Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona
Autor(a) principal: | |
---|---|
Data de Publicação: | 2013 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Manancial - Repositório Digital da UFSM |
Texto Completo: | http://repositorio.ufsm.br/handle/1/6026 |
Resumo: | Polymeric nanocapsules have been studied extensively for drug delivery by various routes of administration. Currently, the nanoencapsulation of drugs is considered the most efficient means of ensuring controlled release, specific targeting and reduction of adverse effects. In this context, the aim of this work was to develop polymeric nanocapsules for pulmonary delivery of beclomethasone dipropionate (BD). Nanocapsules have been prepared from 2 polymers, poly(-caprolactone) (PCL) and ethyl cellulose (EC). To quantify the drug in the nanostructures, the analytical method was developed and validated. This method showed to be specific, linear, precise, accurate and robust. Nanocapsules were prepared by interfacial deposition of preformed polymers and were evaluated as to pH, particle diameter, polydispersity index, drug content, encapsulation efficiency and zeta potential. All samples showed encapsulation efficiency greater than 98%, negative zeta potential, pH value in the range of neutrality and drug contents close to their theoretical values. The size distribution was nanometric (158-270 nm) with polydispersity index lower than 0.2. The results of the photodegradation study showed that polymeric nanocapsules were able to protect BD from UVC radiation when compared to the free drug solution. In vitro release experiments were performed using the dialysis bag technique, which showed, for all formulations, a prolonged drug release mediated by anomalous transport and first order kinetics. Free drug in solution took between 24 and 36 h to reach 100% of release, whereas nanocapsules were able to control the drug release for up to 108 h, depending on the polymer employed. Nanocapsules of EC and PCL were evaluated for in vitro and in vivo toxicity and the results suggest that the proposed formulations are safe. In the final stage of the work, pullulan was proposed as stabilizer agent for PCL nanocapsules and the results obtained for the zeta potential and the drug content suggested that these formulations have become more stable. Thus, the nanocapsules developed in this work represent a promising alternative for the pulmonary delivery of BD in the treatment of asthma and other respiratory disorders. |
id |
UFSM_015cdc0303dd806b36080f268ed9c5c9 |
---|---|
oai_identifier_str |
oai:repositorio.ufsm.br:1/6026 |
network_acronym_str |
UFSM |
network_name_str |
Manancial - Repositório Digital da UFSM |
repository_id_str |
|
spelling |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasonaDevelopment of polymeric nanocapsules for pulmonary delivery of beclomethasone dipropionateDipropionato de beclometasonaNanocápsulasLiberação pulmonarPullulanCitotoxicidade in vitroToxicidade pulmonar in vivoNanocapsulesPulmonary deliveryPullulanIn vitro cytotoxicityBeclomethasone dipropionateIn vivo pulmonary toxicityCNPQ::CIENCIAS DA SAUDE::FARMACIAPolymeric nanocapsules have been studied extensively for drug delivery by various routes of administration. Currently, the nanoencapsulation of drugs is considered the most efficient means of ensuring controlled release, specific targeting and reduction of adverse effects. In this context, the aim of this work was to develop polymeric nanocapsules for pulmonary delivery of beclomethasone dipropionate (BD). Nanocapsules have been prepared from 2 polymers, poly(-caprolactone) (PCL) and ethyl cellulose (EC). To quantify the drug in the nanostructures, the analytical method was developed and validated. This method showed to be specific, linear, precise, accurate and robust. Nanocapsules were prepared by interfacial deposition of preformed polymers and were evaluated as to pH, particle diameter, polydispersity index, drug content, encapsulation efficiency and zeta potential. All samples showed encapsulation efficiency greater than 98%, negative zeta potential, pH value in the range of neutrality and drug contents close to their theoretical values. The size distribution was nanometric (158-270 nm) with polydispersity index lower than 0.2. The results of the photodegradation study showed that polymeric nanocapsules were able to protect BD from UVC radiation when compared to the free drug solution. In vitro release experiments were performed using the dialysis bag technique, which showed, for all formulations, a prolonged drug release mediated by anomalous transport and first order kinetics. Free drug in solution took between 24 and 36 h to reach 100% of release, whereas nanocapsules were able to control the drug release for up to 108 h, depending on the polymer employed. Nanocapsules of EC and PCL were evaluated for in vitro and in vivo toxicity and the results suggest that the proposed formulations are safe. In the final stage of the work, pullulan was proposed as stabilizer agent for PCL nanocapsules and the results obtained for the zeta potential and the drug content suggested that these formulations have become more stable. Thus, the nanocapsules developed in this work represent a promising alternative for the pulmonary delivery of BD in the treatment of asthma and other respiratory disorders.Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorNanocápsulas poliméricas vem sendo estudadas extensivamente para liberação de fármacos por diversas vias de administração. Atualmente a nanoencapsulação de fármacos é considerada o meio mais eficiente de assegurar liberação controlada, direcionamento específico e redução dos efeitos adversos. Neste contexto, o objetivo do presente trabalho foi desenvolver nanocápsulas poliméricas para a liberação pulmonar do dipropionato de beclometasona (DB). Nanocápsulas foram preparadas a partir de 2 polímeros, a poli(-caprolactona) (PCL) e a etilcelulose (EC). Para a quantificação do fármaco nas nanoestruturas, o método analítico foi desenvolvido e validado. Este mostrou ser específico, linear, preciso, exato e robusto. As nanocápsulas foram preparadas por deposição interfacial do polímero pré-formado e avaliadas quanto ao pH, diâmetro de partícula, índice de polidispersão, teor, eficiência de encapsulamento e potencial zeta. Todas as amostras apresentaram eficiência de encapsulamento maior que 98%, valor de potencial zeta negativo, valor de pH na faixa da neutralidade e teores próximos aos teóricos. A distribuição de tamanho foi nanométrica (158-270 nm) com índice de polidispersão menor que 0,2. Os resultados do estudo de fotodegradação mostraram que as nanocápsulas poliméricas foram capazes de proteger o DB da radiação UVC quando comparadas com uma solução do fármaco. Os experimentos de liberação in vitro foram realizados empregando a técnica de sacos de diálise, a qual mostrou, para todas as formulações, uma liberação prolongada do DB, mediada por transporte anômalo e cinética de primeira ordem. A solução etanólica de DB levou entre 24 e 36 h para alcançar 100% de liberação, enquanto que as nanocápsulas foram capazes de controlar a liberação do fármaco por até 108 h, dependendo do polímero empregado. Nanocápsulas de EC e PCL foram avaliadas quanto à toxicidade in vitro e in vivo e os resultados obtidos sugerem que as formulações propostas são seguras. Na etapa final do trabalho, o pullulan foi proposto como agente estabilizador de nanocápsulas de PCL e os resultados obtidos para o potencial zeta e o teor de fármaco sugerem que estas formulações tornaram-se mais estáveis. Desta forma, as nanocápsulas desenvolvidas neste trabalho representam uma alternativa promissora para a liberação pulmonar do DB no tratamento da asma e de outras desordens do trato respiratório.Universidade Federal de Santa MariaBRFarmáciaUFSMPrograma de Pós-Graduação em Ciências FarmacêuticasCruz, Letíciahttp://lattes.cnpq.br/3095970241017527Pohlmann, Adriana Raffinhttp://lattes.cnpq.br/4050543278806170Adams, Andréa Inês Hornhttp://lattes.cnpq.br/6872246935204149Chassot, Janaíne Micheli2015-11-132015-11-132013-03-22info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfapplication/pdfCHASSOT, Janaíne Micheli. DEVELOPMENT OF POLYMERIC NANOCAPSULES FOR PULMONARY DELIVERY OF BECLOMETHASONE DIPROPIONATE. 2013. 110 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013.http://repositorio.ufsm.br/handle/1/6026porinfo:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2022-10-11T15:01:32Zoai:repositorio.ufsm.br:1/6026Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2022-10-11T15:01:32Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false |
dc.title.none.fl_str_mv |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona Development of polymeric nanocapsules for pulmonary delivery of beclomethasone dipropionate |
title |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona |
spellingShingle |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona Chassot, Janaíne Micheli Dipropionato de beclometasona Nanocápsulas Liberação pulmonar Pullulan Citotoxicidade in vitro Toxicidade pulmonar in vivo Nanocapsules Pulmonary delivery Pullulan In vitro cytotoxicity Beclomethasone dipropionate In vivo pulmonary toxicity CNPQ::CIENCIAS DA SAUDE::FARMACIA |
title_short |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona |
title_full |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona |
title_fullStr |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona |
title_full_unstemmed |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona |
title_sort |
Desenvolvimento de nanocápsulas poliméricas para liberação pulmonar do dipropionato de beclometasona |
