Shake-Induced Temporary Ion-Pairing Between Lecithin and Glycolic Acid for Enhanced Exfoliation in a Novel Biphasic Serum: Comparative Ex Vivo and in Vivo Randomised Studies

Skin Res Technol. 2026 Apr;32(4):e70349. doi: 10.1111/srt.70349.

Abstract

Background: Chemical exfoliation efficacy is significantly limited by pH-dependent permeability reduction above the pKa of glycolic acid (3.83), constraining consumer product development.

Objective: To develop and evaluate a biphasic serum utilizing temporary lecithin-glycolate ion-pairing to enhance stratum corneum permeation while maintaining safety at pH 3.9.

Methods: A biphasic formulation containing 10 wt% (weight percent) glycolic acid and 0.1 wt% lecithin was developed. Temporary ion-pairing was characterized by FT-IR spectroscopy. Ex vivo permeation and exfoliation were evaluated using porcine skin models. A 2-week double-blind, split-face clinical study (n = 37) assessed efficacy using instrumental probes (Visioscan, Corneofix, VISIA-CR, and ANTERA 3D) for exfoliation-related parameters and sensitive skin compatibility.

Results: FT-IR analysis confirmed lecithin-glycolate bonding via red-shifted C = O peaks, with spectral comparisons before and after shaking demonstrating the reversible nature of the change. The biphasic serum achieved 4.19-fold higher epidermal glycolic acid delivery compared to conventional formulations with minimal deep penetration. Clinical evaluation demonstrated superior exfoliation (45.52% improvement, p < 0.001), enhanced skin brightness, texture, and hydration. Redness and transepidermal water loss, assessed for sensitive skin suitability, showed significant improvements.

Conclusion: The biphasic system successfully overcomes pH-dependent limitations of glycolic acid through temporary ion-pairing, providing enhanced exfoliation efficacy with a superior safety profile for consumer applications.

Keywords: Stratum corneum permeation; biphasic formulation; chemical exfoliation; glycolic acid; ion‐pairing.

Publication types

  • Randomized Controlled Trial
  • Comparative Study

MeSH terms

  • Adult
  • Animals
  • Double-Blind Method
  • Female
  • Glycolates* / administration & dosage
  • Glycolates* / chemistry
  • Glycolates* / pharmacokinetics
  • Humans
  • Hydrogen-Ion Concentration
  • Lecithins* / administration & dosage
  • Lecithins* / chemistry
  • Lecithins* / pharmacokinetics
  • Male
  • Middle Aged
  • Permeability
  • Skin / drug effects
  • Skin / metabolism
  • Skin Absorption* / drug effects
  • Skin Absorption* / physiology
  • Spectroscopy, Fourier Transform Infrared
  • Swine
  • Young Adult

Substances

  • Lecithins
  • Glycolates
  • glycolic acid