Characterization of an antioxidant surfactant-free topical formulation containing Castanea sativa leaf extract.

CONTEXT: Inclusion of antioxidants in topical formulations can contribute to minimize oxidative stress in the skin, which has been associated with photoaging, several dermatosis and cancer. OBJECTIVE: A Castanea sativa leaf extract with established antioxidant activity was incorporated into a semisolid surfactant-free formulation. The objective of this study was to perform a comprehensive characterization of this formulation. MATERIALS AND METHODS: Physical, microbiological and functional stability were evaluated during 6 months storage at 20 °C and 40 °C. Microstructure elucidation (cryo-SEM), in vitro release and in vivo moisturizing effect (Corneometer® CM 825) were also assessed. RESULTS AND DISCUSSION: Minor changes were observed in the textural and rheological properties of the formulation when stored at 20 °C for 6 months and the antioxidant activity of the plant extract remained constant throughout the storage period. Microbiological quality was confirmed at the end of the study. Under accelerated conditions, higher modifications of the evaluated parameters were observed. Cryo-SEM analysis revealed the presence of oil droplets dispersed into a gelified external phase. The release rate of the antioxidant compounds (610 ± 70 µgh(-0.5)) followed Higuchi model. A significant in vivo moisturizing effect was demonstrated, that lasted at least 4 h after product's application. CONCLUSION: The physical, functional and microbiological stability of the antioxidant formulation was established. Specific storage conditions should be recommended considering the influence of temperature on the stability. A skin hydration effect and good skin tolerance were also found which suggests that this preparation can be useful in the prevention or treatment of oxidative stress-mediated dysfunctions.

Influence of lipid microparticle encapsulation on in vitro efficacy, photostability and water resistance of the sunscreen agents, octyl methoxycinnamate and butyl methoxydibenzoylmethane.

CONTEXT: Essential requirements for the efficacy of sunscreen agents are optimal UV absorption, high photostability and resistance against water removal. OBJECTIVE: Aim of this study was to investigate the effect of encapsulation in lipid microparticles (LMs) on the overall performance of the two most commonly used sunscreen agents, octyl methoxycinnamate (OMC) and butyl methoxydibenzoylmethane (BMDBM). METHODS: LMs loaded with OMC and BMDBM were prepared by melt emulsification and characterized by optical microscopy, UV filter content and release studies. The LMs incorporating OMC and BMDBM or the nonencapsulated sunscreen agents were introduced into a model cream (oil-in-water emulsion). RESULTS: No significant differences were observed between the sun protection factor (SPF) of the formulations containing the free (SPF, 9.4 ± 1.9) or microencapsulated (SPF, 9.6 ± 1.3) UV filters. Irradiation of the creams with a solar simulator demonstrated that the photodecomposition of OMC and BMDBM was significantly decreased by encapsulation in LMs from 55.7 ± 5.3% to 46.1 ± 5.1% and 36.3 ± 3.9% to 20.1 ± 4.7%, respectively. However, in vitro water-resistance studies showed that entrapment in the LMs significantly enhanced the sunscreen agent removal caused by watering (the losses for OMC and BMDBM were 45.1 ± 6.3% and 49.2 ± 8.4%, respectively), as compared to the formulation with the nonencapsulated sunscreen agents (the losses for OMC and BMDBM were 26.7 ± 6.1% and 28.0 ± 6.7%, respectively). CONCLUSION: Incorporation in LMs can have controversial effects on UV filter efficacy. In particular, the water-resistance properties of sun-care formulations containing sunscreens loaded in LMs should be verified to assure that the photoprotective activity is maintained during usage.