Gel Formulations with an Echinocandin for Cutaneous Candidiasis: The Influence of Azone and Transcutol on Biopharmaceutical Features

Caspofungin is a drug that is used for fungal infections that are difficult to treat, including invasive aspergillosis and candidemia, as well as other forms of invasive candidiasis. The aim of this study was to incorporate Azone in a caspofungin gel (CPF-AZ-gel) and compare it with a promoter-free...

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Main Authors: Noelia Pérez-González, Lupe Carolina Espinoza, María Rincón, Lilian Sosa, Mireia Mallandrich, Joaquim Suñer-Carbó, Nuria Bozal-de Febrer, Ana Cristina Calpena, Beatriz Clares-Naveros
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:Gels
Subjects:
Online Access:https://www.mdpi.com/2310-2861/9/4/308
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author Noelia Pérez-González
Lupe Carolina Espinoza
María Rincón
Lilian Sosa
Mireia Mallandrich
Joaquim Suñer-Carbó
Nuria Bozal-de Febrer
Ana Cristina Calpena
Beatriz Clares-Naveros
author_facet Noelia Pérez-González
Lupe Carolina Espinoza
María Rincón
Lilian Sosa
Mireia Mallandrich
Joaquim Suñer-Carbó
Nuria Bozal-de Febrer
Ana Cristina Calpena
Beatriz Clares-Naveros
author_sort Noelia Pérez-González
collection DOAJ
description Caspofungin is a drug that is used for fungal infections that are difficult to treat, including invasive aspergillosis and candidemia, as well as other forms of invasive candidiasis. The aim of this study was to incorporate Azone in a caspofungin gel (CPF-AZ-gel) and compare it with a promoter-free caspofungin gel (CPF-gel). An in vitro release study using a polytetrafluoroethylene membrane and ex vivo permeation into human skin was adopted. The tolerability properties were confirmed by histological analysis, and an evaluation of the biomechanical properties of the skin was undertaken. Antimicrobial efficacy was determined against <i>Candida albicans</i>, <i>Candida glabrata</i>, <i>Candida parapsilosis</i>, and <i>Candida tropicalis</i>. CPF-AZ-gel and CPF-gel, which had a homogeneous appearance, pseudoplastic behavior, and high spreadability, were obtained. The biopharmaceutical studies confirmed that caspofungin was released following a one-phase exponential association model and the CPF-AZ gel showed a higher release. The CPF-AZ gel showed higher retention of caspofungin in the skin while limiting the diffusion of the drug to the receptor fluid. Both formulations were well-tolerated in the histological sections, as well as after their topical application in the skin. These formulations inhibited the growth of <i>C. glabrata</i>, <i>C. parapsilosis</i>, and <i>C. tropicalis</i>, while <i>C. albicans</i> showed resistance. In summary, dermal treatment with caspofungin could be used as a promising therapy for cutaneous candidiasis in patients that are refractory or intolerant to conventional antifungal agents.
