Emulsion-Based Gel Loaded with Ibuprofen and Its Derivatives

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Dermatology

Background:

• Transdermal drug delivery offers advantages over oral administration for non-steroidal anti-inflammatory drugs like ibuprofen (IBU).
• Optimizing vehicle formulation and chemical modification of active compounds are crucial for enhancing skin permeation.

Purpose of the Study:

• To evaluate the impact of vehicle and chemical modifications on ibuprofen skin permeation and accumulation.
• To develop and characterize novel semi-solid formulations for improved transdermal delivery of ibuprofen and its derivatives.

Main Methods:

• Development of emulsion-based gel formulations containing ibuprofen, sodium ibuprofenate (IBUNa), and L-phenylalanine ethyl ester ibuprofenate ([PheOEt][IBU]).
• Characterization of formulation properties: density, refractive index, viscosity, and particle size distribution.
• In vitro permeation studies using pig and human skin models to assess drug release and skin penetration.

Main Results:

• The emulsion-based gel significantly enhanced skin penetration of ibuprofen and its derivatives compared to commercial gel and cream formulations.
• Cumulative mass of ibuprofen after 24h permeation was 1.6-4.0 times higher from the emulsion-based gel.
• Ibuprofen derivatives (IBUNa and [PheOEt][IBU]) demonstrated potent skin penetration enhancement properties.

Conclusions:

• Transdermal emulsion-based gel vehicles, combined with chemical modification of the drug, represent a promising approach for accelerated drug delivery.
• The developed formulations show potential for more effective transdermal administration of ibuprofen and related compounds.