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Drug Dev Ind Pharm. 2019 Jan 15:1-9. doi: 10.1080/03639045.2019.1569032. [Epub ahead of print]

Azelaic acid-loaded nanoemulsion with hyaluronic acid - a new strategy to treat hyperpigmentary skin disorders.

Author information

1
a Graduate Program in Pharmaceutical Sciences, Faculty of Pharmacy, Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre , Brazil.
2
b Department of Dermatology , Brazilian Society of Dermatology, Santa Clara Hospital, Santa Casa de Misericórdia de Porto Alegre , Porto Alegre , Brazil.
3
c Faculty of Pharmacy , Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre , Brazil.

Abstract

OBJECTIVE:

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.

SIGNIFICANCE:

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.

METHODS:

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.

RESULTS:

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.

CONCLUSION:

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.

KEYWORDS:

Melasma; azelaic acid; hyaluronic acid; nanoemulsion; nanotechnology; skin

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