Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery

Luiza A Frank,1 Giuseppina Sandri,2 Francesca D´Autilia,2 Renata V Contri,1 Maria Cristina Bonferoni,2 Carla Caramella,2 Alejandro G Frank,3 Adriana R Pohlmann,1 Silvia S Guterres11Pharmaceutical Science Graduate Program, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil;...

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Autores principales:	Frank LA, Sandri G, D'Autilia F, Contri RV, Bonferoni MC, Caramella C, Frank AG, Pohlmann AR, Guterres SS
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/ba70f3ba9f0e4eada7c112a56fcf1f08
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spelling	oai:doaj.org-article:ba70f3ba9f0e4eada7c112a56fcf1f082021-12-02T02:10:31ZChitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery1178-2013https://doaj.org/article/ba70f3ba9f0e4eada7c112a56fcf1f082014-06-01T00:00:00Zhttp://www.dovepress.com/chitosan-gel-containing-polymeric-nanocapsules-a-new-formulation-for-v-a17395https://doaj.org/toc/1178-2013 Luiza A Frank,1 Giuseppina Sandri,2 Francesca D´Autilia,2 Renata V Contri,1 Maria Cristina Bonferoni,2 Carla Caramella,2 Alejandro G Frank,3 Adriana R Pohlmann,1 Silvia S Guterres11Pharmaceutical Science Graduate Program, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil; 2Department of Drug Sciences, University of Pavia, Pavia, PV, Italy; 3Department of Industrial Engineering, Federal University of Rio Grande do Sul, Porto Alegre, RS, BrazilAbstract: The vaginal route of administration is an alternative for several treatments for either local or systemic pharmacological effects. However, the permanence of a drug in this route represents a challenge for formulation development that can be overcome by using nanoencapsulation and chitosan gel. Thus, this work aimed to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylic-based nanocapsules (Eudragit® RS 100 and Eudragit® S 100, respectively) with Nile red as a model of lipophilic substance in the vaginal route of administration, as measured by increases in the residence time and the penetration of these formulations. Several formulations were prepared with increasing chitosan concentrations, and were analyzed in terms of pH and rheological behavior so that the most suitable formulation could be selected. The enhancement of the adhesion (tensile stress test and washability profile) and penetration (confocal laser scanning microscopy and extraction followed by quantification) properties of the formulations, when applied to porcine vaginal mucosa, were evaluated. The nanocapsule suspensions produced presented adequate properties: size of approximately 200 nm (polydispersity index of ≤0.2); zeta potential around +10 mV for the cationic formulation and -10 mV for the anionic formulation; and pH values of 6.1±0.1 (Eudragit RS 100), 5.3±0.2 (Eudragit S 100), 6.2±0.1 (Nile red loaded Eudragit RS 100), and 5.1±0.1 (Nile red loaded Eudragit S 100). The chitosan formulation presented suitable viscosity for vaginal application and acidic pH (approximately 4.5). The tensile stress test showed that both formulations containing polymeric nanocapsules presented higher mucoadhesion when compared with the formulation without nanocapsules. In the washability experiment, no significant differences were found between formulations. Confocal microscopy and fluorescence quantification after extraction from the mucosa showed higher penetration of Nile red when it was nanoencapsulated, particularly in cationic nanocapsules. The formulations developed based on chitosan gel vehicle at 2.5% weight/weight containing polymeric nanocapsules, especially the cationic nanocapsules, demonstrated applicability for the vaginal delivery of hydrophobic substances.Keywords: Eudragit® RS 100, Eudragit® S 100, vaginal route, nanotechnologyFrank LASandri GD'Autilia FContri RVBonferoni MCCaramella CFrank AGPohlmann ARGuterres SSDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 3151-3161 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Frank LA Sandri G D'Autilia F Contri RV Bonferoni MC Caramella C Frank AG Pohlmann AR Guterres SS Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery
description	Luiza A Frank,1 Giuseppina Sandri,2 Francesca D´Autilia,2 Renata V Contri,1 Maria Cristina Bonferoni,2 Carla Caramella,2 Alejandro G Frank,3 Adriana R Pohlmann,1 Silvia S Guterres11Pharmaceutical Science Graduate Program, Federal University of Rio Grande do Sul, Porto Alegre, RS, Brazil; 2Department of Drug Sciences, University of Pavia, Pavia, PV, Italy; 3Department of Industrial Engineering, Federal University of Rio Grande do Sul, Porto Alegre, RS, BrazilAbstract: The vaginal route of administration is an alternative for several treatments for either local or systemic pharmacological effects. However, the permanence of a drug in this route represents a challenge for formulation development that can be overcome by using nanoencapsulation and chitosan gel. Thus, this work aimed to evaluate the performance of chitosan hydrogels containing cationic and anionic acrylic-based nanocapsules (Eudragit® RS 100 and Eudragit® S 100, respectively) with Nile red as a model of lipophilic substance in the vaginal route of administration, as measured by increases in the residence time and the penetration of these formulations. Several formulations were prepared with increasing chitosan concentrations, and were analyzed in terms of pH and rheological behavior so that the most suitable formulation could be selected. The enhancement of the adhesion (tensile stress test and washability profile) and penetration (confocal laser scanning microscopy and extraction followed by quantification) properties of the formulations, when applied to porcine vaginal mucosa, were evaluated. The nanocapsule suspensions produced presented adequate properties: size of approximately 200 nm (polydispersity index of ≤0.2); zeta potential around +10 mV for the cationic formulation and -10 mV for the anionic formulation; and pH values of 6.1±0.1 (Eudragit RS 100), 5.3±0.2 (Eudragit S 100), 6.2±0.1 (Nile red loaded Eudragit RS 100), and 5.1±0.1 (Nile red loaded Eudragit S 100). The chitosan formulation presented suitable viscosity for vaginal application and acidic pH (approximately 4.5). The tensile stress test showed that both formulations containing polymeric nanocapsules presented higher mucoadhesion when compared with the formulation without nanocapsules. In the washability experiment, no significant differences were found between formulations. Confocal microscopy and fluorescence quantification after extraction from the mucosa showed higher penetration of Nile red when it was nanoencapsulated, particularly in cationic nanocapsules. The formulations developed based on chitosan gel vehicle at 2.5% weight/weight containing polymeric nanocapsules, especially the cationic nanocapsules, demonstrated applicability for the vaginal delivery of hydrophobic substances.Keywords: Eudragit® RS 100, Eudragit® S 100, vaginal route, nanotechnology
format	article
author	Frank LA Sandri G D'Autilia F Contri RV Bonferoni MC Caramella C Frank AG Pohlmann AR Guterres SS
author_facet	Frank LA Sandri G D'Autilia F Contri RV Bonferoni MC Caramella C Frank AG Pohlmann AR Guterres SS
author_sort	Frank LA
title	Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery
title_short	Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery
title_full	Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery
title_fullStr	Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery
title_full_unstemmed	Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery
title_sort	chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/ba70f3ba9f0e4eada7c112a56fcf1f08
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Chitosan gel containing polymeric nanocapsules: a new formulation for vaginal drug delivery

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