Palmitoylethanolamide-Incorporated Elastic Nano-Liposomes for Enhanced Transdermal Delivery and Anti-Inflammation

  • Pharmaceutics. 2024 Jun 29;16(7):876. doi: 10.3390/pharmaceutics16070876.
Chuanpeng Ren  1 ,  Yanyun Ma  2  3 ,  Yizhen Wang  1 ,  Dan Luo  4 ,  Yanhan Hong  4 ,  Xinyuan Zhang  5 ,  Hexiang Mei  1 ,  Wei Liu  6
Affiliations
  • 1. The Institute of Biocelline Precision Dermatology, Shanghai 200031, China.
  • 2. Human Phenome Institute, Fudan University, Shanghai 201210, China.
  • 3. Institute for Six-Sector Economy, Fudan University, Shanghai 201203, China.
  • 4. Wuhan Bestcarrier Biotechnology Co., Ltd., Wuhan 430075, China.
  • 5. Shanghai Skinshield Clinical Testing and Technological Research Ltd., Shanghai 201210, China.
  • 6. National Engineering Research Center for Nanomedicine, Huazhong University of Science and Technology, Wuhan 430074, China.
PMID: 39065574 DOI: 10.3390/pharmaceutics16070876
Abstract

Palmitoylethanolamide (PEA) exhibits multiple skincare functions such as anti-nociceptive and anti-inflammatory effects. However, its topical application is limited due to its difficulty in bypassing the stratum corneum barrier, relatively low bioavailability, and low stability. Herein, elastic nano-liposomes (ENLs) with excellent deformability and elasticity were utilized as a novel Drug Delivery system to encapsulate PEA to overcome the abovementioned issues and enhance the biological effects on the skin. ENL was prepared with phosphatidylcholine, Cholesterol, and cetyl-PG hydroxyethyl palmitamide with a molar ratio mimicking skin epidermal Lipids, and PEA was loaded. The PEA-loaded ENL (PEA-ENL) demonstrated efficient transdermal delivery and enhanced skin retention, with negligible cytotoxicity toward HaCaT cells and no allergic reaction in the human skin patch test. Notably, PEA-ENL treatment increased cell migration and induced significant regulation in the expression of genes associated with anti-nociceptive, anti-inflammatory, and skin barrier repair. The mechanism of the anti-nociceptive and anti-inflammatory effects of PEA was further investigated and explained by molecular docking site analysis. This novel PEA-ENL, with efficient transdermal delivery efficiency and multiple skincare functionalities, is promising for topical application.

Keywords
anti-inflammatory; anti-nociceptive; elastic nano-liposomes; palmitoylethanolamide; transdermal delivery; transient receptor potential vanilloid 1.
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