Mechanistic insights into high permeation vesicle-mediated synergistic enhancement of transdermal drug permeation

Nanomedicine (Lond). 2019 Aug;14(16):2227-2241. doi: 10.2217/nnm-2018-0519. Epub 2019 Aug 9.

Abstract

Aim: To design a nanocarrier platform for enhanced transdermal drug permeation. Materials & methods: Gel-based high permeation vesicles (HPVs) were developed and their performance in terms of transdermal flux improvement, in vitro release and skin irritancy was assessed. The mechanistic insights of permeation enhancement were explored using confocal laser scanning microscopy, ATR-FTIR, DSC and P31 NMR. Results: HPVs exhibited as vesicles with uniform size (∼150 nm), extended drug-release profile (∼48 h) and improved transdermal flux. HPVs were also nontoxic and nonirritant to skin. Enhanced vesicle deformability, improved vesicle membrane fluidity and synergistic permeation enhancement action of synergistic combination of permeation enhancer components was found to be responsible for HPV-mediated permeation enhancement. Conclusion: Overall, the study established that HPVs demonstrate a promising therapeutic advantage over conventional transdermal drug carriers.

Keywords: high permeation vesicles; lipid vesicles; permeation enhancers; transdermal drug delivery; transdermal drug permeation.

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Drug Delivery Systems / methods*
  • Humans
  • Magnetic Resonance Spectroscopy
  • Microscopy, Confocal / methods*
  • Rats
  • Rats, Sprague-Dawley
  • Skin / metabolism*
  • Skin Absorption
  • Spectroscopy, Fourier Transform Infrared
  • Swine