Pouteria macrophylla Fruit Extract Microemulsion for Cutaneous Depigmentation: Evaluation Using a 3D Pigmented Skin Model

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Brathwaite, Ana Clara N. ; Alencar-Silva, Thuany ; Carvalho, Larissa A. C. ; Branquinho, Maryana S. F. ; Ferreira-Nunes, Ricardo ; Cunha-Filho, Marcilio ; Gelfuso, Guilherme M. ; Maria-Engler, Silvya S. ; Carvalho, Juliana Lott ; Silva, Joyce K. R. ; Gratieri, Tais

• Document type: Journal article
• Source: Molecules; v. 27, n. 18, p. 16-pg., 2022-09-01.

Abstract

Here, we verify the depigmenting action of Pouteria macrophylla fruit extract (EXT), incorporate it into a safe topical microemulsion and assess its effectiveness in a 3D pigmented skin model. Melanocytes-B16F10- were used to assess the EXT effects on cell viability, melanin synthesis, and melanin synthesis-related gene transcription factor expression, which demonstrated a 32% and 50% reduction of intra and extracellular melanin content, respectively. The developed microemulsion was composed of Cremophor EL(R)/Span 80 4:1 (w/w), ethyl oleate, and pH 4.5 HEPES buffer and had an average droplet size of 40 nm (PdI 0.40 +/- 0.07). Skin irritation test with reconstituted epidermis (Skin Ethic RHETM) showed that the formulation is non-irritating. Tyrosinase inhibition was maintained after skin permeation in vitro, in which microemulsion showed twice the inhibition of the conventional emulsion (20.7 +/- 2.2% and 10.7 +/- 2.4%, respectively). The depigmenting effect of the microemulsion was finally confirmed in a 3D culture model of pigmented skin, in which histological analysis showed a more pronounced effect than a commercial depigmenting formulation. In conclusion, the developed microemulsion is a promising safe formulation for the administration of cutite fruit extract, which showed remarkable depigmenting potential compared to a commercial formulation. (AU)

• FAPESP's process: 18/14936-1 - Mitochondrial metabolism dictates the heterogeneity and resistance of melanoma
• Grantee: Larissa Anastacio da Costa Carvalho
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 17/04926-6 - Melanoma and chemoresistance: in vitro and in silico models to exploit therapeutic targets
• Grantee: Silvya Stuchi Maria-Engler
• Support Opportunities: Research Projects - Thematic Grants