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spelling doaj.art-ad369fc93205468f8317944d786573b02023-11-17T19:21:37ZengMDPI AGGels2310-28612023-04-019430810.3390/gels9040308Gel Formulations with an Echinocandin for Cutaneous Candidiasis: The Influence of Azone and Transcutol on Biopharmaceutical FeaturesNoelia Pérez-González0Lupe Carolina Espinoza1María Rincón2Lilian Sosa3Mireia Mallandrich4Joaquim Suñer-Carbó5Nuria Bozal-de Febrer6Ana Cristina Calpena7Beatriz Clares-Naveros8Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University Campus of Cartuja, University of Granada, 18071 Granada, SpainDepartamento de Química, Universidad Técnica Particular de Loja, Loja 1101608, EcuadorDepartament de Ciència de Materials i Química Física, Facultat de Química, Universitat de Barcelona (UB), C. Martí i Franquès 1-11, 08028 Barcelona, SpainPharmaceutical Technology Research Group, Faculty of Chemical Sciences and Pharmacy, National Autonomous University of Honduras (UNAH), Tegucigalpa 11101, HondurasInstitut de Nanociència i Nanotecnologia (IN2UB), Universitat de Barcelona (UB), 08028 Barcelona, SpainInstitut de Nanociència i Nanotecnologia (IN2UB), Universitat de Barcelona (UB), 08028 Barcelona, SpainDepartament de Biologia, Sanitat i Medi Ambient, Facultat de Farmàcia i Ciències de l’Alimentació, Universitat de Barcelona (UB), 08028 Barcelona, SpainInstitut de Nanociència i Nanotecnologia (IN2UB), Universitat de Barcelona (UB), 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University Campus of Cartuja, University of Granada, 18071 Granada, SpainCaspofungin is a drug that is used for fungal infections that are difficult to treat, including invasive aspergillosis and candidemia, as well as other forms of invasive candidiasis. The aim of this study was to incorporate Azone in a caspofungin gel (CPF-AZ-gel) and compare it with a promoter-free caspofungin gel (CPF-gel). An in vitro release study using a polytetrafluoroethylene membrane and ex vivo permeation into human skin was adopted. The tolerability properties were confirmed by histological analysis, and an evaluation of the biomechanical properties of the skin was undertaken. Antimicrobial efficacy was determined against <i>Candida albicans</i>, <i>Candida glabrata</i>, <i>Candida parapsilosis</i>, and <i>Candida tropicalis</i>. CPF-AZ-gel and CPF-gel, which had a homogeneous appearance, pseudoplastic behavior, and high spreadability, were obtained. The biopharmaceutical studies confirmed that caspofungin was released following a one-phase exponential association model and the CPF-AZ gel showed a higher release. The CPF-AZ gel showed higher retention of caspofungin in the skin while limiting the diffusion of the drug to the receptor fluid. Both formulations were well-tolerated in the histological sections, as well as after their topical application in the skin. These formulations inhibited the growth of <i>C. glabrata</i>, <i>C. parapsilosis</i>, and <i>C. tropicalis</i>, while <i>C. albicans</i> showed resistance. In summary, dermal treatment with caspofungin could be used as a promising therapy for cutaneous candidiasis in patients that are refractory or intolerant to conventional antifungal agents.https://www.mdpi.com/2310-2861/9/4/308caspofunginechinocandinAzonecandidiasispermeation enhancergel
spellingShingle Noelia Pérez-González
Lupe Carolina Espinoza
María Rincón
Lilian Sosa
Mireia Mallandrich
Joaquim Suñer-Carbó
Nuria Bozal-de Febrer
Ana Cristina Calpena
Beatriz Clares-Naveros
Gel Formulations with an Echinocandin for Cutaneous Candidiasis: The Influence of Azone and Transcutol on Biopharmaceutical Features
Gels
caspofungin
echinocandin
Azone
candidiasis
permeation enhancer
gel
title Gel Formulations with an Echinocandin for Cutaneous Candidiasis: The Influence of Azone and Transcutol on Biopharmaceutical Features
title_full Gel Formulations with an Echinocandin for Cutaneous Candidiasis: The Influence of Azone and Transcutol on Biopharmaceutical Features
title_fullStr Gel Formulations with an Echinocandin for Cutaneous Candidiasis: The Influence of Azone and Transcutol on Biopharmaceutical Features
title_full_unstemmed Gel Formulations with an Echinocandin for Cutaneous Candidiasis: The Influence of Azone and Transcutol on Biopharmaceutical Features
title_short Gel Formulations with an Echinocandin for Cutaneous Candidiasis: The Influence of Azone and Transcutol on Biopharmaceutical Features
title_sort gel formulations with an echinocandin for cutaneous candidiasis the influence of azone and transcutol on biopharmaceutical features
topic caspofungin
echinocandin
Azone
candidiasis
permeation enhancer
gel
url https://www.mdpi.com/2310-2861/9/4/308
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