Sulfate-conjugated methylprednisolone as a colon-targeted methylprednisolone prodrug with improved therapeutic properties against rat colitis Colon-targeted methylprednisolone prodrug

Hyesik Kong, Younghyun Lee, Sungchae Hong, Jeongoh Han, Biom Choi, Yunjin Jung, Young Mi Kim

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

Methylprednisolone (MP) is one of the most widely used corticosteroids for the treatment of inflammatory bowel disease (IBD). However, systemic adverse effects of MP limit its availability for the disease. In present study, sulfate-conjugated methylprednisolone (MPS) was evaluated in vivo as a colon-targeted prodrug of MP and its therapeutic properties against 2,4,6-trinitrobenzenesulfonic acidinduced rat colitis were investigated. Upon oral administration, a large fraction of MPS reached the large intestine, where MPS was converted to MP implying that MPS would deliver MP effectively to the large intestine. The fecal recovery of MP (after MPS administration) was much greater than that after MP administration and the urinary recovery of MP (after MPS administration) was much less than that after MP administration, suggesting that MPS should exhibit enhanced therapeutic activity and reduced systemic adverse effects. Consistent with this notion, MPS was more effective than MP in ameliorating rat colitis. Moreover, the adverse effects of MPS on adrenal function and thymus were much lower than those of MP. Taken together, MPS may be therapeutically superior to MP in IBD treatment.

Original languageEnglish
Pages (from-to)450-458
Number of pages9
JournalJournal of Drug Targeting
Volume17
Issue number6
DOIs
StatePublished - Jul 2009

Keywords

  • Colonic delivery
  • Inflammatory bowel disease
  • Methylprednisolone
  • Prodrug
  • Sulfate conjugation

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