Whey Protein/Polysaccharide-Stabilized Emulsions: Effect of Polymer Type and pH on Release and Topical Delivery of Salicylic Acid

• Published in: AAPS PharmSciTech Vol. 15; no. 3; pp. 588 - 600
• Main Authors: Combrinck, Johann, Otto, Anja, du Plessis, Jeanetta
• Format: Journal Article
• Language: English
• Published: Boston Springer US 01-06-2014
• Subjects: Administration, Cutaneous; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - chemistry; Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Carrageenan - chemistry; Chemistry, Pharmaceutical; Chitosan - chemistry; Emulsions; Excipients - chemistry; Humans; Hydrogen-Ion Concentration; Kinetics; Milk Proteins - chemistry; Models, Chemical; Particle Size; Pharmacology/Toxicology; Pharmacy; Research Article; Salicylic Acid - administration & dosage; Salicylic Acid - chemistry; Salicylic Acid - metabolism; Skin - metabolism; Skin Absorption; Solubility; Static Electricity; Surface Properties; Technology, Pharmaceutical - methods; Whey Proteins; emulsion; topical; salicylic acid; transdermal; release
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-014-0081-3

Emulsions are widely used as topical formulations in the pharmaceutical and cosmetic industries. They are thermodynamically unstable and require emulsifiers for stabilization. Studies have indicated that emulsifiers could affect topical delivery of actives, and this study was therefore designed to investigate the effects of different polymers, applied as emulsifiers, as well as the effects of pH on the release and topical delivery of the active. O/w emulsions were prepared by the layer-by-layer technique, with whey protein forming the first layer around the oil droplets, while either chitosan or carrageenan was subsequently adsorbed to the protein at the interface. Additionally, the emulsions were prepared at three different pH values to introduce different charges to the polymers. The active ingredient, salicylic acid, was incorporated into the oil phase of the emulsions. Physical characterization of the resulting formulations, i.e., droplet size, zeta potential, stability, and turbidity in the water phase, was performed. Release studies were conducted, after which skin absorption studies were performed on the five most stable emulsions, by using Franz type diffusion cells and utilizing human, abdominal skin membranes. It was found that an increase in emulsion droplet charge could negatively affect the release of salicylic acid from these formulations. Contrary, positively charged emulsion droplets were found to enhance dermal and transdermal delivery of salicylic acid from emulsions. It was hypothesized that electrostatic complex formation between the emulsifier and salicylic acid could affect its release, whereas electrostatic interaction between the emulsion droplets and skin could influence dermal/transdermal delivery of the active.