Optimizing delivery of flurbiprofen to the colon using a targeted prodrug approach.

Author: DubeyRajesh K, PathakKamla, PhilipAnil K

Paper Details 
Original Abstract of the Article :
The carboxylic group responsible for the gastric side-effects of the propionic acid derivative, flurbiprofen, was masked temporarily to overcome these side-effects and to accomplish colon-specific delivery of the drug. An amide prodrug (FLU-GLY) was synthesized by coupling flurbiprofen with L-glycin...See full text at original site
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引用元:
https://doi.org/10.1211/jpp.60.5.0006

データ提供:米国国立医学図書館(NLM)

Targeted Prodrug Delivery: Optimizing Flurbiprofen for Colon-Specific Delivery

Flurbiprofen is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation. However, it can cause gastric side effects. This study investigates a novel approach to delivering flurbiprofen specifically to the colon, minimizing the risk of gastric irritation.

Flurbiprofen Prodrug: A Targeted Delivery Strategy

The researchers synthesized a prodrug of flurbiprofen, called FLU-GLY, which is a modified form of the drug designed to remain inactive until it reaches the colon. They found that FLU-GLY remained intact in the stomach and upper intestine but was hydrolyzed by colonic microfloral enzymes, releasing the active drug in the colon.

Reduced Toxicity and Ulcerogenic Potential

In vivo studies confirmed that FLU-GLY was significantly less toxic and had less ulcerogenic activity than the parent drug, flurbiprofen. This demonstrates the potential of the prodrug approach to reduce the side effects of NSAIDs while maintaining therapeutic efficacy.

Dr.Camel's Conclusion

This research, like a clever camel adapting to a changing desert landscape, explores a creative strategy for delivering medications to specific targets within the body. By developing prodrugs that are activated only at specific sites, we can minimize side effects and improve treatment outcomes, offering a promising avenue for optimizing drug delivery and enhancing patient well-being.

Date :
  1. Date Completed 2008-09-19
  2. Date Revised 2013-11-21
Further Info :

Pubmed ID

18416937

DOI: Digital Object Identifier

10.1211/jpp.60.5.0006

Related Literature

SNS
PICO Info
in preparation
Languages

English

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