Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia

Detalhes bibliográficos
Autor(a) principal: de Almeida, Ana Cláudia Pedreira
Data de Publicação: 2018
Outros Autores: Pinto, Luciana Matos Alves, Alves, Giuliana Piovesan, Ribeiro, Lígia Nunes de Morais, Santana, Maria Helena Andrade, Cereda, Cíntia Maria Saia, Fraceto, Leonardo Fernandes [UNESP], de Paula, Eneida
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNESP
Texto Completo: http://dx.doi.org/10.1080/08982104.2018.1483947
http://hdl.handle.net/11449/180175
Resumo: This study describes the encapsulation of the local anaesthetic lidocaine (LDC) in large unilamellar liposomes (LUV) prepared in a scalable procedure, with hydrogenated soybean phosphatidylcholine, cholesterol and mannitol. Structural properties of the liposomes were assessed by dynamic light scattering, nanoparticle tracking analysis and transmission electron microscopy. A modified, two-compartment Franz-cell system was used to evaluate the release kinetics of LDC from the liposomes. The in vivo anaesthetic effect of liposomal LDC 2% (LUVLDC) was compared to LDC 2% solution without (LDCPLAIN) or with the vasoconstrictor epinephrine (1:100 000) (LDCVASO), in rat infraorbital nerve blockade model. The structural characterization revealed liposomes with spherical shape, average size distribution of 250 nm and low polydispersity even after LDC incorporation. Zeta potential laid around –30 mV and the number of suspended liposomal particles was in the range of 1012 vesicles/mL. Also the addition of cryoprotectant (mannitol) did not provoke structural changes in liposomes properties. In vitro release profile of LDC from LUV fits well with a biexponential model, in which the LDC encapsulated (EE% = 24%) was responsible for an increase of 67% in the release time in relation to LDCPLAIN (p < 0.05). Also, the liposomal formulation prolonged the sensorial nervous blockade duration (∼70 min), in comparison with LDCPLAIN (45 min), but less than LDCVASO (130 min). In this context, this study showed that the liposomal formulations prepared by scalable procedure were suitable to promote longer and safer buccal anaesthesia, avoiding side effects of the use of vasoconstrictors.
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spelling Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesiadentistrydrug–deliveryhydrogenated soybean phosphatidylcholineinfraorbital nerve blockadelidocaineLiposomesThis study describes the encapsulation of the local anaesthetic lidocaine (LDC) in large unilamellar liposomes (LUV) prepared in a scalable procedure, with hydrogenated soybean phosphatidylcholine, cholesterol and mannitol. Structural properties of the liposomes were assessed by dynamic light scattering, nanoparticle tracking analysis and transmission electron microscopy. A modified, two-compartment Franz-cell system was used to evaluate the release kinetics of LDC from the liposomes. The in vivo anaesthetic effect of liposomal LDC 2% (LUVLDC) was compared to LDC 2% solution without (LDCPLAIN) or with the vasoconstrictor epinephrine (1:100 000) (LDCVASO), in rat infraorbital nerve blockade model. The structural characterization revealed liposomes with spherical shape, average size distribution of 250 nm and low polydispersity even after LDC incorporation. Zeta potential laid around –30 mV and the number of suspended liposomal particles was in the range of 1012 vesicles/mL. Also the addition of cryoprotectant (mannitol) did not provoke structural changes in liposomes properties. In vitro release profile of LDC from LUV fits well with a biexponential model, in which the LDC encapsulated (EE% = 24%) was responsible for an increase of 67% in the release time in relation to LDCPLAIN (p < 0.05). Also, the liposomal formulation prolonged the sensorial nervous blockade duration (∼70 min), in comparison with LDCPLAIN (45 min), but less than LDCVASO (130 min). In this context, this study showed that the liposomal formulations prepared by scalable procedure were suitable to promote longer and safer buccal anaesthesia, avoiding side effects of the use of vasoconstrictors.Department of Biochemistry and Tissue Biology Institute of Biology University of Campinas-UNICAMPFaculty of Odontology Federal University of Alfenas–UNIFALDepartment of Chemistry Federal University of LavrasCristália Produtos Químicos e Farmacêuticos LtdaDepartment of Biotechnological Processes Faculty of Chemistry Engineering UNICAMPInstitute of Science and Technology São Paulo State University (UNESP)Institute of Science and Technology São Paulo State University (UNESP)Universidade Estadual de Campinas (UNICAMP)Federal University of Alfenas–UNIFALFederal University of LavrasCristália Produtos Químicos e Farmacêuticos LtdaUniversidade Estadual Paulista (Unesp)de Almeida, Ana Cláudia PedreiraPinto, Luciana Matos AlvesAlves, Giuliana PiovesanRibeiro, Lígia Nunes de MoraisSantana, Maria Helena AndradeCereda, Cíntia Maria SaiaFraceto, Leonardo Fernandes [UNESP]de Paula, Eneida2018-12-11T17:38:28Z2018-12-11T17:38:28Z2018-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1080/08982104.2018.1483947Journal of Liposome Research.1532-23940898-2104http://hdl.handle.net/11449/18017510.1080/08982104.2018.14839472-s2.0-85053229121Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengJournal of Liposome Research0,6500,650info:eu-repo/semantics/openAccess2021-10-23T10:18:41Zoai:repositorio.unesp.br:11449/180175Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462021-10-23T10:18:41Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false
