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

• Published in: Macromolecular bioscience 2021-05, Vol.21 (5), p.e2000413-n/a
• Main Authors: Lee, Mi So, Lee, Ju Won, Kim, Su Ji, Pham‐Nguyen, Oanh‐Vu, Park, Jongmin, Park, Ju Hyun, Jung, Young Mee, Lee, Jun Bae, Yoo, Hyuk Sang
• Format: Article
• Language: English
• Subjects: cationic liposome; Cations; charged liposome; Cornea; Cryoelectron Microscopy - methods; Diffusion cells; Drug Carriers; Epithelium; Fluorescence; HEK293 Cells; Humans; Light scattering; Liposomes; Melanin; melanin formation; Microscopy, Electron, Transmission - methods; Models, Biological; Morphology; niacinamide; Nicotinamide; Penetration; Phospholipids; Photon correlation spectroscopy; Skin; Skin - metabolism; Skin Absorption; Skin Lightening Preparations - pharmacokinetics; Skin Pigmentation; Tissues; Transmission electron microscopy
• ISSN: 1616-5187; 1616-5195
• DOI: 10.1002/mabi.202000413

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. To enhance the permeation of liposomes and incorporation of bioactive agents, the transdermal delivery efficiency of the cationic, neutral and anionic liposome are investigated on the 3D skin model. Cationic liposome exhibits higher penetration efficiency to the epidermis and the stratum corneum than others. Niacinamide‐encapsulated cationic liposomes effectively attenuate melanin formation and transfer in the epidermis in 3D skin model.