The Topical Nanodelivery of Vismodegib Enhances Its Skin Penetration and Performance In Vitro While Reducing Its Toxicity In Vivo

被引：6
|
作者：
Natalia Calienni, Maria [1 ,2 ,3 ]
Maza Vega, Daniela [1 ,2 ]
Facundo Temprana, C. [4 ,5 ]
Cecilia Izquierdo, Maria [1 ,2 ]
Ybarra, David E. [1 ,2 ]
Bernabeu, Ezequiel [5 ,6 ]
Moretton, Marcela [5 ,6 ]
Alvira, Fernando C. [1 ,2 ]
Chiappetta, Diego [5 ,6 ]
Del Valle Alonso, Silvia [1 ,2 ]
Jimena Prieto, Maria [1 ,2 ]
Montanari, Jorge [1 ,2 ,3 ]
机构：
[1] Univ Nacl Quilmes, Dept Ciencia & Tecnol, Lab Bionanotecnol, RA-1876 Buenos Aires, DF, Argentina
[2] IMBICE CONICET CCT La Plata, Grp Biol Estruct & Biotecnol GBEyB, RA-1906 Buenos Aires, DF, Argentina
[3] Univ Nacl Hurlingham UNAHUR, RA-1688 Hurlingham, Buenos Aires, Argentina
[4] Univ Nacl Quilmes, Dept Ciencia & Tecnol, Lab Inmunol & Virol LIV, RA-1876 Bernal, Buenos Aires, Argentina
[5] Consejo Nacl Invest Cient & Tecn CONICET, RA-1425 Buenos Aires, DF, Argentina
[6] Univ Buenos Aires, Fac Farm & Bioquim, Catedra Tecnol Farmaceut 1, RA-1113 Buenos Aires, DF, Argentina
来源：
PHARMACEUTICS | 2021年 / 13卷 / 02期
关键词：
vismodegib; skin cancer; drug-delivery nanosystems; skin penetration; cytotoxicity; cellular uptake; zebrafish;
D O I：
10.3390/pharmaceutics13020186
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Vismodegib is a first-in-class inhibitor for advanced basal cell carcinoma treatment. Its daily oral doses present a high distribution volume and several side effects. We evaluated its skin penetration loaded in diverse nanosystems as potential strategies to reduce side effects and drug quantities. Ultradeformable liposomes, ethosomes, colloidal liquid crystals, and dendrimers were able to transport Vismodegib to deep skin layers, while polymeric micelles failed at this. As lipidic systems were the most effective, we assessed the in vitro and in vivo toxicity of Vismodegib-loaded ultradeformable liposomes, apoptosis, and cellular uptake. Vismodegib emerges as a versatile drug that can be loaded in several delivery systems for topical application. These findings may be also useful for the consideration of topical delivery of other drugs with a low water solubility.
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页数：22
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