2007 Fiscal Year Final Research Report Summary
Development of bifunctional colon-specific delivery system of prednisolone using chitosan capsules and inhibitors of efflux transporters
| Project/Area Number |
18390055
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Medical pharmacy
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| Research Institution | Kyoto Pharmaceutical University |
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Principal Investigator |
YAMAMOTO Akira Kyoto Pharmaceutical University, Dept. of Biopharmaceutics, Professor (00166779)
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| Project Period (FY) |
2006 – 2007
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| Keywords | Chitosan capsules / Prednisolone / Colon-specific drug delivery / Inhibitor of efflux transporter / Inflammatory bowel disease |
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| 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.
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