β-Cyclodextrins as Carriers for the Targeted Delivery of Pharmaceutical Substances against Lipase from Malassezia spp. ^†

Abstract

Seborrheic dermatitis (SD) and dandruff are the most prevalent scalp diseases in populations around the world. The main etiopathogenetic factor of these diseases is an altered abundance of Malassezia species that secrete several lipases and turn acylglycerides into fatty acids associated with an inflammatory reaction, itching, and scalp dryness. The investigated synthetic and natural-based agents showed activity against Malassezia lipase, but they have low solubility and therefore bioavailability. β-cyclodextrins (β-CDs) and their derivatives are promising carriers and additives with which to improve the solubility of molecules and carry out possible targeted drug delivery. Therefore, this research aimed to evaluate the β-CD–lipase interaction as well as the influence of β-CDs on lipase activity. Modern methods are used to model the structural elucidation of β-CDs with lipase. In this study, transmission electron microscopy (TEM) showed that β-CD–lipase complexes were formed in the form of grape bunches to maintain stability. Additionally, β-CDs interacted with the active site and terminal subunits of lipase. Moreover, β-CDs changed the configuration of lipase in a dose-dependent manner, identified by UV spectroscopy and fluorescence assays. Furthermore, lipase activity, measured by oleic acid yield, was significantly decreased due to the presence of different β-CD concentrations. Thus, β-CDs strongly interacted with lipase and influenced its enzymatic activity, meaning that they could be considered as drug delivery systems for novel therapies of SD and dandruff.