Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A

Detalhes bibliográficos
Autor(a) principal: Assunção, Daniele Priscila da Silva Fardin de
Data de Publicação: 2013
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Biblioteca Digital de Teses e Dissertações da UEPG
Texto Completo: http://tede2.uepg.br/jspui/handle/prefix/113
Resumo: Cutaneous aging is a complex biological phenomenon that depends on a number of intrinsic, responsible for chronological aging and the extrinsic factors, which is responsible for cutaneous photo aging. Another important factor that must be taken into account is the appearance of wrinkles caused by repeated movements of the facial muscles. Currently there is a huge demand for anti-aging products and one of the strategies that is most commonly employed for this end, is the application of botulinum toxin Type A which is regarded as the principal treatment for the mitigation of wrinkles. Another active substance which functions in the same way as botulinum toxin A, is acetyl hexapeptide-3, which is marketed under the name of Argireline. This anti-aging agent acts in a similar way to botulinum toxin by smoothing out the expressive lines and wrinkles caused by repeated movements. Both the active agents are responsible for the release of acetylcholine at the neuromuscular junction. One of the main differences between these active agents is in their form of application since, whereas botulinum toxin A is administered by injection, acetyl hexapeptide-3 is used in the form of a cream for topical application. Given the fact that the two active agents are hydrophilic neuropeptides of high molecular mass, their ability to penetrate the skin is improbable. Thus, the purpose of this study was to develop, characterize and evaluate systems comprising nanocarriers that are able to allow or improve the permeation of these active agents through the skin. Acetyl hexapeptide-3 was encapsulated in liposomes and botulinum toxin was encapsulated through two systems, liposomes and polymeric nanoparticles. The evaluation of the acetyl-hexapeptide-3 showed an encapsulation efficiency of 95%. The vesicles showed a zeta potential of -31 mV. The results demonstrated that the active agent had a good cutaneous permeation and its encapsulation did not affect the permeation through the skin. The botulinum toxin Type A were successfully encapsulated into nanoparticles by multiple emulsion method and solvent evaporation. The nanoparticles had an average size of approximately 570 nm and a zeta potential of -7,40 mV, which is characteristic of the polyester used. The multilamellar liposomes were obtained through a method that involved hydrating the lipid film and showed an average size of approximately 1370 nm and a zeta potential of -37 mV. It was possible to demonstrate by means of infrared fourier transform spectroscopy, the presence of botulinum toxin Type A in the polymeric nanoparticles and the liposomes. The in vitro assays that were carried out suggested that the liposomes that contained the botulinum toxin Type A had an effect on the neurotransmitters in the assays that were conducted, whereas it was not possible to identify the same effect in the nanoparticles that contained the botulinum toxin.These results showed that the encapsulation of botulinum toxin A can be an alternative for the topical application of botulinum toxin Type A in a non-invasive way and with a good deal of comfort to the patient. With regard to acetyl hexapeptide-3, it can be claimed that this active agent when released shows the same degree of penetration through the skin as the encapsulated active agent. This suggests that the penetration of acetyl hexapeptide-3 does not undergo any alteration when encapsulated in liposomes. Thus, the active agent can be applied topically in this way.
