4.5 Article

Dextran successful carrier molecule for the delivery of NSAIDs with reduced gastrointestinal effect

Journal

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
Volume 20, Issue 2, Pages 135-142

Publisher

ELSEVIER SCIENCE BV
DOI: 10.1016/S1773-2247(10)50018-2

Keywords

Synthesis; Characterization; In vitro hydrolysis; Anti-inflammatory; Analgesic and ulcerogenic activity

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The dextron ester polymeric prodrug of aceclofenac and mefenamic acid was synthesized through carbonyldiimidazole coupling agent, The prepared polymeric prodrug was characterized by UV IR. X-RD and Ill NAIR. The in vitro hydrolysis study was performed by HPLC and polymeric conjugate subjected for in vitro hydrolysis showed negligible hydrolysis in simulated gastric fluid pH 1.2 for 3 h. The half-life of the aceclofenac dextral( conjugate in simulated intestinal fluid (SIF) pH 7.4 and phosphate buffer solution (PBS) pH 9.0 was found to he 8.51 h and 33.72 min, respectively. The half-life 4.66 h and 25.4 min was found in STF pH 7.4 and PBS 9.0, respectively for mcienamic acid conjugates. Phe conjugate.s. were screened jbr biological activity such as anti-inflammatory, analgesic and ulcerogenic activity.Phe statistical data obtained from the biological experiment suggested that the value was Plaid to be significant willi respect to normal control.

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