welcome to oneFAPvoice
- a positively charged Familial Adenomatous Polyposis community.- join today!
- login
Colon-Specific Delivery of Celecoxib is a Potential Strategy to Improve Toxicological and Pharmacological Properties of the Selective Cox-2 Inhibitor: Implication in Treatment of Familiar Adenomatous Polyposis
source: Journal of drug targeting
year: 2012
authors: Yonghyun Lee, Hyunjeong Kim, Wooseong Kim, Jeong Hyun Yoon, Yunjin Jung, Seong Hoon Jeong
summary/abstract:In general, colon-specific delivery of a drug decreases systemic absorption and increases therapeutic concentration of the drug at the target site. N-succinylglutam-1 or 5-yl celecoxib (SG1C and SG5C) were prepared as a colon-specific prodrug of celecoxib, a selective Cox-2 inhibitor, and investigated whether the celecoxib derivatives could deliver celecoxib to the target site and improve cardiovascular toxicity and therapeutic effectiveness for the treatment of familiar adenomatous polyposis. SG1C and SA5C were cleaved to release celecoxib in the cecal contents while stable in small intestinal contents. The cecal release of celecoxib was much greater for SG1C than SG5C. SG1C administered orally was barely detected in the blood and urine. SG1C delivered much greater amount of celecoxib to the large intestine while keeping the plasma concentration of celecoxib at much lower level compared with oral administration of free celecoxib. Consistent with these pharmacokinetic results, SG1C supplied a greater concentration of celecoxib for the entire colonic tissue and did not change the serum level of 6-keto-PGF(1α) whose decrease is associated with the cardiovascular toxicity of celecoxib. Taken together, colon-specific delivery of celecoxib using a prodrug approach may be a useful strategy to improve toxicological and pharmacological properties of celecoxib.
organization: Pusan National UniversityDOI: 10.3109/1061186X.2012.693498
read more full text source
expertly curated content related to this topic
-
Eviendep Reduces Number and Size of Duodenal Polyps in Familial Adenomatous Polyposis Patients With Ileal Pouch-Anal...AIM: To evaluate if 3 mo oral supplemen...
-
Rectal Proliferation and Polyp Occurrence in Pateints with Familial Adenomatous Polyposis after Sulindac TreatmentBACKGROUND/AIMS : Sulindac, a nonsteroid...
-
Teamwork Makes a Life-Changing Difference for Luishttps://www.youtube.com/watch?v=bpnoHHL0...
-
Imatinib for Progressive and Recurrent Aggressive Fibromatosis (Desmoid Tumors): An FNCLCC/French Sarcoma Group Phas...BACKGROUND: Imatinib evaluated as a new...
-
Familial Risk-Colorectal Cancer: ESMO Clinical Practice GuidelinesLynch syndrome is the most common heredi...
-
A Randomized, Double-Blind, Placebo-Controlled Trial of the Effects of Rofecoxib, a Selective Cyclooxygenase-2 Inhib...PURPOSE : The aim of this study was to e...
-
Colorectal Polyps in ChildhoodPURPOSE OF REVIEW: Colorectal polyps ar...