壬二酸
酪氨酸酶
化学
Zeta电位
透明质酸
细胞毒性
透皮
真皮
渗透(战争)
药理学
色谱法
体外
纳米颗粒
生物化学
纳米技术
材料科学
医学
酶
工程类
解剖
运筹学
作者
Simone Jacobus Berlitz,Damiê De Villa,Luiz Augusto Maschmann Inácio,Samuel Davies,Kelly Cristine Zatta,Sílvia Stanisçuaski Guterres,Irene Clemes Külkamp‐Guerreiro
标识
DOI:10.1080/03639045.2019.1569032
摘要
To develop an azelaic acid (AzA)-loaded nanoemulsion with hyaluronic acid (HA) as a double targeting strategy to increase drug retention and tyrosinase inhibition activity.Dermic melasma is a recalcitrant disease. Therefore, the development of new technologies that allow a deeper penetration in the skin while enhancing the efficacy of a safe and well-known dermatological active, like AzA, is a very promising alternative to improve the treatment of this disease.An oil-in-water nanoemulsion was developed and characterized according to its droplet size distribution, zeta potential, pH value, drug content, encapsulation efficiency, spectroscopic characteristics, morphology, and stability. In vitro mushroom tyrosinase inhibition assay, cytotoxicity, and permeation studies were performed. A descriptive sensory evaluation was also carried out.Drug content was 10 mg/ml, particle size 419 ± 23 nm with monomodal distribution, encapsulation efficiency was 84.65%, zeta potential -10.9 ± 0.44 mV and pH 5.01 ± 0.01. The nanoemulsion was stable for 30 days (30 °C/65% RH). The nanoemulsion decreased tyrosinase activity and permeated through the skin, reaching viable epidermis and dermis and did not show signs of cytotoxicity. Sensory evaluation profile showed a higher spreadability with lesser whitening residue.The nanoemulsion presented characteristics within the nanoscale and reached the deeper layers of the skin while improving in vitro tyrosinase inhibition; hence, it could be a promising treatment to dermic melasma.
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