Enhanced topical delivery of small hydrophilic or lipophilic active agents and epidermal growth factor by fractional radiofrequency microporation

Pharm Res. 2012 Jul;29(7):2017-29. doi: 10.1007/s11095-012-0729-1. Epub 2012 Mar 8.


Purpose: To evaluate the ability of a novel radiofrequency (RF) microporation technology based on ablation of the skin barrier to enhance topical delivery of active ingredients

Methods: The influence of RF fluence and the molecular size of the absorbent on the permeation enhancement was confirmed by in vitro skin permeation study using Franz diffusion cells. The improved skin rejuvenation effects, such as depigmentation and anti-wrinkle effects, by enhanced topical delivery of α-bisabolol and epidermal growth factor (EGF) through the RF microchannels were investigated in photo-damaged skin.

Results: The cumulative amounts of active ingredients through the RF microporated skin were significantly increased. Topically applied α-bisabolol after RF microporation induced rapid onset of skin whitening and significantly increased the ΔL-value of UVB-induced hyperpigmented melanin hairless mouse skin. In addition, wrinkle formation after topical application of EGF with RF microporation was significantly reduced and prevented after 12 weeks, and all parameters involving wrinkles in a replica analysis were similar to those in the negative control.

Conclusions: RF microporation enhances the topical delivery of active ingredients with high molecular weight or of small hydrophilic or lipophilic molecules. Thus, this technology can effectively improve photo-induced hyperpigmentation and wrinkle formation by enhancing topical delivery of active agents.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Drug Delivery Systems / methods*
  • Epidermal Growth Factor / administration & dosage*
  • Epidermal Growth Factor / pharmacokinetics
  • Epidermal Growth Factor / pharmacology
  • Mice
  • Mice, Hairless
  • Monocyclic Sesquiterpenes
  • Radio Waves
  • Sesquiterpenes / administration & dosage*
  • Sesquiterpenes / pharmacokinetics
  • Sesquiterpenes / pharmacology
  • Skin / drug effects
  • Skin / metabolism*
  • Skin / ultrastructure
  • Skin Absorption
  • Skin Aging / drug effects
  • Skin Pigmentation / drug effects


  • Monocyclic Sesquiterpenes
  • Sesquiterpenes
  • bisabolol
  • Epidermal Growth Factor