Synthesis, Characteristics, and Pharmaceutical Properties of Ibuprofen-Cyclodextrin-PEG Conjugate

Abstract

The NSAIDs ibuprofen was chemically conjugated to the PEG-graft-β-CyD with an ester bond and its aqueous solubility was clearly improved. The preliminary release profile of ibuprofen in rat gastrointestinal tract contents was performed at 37°C within 12 hours. The polymeric conjugate almost did not release ibuprofen in the contents of stomach, released ibuprofen only 7.4% in the contents of small intestine, and evidently released ibuprofen up to 58.7% in the contents of colon, respectively. These results demonstrated that the polymeric conjugate was site-specifically biodegraded in the rat colonic contents. On the other hand, the xylene-induced ear swelling technique, the hot plate test, and the brewer's yeast-induced hyperthermia model in mice were performed for evaluating the anti-inflammatory, analgesic, and antipyretic activities of the polymeric conjugate, respectively. The results revealed that the polymeric conjugate maintained a long and stable pharmacodynamic efficiency over a period of 24 hours. Hence, the present polymeric ibuprofen-cyclodextrin-PEG conjugate may be of value as an orally administered long-acting prodrug of ibuprofen through colon-targeting delivery.

Zinc(II) complexes derived from ibuprofen Schiff base ligands: synthesis, characterization and biological activity

“…Therefore, one of the most important tasks in the field of drug research today is to produce bioactive chemicals with low side effects, particularly those that can be utilised as antiinflammatory medications. Antibacterial, antifungal, antitumor, and antiviral properties of metal complexes [7]. When a metal ion and a ligand engage, a variety of coordination numbers, oxidation states, and geometries can be produced.…”