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Non-ionic surfactant effects on hairless mouse skin permeability characteristics
K A Walters1, M Walker, O Olejnik
1Fisons plc, Pharmaceutical Division, Loughborough, UK.
The Journal of Pharmacy and Pharmacology
|August 1, 1988
Summary
Certain polyethoxylated non-ionic surfactants enhance methyl nicotinate transport across skin. Optimal enhancement occurred with linear alkyl chain surfactants, suggesting specific structural requirements for skin permeation.
Area of Science:
- Dermatology and Pharmaceutical Sciences
- Materials Science and Engineering
Background:
- Transdermal drug delivery aims to improve therapeutic efficacy and patient compliance.
- Stratum corneum lipid bilayers and corneocyte structures present significant barriers to drug permeation.
- Non-ionic surfactants are explored as penetration enhancers due to their amphipathic nature.
Purpose of the Study:
- To investigate the influence of polyethoxylated non-ionic surfactants on methyl nicotinate transport across hairless mouse skin in vitro.
- To identify structural characteristics of surfactants that correlate with enhanced skin permeation.
- To elucidate potential mechanisms by which surfactants facilitate methyl nicotinate penetration.
Main Methods:
- In vitro permeation studies using standard two-compartment diffusion cells.
- Hairless mouse skin as the biological barrier.
- Systematic variation of surfactant hydrophobic (alkyl chain length, branching) and hydrophilic (ethylene oxide chain length) components.
- Quantification of methyl nicotinate flux.
Main Results:
- Surfactants with linear alkyl chains ( > C8) and shorter ethylene oxide chains ( < E14) significantly increased methyl nicotinate flux.
- Branched or aromatic hydrophobic moieties rendered surfactants ineffective.
- Polyoxyethylene (10) lauryl ether (Brij 36T) demonstrated maximum flux enhancement.
- A C12 surfactant exhibited maximal activity, suggesting structural specificity.
Conclusions:
- The efficacy of polyethoxylated non-ionic surfactants as skin penetration enhancers is highly structure-dependent.
- Surfactants likely enhance permeation by disrupting stratum corneum intercellular lipids and/or interacting with intracellular keratin.
- Polyoxyethylene (10) lauryl ether represents a promising candidate for enhancing transdermal delivery of methyl nicotinate.