Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel

Detalhes bibliográficos
Ano de defesa: 2013
Autor(a) principal: Martins, Kelly Fernanda
Orientador(a): Duek, Eliana Aparecida de Rezende lattes
Banca de defesa: Leite, Fábio de Lima lattes
Tipo de documento: Dissertação
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: Universidade Federal de São Carlos
Programa de Pós-Graduação: Programa de Pós-Graduação em Ciência dos Materiais - PPGCM-So
Departamento: Não Informado pela instituição
País: BR
Palavras-chave em Português:
Palavras-chave em Inglês:
Área do conhecimento CNPq:
Link de acesso: https://repositorio.ufscar.br/handle/ufscar/1170
Resumo: In order to minimize the side effects of chemotherapy concurrently with the enhancement of its therapeutic action is to use it on devices that enable a controlled drug release, by vectors, such as polymeric microspheres, which act as a drug carrier, modifying its distribution pattern in the organism. Paclitaxel ((Taxol®) is a drug used primarily in the treatment of ovarian, breast, lung and bladder cancer. Due to its antimitotic and antiproliferative action, there is a potential interest in cancer therapy. However, the success of this clinical application is limited to low solubility in water and toxic action. The objective of this study was to obtain and characterize physic-chemically the bioresorbable and biocompatible copolymer poly (L-co-D, L lactic acid) (PLDLA) microspheres encapsulating the paclitaxel chemotherapy. The simple emulsion technique allowed to obtain spherical microspheres, verified by scanning electron microscopy (SEM) and atomic force microscopy (AFM). The average size of the microspheres PLDA pure and containing paclitaxel were, respectively, 10.3 μm ± 1.7 and 12.7 μm ± 1.3, obtained by the technique of laser light scattering (LLS). Moreover the essay of differential scanning calorimetry (DSC) suggests that the drug paclitaxel is homogeneously dispersed in the microspheres PLDLA. The encapsulation efficiency of the microspheres PLDLA paclitaxel was 98.0% ± 0.3, obtained by high performance liquid chromatography (HPLC). The in vitro release study performed on HPLC showed initial burst release followed by a slower release, which characterizes large diameter distribution systems. PLDLA microspheres released 90% ± 4.0 of the drug paclitaxel up to 30th day of study while the degradation process occurred. Thus, the microspheres obtained PLDLA devices are promising as carriers of paclitaxel, with potential for future applications in drug delivery systems.
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spelling Martins, Kelly FernandaDuek, Eliana Aparecida de Rezendehttp://lattes.cnpq.br/4147198882685212Leite, Fábio de Limahttp://lattes.cnpq.br/5490031389817518http://lattes.cnpq.br/91375486507451702016-06-02T19:19:55Z2013-08-012016-06-02T19:19:55Z2013-02-05https://repositorio.ufscar.br/handle/ufscar/1170In order to minimize the side effects of chemotherapy concurrently with the enhancement of its therapeutic action is to use it on devices that enable a controlled drug release, by vectors, such as polymeric microspheres, which act as a drug carrier, modifying its distribution pattern in the organism. Paclitaxel ((Taxol®) is a drug used primarily in the treatment of ovarian, breast, lung and bladder cancer. Due to its antimitotic and antiproliferative action, there is a potential interest in cancer therapy. However, the success of this clinical application is limited to low solubility in water and toxic action. The objective of this study was to obtain and characterize physic-chemically the bioresorbable and biocompatible copolymer poly (L-co-D, L lactic acid) (PLDLA) microspheres encapsulating the paclitaxel chemotherapy. The simple emulsion technique allowed to obtain spherical microspheres, verified by scanning electron microscopy (SEM) and atomic force microscopy (AFM). The average size of the microspheres PLDA pure and containing paclitaxel were, respectively, 10.3 μm ± 1.7 and 12.7 μm ± 1.3, obtained by the technique of laser light scattering (LLS). Moreover the essay of differential scanning calorimetry (DSC) suggests that the drug paclitaxel is homogeneously dispersed in the microspheres PLDLA. The encapsulation efficiency of the microspheres PLDLA paclitaxel was 98.0% ± 0.3, obtained by high performance liquid chromatography (HPLC). The in vitro release study performed on HPLC showed initial burst release followed by a slower release, which characterizes large diameter distribution systems. PLDLA microspheres released 90% ± 4.0 of the drug paclitaxel up to 30th day of study while the degradation process occurred. Thus, the microspheres obtained PLDLA devices are promising as carriers of paclitaxel, with potential for future applications in drug delivery systems.Uma forma de minimizar os efeitos colaterais de quimioterápicos concomitantemente ao processo de potencialização de sua ação teraupêutica é empregá-los em dispositivos de liberação controlada de drogas, por meio de veículos, como microesferas poliméricas, que agem como carreadores de fármacos, modificando seu perfil de distribuição no organismo. O paclitaxel (Taxol®) é um quimioterápico utilizado principalmente no tratamento do câncer de ovário, mama, pulmão e bexiga. Devido à sua relevante ação antimitótica e antiproliferativa, existe potencial interesse de seu uso na terapia do câncer, porém o sucesso de sua aplicação clínica é limitado devido sua baixa solubilidade em água e sua ação tóxica. O objetivo desse estudo foi o de obter e caracterizar, físico-quimicamente, microesferas do copolímero biorreabsorvível e biocompatível poli(L-co-D,L ácido láctico) (PLDLA) encapsulando o quimioterápico paclitaxel. A técnica de simples emulsão permitiu a obtenção de microesferas na forma esférica, verificado por microscopia eletrônica de varredura (MEV) e microscopia de força atômica (AFM). O tamanho médio das microesferas de PLDLA puro e contendo paclitaxel, foi, respectivamente, de 10,3μm±1,7 e 12,7μm±1,3, obtidos pela técnica de espalhamento de luz laser (LLS). Já o ensaio de calorimetria diferencial exploratória (DSC), sugere que o fármaco paclitaxel está disperso de forma homogênea nas microesferas de PLDLA. A eficiência de encapsulação do paclitaxel nas microesferas de PLDLA foi de 98,0%±0,3, obtidos pela cromatografia líquida de alta eficiência (HPLC). O estudo de liberação do fármaco in vitro realizado no HPLC apresentou liberação inicial em explosão, seguida de uma liberação mais lenta, características de microesferas que apresentam diâmetros variados. As microesferas de PLDLA liberaram 90%±4,0 do fármaco paclitaxel até o 30° dia de estudo enquanto se degradavam. Assim, as microesferas de PLDLA obtidas são dispositivos promissores como carreadores do paclitaxel, com potencial para futura aplicação em sistemas de liberação de fármacos.Financiadora de Estudos e Projetosapplication/pdfporUniversidade Federal de São CarlosPrograma de Pós-Graduação em Ciência dos Materiais - PPGCM-SoUFSCarBRBiomateriaispolímeros (materiais)microesferas - uso terapêuticoPLDLAmicroesferaspaclitaxelquimioterápicomicrospheresPLDLApaclitaxelchemotherapeuticCIENCIAS EXATAS E DA TERRAObtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxelObtaining and characterization of the copolymer PLDLA microspheres containing paclitaxelinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFSCARinstname:Universidade Federal de São Carlos (UFSCAR)instacron:UFSCARORIGINALMARTINS_Kelly_2013.pdfapplication/pdf1489805https://{{ getenv "DSPACE_HOST" "repositorio.ufscar.br" }}/bitstream/ufscar/1170/1/MARTINS_Kelly_2013.pdf32aed5a1b752893511324c4670fcbcd5MD51TEXTMARTINS_Kelly_2013.pdf.txtMARTINS_Kelly_2013.pdf.txtExtracted texttext/plain0https://{{ getenv "DSPACE_HOST" "repositorio.ufscar.br" }}/bitstream/ufscar/1170/2/MARTINS_Kelly_2013.pdf.txtd41d8cd98f00b204e9800998ecf8427eMD52THUMBNAILMARTINS_Kelly_2013.pdf.jpgMARTINS_Kelly_2013.pdf.jpgIM Thumbnailimage/jpeg5774https://{{ getenv "DSPACE_HOST" "repositorio.ufscar.br" }}/bitstream/ufscar/1170/3/MARTINS_Kelly_2013.pdf.jpg0b1535215f547889acd9dc48e4a7be5eMD53ufscar/11702019-09-11 04:05:28.699oai:repositorio.ufscar.br:ufscar/1170Repositório InstitucionalPUBhttps://repositorio.ufscar.br/oai/requestopendoar:43222023-05-25T12:44:13.877403Repositório Institucional da UFSCAR - Universidade Federal de São Carlos (UFSCAR)false
