Nanostructured lipid carriers enhances the safety profile of tretinoin: in vitro and healthy human volunteers' studies

Author(s)

Lima, Flavia A. ^[1] ; Vilela, Raquel V. R. ^{[2, 3, 4]} ; Orefice, Rodrigo L. ^[5] ; Silva, Izabela R. ^[1] ; Reis, Eduardo C. O. ^[1] ; Carvalho, Larissa A. C. ^[6] ; Maria-Engler, Silvya S. ^[6] ; Ferreira, Lucas A. M. ^[1] ; Goulart, Gisele A. C. ^[1]

Affiliation

^[1] Univ Fed Minas Gerais, Dept Pharmaceut, Fac Pharm, BR-31270901 Belo Horizonte, MG - Brazil

^[2] Michigan State Univ, Dept Microbiol & Mol Genet, E Lansing, MI 48824 - USA

^[3] Univ Fed Minas Gerais, Fac Pharm, Dept Clin & Toxicol Anal, BR-31270901 Belo Horizonte, MG - Brazil

^[4] Michigan State Univ, Biomed Lab Diagnost, E Lansing, MI 48824 - USA

^[5] Univ Fed Minas Gerais, Sch Engn, Dept Met & Mat Engn, BR-31270901 Belo Horizonte, MG - Brazil

^[6] Univ Sao Paulo, Sch Pharmaceut Sci, Dept Clin & Toxicol Anal, BR-05508000 Sao Paulo, SP - Brazil

• Document type: Journal article
• Source: Nanomedicine; v. 16, n. 16, p. 1391-1409, APR 2021.
• Web of Science Citations: 0

Abstract

Aim: To enhance the tretinoin (TRE) safety profile through the encapsulation in nanostructured lipid carriers (NLC). Materials \& methods: NLC-TRE was developed using a 2(3) experimental factorial design, characterized (HPLC, dynamic light scattering, differential scanning calorimetry, x-ray diffraction analysis, transmission electron microscopy, cryo-transmission electron microscopy) and evaluated by in vitro studies and in healthy volunteers. Results: The NLC-TRE presented spherical structures, average particle size of 130 nm, zeta potential of 24 mV and encapsulation efficiency of 98%. The NLC-TRE protected TRE against oxidation (p < 0.0001) and promoted epidermal targeting (p < 0.0001) compared with the marketed product, both 0.05% TRE. The in vitro assay on reconstructed human epidermis and the measurement of transepidermal water loss in healthy volunteers demonstrated an enhanced safety profile in comparison to the marketed product (p < 0.0002). Conclusion: The NLC-TRE enhances the epidermal targeting and safety profile of TRE, representing a potential safer alternative for the topical treatment of skin disorders using TRE. (AU)

• 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
• 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