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Updated: Jun 11, 2026
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Visualizing and Quantifying Pharmaceutical Compounds within Skin using Coherent Raman Scattering Imaging
Published on: November 24, 2021
Percutaneous penetration modifiers and formulation effects: thermal and spectral analyses.
Diksha Kaushik1, Bozena Michniak-Kohn
1Ernest Mario School of Pharmacy, Rutgers-The State University of New Jersey, Piscataway, New Jersey 08854, USA.
AAPS Pharmscitech
|June 29, 2010
Summary
Skin penetration enhancers can become retardants based on formulation vehicle. This study reveals how laurocapram and iminosulfurane modifiers interact with stratum corneum lipids and proteins, explaining formulation-dependent efficacy.
Area of Science:
- Dermatology
- Materials Science
- Physical Chemistry
Background:
- Understanding skin penetration enhancers is crucial for drug delivery.
- The stratum corneum lipid barrier presents a significant challenge for transdermal transport.
- The role of formulation vehicles in modulating penetration modifier efficacy is not fully understood.
Purpose of the Study:
- To investigate the formulation effects of laurocapram and iminosulfurane derivatives on human stratum corneum.
- To elucidate the mechanisms by which these penetration modifiers act as enhancers or retardants.
- To explain the vehicle-dependent behavior of penetration modifiers.
Main Methods:
- Formulation of penetration modifiers (laurocapram, N-0915, DMBIS, DMMCBI, TBDOC) in various vehicles (water, PG, ethanol, PEG 400).
- Assessment of enhancer/retardant properties using diethyl-m-toluamide as a model permeant.
- Analysis of mechanisms using differential scanning calorimetry (DSC) and attenuated total reflectance Fourier-transform infra-red spectroscopy (ATR-FTIR).
Main Results:
- Penetration enhancers primarily disrupt and fluidize stratum corneum lipid bilayers, evidenced by DSC and blue shifts in IR spectra.
- Retardation of permeation is associated with elevated melting points (T(m2)) and strengthened lipid-protein complexes, indicated by DSC.
- IR spectroscopy revealed increased hydrogen bonding and lipid organization in the stratum corneum, suggesting a mechanism for retardation.
Conclusions:
- The formulation vehicle significantly influences the efficacy of penetration modifiers, determining whether they enhance or retard permeation.
- Laurocapram and iminosulfurane derivatives modulate stratum corneum structure through lipid bilayer disruption (enhancement) or lipid-protein organization via hydrogen bonding (retardation).
- This study provides novel insights into the molecular mechanisms underlying formulation-dependent skin penetration modulation.
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