Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms

Giovana Maria Fioramonti Calixto,1 Cristiane Duque,2 Kelly Limi Aida,2 Vanessa Rodrigues dos Santos,2 Loiane Massunari,2 Marlus Chorilli1 1School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, Brazil; 2School of Dentistry, São Paulo State Universit...

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Autores principales:	Calixto GMF, Duque C, Aida KL, Santos VR, Massunari L, Chorilli M
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	drug delivery system liquid crystalline system peptidic drugs dental caries biofilm cytotoxicity Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/49b041d60f2d49c6a2b075da710f0ee9
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spelling	oai:doaj.org-article:49b041d60f2d49c6a2b075da710f0ee92021-12-02T00:12:15ZDevelopment and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms1178-2013https://doaj.org/article/49b041d60f2d49c6a2b075da710f0ee92017-12-01T00:00:00Zhttps://www.dovepress.com/development-and-characterization-of-p1025-loaded-bioadhesive-liquid-cr-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Giovana Maria Fioramonti Calixto,1 Cristiane Duque,2 Kelly Limi Aida,2 Vanessa Rodrigues dos Santos,2 Loiane Massunari,2 Marlus Chorilli1 1School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, Brazil; 2School of Dentistry, São Paulo State University (UNESP), Araçatuba, Brazil Abstract: Formation of a dental biofilm by Streptococcus mutans can cause dental caries, and remains a costly health problem worldwide. Recently, there has been a growing interest in the use of peptidic drugs, such as peptide p1025, analogous to the fragments 1025–1044 of S. mutans cellular adhesin, responsible for the adhesion and formation of dental biofilm. However, peptides have physicochemical characteristics that may affect their biological action, limiting their clinical performance. Therefore, drug-delivery systems, such as a bioadhesive liquid-crystalline system (LCS), may be attractive strategies for peptide delivery. Potentiation of the action of LCS can be achieved with the use of bioadhesive polymers to prolong their residence on the teeth. In line with this, three formulations – polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol, oleic acid, and Carbopol C974P in different combinations (F1C, F2C, and F3C) were developed to observe the influence of water in the LCS, with the aim of achieving in situ gelling in the oral environment. These formulations were assessed by polarized light microscopy, small-angle X-ray scattering, rheological analysis, and in vitro bioadhesion analysis. Then, p1025 and a control (chlorhexidine) were incorporated into the aqueous phase of the formulation (F + p1025 and F + chlorhexidine), to determine their antibiofilm effect and toxicity on epithelial cells. Polarized light microscopy and small-angle X-ray scattering showed that F1C and F2C were LCS, whereas F3C was a microemulsion. F1C and F2C showed pseudoplastic behavior and F3C Newtonian behavior. F1C showed the highest elastic and bioadhesive characteristics compared to other formulations. Antibiofilm effects were observed for F + p1025 when applied in the surface-bound salivary phase. The p1025-loaded nanostructured LCS presented limited cytotoxicity and effectively reduced S. mutans biofilm formation, and could be a promising p1025-delivery strategy to prevent the formation of S. mutans dental biofilm. Keywords: liquid crystal, formulation, polymer, peptide, bacterium, dental caries Calixto GMFDuque CAida KLSantos VRMassunari LChorilli MDove Medical Pressarticledrug delivery systemliquid crystalline systempeptidic drugsdental cariesbiofilmcytotoxicityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 31-41 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	drug delivery system liquid crystalline system peptidic drugs dental caries biofilm cytotoxicity Medicine (General) R5-920
spellingShingle	drug delivery system liquid crystalline system peptidic drugs dental caries biofilm cytotoxicity Medicine (General) R5-920 Calixto GMF Duque C Aida KL Santos VR Massunari L Chorilli M Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms
description	Giovana Maria Fioramonti Calixto,1 Cristiane Duque,2 Kelly Limi Aida,2 Vanessa Rodrigues dos Santos,2 Loiane Massunari,2 Marlus Chorilli1 1School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, Brazil; 2School of Dentistry, São Paulo State University (UNESP), Araçatuba, Brazil Abstract: Formation of a dental biofilm by Streptococcus mutans can cause dental caries, and remains a costly health problem worldwide. Recently, there has been a growing interest in the use of peptidic drugs, such as peptide p1025, analogous to the fragments 1025–1044 of S. mutans cellular adhesin, responsible for the adhesion and formation of dental biofilm. However, peptides have physicochemical characteristics that may affect their biological action, limiting their clinical performance. Therefore, drug-delivery systems, such as a bioadhesive liquid-crystalline system (LCS), may be attractive strategies for peptide delivery. Potentiation of the action of LCS can be achieved with the use of bioadhesive polymers to prolong their residence on the teeth. In line with this, three formulations – polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol, oleic acid, and Carbopol C974P in different combinations (F1C, F2C, and F3C) were developed to observe the influence of water in the LCS, with the aim of achieving in situ gelling in the oral environment. These formulations were assessed by polarized light microscopy, small-angle X-ray scattering, rheological analysis, and in vitro bioadhesion analysis. Then, p1025 and a control (chlorhexidine) were incorporated into the aqueous phase of the formulation (F + p1025 and F + chlorhexidine), to determine their antibiofilm effect and toxicity on epithelial cells. Polarized light microscopy and small-angle X-ray scattering showed that F1C and F2C were LCS, whereas F3C was a microemulsion. F1C and F2C showed pseudoplastic behavior and F3C Newtonian behavior. F1C showed the highest elastic and bioadhesive characteristics compared to other formulations. Antibiofilm effects were observed for F + p1025 when applied in the surface-bound salivary phase. The p1025-loaded nanostructured LCS presented limited cytotoxicity and effectively reduced S. mutans biofilm formation, and could be a promising p1025-delivery strategy to prevent the formation of S. mutans dental biofilm. Keywords: liquid crystal, formulation, polymer, peptide, bacterium, dental caries
format	article
author	Calixto GMF Duque C Aida KL Santos VR Massunari L Chorilli M
author_facet	Calixto GMF Duque C Aida KL Santos VR Massunari L Chorilli M
author_sort	Calixto GMF
title	Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms
title_short	Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms
title_full	Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms
title_fullStr	Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms
title_full_unstemmed	Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms
title_sort	development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of streptococcus mutans biofilms
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/49b041d60f2d49c6a2b075da710f0ee9
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Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of Streptococcus mutans biofilms

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