RESUMO
DeoxyArbutin (dA) is a tyrosinase inhibitor that has effective skin-lightening activity and has no obvious cytotoxicity toward melanocytes. With the aim of directly evaluating the effects of microemulsions containing dA on cells, we developed oil-in-water (O/W) microemulsions with relatively lower cytotoxicities by using polysorbate-series surfactants. Measurement of the transparent properties and particle size analysis at different storage time periods revealed that the developed microemulsions were stable. Moreover, the developed microemulsions had direct effects on B16-F10 mouse melanoma cells. The anti-melanogenesis activities of dA-containing microemulsions were evidently better than that of the free dA group. The results demonstrated that the developed microemulsion encapsulating dA may allow the use of deoxyArbutin instead of hydroquinone to treat dermal hyperpigmentation disorders in the future.
Assuntos
Arbutina/análogos & derivados , Cosméticos/farmacologia , Melaninas/metabolismo , Melanoma Experimental/metabolismo , Animais , Arbutina/química , Arbutina/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Cosméticos/química , Composição de Medicamentos , Emulsões , Melanoma Experimental/tratamento farmacológico , Camundongos , Tamanho da PartículaRESUMO
Arbutin (Arb) and deoxyArbutin (dA) are both effective hypopigmentation agents. However, they are glucoside derivatives of hydroquinone (HQ), which may be decayed into HQ under higher energy environments. Therefore, safety and toxicity are very important issues when considering the usage of these compounds. However, no study has verified the properties of Ultra-Violet B (UVB)-irradiated Arb and dA. In this work, we investigated the cytotoxicity and hypopigmentation effects of UVB-irradiated Arb and dA in Detroit 551 human fibroblast cells and B16-F10 mouse melanoma cells. The results showed that UVB-irradiated Arb and dA have strong cytotoxicity for the fibroblast cells, especially for dA, the caspase-3 is also activated by the treatment of UVB-irradiated dA in Detroit 551 cells. The results correlated with the produced HQ. In addition, UVB-irradiated Arb and dA suppressed the production of melanin in melanoma cells; this is due to the release of HQ that compensates for the UVB triggered Arb and dA decomposition.
Assuntos
Arbutina/análogos & derivados , Sobrevivência Celular/efeitos dos fármacos , Hidroquinonas/toxicidade , Hipopigmentação/induzido quimicamente , Animais , Arbutina/efeitos da radiação , Arbutina/toxicidade , Caspase 3/efeitos dos fármacos , Células Cultivadas , Fibroblastos/efeitos dos fármacos , Glucosídeos , Humanos , Hidroquinonas/efeitos da radiação , Melaninas/antagonistas & inibidores , Melanócitos/efeitos dos fármacos , Melanoma Experimental , Camundongos , Raios UltravioletaRESUMO
Arbutin and deoxy arbutin may release hydroquinone under some conditions. We therefore investigated the photostability of arbutin and deoxy arbutin in an aqueous solution. The results revealed arbutin and deoxy arbutin to be photolabile in an aqueous solution. Deoxy arbutin was less stable than arbutin when exposed to UV radiation. The hydroquinone concentration was also increased during the radiation period in both solutions. Benzophenone-4 could clearly improve the photostability of arbutin during the period of UV radiation, but only slightly enhance the photostability of deoxy arbutin.