Nanostructured Etodolac Carriers in Transdermal Gel: Optimization and Characterization

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Etodolac (ETD), a non-steroidal anti-inflammatory drug, faces challenges with conventional oral administration, including first-pass metabolism and gastrointestinal side effects.
• Its classification as a Class-II drug with low solubility further complicates effective delivery.
• Nanostructured Lipid Carriers (NLCs) offer a promising approach to enhance drug solubility, stability, and transdermal permeation.

Purpose of the Study:

• To optimize, formulate, and evaluate a Nanostructured Lipid Carrier (NLC) based transdermal gel of Etodolac (ETD).
• To achieve a faster onset of action, increased drug penetration and permeation, and extended release of Etodolac.
• To circumvent the limitations associated with conventional Etodolac administration routes.

Main Methods:

• A 3^2 factorial design was employed for experimental planning and optimization.
• Nanostructured Lipid Carriers (NLCs) were prepared using melt emulsification and ultrasonication techniques.
• Characterization involved particle size analysis (photon correlation spectroscopy, SEM), zeta potential, entrapment efficiency, and in vitro drug release studies using artificial diffusion cells.

Main Results:

• The optimized Etodolac NLC formulation exhibited a spherical shape with a particle size of 241.3 nm and a zeta potential of -29 mV.
• Entrapment efficiency was 64.21 ± 1.23%, with cumulative drug release reaching 70.12 ± 2.10% after 12 hours.
• The NLC gel demonstrated zero-order release kinetics, non-Fickian transport, a transdermal flux of 0.1619 mg/cm²/hr, and prolonged therapeutic activity up to 24 hours.

Conclusions:

• The central composite design successfully optimized the Etodolac NLC formulation.
• Established relationships between NLC components (lipid:drug ratio, surfactant concentration) and critical quality attributes (particle size, entrapment, release).
• The optimized Etodolac NLC gel shows significant potential for improved transdermal drug delivery compared to micellar formulations.