Journal
PHARMACEUTICS
Volume 13, Issue 12, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics13122042
Keywords
oxidative stress; drug delivery systems; bioactive compounds; solid lipid nanoparticles; nanostructured lipid carriers
Categories
Funding
- Laboratory for Process Engineering, Environment, Biotechnology, and Energy (LEPABE) - FCT/MCTES (PIDDAC) [UIDB/00511/2020]
- Project 2SMART-engineered smart materials for smart citizens - Norte Portugal Regional Operational Program (NORTE 2020) under the PORTUGAL 2020 Partnership Agreement through the European Regional Development Fund (ERDF) [NORTE-01-0145-FEDER-000054]
- FCT [CEECINST/00049/2018]
- FCT-Fundacao para a Ciencia e a Tecnologia, I.P. [UIDP/04378/2020, UIDB/04378/2020, LA/P/0140/2020]
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Encapsulating naringenin, NDGA, and kaempferol into nanostructured lipid carriers showed promising results for developing an antioxidant skin care formulation.
Oxidative stress, triggered by UV radiation, is one of the major causes of free radical-associated disorders, such as skin cancer. The application of natural compounds (NCs) with antioxidant effects can attenuate free radicals' accumulation and, therefore, provide a strategy for skin care and cancer prevention. In this work, three natural compounds, naringenin, nordihydroguaiaretic acid (NDGA), and kaempferol, were encapsulated into nanostructured lipid carriers (NLCs) aiming for the development of a formulation for cutaneous application with antioxidant properties. For the experiments, different formulation parameters were evaluated to optimize the NLCs that showed a diameter around 200 nm, which is an adequate particle size for incorporation in cosmetics. Transmission electron microscopy (TEM) analysis confirmed the NLCs' typical spherical morphology. Encapsulation efficiency (EE) and loading capacity (LC) values revealed an effective production process, with EEs over 90% and LCs near the maximum value. The developed NLCs revealed a prolonged in vitro release of the natural compounds. The NLCs were stable under storage conditions, maintaining their psychochemical characteristics for 30 days. Additionally, they did not show any physical instability in accelerated stability studies, which also suggests long-term stability. Finally, the NCs antioxidant activity was evaluated. Interestingly, the NDGA and kaempferol mixture provided an antioxidant synergic effect. The NLC formulations' cytotoxicity was tested in vitro in immortalized human keratinocytes (HaCaT). In addition, putative antioxidant effects of the developed NLC formulations against tert-butyl hydroperoxide (t-BHP)-induced oxidative stress were studied, and the NDGA-loaded NLC was revealed to be the one with the most protective effect. Therefore, we concluded that the naringenin, NDGA, and kaempferol incorporation into NLCs constitutes a promising strategy to increase their bioavailability and delivery to the skin.
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