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spelling Paula, Josiane de Fatima Padilha deCPF:49618768953http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4702484Y6Farago, Paulo VitorCPF:02688357999Canteri, Maria HeleneCPF:88289796900http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4705338T4CPF:03553925930http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4499168E2Assunção, Daniele Priscila da Silva Fardin de2017-07-21T14:13:12Z2013-10-162017-07-21T14:13:12Z2013-02-25ASSUNÇÃO, Daniele Priscila da Silva Fardin de. Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A. 2013. 64 f. Dissertação (Mestrado em Farmacos, Medicamentos e Biociências Aplicadas à Farmácia) - UNIVERSIDADE ESTADUAL DE PONTA GROSSA, Ponta Grossa, 2013.http://tede2.uepg.br/jspui/handle/prefix/113Cutaneous aging is a complex biological phenomenon that depends on a number of intrinsic, responsible for chronological aging and the extrinsic factors, which is responsible for cutaneous photo aging. Another important factor that must be taken into account is the appearance of wrinkles caused by repeated movements of the facial muscles. Currently there is a huge demand for anti-aging products and one of the strategies that is most commonly employed for this end, is the application of botulinum toxin Type A which is regarded as the principal treatment for the mitigation of wrinkles. Another active substance which functions in the same way as botulinum toxin A, is acetyl hexapeptide-3, which is marketed under the name of Argireline. This anti-aging agent acts in a similar way to botulinum toxin by smoothing out the expressive lines and wrinkles caused by repeated movements. Both the active agents are responsible for the release of acetylcholine at the neuromuscular junction. One of the main differences between these active agents is in their form of application since, whereas botulinum toxin A is administered by injection, acetyl hexapeptide-3 is used in the form of a cream for topical application. Given the fact that the two active agents are hydrophilic neuropeptides of high molecular mass, their ability to penetrate the skin is improbable. Thus, the purpose of this study was to develop, characterize and evaluate systems comprising nanocarriers that are able to allow or improve the permeation of these active agents through the skin. Acetyl hexapeptide-3 was encapsulated in liposomes and botulinum toxin was encapsulated through two systems, liposomes and polymeric nanoparticles. The evaluation of the acetyl-hexapeptide-3 showed an encapsulation efficiency of 95%. The vesicles showed a zeta potential of -31 mV. The results demonstrated that the active agent had a good cutaneous permeation and its encapsulation did not affect the permeation through the skin. The botulinum toxin Type A were successfully encapsulated into nanoparticles by multiple emulsion method and solvent evaporation. The nanoparticles had an average size of approximately 570 nm and a zeta potential of -7,40 mV, which is characteristic of the polyester used. The multilamellar liposomes were obtained through a method that involved hydrating the lipid film and showed an average size of approximately 1370 nm and a zeta potential of -37 mV. It was possible to demonstrate by means of infrared fourier transform spectroscopy, the presence of botulinum toxin Type A in the polymeric nanoparticles and the liposomes. The in vitro assays that were carried out suggested that the liposomes that contained the botulinum toxin Type A had an effect on the neurotransmitters in the assays that were conducted, whereas it was not possible to identify the same effect in the nanoparticles that contained the botulinum toxin.These results showed that the encapsulation of botulinum toxin A can be an alternative for the topical application of botulinum toxin Type A in a non-invasive way and with a good deal of comfort to the patient. With regard to acetyl hexapeptide-3, it can be claimed that this active agent when released shows the same degree of penetration through the skin as the encapsulated active agent. This suggests that the penetration of acetyl hexapeptide-3 does not undergo any alteration when encapsulated in liposomes. Thus, the active agent can be applied topically in this way.O envelhecimento cutâneo é um fenômeno biológico complexo que depende da combinação de fatores intrínsecos, responsáveis pelo envelhecimento cronológico e extrínsecos, responsáveis pelo fotoenvelhecimento cutâneo. Outro fator importante a ser considerado é o aparecimento de rugas causadas pelos movimentos faciais repetitivos. Atualmente é grande a procura por produtos antienvelhecimento e, uma das estratégias mais empregada para esse fim é a aplicação da toxina botulínica do tipo A, que é considerada a principal atenuante de rugas. Outro ativo empregado com a mesma função da toxina botulínica é o acetil hexapeptídeo-3, comercialmente conhecido como Argireline. Este agente antienvelhecimento age de forma similar à toxina botulínica, reduzindo as linhas e rugas de expressão, ambos atuam na liberação da acetilcolina na junção neuromuscular. Uma das principais diferenças entre esses ativos