Dextrans - potential polymeric drug carriers for suprofen

• Published in: Pharmazie Vol. 58; no. 11; pp. 804 - 806
• Main Authors: Shrivastava, S. K., Jain, D. K., Trivedi, P.
• Format: Journal Article
• Language: English
• Published: Eschborn Govi-Verlag 01.11.2003; Govi
• Subjects: Animals; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - chemistry; Anti-Inflammatory Agents, Non-Steroidal - pharmacology; Biological and medical sciences; Bones, joints and connective tissue. Antiinflammatory agents; Carrageenan; Chemical Phenomena; Chemistry, Physical; Dextrans - chemistry; Drug Carriers - chemistry; Edema - chemically induced; Edema - drug therapy; Hydrolysis; Magnetic Resonance Spectroscopy; Medical sciences; Pharmacology. Drug treatments; Rats; Spectrophotometry, Ultraviolet; Stomach Ulcer - chemically induced; Stomach Ulcer - pathology; Suprofen - administration & dosage; Suprofen - chemistry; Suprofen - pharmacology; Viscosity; Biological fluid; Rat; Toxicity; Drug carrier; Blood; Blood plasma; Gastroduodenal; Suprofen; Arylpropionic acid derivatives; Ulcer; Human; Control release polymer; Rodentia; Oral administration; Prodrug; Biological activity; Non steroidal antiinflammatory agent; Dextran; Hydrolysis resistance; Vertebrata; Chemotherapy; Mammalia; Treatment; Animal; Conjugated compound; Polysaccharide
• ISSN: 0031-7144

Dextrans are clinically useful biodegradable polysaccharide macromolecules and have been utilized as carriers for suprofen. Conjugates of suprofen were synthesized by preparing their acylimidazol derivatives which were condensed in situ with dextrans of different molecular weights (40000, 60000, 110000 and 200000). The structures of the synthesized conjugates were confirmed by IR and NMR spectroscopy. The degrees of substitution obtained were between 7.5 and 9.0%. The molecular weight was determined by the Mark-Howin Sakurada viscosity equation. Hydrolysis was studied in different buffer solutions (pH 1.2, 7.4, 9.0) and 80% human plasma (pH 7.4) and followed first order kinetics. Much faster hydrolysis was observed at pH 9.0 compared to pH 7.4 buffer solution and 80% human plasma (pH 7.4). Biological evaluation for acute and chronic anti-inflammatory activity was performed and the results were found to be comparable with the parent drug. The ulcerogenic index of conjugates showed a remarkable reduction compared to the parent suprofen.