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Dextrans--potential polymeric drug carriers for flurbiprofen
S K Shrivastava1, D K Jain, P Trivedi
1College of Pharmacy, Shri G.S. Institute of Technology and Science, Indore (MP), India.
Die Pharmazie
|July 15, 2003
Summary
Novel dextran-flurbiprofen conjugates were synthesized, showing comparable anti-inflammatory activity to flurbiprofen but with significantly reduced ulcerogenicity. These drug delivery systems offer a promising alternative for managing inflammation with improved safety.
Area of Science:
- Pharmaceutical Chemistry
- Drug Delivery Systems
- Medicinal Chemistry
Background:
- Dextrans serve as effective carriers for drug delivery.
- Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) with known gastrointestinal side effects.
Purpose of the Study:
- To synthesize and characterize dextran-flurbiprofen conjugates.
- To evaluate the anti-inflammatory activity and ulcerogenicity of these novel conjugates.
Main Methods:
- Synthesis of flurbiprofen acylimidazol derivatives and their condensation with dextrans of varying molecular weights.
- Structural confirmation using IR and NMR spectroscopy.
- Hydrolysis studies in various pH buffers and human plasma.
- In vivo evaluation of anti-inflammatory and anti-ulcerogenic properties.
Main Results:
- Dextran-flurbiprofen conjugates were successfully synthesized with substitution degrees of 8.0-9.5%.
- Hydrolysis followed first-order kinetics, with faster release at pH 9.0.
- Conjugates demonstrated comparable acute and chronic anti-inflammatory activity to flurbiprofen.
- A significant reduction in ulcerogenicity was observed for the conjugates compared to the parent drug.
Conclusions:
- Dextran conjugation effectively reduces the ulcerogenic potential of flurbiprofen while retaining its anti-inflammatory efficacy.
- These conjugates represent a safer drug delivery strategy for flurbiprofen, mitigating gastrointestinal toxicity.