está em sua forma de aplicação, enquanto a toxina botulínica é aplicada por meio de injeções intramusculares, o acetil hexapeptídeo-3 é empregado na forma de creme para aplicação tópica. Considerando que os dois ativos são neuropeptídios hidrofílicos de elevada massa molar, sua penetração através da pele é improvável. Assim, o objetivo deste trabalho foi desenvolver, caracterizar e avaliar sistemas constituídos por nanocarreadores capazes de permitir ou melhorar a permeação destes ativos através da pele. O acetil hexapeptídeo-3 foi encapsulado em lipossomas e a toxina botulínica foi encapsulada em dois sistemas, lipossomas e nanopartículas poliméricas. A avaliação do acetil exapeptídeo-3 mostrou uma eficiência de encapsulação de 95%. As vesículas apresentaram um potencial zeta de -31 mV. Os resultados demonstraram que o ativo apresentou boa permeação cutânea e sua encapsulação não afetou a permeação através da pele. A toxina botulínica foi encapsulada com sucesso em nanopartículas poliméricas, pelo método de emulsão múltipla e evaporação do solvente. As nanopartículas apresentaram tamanho médio de aproximadamente 570 nm e potencial zeta de –7,40 mV, característico do poliéster utilizado. Os lipossomas multilamelares obtidos por hidratação do filme lipídico apresentaram diâmetro médio de aproximadamente 1370 nm e potencial zeta de -37mV. Foi possível demonstrar, por meio dos espectros de infravermelho com Transformada de Fourier, a presença da toxina botulínica tipo A nas nanopartículas poliméricas e nos lipossomas. Os ensaios realizados in vitro indicaram que os lipossomas contendo a toxina botulínica tipo A apresentaram efeito sobre os neurotransmissores nos ensaios realizados, entretanto não foi possível identificar o mesmo efeito nas nanopartículas contendo a toxina botulínica. Esses resultados mostraram que a encapsulação da toxina botulínica A pode ser uma alternativa para sua aplicação tópica, de forma não invasiva e com muito conforto ao paciente. Quanto ao acetil hexapeptídeo-3, pôde-se constatar que este ativo na forma livre apresentou a mesma penetração através da pele do que o ativo encapsulado, o que indica que a penetração do acetil hexapeptídeo-3 não sofre alteração quando encapsulado em lipossomas. Desta forma o ativo pode ser aplicado de forma direta.Made available in DSpace on 2017-07-21T14:13:12Z (GMT). No. of bitstreams: 1 Daniele Priscila.pdf: 2574355 bytes, checksum: 6ecd817b9f806a21743e5671cf9f96c5 (MD5) Previous issue date: 2013-02-25application/pdfporUNIVERSIDADE ESTADUAL DE PONTA GROSSAPrograma de Pós Graduação Ciências FarmacêuticasUEPGBRFarmacos, Medicamentos e Biociências Aplicadas à Farmáciatoxina botulínicahexapeptídeo-3nanopartículaslipossomaspermeação cutâneabotulinum toxinhexapeptide-3nanoparticlesliposomespermeationCNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIADesenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo Ainfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisinfo:eu-repo/semantics/openAccessreponame:Biblioteca Digital de Teses e Dissertações da UEPGinstname:Universidade Estadual de Ponta Grossa (UEPG)instacron:UEPGORIGINALDaniele Priscila.pdfapplication/pdf2574355http://tede2.uepg.br/jspui/bitstream/prefix/113/1/Daniele%20Priscila.pdf6ecd817b9f806a21743e5671cf9f96c5MD51prefix/1132017-07-21 11:13:12.384oai:tede2.uepg.br:prefix/113Biblioteca Digital de Teses e Dissertaçõeshttps://tede2.uepg.br/jspui/PUBhttp://tede2.uepg.br/oai/requestbicen@uepg.br||mv_fidelis@yahoo.com.bropendoar:2017-07-21T14:13:12Biblioteca Digital de Teses e Dissertações da UEPG - Universidade Estadual de Ponta Grossa (UEPG)false
dc.title.por.fl_str_mv Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A
title Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A
spellingShingle Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A
Assunção, Daniele Priscila da Silva Fardin de
toxina botulínica
hexapeptídeo-3
nanopartículas
lipossomas
permeação cutânea
botulinum toxin
hexapeptide-3
nanoparticles
liposomes
permeation
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
title_short Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A
title_full Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A
title_fullStr Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A
title_full_unstemmed Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A
title_sort Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A
author Assunção, Daniele Priscila da Silva Fardin de
author_facet Assunção, Daniele Priscila da Silva Fardin de
author_role author
dc.contributor.advisor1.fl_str_mv Paula, Josiane de Fatima Padilha de
dc.contributor.advisor1ID.fl_str_mv CPF:49618768953
dc.contributor.advisor1Lattes.fl_str_mv http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4702484Y6
dc.contributor.referee1.fl_str_mv Farago, Paulo Vitor
dc.contributor.referee1ID.fl_str_mv CPF:02688357999
dc.contributor.referee2.fl_str_mv Canteri, Maria Helene
dc.contributor.referee2ID.fl_str_mv CPF:88289796900
dc.contributor.referee2Lattes.fl_str_mv http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4705338T4
dc.contributor.authorID.fl_str_mv CPF:03553925930
