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Increased skin permeability for lipophilic molecules.

Journal of Pharmaceutical Sciences

|August 1, 1984

Summary

Surfactants enhance polar molecule transport but not lipophilic ones. Adding polar lipids like fatty acids to propylene glycol vehicles significantly boosts the skin absorption of nonpolar drugs, such as salicylic acid.

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Area of Science:

Dermatology
Pharmaceutics
Materials Science

Background:

Surfactant treatments improve epidermal transport of polar molecules.
Transport of nonpolar (lipophilic) molecules across the epidermis is minimally enhanced by surfactants.
Novel vehicle systems are required to improve lipophilic molecule delivery.

Purpose of the Study:

To investigate methods for enhancing the transdermal transport of nonpolar (lipophilic) molecules.
To evaluate the efficacy of polar lipids in combination with propylene glycol for improving drug delivery.

Main Methods:

Formulations containing propylene glycol as a base vehicle were prepared.
Small quantities of polar lipids, specifically fatty acids or alcohols, were incorporated into the base vehicle.
The transport of nonpolar substances, exemplified by salicylic acid, across the epidermis was measured.

Main Results:

The addition of polar lipids to propylene glycol formulations significantly increased the transport of nonpolar molecules.
The transport enhancement for nonpolar materials like salicylic acid was approximately an order of magnitude.
The combined system of polar lipids in a propylene glycol base demonstrated a synergistic effect, greatly exceeding the impact of individual components.

Conclusions:

Incorporating small amounts of polar lipids into propylene glycol-based vehicles is an effective strategy for enhancing the transdermal delivery of nonpolar (lipophilic) compounds.
This approach offers a significant improvement over traditional surfactant-based methods for lipophilic molecule transport.
The synergistic effect of mixed vehicle systems presents a promising avenue for optimizing topical drug delivery.

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