dc.title.none.fl_str_mv Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia
title Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia
spellingShingle Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia
de Almeida, Ana Cláudia Pedreira
dentistry
drug–delivery
hydrogenated soybean phosphatidylcholine
infraorbital nerve blockade
lidocaine
Liposomes
title_short Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia
title_full Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia
title_fullStr Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia
title_full_unstemmed Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia
title_sort Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia
author de Almeida, Ana Cláudia Pedreira
author_facet de Almeida, Ana Cláudia Pedreira
Pinto, Luciana Matos Alves
Alves, Giuliana Piovesan
Ribeiro, Lígia Nunes de Morais
Santana, Maria Helena Andrade
Cereda, Cíntia Maria Saia
Fraceto, Leonardo Fernandes [UNESP]
de Paula, Eneida
author_role author
author2 Pinto, Luciana Matos Alves
Alves, Giuliana Piovesan
Ribeiro, Lígia Nunes de Morais
Santana, Maria Helena Andrade
Cereda, Cíntia Maria Saia
Fraceto, Leonardo Fernandes [UNESP]
de Paula, Eneida
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade Estadual de Campinas (UNICAMP)
Federal University of Alfenas–UNIFAL
Federal University of Lavras
Cristália Produtos Químicos e Farmacêuticos Ltda
Universidade Estadual Paulista (Unesp)
dc.contributor.author.fl_str_mv de Almeida, Ana Cláudia Pedreira
Pinto, Luciana Matos Alves
Alves, Giuliana Piovesan
Ribeiro, Lígia Nunes de Morais
Santana, Maria Helena Andrade
Cereda, Cíntia Maria Saia
Fraceto, Leonardo Fernandes [UNESP]
de Paula, Eneida
dc.subject.por.fl_str_mv dentistry
drug–delivery
hydrogenated soybean phosphatidylcholine
infraorbital nerve blockade
lidocaine
Liposomes
topic dentistry
drug–delivery
hydrogenated soybean phosphatidylcholine
infraorbital nerve blockade
lidocaine
Liposomes
description This study describes the encapsulation of the local anaesthetic lidocaine (LDC) in large unilamellar liposomes (LUV) prepared in a scalable procedure, with hydrogenated soybean phosphatidylcholine, cholesterol and mannitol. Structural properties of the liposomes were assessed by dynamic light scattering, nanoparticle tracking analysis and transmission electron microscopy. A modified, two-compartment Franz-cell system was used to evaluate the release kinetics of LDC from the liposomes. The in vivo anaesthetic effect of liposomal LDC 2% (LUVLDC) was compared to LDC 2% solution without (LDCPLAIN) or with the vasoconstrictor epinephrine (1:100 000) (LDCVASO), in rat infraorbital nerve blockade model. The structural characterization revealed liposomes with spherical shape, average size distribution of 250 nm and low polydispersity even after LDC incorporation. Zeta potential laid around –30 mV and the number of suspended liposomal particles was in the range of 1012 vesicles/mL. Also the addition of cryoprotectant (mannitol) did not provoke structural changes in liposomes properties. In vitro release profile of LDC from LUV fits well with a biexponential model, in which the LDC encapsulated (EE% = 24%) was responsible for an increase of 67% in the release time in relation to LDCPLAIN (p < 0.05). Also, the liposomal formulation prolonged the sensorial nervous blockade duration (∼70 min), in comparison with LDCPLAIN (45 min), but less than LDCVASO (130 min). In this context, this study showed that the liposomal formulations prepared by scalable procedure were suitable to promote longer and safer buccal anaesthesia, avoiding side effects of the use of vasoconstrictors.
publishDate 2018
dc.date.none.fl_str_mv 2018-12-11T17:38:28Z
2018-12-11T17:38:28Z
2018-01-01
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://dx.doi.org/10.1080/08982104.2018.1483947
Journal of Liposome Research.
1532-2394
0898-2104
http://hdl.handle.net/11449/180175
10.1080/08982104.2018.1483947
2-s2.0-85053229121
url http://dx.doi.org/10.1080/08982104.2018.1483947
http://hdl.handle.net/11449/180175
identifier_str_mv Journal of Liposome Research.
1532-2394
0898-2104
10.1080/08982104.2018.1483947
2-s2.0-85053229121
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Journal of Liposome Research
0,650
0,650
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.source.none.fl_str_mv Scopus
reponame:Repositório Institucional da UNESP
instname:Universidade Estadual Paulista (UNESP)
instacron:UNESP
instname_str Universidade Estadual Paulista (UNESP)
instacron_str UNESP
institution UNESP
reponame_str Repositório Institucional da UNESP
collection Repositório Institucional da UNESP
repository.name.fl_str_mv Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)
repository.mail.fl_str_mv
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