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

Aim: To enhance the tretinoin (TRE) safety profile through the encapsulation in nanostructured lipid carriers (NLC).

Materials & methods: NLC-TRE was developed using a 2³ 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.

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Article information: Flávia A Lima, Raquel VR Vilela, Rodrigo L Oréfice, Izabela R Silva, Eduardo CO Reis, Larissa AC Carvalho, Silvya S Maria-Engler, Lucas AM Ferreira, and Gisele AC Goulart. Nanomedicine 0 0:0