RT Journal Article
T1 Ultradeformable Lipid Vesicles Localize Amphotericin B in the Dermis for the Treatment of Infectious Skin Diseases
A1 Fernández García, Raquel
A1 Statts, Larry
A1 Jesus, Jéssica A. De
A1 Dea-Ayuela, María Auxiliadora
A1 Bautista Chávez, Liliana
A1 Simão, Rubén
A1 Bolas Fernández, Francisco
A1 Ballesteros Papantonakis, María De La Paloma
A1 Laurenti, Marcia Dalastra
A1 Passero, Luiz F. D.
A1 Lalatsa, Aikaterini
A1 Serrano López, Dolores Remedios
AB Cutaneous fungal and parasitic diseases remain challenging to treat, as available therapies are unable to permeate the skin barrier. Thus, treatment options rely on systemic therapy,which fail to produce high local drug concentrations but can lead tosignificant systemic toxicity. Amphotericin B (AmB) is highly efficacious in the treatment of both fungal and parasitic diseases such as cutaneous leishmaniasis but is reserved for parenteraladministration in patients with severe pathophysiology. Here, we have designed and optimized AmB-transfersomes [93.5% encapsulationefficiency, 150 nm size, and good colloidal stability (−35.02mV)] that can remain physicochemically stable (>90% drug content)at room temperature and 4 °C over 6 months when lyophilized and stored under desiccated conditions. AmB-transfersomes possessed good permeability across mouse skin (4.91 ± 0.41 μg/cm2/h) and 10-fold higher permeability across synthetic Strat-M membranes. In vivo studies after a single topical application in mice showed permeability and accumulation within the dermis (>25 μg AmB/g skin 6 h postadministration), indicating the delivery of therapeutic amounts of AmB for mycoses and cutaneous leishmaniasis, while a single daily administration in Leishmania (Leishmania) amazonensis infected mice over 10 days, resulted in excellent efficacy (98% reduction in Leishmania parasites). Combining the application of AmB-transfersomes with metallic microneedles in vivo increased the levels in the SC and dermis but was unlikely to elicit transdermal levels. In conclusion, AmB-transfersomes are promising and stable topical nanomedicines that can be readily translated for parasitic and fungal infectious diseases.
PB ACS Publications
SN 2373-8227
YR 2020
FD 2020
LK https://hdl.handle.net/20.500.14352/92726
UL https://hdl.handle.net/20.500.14352/92726
LA eng
NO Fernández-García R, Statts L, De Jesus JA, Dea-Ayuela MA, Bautista L, Simão R, et al. Ultradeformable Lipid Vesicles Localize Amphotericin B in the Dermis for the Treatment of Infectious Skin Diseases. ACS Infect Dis 2020;6:2647–60. https://doi.org/10.1021/acsinfecdis.0c00293.
NO Universidad Complutense de Madrid
NO Fondo Colaborativo de Unión Iberoamericana de Universidades
NO Universidad de São Paulo
DS Docta Complutense
RD 11 abr 2025