4.7 Article

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

期刊

NANOMEDICINE
卷 16, 期 16, 页码 1391-1409

出版社

FUTURE MEDICINE LTD
DOI: 10.2217/nnm-2021-0031

关键词

nanostructured lipid carrier; reconstructed human epidermis; safety profile; transepidermal water loss; tretinoin

资金

  1. FAPEMIG
  2. FAPESP [17/04926-6, 18/14936-1]
  3. CAPES
  4. CNPq
  5. Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [17/04926-6, 18/14936-1] Funding Source: FAPESP

向作者/读者索取更多资源

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.
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.

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