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 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.

Automated summary

The study aimed to enhance the safety profile of tretinoin (TRE) by encapsulating it in nanostructured lipid carriers (NLC). NLC-TRE demonstrated spherical structures, with an average particle size of 130 nm, zeta potential of 24 mV, and encapsulation efficiency of 98%. Compared to the marketed product, NLC-TRE showed improved epidermal targeting and protection against oxidation, leading to a higher safety profile in in vitro studies and in healthy volunteers.