[Study on the colon specific delivery of prednisolone using chitosan capsules].
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 effects 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-induced colitis by measuring myeloperoxidase (MPO) activity and colon wet weight/body weight (C/B) ratio. MPO activities and C/B ratios were significantly reduced when prednisolone was administered orally using chitosan capsules, in comparison with the case of gelatin capsules. Moreover, the weight of the thymus, which is an index of the side effects of prednisolone, markedly decreased after oral administration of prednisolone using gelatin capsules, whereas its weight did not change as much when prednisolone was administered orally using chitosan capsules. These findings indicate 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 in reducing the side effects of prednisolone due to its decreased intestinal transfer to the systemic circulation.
Yamamoto
Akira
A
Department of Biopharmaceutics, Kyoto Pharmaceutical University, Japan. yamamoto@mb.kyoto-phu.ac.jp
D000284:Administration, Oral; D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics*; D002214:Capsules; D048271:Chitosan; D003093:Colitis, Ulcerative / Q000188:drug therapy; D003106:Colon / Q000378:metabolism*; D016503:Drug Delivery Systems; D005780:Gelatin; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism; D011239:Prednisolone / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D051381:Rats
D000890:Anti-Infective Agents; D002214:Capsules; D005780:Gelatin; D048271:Chitosan; D011239:Prednisolone