A QbD-Navigated Approach to the Development and Evaluation of Etodolac-Phospholipid Complex Containing Polymeric...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Transdermal drug delivery offers a non-invasive route for systemic drug administration.
• Etodolac, a non-steroidal anti-inflammatory drug (NSAID), faces challenges in transdermal permeation.
• Phospholipid complexation is a strategy to enhance drug solubility and membrane permeability.

Purpose of the Study:

• To develop and optimize etodolac-phospholipid complex-loaded films for enhanced transdermal permeation.
• To evaluate the anti-inflammatory efficacy of the developed transdermal films.
• To investigate the impact of phospholipid complexation on etodolac's physicochemical properties.

Main Methods:

• Etodolac-phospholipid complex formation via solvent evaporation method.
• Characterization of the complex using DSC, XRD, FTIR, and 1H-NMR.
• Film formulation optimization using a central composite design and response surface methodology.
• Evaluation of film properties: swelling index, contact angle, tensile strength, and water vapor transmission rate.
• In vitro skin permeation studies and in vivo anti-inflammatory assays.

Main Results:

• The etodolac-phospholipid complex exhibited a conversion from crystalline to amorphous form.
• Optimized films demonstrated desirable properties: swelling index (60.14 ± 1.01%), contact angle (31.6 ± 0.03), tensile strength (2.44 ± 0.39 kg/cm2), and water vapor transmission rate (15.38 g/hm2).
• The optimized formulation showed significantly improved drug diffusion and permeation across the skin.
• In vivo studies confirmed enhanced anti-inflammatory activity of the complex-loaded films.

Conclusions:

• Etodolac-phospholipid complexation effectively enhances the transdermal permeation of etodolac.
• The developed transdermal films provide a promising platform for improved topical and systemic delivery of etodolac.
• Phospholipid complex-loaded films offer superior anti-inflammatory effects compared to the un-complexed drug, highlighting their therapeutic potential.