Effects of penetration enhancers on in vitro permeability of meloxicam gels

Area of Science:

• Pharmaceutical Sciences
• Dermal Drug Delivery
• Formulation Development

Background:

• Meloxicam (MLX) is a nonsteroidal anti-inflammatory drug often administered orally.
• Transdermal delivery of MLX offers potential for localized treatment and reduced systemic side effects.
• Developing effective topical formulations for MLX requires optimizing drug permeability through the skin.

Purpose of the Study:

• To formulate a 0.3% meloxicam (MLX) hydroxypropylcellulose gel.
• To evaluate the in vitro skin permeability of MLX from various gel formulations containing different co-solvents and penetration enhancers.
• To identify an optimal MLX gel formulation for potential transdermal therapeutic delivery.

Main Methods:

• Formulation of a 0.3% MLX gel using hydroxypropylcellulose (Klucel) and optimized co-solvents.
• In vitro permeability studies using isopropyl myristate (IPM)-saturated cellulose membranes and human cadaver skin.
• Assessment of penetration enhancers including dimethylsulfoxide (DMSO), tween20 (TW20), oleic acid (OA), and menthol (MT) at various concentrations.

Main Results:

• A base gel composed of 2.5% Klucel, propylene glycol, ethanol, and water (1:1:1) demonstrated superior MLX permeability.
• Menthol significantly increased MLX flux in a dose-dependent manner, with optimal results at 5% (2.43±0.47 µg/cm²/h).
• DMSO and TW20 did not enhance MLX permeability, while oleic acid showed a peak at 1% and decreased at 5%.

Conclusions:

• A 0.3% MLX gel containing 5% menthol significantly enhances meloxicam skin permeability.
• This formulation holds promise for delivering therapeutically relevant doses of meloxicam transdermally.
• Further investigation into the clinical efficacy and safety of this menthol-enhanced MLX gel is warranted.