dc.title.por.fl_str_mv Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel
dc.title.alternative.eng.fl_str_mv Obtaining and characterization of the copolymer PLDLA microspheres containing paclitaxel
title Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel
spellingShingle Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel
Martins, Kelly Fernanda
Biomateriais
polímeros (materiais)
microesferas - uso terapêutico
PLDLA
microesferas
paclitaxel
quimioterápico
microspheres
PLDLA
paclitaxel
chemotherapeutic
CIENCIAS EXATAS E DA TERRA
title_short Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel
title_full Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel
title_fullStr Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel
title_full_unstemmed Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel
title_sort Obtenção e caracterização de microesferas de copolímero PLDLA contendo paclitaxel
author Martins, Kelly Fernanda
author_facet Martins, Kelly Fernanda
author_role author
dc.contributor.authorlattes.por.fl_str_mv http://lattes.cnpq.br/9137548650745170
dc.contributor.author.fl_str_mv Martins, Kelly Fernanda
dc.contributor.advisor1.fl_str_mv Duek, Eliana Aparecida de Rezende
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/4147198882685212
dc.contributor.referee1.fl_str_mv Leite, Fábio de Lima
dc.contributor.referee1Lattes.fl_str_mv http://lattes.cnpq.br/5490031389817518
contributor_str_mv Duek, Eliana Aparecida de Rezende
Leite, Fábio de Lima
dc.subject.por.fl_str_mv Biomateriais
polímeros (materiais)
microesferas - uso terapêutico
PLDLA
microesferas
paclitaxel
quimioterápico
topic Biomateriais
polímeros (materiais)
microesferas - uso terapêutico
PLDLA
microesferas
paclitaxel
quimioterápico
microspheres
PLDLA
paclitaxel
chemotherapeutic
CIENCIAS EXATAS E DA TERRA
dc.subject.eng.fl_str_mv microspheres
PLDLA
paclitaxel
chemotherapeutic
dc.subject.cnpq.fl_str_mv CIENCIAS EXATAS E DA TERRA
description In order to minimize the side effects of chemotherapy concurrently with the enhancement of its therapeutic action is to use it on devices that enable a controlled drug release, by vectors, such as polymeric microspheres, which act as a drug carrier, modifying its distribution pattern in the organism. Paclitaxel ((Taxol®) is a drug used primarily in the treatment of ovarian, breast, lung and bladder cancer. Due to its antimitotic and antiproliferative action, there is a potential interest in cancer therapy. However, the success of this clinical application is limited to low solubility in water and toxic action. The objective of this study was to obtain and characterize physic-chemically the bioresorbable and biocompatible copolymer poly (L-co-D, L lactic acid) (PLDLA) microspheres encapsulating the paclitaxel chemotherapy. The simple emulsion technique allowed to obtain spherical microspheres, verified by scanning electron microscopy (SEM) and atomic force microscopy (AFM). The average size of the microspheres PLDA pure and containing paclitaxel were, respectively, 10.3 μm ± 1.7 and 12.7 μm ± 1.3, obtained by the technique of laser light scattering (LLS). Moreover the essay of differential scanning calorimetry (DSC) suggests that the drug paclitaxel is homogeneously dispersed in the microspheres PLDLA. The encapsulation efficiency of the microspheres PLDLA paclitaxel was 98.0% ± 0.3, obtained by high performance liquid chromatography (HPLC). The in vitro release study performed on HPLC showed initial burst release followed by a slower release, which characterizes large diameter distribution systems. PLDLA microspheres released 90% ± 4.0 of the drug paclitaxel up to 30th day of study while the degradation process occurred. Thus, the microspheres obtained PLDLA devices are promising as carriers of paclitaxel, with potential for future applications in drug delivery systems.
publishDate 2013
dc.date.available.fl_str_mv 2013-08-01
2016-06-02T19:19:55Z
dc.date.issued.fl_str_mv 2013-02-05
dc.date.accessioned.fl_str_mv 2016-06-02T19:19:55Z
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