Zinc-aceclofenac complex: synthesis, hydrolysis study and antiinflammatory studies

Area of Science:

• Pharmaceutical Chemistry
• Drug Development
• Medicinal Chemistry

Background:

• Aceclofenac, a nonsteroidal anti-inflammatory drug (NSAID), can cause gastric ulcers.
• Zinc ions exhibit known anti-ulcer and anti-inflammatory properties.
• Gastroenteropathies are common side effects of NSAIDs like aceclofenac.

Purpose of the Study:

• To synthesize and characterize a zinc complex of aceclofenac.
• To evaluate the anti-ulcer and anti-inflammatory potential of the zinc-aceclofenac complex.
• To reduce the gastrointestinal side effects associated with aceclofenac therapy.

Main Methods:

• Preparation and characterization of the zinc-aceclofenac complex using spectroscopy and differential scanning calorimetry.
• In vitro hydrolysis studies in acidic (pH 1.2) and neutral (pH 7.4) buffers.
• In silico analysis using Prediction of Activity Spectra of Substances (PASS) software.
• In vivo anti-inflammatory testing using the carrageenan-induced rat paw edema model.

Main Results:

• The zinc-aceclofenac complex demonstrated enhanced stability in acidic conditions, simulating gastric environments.
• In silico predictions suggested potential anti-inflammatory activity for the complex.
• In vivo studies confirmed comparable anti-inflammatory activity to aceclofenac, with a reduced ulcer index.
• The zinc complex showed improved gastrointestinal safety profile compared to the parent drug.

Conclusions:

• The synthesized zinc-aceclofenac complex offers a promising alternative to aceclofenac for managing inflammatory conditions.
• The complex exhibits significant anti-inflammatory efficacy with a reduced risk of gastric ulceration.
• This formulation strategy effectively mitigates the gastrointestinal adverse effects of aceclofenac.