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Fluorescent Leakage Assay to Investigate Membrane Destabilization by Cell-Penetrating Peptide
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Published on: December 19, 2020

Fluorescent penetration enhancers for transdermal applications.

Jennifer E Seto1, Baris E Polat, Brett VanVeller

  • 1Department of Chemical Engineering, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|November 9, 2011
PubMed
Summary

Researchers identified naturally fluorescent penetration enhancers (FPEs) to directly study their behavior in skin using fluorescence techniques. This novel approach offers direct visualization of FPEs within the skin barrier.

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Area of Science:

  • Pharmacology and Pharmaceutical Sciences
  • Biophysics
  • Materials Science

Background:

  • Transdermal drug delivery relies on chemical penetration enhancers, but their mechanisms within skin remain unclear.
  • Directly visualizing enhancer behavior in skin is crucial for understanding and optimizing transdermal delivery.

Purpose of the Study:

  • To identify naturally fluorescent penetration enhancers (FPEs) for direct visualization of their behavior in skin.
  • To establish a novel method for studying skin penetration enhancer mechanisms using fluorescence techniques.

Main Methods:

  • Evaluated 12 amphiphilic fluorescent molecules as potential skin penetration enhancers.
  • Determined enhancer activity using skin current enhancement ratios.
  • Utilized two-photon fluorescence microscopy (TPM) for direct, non-invasive visualization of FPEs within skin.

Main Results:

  • Eight of the 12 evaluated molecules demonstrated significant skin penetration enhancement activity.
  • Successfully visualized FPE behavior within the skin barrier using TPM.
  • Demonstrated visualization of glycerol-mitigated and ultrasound-enhanced FPE penetration.

Conclusions:

  • Naturally fluorescent penetration enhancers (FPEs) enable direct, non-invasive visualization of their behavior in skin.
  • This approach overcomes limitations of previous indirect visualization methods.
  • The combination of FPEs and fluorescence microscopy provides valuable physical insights into enhancer-skin interactions, paving the way for FPE design principles.