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

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
• nanotechnology
• azelaic acid
• skin
• hyaluronic acid
• nanoemulsion

Disclosure statement

The authors confirm that this article content has no conflict of interest.

Additional information

Funding

The authors wish to acknowledge the financial support and scholarships from CAPES (Coordenação de Aperfeiçoamento de Pessoal de Nível Superior) and from PPGCF/UFRGS (Graduate Program in Pharmaceutical Sciences).