Fabrication of astaxanthin-loaded electrospun nanofiber-based mucoadhesive patches with water-insoluble backing for the treatment of oral premalignant lesions

Oral premalignant lesions (OPL) are one of the most common oral diseases, affecting the quality of life and even leading to oral cancer. Current treatments commonly use steroids/retinoids in mouthwashes, films, or ointments. However, conventional drugs/formulations have significant side effects/limitations. Herein, astaxanthin-loaded polycaprolactone (PCL)/gelatin (GT) nanofiber-based mucoadhesive patches (PGA) with the water-insoluble PCL nanofiber backing (PCL/PGA) are developed via electrospinning for the management of OPL. The saliva-insoluble PCL backing could greatly prevent drug loss after applica-tion in the oral cavity. The prepared PCL/PGA patches exhibit a suitable astaxanthin release rate for achieving high local drug concentration, which permeated into buccal mucosa. In addition, the developed thin patches display excellent wet tissue adhesion and great air permeability due to their high porosity. Notably, the in vivo experiment shows that the bioactive mucoadhesive patches significantly promote the recovery of OPL by suppressing the expression of Ki67 and cyclooxygenase-2 (COX-2), comparable to clinical tretinoin cream formulation. Also, the patches did not induce any side effects (i.e., hair loss and oral ulcers) compared to clinical tretinoin cream formulation. The results demonstrate that this novel electrospun mucoadhesive bilayer patch holds great potential for the treatment of OPL.(c) 2022 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (http:// creativecommons.org/licenses/by/4.0/).