Project

Project/Area Number 18390055
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section一般
Research Field Medical pharmacy
Research InstitutionKyoto Pharmaceutical University

Principal Investigator

YAMAMOTO Akira  Kyoto Pharmaceutical University, Dept. of Biopharmaceutics, Professor (00166779)

Project Period (FY) 2006 – 2007
Project Status Completed (Fiscal Year 2007)
Budget Amount *help
¥16,570,000 (Direct Cost: ¥14,800,000、Indirect Cost: ¥1,770,000)
Fiscal Year 2007: ¥7,670,000 (Direct Cost: ¥5,900,000、Indirect Cost: ¥1,770,000)
Fiscal Year 2006: ¥8,900,000 (Direct Cost: ¥8,900,000)
KeywordsChitosan capsules / Prednisolone / Colon-specific drug delivery / Inhibitor of efflux transporter / Inflammatory bowel disease
Research Abstract

In this study, we examined the effectiveness of chitosan capsules for the colon-specific delivery of prednisolone in rats. We also evaluated the effectiveness and side effect of prednisolone using chitosan capsules compared with the conventional dosage form (gelatin capsules). We found a significant increase in the concentration of prednisolone in the large intestinal mucosa when prednisolone was administered orally using chitosan capsules, as compared with the case using gelatin capsules. On the other hand, the plasma concentrations of prednisolone after oral administration using chitosan capsules were much lower than those in the case of gelatin capsules. We also assessed the effectiveness of prednisolone for the healing of trinitrobenzene sulfonic acid (TNBS)-induced colitis by measuring the rnyeloperoxidase (MPO) activities and colon wet weight/body weight (C/B) ratios. The MPO activities and C/B ratios significantly reduced when prednisolone was administered orally using chitosan capsules, in comparison with the case of gelatin capsules. Moreover, the weight of thymus, which is an index of side effect of prednisolone, remarkably decreased after oral administration of prednisolone using gelatin capsules, whereas its weight was not so much changed when prednisolone was administered orally using chitosan capsules.
These findings indicated that chitosan capsules might be useful for the colon specific delivery of prednisolone and its enhanced effectiveness for the healing of colitis in rats. Moreover, chitosan capsules might be also effective for reducing the side-effect of prednisolone due to its decreased intestinal transfer to the systemic circulation.

Report

(3 results)
  • 2007 Annual Research Report   Final Research Report Summary
  • 2006 Annual Research Report
  • Research Products

    (3 results)

All 2007

All Journal Article (3 results) (of which Peer Reviewed: 2 results)

  • [Journal Article] キトサンカプセルを用いたプレドニゾロンの大腸特異的送達法の開発に関する研究2007

    • Author(s)
      山本 昌
    • Journal Title

      薬学雑誌 127

      Pages: 621-630

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      2007 Final Research Report Summary
    • Peer Reviewed
  • [Journal Article] Study on the colon-specific delivery of prednisolone using chitosan capsules2007

    • Author(s)
      Akira Yamamoto
    • Journal Title

      Yakugaku Zasshi 127

      Pages: 621-630

    • NAID

      110006242866

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      2007 Final Research Report Summary
  • [Journal Article] キトサンカプセル剤を用いたプレドニゾロンの大腸送達法の開発に関する研究2007

    • Author(s)
      山本 昌
    • Journal Title

      薬学雑誌 127

      Pages: 621-630

    • Related Report
      2007 Annual Research Report
    • Peer Reviewed

URL: 

Published: 2006-04-01   Modified: 2016-04-21  

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