author |
Chassot, Janaíne Micheli |
author_facet |
Chassot, Janaíne Micheli |
author_role |
author |
dc.contributor.none.fl_str_mv |
Cruz, Letícia http://lattes.cnpq.br/3095970241017527 Pohlmann, Adriana Raffin http://lattes.cnpq.br/4050543278806170 Adams, Andréa Inês Horn http://lattes.cnpq.br/6872246935204149 |
dc.contributor.author.fl_str_mv |
Chassot, Janaíne Micheli |
dc.subject.por.fl_str_mv |
Dipropionato de beclometasona Nanocápsulas Liberação pulmonar Pullulan Citotoxicidade in vitro Toxicidade pulmonar in vivo Nanocapsules Pulmonary delivery Pullulan In vitro cytotoxicity Beclomethasone dipropionate In vivo pulmonary toxicity CNPQ::CIENCIAS DA SAUDE::FARMACIA |
topic |
Dipropionato de beclometasona Nanocápsulas Liberação pulmonar Pullulan Citotoxicidade in vitro Toxicidade pulmonar in vivo Nanocapsules Pulmonary delivery Pullulan In vitro cytotoxicity Beclomethasone dipropionate In vivo pulmonary toxicity CNPQ::CIENCIAS DA SAUDE::FARMACIA |
description |
Polymeric nanocapsules have been studied extensively for drug delivery by various routes of administration. Currently, the nanoencapsulation of drugs is considered the most efficient means of ensuring controlled release, specific targeting and reduction of adverse effects. In this context, the aim of this work was to develop polymeric nanocapsules for pulmonary delivery of beclomethasone dipropionate (BD). Nanocapsules have been prepared from 2 polymers, poly(-caprolactone) (PCL) and ethyl cellulose (EC). To quantify the drug in the nanostructures, the analytical method was developed and validated. This method showed to be specific, linear, precise, accurate and robust. Nanocapsules were prepared by interfacial deposition of preformed polymers and were evaluated as to pH, particle diameter, polydispersity index, drug content, encapsulation efficiency and zeta potential. All samples showed encapsulation efficiency greater than 98%, negative zeta potential, pH value in the range of neutrality and drug contents close to their theoretical values. The size distribution was nanometric (158-270 nm) with polydispersity index lower than 0.2. The results of the photodegradation study showed that polymeric nanocapsules were able to protect BD from UVC radiation when compared to the free drug solution. In vitro release experiments were performed using the dialysis bag technique, which showed, for all formulations, a prolonged drug release mediated by anomalous transport and first order kinetics. Free drug in solution took between 24 and 36 h to reach 100% of release, whereas nanocapsules were able to control the drug release for up to 108 h, depending on the polymer employed. Nanocapsules of EC and PCL were evaluated for in vitro and in vivo toxicity and the results suggest that the proposed formulations are safe. In the final stage of the work, pullulan was proposed as stabilizer agent for PCL nanocapsules and the results obtained for the zeta potential and the drug content suggested that these formulations have become more stable. Thus, the nanocapsules developed in this work represent a promising alternative for the pulmonary delivery of BD in the treatment of asthma and other respiratory disorders. |
publishDate |
2013 |
dc.date.none.fl_str_mv |
2013-03-22 2015-11-13 2015-11-13 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/masterThesis |
format |
masterThesis |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
CHASSOT, Janaíne Micheli. DEVELOPMENT OF POLYMERIC NANOCAPSULES FOR PULMONARY DELIVERY OF BECLOMETHASONE DIPROPIONATE. 2013. 110 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013. http://repositorio.ufsm.br/handle/1/6026 |
identifier_str_mv |
CHASSOT, Janaíne Micheli. DEVELOPMENT OF POLYMERIC NANOCAPSULES FOR PULMONARY DELIVERY OF BECLOMETHASONE DIPROPIONATE. 2013. 110 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013. |
url |
http://repositorio.ufsm.br/handle/1/6026 |
dc.language.iso.fl_str_mv |
por |
language |
por |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf application/pdf |
dc.publisher.none.fl_str_mv |
Universidade Federal de Santa Maria BR Farmácia UFSM Programa de Pós-Graduação em Ciências Farmacêuticas |
publisher.none.fl_str_mv |
Universidade Federal de Santa Maria BR Farmácia UFSM Programa de Pós-Graduação em Ciências Farmacêuticas |
dc.source.none.fl_str_mv |
reponame:Manancial - Repositório Digital da UFSM instname:Universidade Federal de Santa Maria (UFSM) instacron:UFSM |
instname_str |
Universidade Federal de Santa Maria (UFSM) |
instacron_str |
UFSM |
institution |
UFSM |
reponame_str |
Manancial - Repositório Digital da UFSM |
collection |
Manancial - Repositório Digital da UFSM |
repository.name.fl_str_mv |
Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM) |
repository.mail.fl_str_mv |
atendimento.sib@ufsm.br||tedebc@gmail.com |
_version_ |
1805922025771892736 |