Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles

Autores
Glisoni, Romina Julieta; Sosnik, Alejandro Dario
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Nitazoxanide (NTZ) is a highly hydrophobic nitrothiazolyl-salicylamide that displays antimicrobial activity against a variety of parasites, anaerobic bacteria and viruses. More recently, its effectiveness in the pharmacotherapy of chronic hepatitis, the leading cause of liver cirrhosis and hepatocellular carcinoma (HCC), has been reported. On the other hand, the extremely low aqueous solubility of the drug challenges its administration by different routes. The present work explored for the first time the encapsulation of NTZ within pristine, lactosylated and mixed poly(ethylene oxide)-poly(propylene oxide) (PEO-PPO) polymeric micelles (PMs) of different architectures, molecular weights and hydrophilic-lipophilic balance (HLB) as a strategy to improve its aqueous solubility and to potentially target it to the liver parenchyma. The solubility was increased up to 609 times. The drug encapsulation modified the selfaggregation pattern of the different amphiphiles, resulting in a sharp growth of the micellar size. The encapsulation capacity of the lactosylated derivatives was smaller than that of the pristine counterparts, though the development of mixed PMs that combine a highly hydrophilic lactosylated amphiphile (e.g., poloxamer F127 or poloxamine T1107) that forms the micellar template and a more hydrophobic unmodified poloxamine (T904) that increases the hydrophobicity of the core resulted in the synergistic encapsulation of the drug and a substantial increase of the physical stability over time. Overall findings confirmed the extremely great versatility of the poloxamer/poloxamine mixed self-assembly systems as Trojan nanocarriers for the encapsulation of NTZ towards its targeting to the liver.
Fil: Glisoni, Romina Julieta. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Nanobiotecnología. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Nanobiotecnología; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
Fil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Nanobiotecnología. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Nanobiotecnología; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
Materia
Nitazoxanide
Viral Hepatitis
Polymeric Micelles
Lactosylated Nanocarriers
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/30654
Acceder
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network_name_str CONICET Digital (CONICET)
spelling Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric MicellesGlisoni, Romina JulietaSosnik, Alejandro DarioNitazoxanideViral HepatitisPolymeric MicellesLactosylated Nanocarriershttps://purl.org/becyt/ford/2.10https://purl.org/becyt/ford/2Nitazoxanide (NTZ) is a highly hydrophobic nitrothiazolyl-salicylamide that displays antimicrobial activity against a variety of parasites, anaerobic bacteria and viruses. More recently, its effectiveness in the pharmacotherapy of chronic hepatitis, the leading cause of liver cirrhosis and hepatocellular carcinoma (HCC), has been reported. On the other hand, the extremely low aqueous solubility of the drug challenges its administration by different routes. The present work explored for the first time the encapsulation of NTZ within pristine, lactosylated and mixed poly(ethylene oxide)-poly(propylene oxide) (PEO-PPO) polymeric micelles (PMs) of different architectures, molecular weights and hydrophilic-lipophilic balance (HLB) as a strategy to improve its aqueous solubility and to potentially target it to the liver parenchyma. The solubility was increased up to 609 times. The drug encapsulation modified the selfaggregation pattern of the different amphiphiles, resulting in a sharp growth of the micellar size. The encapsulation capacity of the lactosylated derivatives was smaller than that of the pristine counterparts, though the development of mixed PMs that combine a highly hydrophilic lactosylated amphiphile (e.g., poloxamer F127 or poloxamine T1107) that forms the micellar template and a more hydrophobic unmodified poloxamine (T904) that increases the hydrophobicity of the core resulted in the synergistic encapsulation of the drug and a substantial increase of the physical stability over time. Overall findings confirmed the extremely great versatility of the poloxamer/poloxamine mixed self-assembly systems as Trojan nanocarriers for the encapsulation of NTZ towards its targeting to the liver.Fil: Glisoni, Romina Julieta. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Nanobiotecnología. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Nanobiotecnología; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; ArgentinaFil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Nanobiotecnología. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Nanobiotecnología; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; ArgentinaAmerican Scientific Publishers2014-06info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/30654Glisoni, Romina Julieta; Sosnik, Alejandro Dario; Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles; American Scientific Publishers; Journal of Nanoscience and Nanotechnology; 14; 6; 6-2014; 4670-46821533-4880CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1166/jnn.2014.8647info:eu-repo/semantics/altIdentifier/url/http://www.ingentaconnect.com/content/asp/jnn/2014/00000014/00000006/art00103info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-29T10:06:23Zoai:ri.conicet.gov.ar:11336/30654instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-29 10:06:23.577CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles
title Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles
spellingShingle Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles
Glisoni, Romina Julieta
Nitazoxanide
Viral Hepatitis
Polymeric Micelles
Lactosylated Nanocarriers