dc.contributor.authorLattes.fl_str_mv http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4499168E2
dc.contributor.author.fl_str_mv Assunção, Daniele Priscila da Silva Fardin de
contributor_str_mv Paula, Josiane de Fatima Padilha de
Farago, Paulo Vitor
Canteri, Maria Helene
dc.subject.por.fl_str_mv toxina botulínica
hexapeptídeo-3
nanopartículas
lipossomas
permeação cutânea
topic toxina botulínica
hexapeptídeo-3
nanopartículas
lipossomas
permeação cutânea
botulinum toxin
hexapeptide-3
nanoparticles
liposomes
permeation
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
dc.subject.eng.fl_str_mv botulinum toxin
hexapeptide-3
nanoparticles
liposomes
permeation
dc.subject.cnpq.fl_str_mv CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
description Cutaneous aging is a complex biological phenomenon that depends on a number of intrinsic, responsible for chronological aging and the extrinsic factors, which is responsible for cutaneous photo aging. Another important factor that must be taken into account is the appearance of wrinkles caused by repeated movements of the facial muscles. Currently there is a huge demand for anti-aging products and one of the strategies that is most commonly employed for this end, is the application of botulinum toxin Type A which is regarded as the principal treatment for the mitigation of wrinkles. Another active substance which functions in the same way as botulinum toxin A, is acetyl hexapeptide-3, which is marketed under the name of Argireline. This anti-aging agent acts in a similar way to botulinum toxin by smoothing out the expressive lines and wrinkles caused by repeated movements. Both the active agents are responsible for the release of acetylcholine at the neuromuscular junction. One of the main differences between these active agents is in their form of application since, whereas botulinum toxin A is administered by injection, acetyl hexapeptide-3 is used in the form of a cream for topical application. Given the fact that the two active agents are hydrophilic neuropeptides of high molecular mass, their ability to penetrate the skin is improbable. Thus, the purpose of this study was to develop, characterize and evaluate systems comprising nanocarriers that are able to allow or improve the permeation of these active agents through the skin. Acetyl hexapeptide-3 was encapsulated in liposomes and botulinum toxin was encapsulated through two systems, liposomes and polymeric nanoparticles. The evaluation of the acetyl-hexapeptide-3 showed an encapsulation efficiency of 95%. The vesicles showed a zeta potential of -31 mV. The results demonstrated that the active agent had a good cutaneous permeation and its encapsulation did not affect the permeation through the skin. The botulinum toxin Type A were successfully encapsulated into nanoparticles by multiple emulsion method and solvent evaporation. The nanoparticles had an average size of approximately 570 nm and a zeta potential of -7,40 mV, which is characteristic of the polyester used. The multilamellar liposomes were obtained through a method that involved hydrating the lipid film and showed an average size of approximately 1370 nm and a zeta potential of -37 mV. It was possible to demonstrate by means of infrared fourier transform spectroscopy, the presence of botulinum toxin Type A in the polymeric nanoparticles and the liposomes. The in vitro assays that were carried out suggested that the liposomes that contained the botulinum toxin Type A had an effect on the neurotransmitters in the assays that were conducted, whereas it was not possible to identify the same effect in the nanoparticles that contained the botulinum toxin.These results showed that the encapsulation of botulinum toxin A can be an alternative for the topical application of botulinum toxin Type A in a non-invasive way and with a good deal of comfort to the patient. With regard to acetyl hexapeptide-3, it can be claimed that this active agent when released shows the same degree of penetration through the skin as the encapsulated active agent. This suggests that the penetration of acetyl hexapeptide-3 does not undergo any alteration when encapsulated in liposomes. Thus, the active agent can be applied topically in this way.
publishDate 2013
dc.date.available.fl_str_mv 2013-10-16
2017-07-21T14:13:12Z
dc.date.issued.fl_str_mv 2013-02-25
dc.date.accessioned.fl_str_mv 2017-07-21T14:13:12Z
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dc.identifier.citation.fl_str_mv ASSUNÇÃO, Daniele Priscila da Silva Fardin de. Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A. 2013. 64 f. Dissertação (Mestrado em Farmacos, Medicamentos e Biociências Aplicadas à Farmácia) - UNIVERSIDADE ESTADUAL DE PONTA GROSSA, Ponta Grossa, 2013.
dc.identifier.uri.fl_str_mv http://tede2.uepg.br/jspui/handle/prefix/113
identifier_str_mv ASSUNÇÃO, Daniele Priscila da Silva Fardin de. Desenvolvimento, caracterização e avaliação de nanocarreadores contendo acetil hexapeptídeo-3 e toxina botulínica tipo A. 2013. 64 f. Dissertação (Mestrado em Farmacos, Medicamentos e Biociências Aplicadas à Farmácia) - UNIVERSIDADE ESTADUAL DE PONTA GROSSA, Ponta Grossa, 2013.
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