Comparison Study of the Effects of Cationic Liposomes on Delivery across 3D Skin Tissue and Whitening Effects in Pigmented 3D Skin

Macromol Biosci. 2021 May;21(5):e2000413. doi: 10.1002/mabi.202000413. Epub 2021 Mar 13.

Abstract

Charged phospholipids are employed to formulate liposomes with different surface charges to enhance the permeation of active ingredients through epidermal layers. Although 3D skin tissue is widely employed as an alternative to permeation studies using animal skin, only a small number of studies have compared the difference between these skin models. Liposomal delivery strategies are investigated herein, through 3D skin tissue based on their surface charges. Cationic, anionic, and neutral liposomes are formulated and their size, zeta-potential, and morphology are characterized using dynamic light scattering and cryogenic-transmission electron microscopy (cryo-TEM). A Franz diffusion cell is employed to determine the delivery efficiency of various liposomes, where all liposomes do not exhibit any recognizable difference of permeation through the synthetic membrane. When the fluorescence liposomes are applied to 3D skin, considerable fluorescence intensity is observed at the stratum cornea and epithelium layers. Compared to other liposomes, cationic liposomes exhibit the highest fluorescence intensity, suggesting the enhanced permeation of liposomes through the 3D skin layers. Finally, the ability of niacinamide (NA)-incorporated liposomes to suppress melanin transfer in pigmented 3D skin is examined, where cationic liposomes exhibit the highest degree of whitening effects.

Keywords: cationic liposome; charged liposome; melanin formation; niacinamide.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cations
  • Cryoelectron Microscopy / methods
  • Drug Carriers
  • HEK293 Cells
  • Humans
  • Liposomes*
  • Microscopy, Electron, Transmission / methods
  • Models, Biological*
  • Skin / metabolism*
  • Skin Absorption*
  • Skin Lightening Preparations / pharmacokinetics*
  • Skin Pigmentation*

Substances

  • Cations
  • Drug Carriers
  • Liposomes
  • Skin Lightening Preparations