title_short Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles
title_full Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles
title_fullStr Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles
title_full_unstemmed Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles
title_sort Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles
dc.creator.none.fl_str_mv Glisoni, Romina Julieta
Sosnik, Alejandro Dario
author Glisoni, Romina Julieta
author_facet Glisoni, Romina Julieta
Sosnik, Alejandro Dario
author_role author
author2 Sosnik, Alejandro Dario
author2_role author
dc.subject.none.fl_str_mv Nitazoxanide
Viral Hepatitis
Polymeric Micelles
Lactosylated Nanocarriers
topic Nitazoxanide
Viral Hepatitis
Polymeric Micelles
Lactosylated Nanocarriers
purl_subject.fl_str_mv https://purl.org/becyt/ford/2.10
https://purl.org/becyt/ford/2
dc.description.none.fl_txt_mv Nitazoxanide (NTZ) is a highly hydrophobic nitrothiazolyl-salicylamide that displays antimicrobial activity against a variety of parasites, anaerobic bacteria and viruses. More recently, its effectiveness in the pharmacotherapy of chronic hepatitis, the leading cause of liver cirrhosis and hepatocellular carcinoma (HCC), has been reported. On the other hand, the extremely low aqueous solubility of the drug challenges its administration by different routes. The present work explored for the first time the encapsulation of NTZ within pristine, lactosylated and mixed poly(ethylene oxide)-poly(propylene oxide) (PEO-PPO) polymeric micelles (PMs) of different architectures, molecular weights and hydrophilic-lipophilic balance (HLB) as a strategy to improve its aqueous solubility and to potentially target it to the liver parenchyma. The solubility was increased up to 609 times. The drug encapsulation modified the selfaggregation pattern of the different amphiphiles, resulting in a sharp growth of the micellar size. The encapsulation capacity of the lactosylated derivatives was smaller than that of the pristine counterparts, though the development of mixed PMs that combine a highly hydrophilic lactosylated amphiphile (e.g., poloxamer F127 or poloxamine T1107) that forms the micellar template and a more hydrophobic unmodified poloxamine (T904) that increases the hydrophobicity of the core resulted in the synergistic encapsulation of the drug and a substantial increase of the physical stability over time. Overall findings confirmed the extremely great versatility of the poloxamer/poloxamine mixed self-assembly systems as Trojan nanocarriers for the encapsulation of NTZ towards its targeting to the liver.
Fil: Glisoni, Romina Julieta. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Nanobiotecnología. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Nanobiotecnología; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
Fil: Sosnik, Alejandro Dario. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Nanobiotecnología. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Nanobiotecnología; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Tecnología Farmacéutica; Argentina
description Nitazoxanide (NTZ) is a highly hydrophobic nitrothiazolyl-salicylamide that displays antimicrobial activity against a variety of parasites, anaerobic bacteria and viruses. More recently, its effectiveness in the pharmacotherapy of chronic hepatitis, the leading cause of liver cirrhosis and hepatocellular carcinoma (HCC), has been reported. On the other hand, the extremely low aqueous solubility of the drug challenges its administration by different routes. The present work explored for the first time the encapsulation of NTZ within pristine, lactosylated and mixed poly(ethylene oxide)-poly(propylene oxide) (PEO-PPO) polymeric micelles (PMs) of different architectures, molecular weights and hydrophilic-lipophilic balance (HLB) as a strategy to improve its aqueous solubility and to potentially target it to the liver parenchyma. The solubility was increased up to 609 times. The drug encapsulation modified the selfaggregation pattern of the different amphiphiles, resulting in a sharp growth of the micellar size. The encapsulation capacity of the lactosylated derivatives was smaller than that of the pristine counterparts, though the development of mixed PMs that combine a highly hydrophilic lactosylated amphiphile (e.g., poloxamer F127 or poloxamine T1107) that forms the micellar template and a more hydrophobic unmodified poloxamine (T904) that increases the hydrophobicity of the core resulted in the synergistic encapsulation of the drug and a substantial increase of the physical stability over time. Overall findings confirmed the extremely great versatility of the poloxamer/poloxamine mixed self-assembly systems as Trojan nanocarriers for the encapsulation of NTZ towards its targeting to the liver.
publishDate 2014
dc.date.none.fl_str_mv 2014-06
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/30654
Glisoni, Romina Julieta; Sosnik, Alejandro Dario; Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles; American Scientific Publishers; Journal of Nanoscience and Nanotechnology; 14; 6; 6-2014; 4670-4682
1533-4880
CONICET Digital
CONICET
url http://hdl.handle.net/11336/30654
identifier_str_mv Glisoni, Romina Julieta; Sosnik, Alejandro Dario; Encapsulation of the Antimicrobial and Immunomodulator Agent Nitazoxanide Within Polymeric Micelles; American Scientific Publishers; Journal of Nanoscience and Nanotechnology; 14; 6; 6-2014; 4670-4682
1533-4880
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1166/jnn.2014.8647
info:eu-repo/semantics/altIdentifier/url/http://www.ingentaconnect.com/content/asp/jnn/2014/00000014/00000006/art00103
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv American Scientific Publishers
publisher.none.fl_str_mv American Scientific Publishers
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 13.070432

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