Development of a novel human stratum corneum mimetic phospholipid ­vesicle-based permeation assay models for in vitro permeation studies

Abstract

Objectives

To develop and evaluate a novel human stratum corneum (SC) mimetic phospholipid vesicle-based permeation assay (PVPA_SC) model for in vitro permeation studies.

Significance

Due to the increasing restrictions on the use of human and animal skins, artificial skin models have attracted substantial interest in pharmaceuticals and cosmetic industries. In this study, a modified PVPA_SC model containing both SC lipids and proteins was developed.

Methods

The PVPA_SC model was optimized by altering the lipid composition and adding keratin in the formulation of large liposomes. The barrier properties were monitored by measuring the electrical resistance (ER) and permeability of Rhodamine B (RB). The modified PVPA_SC model was characterized in terms of the surface topography, solvent influence and storage stability. The permeation studies of the active components in Compound Nanxing Zhitong Plaster (CNZP) were performed to examine the capability of PVPA_SC in the application of skin penetration.

Results

The ER and P_app values of RB obtained from the optimized PVPA_SC model indicated a similar barrier property to porcine ear skin. Scanning electron microscope analysis demonstrated a mimic ‘brick-and-mortar’ structure. The PVPA_SC model can be stored for three weeks at −20 °C, and withstand the presence of different receptor medium for 24 h. The permeation studies of the active components demonstrated a good correlation (r² = 0.9136) of P_app values between the drugs’ permeation through the PVPA_SC model and porcine ear skin.

Conclusion

Keratin contained composite phospholipid vesicle-based permeation assay models have been proven to be potential skin tools in topical/transdermal permeation studies.

Keywords:

• PVPA_SC
• skin mimetic models
• permeation studies
• keratin
• composite phospholipid

Disclosure statement

No potential conflict of interest was reported by the author(s).

Data Availability Statement

The datasets generated during and/or analyzed during the current study are available from the corresponding author on reasonable request.

Additional information

Funding

The authors acknowledge the support for this work by the State Key Laboratory of New Technology in Traditional Chinese Medicine Pharmaceutical Process (SKL2020Z0202), the Project of Jiangsu Collaborative Innovation Centre of Chinese Medicinal Resources Industrialization (ZDXM-2020-25), and the National Natural Science Foundation of China (No. 82003305).