Formulation of a eugenol-based O/W emulsion for application as a topical and oral anesthetic by low-energy emulsification

Abstract

Emulsions are systems formed by two immiscible liquids, one of which is dispersed in the other as droplets with relative stability. These have multiple applications, among them, in the formulation of pharmaceutical and cosmetic products. Its preparation requires generating a large interfacial area, which is usually attained by using the physicochemical formulation know-how on surfactant-oil-water (SOW) systems. Among the applications in the pharmaceutical industry, topical creams, and emulsions for intravenous and for oral administration can be found. Eugenol can be extracted from cloves (Syzygium aromaticum) by various methods, including steam distillation, hydrodistillation and Soxhlet extraction. Furthermore, emul-sions based on eugenol can be obtained for a variety of applications, including as topical and oral anesthetic. Nanoemulsions can be formulated with a mixture of nonionic surfactants Span 20/Tween 80 at an HLB of 11 to 13 and a total surfactant concentration of 4%, using the dilution phase transition method (so-called spontaneous emulsification) to attain stable O/W eugenol-based emulsions. Paraffin oil/eugenol ratio of 4/1 can be used to reach a final emulsion internal oil phase content of 10% with 4% surfactant and 86% aqueous phase. Different polymers are used as viscosifying agents, including carbox-ymethylcellulose. Under these conditions, eugenol-based emulsions with an average droplet size of less than 2 µm can be attained, with topical and oral anesthetic characteristics.