Liquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of Syngonanthus nitens (Bong.) Ruhland against infection by Candida krusei

Matheus Aparecido dos Santos Ramos,1 Giovana Calixto,2 Luciani Gaspar de Toledo,3 Bruna Vidal Bonifácio,1 Lourdes Campaner dos Santos,4 Margarete Teresa Gottardo de Almeida,3 Marlus Chorilli,2 Taís Maria Bauab1 1Department of Biological Sciences, School of Pharmaceutical Scien...

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Autores principales: dos Santos Ramos MA, Calixto G, de Toledo LG, Bonifácio BV, dos Santos LC, de Almeida MT, Chorilli M, Bauab TM
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Publicado: Dove Medical Press 2015
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record_format dspace
institution DOAJ
collection DOAJ
language EN
topic Candida krusei
Precursor system of mucoadhesive liquid crystal
Nanostructured system
Syngonanthus nitens
Prophylaxis.
Medicine (General)
R5-920
spellingShingle Candida krusei
Precursor system of mucoadhesive liquid crystal
Nanostructured system
Syngonanthus nitens
Prophylaxis.
Medicine (General)
R5-920
dos Santos Ramos MA
Calixto G
de Toledo LG
Bonifácio BV
dos Santos LC
de Almeida MT
Chorilli M
Bauab TM
Liquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of Syngonanthus nitens (Bong.) Ruhland against infection by Candida krusei
description Matheus Aparecido dos Santos Ramos,1 Giovana Calixto,2 Luciani Gaspar de Toledo,3 Bruna Vidal Bonifácio,1 Lourdes Campaner dos Santos,4 Margarete Teresa Gottardo de Almeida,3 Marlus Chorilli,2 Taís Maria Bauab1 1Department of Biological Sciences, School of Pharmaceutical Sciences, 2Department of Drugs and Medicine, School of Pharmaceutical Sciences, São Paulo State University, Araraquara, 3Department of Infectious Diseases, Faculty of Medicine of São José do Rio Preto, São José do Rio Preto, 4Department of Organic Chemistry, Chemistry Institute, São Paulo State University, Araraquara, São Paulo, Brazil Abstract: Vaginal infections caused by Candida krusei are a problem of extreme complexity due to the intrinsic resistance to azole drugs. The species Syngonanthus nitens (Bong.) Ruhland is a plant of the Eriocaulaceae family that has demonstrated promising antifungal activity. In phyto-formulation research, liquid crystal precursor mucoadhesive systems (LCPM) stand out as drug delivery systems for vaginal administration because they increase the activity and overcome the problems associated with plant-based medicines. Therefore, the objective of this study was to evaluate the potential of the methanolic extract of scapes of S. nitens (S. nitens extract [SNE]) and an SNE-loaded LCPM against C. krusei as prophylaxis for vulvovaginal candidiasis. LCPM formulation developed consisted of oleic acid as the oil phase (50% w/w), polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol (40% w/w) as the surfactant and a polymeric dispersion containing 2.5% Carbopol® 974P and 2.5% polycarbophil (10% w/w) as the aqueous phase. LCPM formulation developed was characterized using polarized light microscopy, rheological analysis, and in vitro mucoadhesive studies. Different strains of C. krusei, including one standard strain (American Type Culture Collection 6258) and three clinically isolated strains from the vaginal region (CKV1, 2, and 3), were used to determine the minimum inhibitory concentration, inhibition of biofilms, and time kill. The in vivo prophylaxis assay was performed using the standard strain (American Type Culture Collection 6258). The analyses of F by polarized light microscopy and rheology showed isotropy; however, the addition of 100% artificial vaginal mucus (F100) made it more viscous and anisotropic. Moreover, the mucoadhesive strength was modified, which makes F an excellent formulation for vaginal applications. SNE was active against all strains studied, with minimum inhibitory concentration values ranging from 125 to 62.5 µg/mL; after incorporating SNE into F (FE), these values decreased to 62.5 to 31.2 µg/mL, demonstrating that incorporation into the formulation potentiated the action of SNE. Additionally, the time kill assays showed that both forms of SNE were capable of controlling growth, thereby suggesting a possible fungistatic mechanism. Unloaded SNE was not active against C. krusei biofilms, but FE was active against a clinical strain (CKV2). In vivo analysis showed that FE was able to prevent the development of infection following 10 days of administration. We concluded that the formulation developed in this study was an important vehicle for the delivery of SNE based on the improved antifungal activity in all in vitro and in vivo analyses. Furthermore, the extract incorporated into the system may serve as an important prophylactic agent against vaginal infections caused by C. krusei. Keywords: precursor system of mucoadhesive liquid crystal, nanostructured system, ­prophylaxis, Candida krusei
format article
author dos Santos Ramos MA
Calixto G
de Toledo LG
Bonifácio BV
dos Santos LC
de Almeida MT
Chorilli M
Bauab TM
author_facet dos Santos Ramos MA
Calixto G
de Toledo LG
Bonifácio BV
dos Santos LC
de Almeida MT
Chorilli M
Bauab TM
author_sort dos Santos Ramos MA
title Liquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of Syngonanthus nitens (Bong.) Ruhland against infection by Candida krusei
