Vitiligo is a chronic cutaneous disorder characterized by skin and hair depigmentation. Drugs that are currently used to treat vitiligo lack of efficacy and had low local accumulation due to the skin barrier properties and drug metabolism/inactivation. Therefore, the topical use of ultradeformable nanomedicines can offer a clinically relevant approach. The aim of this study was the preparation of ultradeformable nanocarriers for the percutaneous co-delivering of khellin and idebenone. The nanocarriers were physicochemical characterized. Namely, average size, size distribution, zeta potential, long-term stability and entrapment efficiency were carried out. Ethosomes made up from phospholipon 90G 1 % (w/v) and ethanol 30 % (w/v), and transfersomes had the best physicochemical properties and stability for skin topical application and were used for further in vitro experiments. The percutaneous permeation studies using human stratum corneum and epidermis membranes demonstrated that transfersomes had the best profiles and improved the delivery of khellin and idebenone across the skin. Primary human melanocytes, HEMa cells, pre-treated with H2O2 were used as an in vitro vitiligo model to test the efficacy of the investigated nanomedicines. The results demonstrated that khellin/idebenone co-loaded ultradeformable nanocarriers stimulated the melanin production and the recovery of normal skin pigmentation. In vivo studies on human volunteers demonstrated a suitable transfersomes safety, thus confirming their relevance for a possible clinical use. Finally, this research evidenced the ductility of the investigated vesicular nanomedicine to effectively co-delivery two drugs, idebenone and khellin, an antioxidant and a furanochromone drug, which seems to be a promising clinical approach for the treatment of vitiligo.
Assessing effectiveness of multistage nanomedicines for multidrug therapy of vitiligo.
Nicola d’Avanzo;Christian Celia
;Massimo Fresta
2025-01-01
Abstract
Vitiligo is a chronic cutaneous disorder characterized by skin and hair depigmentation. Drugs that are currently used to treat vitiligo lack of efficacy and had low local accumulation due to the skin barrier properties and drug metabolism/inactivation. Therefore, the topical use of ultradeformable nanomedicines can offer a clinically relevant approach. The aim of this study was the preparation of ultradeformable nanocarriers for the percutaneous co-delivering of khellin and idebenone. The nanocarriers were physicochemical characterized. Namely, average size, size distribution, zeta potential, long-term stability and entrapment efficiency were carried out. Ethosomes made up from phospholipon 90G 1 % (w/v) and ethanol 30 % (w/v), and transfersomes had the best physicochemical properties and stability for skin topical application and were used for further in vitro experiments. The percutaneous permeation studies using human stratum corneum and epidermis membranes demonstrated that transfersomes had the best profiles and improved the delivery of khellin and idebenone across the skin. Primary human melanocytes, HEMa cells, pre-treated with H2O2 were used as an in vitro vitiligo model to test the efficacy of the investigated nanomedicines. The results demonstrated that khellin/idebenone co-loaded ultradeformable nanocarriers stimulated the melanin production and the recovery of normal skin pigmentation. In vivo studies on human volunteers demonstrated a suitable transfersomes safety, thus confirming their relevance for a possible clinical use. Finally, this research evidenced the ductility of the investigated vesicular nanomedicine to effectively co-delivery two drugs, idebenone and khellin, an antioxidant and a furanochromone drug, which seems to be a promising clinical approach for the treatment of vitiligo.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.