Preparation and Evaluation of Azelaic Acid Topical Microemulsion Formulation: In Vitro and In Vivo Study

Abstract

The aim of this study was to design oil in water (O/W) microemulsion formulations for the topical administration of azelaic acid. The permeability of azelaic acid through rat skin and the anti-inflammatory activities of the formulations were conducted to examine the efficacy of the designed formulations. Skin irritation and stability tests were also performed. The permeability of azelaic acid was significantly increased by using O/W microemulsions as carriers. The edema index of ear swelling percentage was significantly recovered by the 5% drug-loaded formulation and a 20% commercial product, demonstrating that the experimental formulation possessed comparable effect with the commercial product on the improvement of inflammation. The experimental formulation did not cause significant skin irritation compared to the negative control group. Moreover, the drug-loaded formulation also showed thermodynamic stability and chemical stability after storage for 30 days. In conclusion, the O/W microemulsion was a potential drug delivery carrier for azelaic acid topical application.

Calendula officinalis L. bitkisinin morfolojik özellikleri, ekstre içeren topikal ilaç formülasyonu geliştirilmesi ve in vitro değerlendirilmesi

“…Geliştirilen tüm formülasyonların 0.5'in altındaki PDI değerine sahip olması, damlacıkların tekdüzeliğinin göstermekte ve damlacıkların boyutlarının yakın aralıkta olduğuna işaret etmektedir. 9,23 Mikroemülsiyonların zeta potansiyel değerleri, noniyonik yüzey aktif maddeler içermesi sebebi ile nötr bir değere yakın bulunmuştur. Bu veri, yağ globülü yüzeyinde iyonik olmayan yüzey etkin maddenin herhangi bir önemli yük (> ± 30 mV) oluşturmadığını göstermiştir.…”

Novel Hydrogels for Topical Applications: An Updated Comprehensive Review Based on Source

“…The formation of microemulsion (ME) is straightforward, comprising an oil phase, a surfactant, a cosurfactant, and aqueous phases, and can easily be prepared through gentle stirring. ME is an encouraging nanocarrier for the topical administration of poorly water-soluble drugs [ 46 ]. Ibuprofen (IBU) is a non-steroidal anti-inflammatory poor water-soluble drug.…”

Insights from a Box–Behnken Optimization Study of Microemulsions with Salicylic Acid for Acne Therapy

“…To exemplify this, Hung W.H. et al established the use of a maximum oil concentration of 10% for anti-acne microemulsions [33]. Inclusion of calculated amounts of surfactant and cosurfactant is related to two main attributes-promotion of high solubilization of the oil phase and active substances, and a decrease in the interfacial tension at the O/W interface up to ultralow values.…”

“…In the same manner, the stabilizers function as skin penetration enhancers, implied in lipid fluidization, and temporarily disrupt effects on lipidic membrane domains, assuring accumulation of a higher concentration of the active pharmaceutical ingredient (API) in dermis structures [36,37]. Those qualities were appreciated in several new studies designed to assure superior therapeutic effects for azelaic acid [33], adapalene [38], nicotinamide [39], or fusidic acid [40].…”

“…The application of a transparent formulation on the skin site can offer a pleasant experience, without leaving colored traces. Its elegant appearance, completed by appropriate pharmaceutical attributes increases confidence and adherence in affected patients [33].…”