title_short Liquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of Syngonanthus nitens (Bong.) Ruhland against infection by Candida krusei
title_full Liquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of Syngonanthus nitens (Bong.) Ruhland against infection by Candida krusei
title_fullStr Liquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of Syngonanthus nitens (Bong.) Ruhland against infection by Candida krusei
title_full_unstemmed Liquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of Syngonanthus nitens (Bong.) Ruhland against infection by Candida krusei
title_sort liquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of syngonanthus nitens (bong.) ruhland against infection by candida krusei
publisher Dove Medical Press
publishDate 2015
url https://doaj.org/article/8ceab0430a89469fb7e7ae7051cec0e8
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spelling oai:doaj.org-article:8ceab0430a89469fb7e7ae7051cec0e82021-12-02T03:58:33ZLiquid crystal precursor mucoadhesive system as a strategy to improve the prophylactic action of Syngonanthus nitens (Bong.) Ruhland against infection by Candida krusei1178-2013https://doaj.org/article/8ceab0430a89469fb7e7ae7051cec0e82015-12-01T00:00:00Zhttps://www.dovepress.com/liquid-crystal-precursor-mucoadhesive-system-as-a-strategy-to-improve--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Matheus Aparecido dos Santos Ramos,1 Giovana Calixto,2 Luciani Gaspar de Toledo,3 Bruna Vidal Bonifácio,1 Lourdes Campaner dos Santos,4 Margarete Teresa Gottardo de Almeida,3 Marlus Chorilli,2 Taís Maria Bauab1 1Department of Biological Sciences, School of Pharmaceutical Sciences, 2Department of Drugs and Medicine, School of Pharmaceutical Sciences, São Paulo State University, Araraquara, 3Department of Infectious Diseases, Faculty of Medicine of São José do Rio Preto, São José do Rio Preto, 4Department of Organic Chemistry, Chemistry Institute, São Paulo State University, Araraquara, São Paulo, Brazil Abstract: Vaginal infections caused by Candida krusei are a problem of extreme complexity due to the intrinsic resistance to azole drugs. The species Syngonanthus nitens (Bong.) Ruhland is a plant of the Eriocaulaceae family that has demonstrated promising antifungal activity. In phyto-formulation research, liquid crystal precursor mucoadhesive systems (LCPM) stand out as drug delivery systems for vaginal administration because they increase the activity and overcome the problems associated with plant-based medicines. Therefore, the objective of this study was to evaluate the potential of the methanolic extract of scapes of S. nitens (S. nitens extract [SNE]) and an SNE-loaded LCPM against C. krusei as prophylaxis for vulvovaginal candidiasis. LCPM formulation developed consisted of oleic acid as the oil phase (50% w/w), polyoxypropylene (5) polyoxyethylene (20) cetyl alcohol (40% w/w) as the surfactant and a polymeric dispersion containing 2.5% Carbopol® 974P and 2.5% polycarbophil (10% w/w) as the aqueous phase. LCPM formulation developed was characterized using polarized light microscopy, rheological analysis, and in vitro mucoadhesive studies. Different strains of C. krusei, including one standard strain (American Type Culture Collection 6258) and three clinically isolated strains from the vaginal region (CKV1, 2, and 3), were used to determine the minimum inhibitory concentration, inhibition of biofilms, and time kill. The in vivo prophylaxis assay was performed using the standard strain (American Type Culture Collection 6258). The analyses of F by polarized light microscopy and rheology showed isotropy; however, the addition of 100% artificial vaginal mucus (F100) made it more viscous and anisotropic. Moreover, the mucoadhesive strength was modified, which makes F an excellent formulation for vaginal applications. SNE was active against all strains studied, with minimum inhibitory concentration values ranging from 125 to 62.5 µg/mL; after incorporating SNE into F (FE), these values decreased to 62.5 to 31.2 µg/mL, demonstrating that incorporation into the formulation potentiated the action of SNE. Additionally, the time kill assays showed that both forms of SNE were capable of controlling growth, thereby suggesting a possible fungistatic mechanism. Unloaded SNE was not active against C. krusei biofilms, but FE was active against a clinical strain (CKV2). In vivo analysis showed that FE was able to prevent the development of infection following 10 days of administration. We concluded that the formulation developed in this study was an important vehicle for the delivery of SNE based on the improved antifungal activity in all in vitro and in vivo analyses. Furthermore, the extract incorporated into the system may serve as an important prophylactic agent against vaginal infections caused by C. krusei. Keywords: precursor system of mucoadhesive liquid crystal, nanostructured system, ­prophylaxis, Candida kruseidos Santos Ramos MACalixto Gde Toledo LGBonifácio BVdos Santos LCde Almeida MTChorilli MBauab TMDove Medical PressarticleCandida kruseiPrecursor system of mucoadhesive liquid crystalNanostructured systemSyngonanthus nitensProphylaxis.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 7455-7466 (2015)