Optimization of fibroin nanoparticles through experimental design and response surface methodology for transdermal application.
Alopecia: Minoxidil; Nanoparticles; Fibroin; Polymeric matrix.
Transdermal drug administration has limitations due to the stratum corneum, whose function as a physicochemical barrier of the skin hinders drug permeation, particularly for hydrophilic molecules and those with high molecular weight. As a result, bioavailability becomes insufficient and the therapeutic efficacy of the drug is compromised. Therefore, polymeric nanoparticles represent a strategic approach to overcoming low skin permeability, enabling encapsulation, protection, and controlled release of drugs.Accordingly, the main objective is to develop and optimize fibroin nanocapsules obtained from silk fibroin residues for the loading of active ingredients such as minoxidil and niacinamide for transdermal application. In addition, silk fibroin powder sold for cosmetic use was employed in the preparation of nanoparticles to encapsulate ferulic acid and mandelic acid.Fibroin was separated from the silkworm (Bombyx mori) by a degumming process, and fibroin extraction was carried out using a ternary solution of calcium chloride, ethanol, and water. Before synthesizing fibroin nanoparticles by the desolvation method, a comparative test was performed using the desolvating agents acetone, grain alcohol, ethanol, and propylene glycol to select which solvent would be used in the process.The high encapsulation efficiencies, ranging from 89% to 92%, demonstrated the ability of silk fibroin as a polymeric matrix to encapsulate poorly water-soluble molecules such as minoxidil, as well as highly hydrophilic actives such as niacinamide. Therefore, the systems developed are promising for transdermal application.