1. Evaluation of the safety and efficacy of skin penetration enhancer Putocrin®.
- Author
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Cen Z, Chen Z, Wang D, Chen X, and Chen J
- Subjects
- Animals, Humans, Swine, Cell Survival drug effects, Administration, Cutaneous, Tranexamic Acid administration & dosage, Tranexamic Acid pharmacokinetics, Tranexamic Acid pharmacology, Drug Combinations, Membrane Proteins, Skin Absorption drug effects, Zebrafish, Filaggrin Proteins, Keratinocytes drug effects, Skin drug effects, Skin metabolism
- Abstract
Background: Substances that can efficiently enhance skin penetration while exerting no adverse effect are useful for drug and cosmetics formulation., Objective: To investigate the safety and enhance skin penetration efficacy of Putocrin®, a combination containing 2% isosorbide dimethyl ether, 1% pentanediol, and 0.5% inositol., Methods: An in vitro keratinocyte cell assay using 3-(4,5-dimethylthiazolyl-2)-2,5 diphenyltetrazolium bromide (MTT), and an in vitro EpiKutis® skin study adopted hematoxylin and eosin staining, immunostaining, and liquid chromatography-mass spectrometry (LC-MS) analysis were carried out to investigate the safety of Putocrin®. A pigskin-Franz cell system experiment applied high-performance liquid chromatography (HPLC) to compare the skin penetration efficiency of fluorescein isothiocyanate (Fitc)-labeled tranexamic acid with or without the assistance of Putocrin®. The safety and efficacy of Putocrin® was further evaluated on zebrafish embryos., Results: The MTT assay showed that Putocrin® at concentration ≤2.5% did not significantly affect cell viability. The in vitro EpiKutis® skin study revealed that 2.5% Putocrin® did not affect skin morphology, filaggrin content, ceramide/protein, or fatty acid/protein ratios, but significantly increased loricrin content by 86.00% (p < 0.001). The pigskin-Franz cell penetration experiment demonstrated that Fitc-labeled tranexamic acid could barely penetrate the skin (with penetration rate of 1.121%), while Putocrin® significantly enhanced the penetration rate up to 83.983%, which was close to unlabeled tranexamic acid (90.013%). The zebrafish embryo study showed that 2.5% Putocrin® did not exert observable toxicity and obviously assisted the skin penetration of Fitc-labeled tranexamic acid into fish embryos. These results indicate the strong enhancing skin penetration potency of Putocrin®., Conclusion: This study demonstrated the safety as well as the strong enhancing skin penetration potency of Putocrin® for cosmetics formulation use., (© 2024 The Author(s). Journal of Cosmetic Dermatology published by Wiley Periodicals LLC.)
- Published
- 2024
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