Affiliation:
1. Guangzhou Luanying Cosmetics Co., Ltd Guangzhou China
2. Centre for Biotech Big Data Research & Development Research Institute of Tsinghua Pearl River Delta China
3. Vitargent (International) Biotechnology Limited Hong Kong China
Abstract
AbstractBackgroundSubstances that can efficiently enhance skin penetration while exerting no adverse effect are useful for drug and cosmetics formulation.ObjectiveTo investigate the safety and enhance skin penetration efficacy of Putocrin®, a combination containing 2% isosorbide dimethyl ether, 1% pentanediol, and 0.5% inositol.MethodsAn 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.ResultsThe 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®.ConclusionThis study demonstrated the safety as well as the strong enhancing skin penetration potency of Putocrin® for cosmetics formulation use.