Potential of Icariin–Glucosamine Combination in the Treatment of Osteoarthritis by Topical Application: Development of Topical Formulation and In Vitro Permeation Study

Abstract

The aim of this study was to develop a topically applied formulation with the potential to alleviate arthritis ailments. A combination of two active ingredients, icariin from Epimedium L. (Species: Epimedium Koreanum) extract as a potential promoter of chondrogenesis and glucosamine sulfate as a precursor of cartilage tissues, was tested. In permeation studies, the potential for skin permeation of both substances was confirmed; however, the in vitro release test did not accurately reflect the degree of skin permeation. The in vitro release of icariin was at a level of 15.0–19.0% for the plant-extract-derived icariin and 29.0–35.0% for the pure substance. The level of glucosamine sulfate release was 38.4% (on average). For icariin of both origins, the release results were higher than those obtained via oral administration (about 12.0%), which shows the potential superiority of topical application. In addition, the physicochemical parameters that affect the in vitro release and performance of topical formulations were addressed. This preliminary research and permeation analysis of the formulation produced a promising picture of its prospects regarding arthritis treatment, although further investigation is needed.

Keywords

• icariin
• <i>Epimedium</i> L. extract
• glucosamine sulfate
• osteoarthritis
• topical application
• in vitro release