Preparation and characterization of paclitaxel-loaded PLDLA microspheres

Detalhes bibliográficos
Autor(a) principal: Martins,Kelly F.
Data de Publicação: 2014
Outros Autores: Messias,André D., Leite,Fábio L., Duek,Eliana A.R.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Materials research (São Carlos. Online)
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S1516-14392014000300016
Resumo: Paclitaxel (Taxol®), is a drug used to treat ovarian, breast, lung and bladder cancer. However, the low solubility of this drug in water is a major limitation in its clinical use. One strategy to overcome this limitation would be to encapsulate paclitaxel in polymeric microspheres that are biocompatible and can be used as drug carriers. The aim of this study was to use the bioresorbable, biocompatible copolymer poly-L-co-D,L-lactic acid (PLDLA) in the 70:30 rate to produce and characterize microspheres containing paclitaxel. The simple emulsion technique was used to obtain spherical microspheres that were studied by scanning electron microscopy (SEM) and atomic force microscopy (AFM). The average size of PLDLA microspheres without and with paclitaxel was 10.3 ± 1.7 μm and 12.7 ± 1.3 μm, respectively, as determined by laser light scattering (LLS). Differential scanning calorimetry (DSC) showed that pure paclitaxel had an endothermic peak corresponding to a melting point of 220 °C, which indicated its crystalline nature. The same peak was observed in a physical mixture of PLDLA + paclitaxel in which both components were present in the same proportions used to prepare the microspheres . In contrast, this peak was not observed for the drug, indicating that paclitaxel did not crystallize in PLDLA microspheres. Differential scanning calorimetry (DSC) indicated that paclitaxel was homogeneously dispersed in the PLDLA microspheres, the incorporation of paclitaxel into the microspheres did not alter the thermal properties of PLDLA. The Fourier transform infrared spectroscopy (FTIR) analysis seems to indicate the absence of chemical interaction between polymer and drugs in microspheres and the presence of drugs as a molecular dispersion in the polymer matrix. The efficiency of paclitaxel encapsulation in PLDLA microspheres was 98.0 ± 0.3%, as assessed by high performance liquid chromatography (HPLC). A kinetic study of drug release in vitro using HPLC showed an initial burst release followed by a slower release characteristic of large diameter distribution systems. PLDLA microspheres released 90 ± 4% of the drug over a 30-day period. These findings indicate that PLDLA microspheres are promising carriers for paclitaxel, with a potential for future applications in drug delivery systems.
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spelling Preparation and characterization of paclitaxel-loaded PLDLA microsphereschemotherapymicrospherespaclitaxelPLDLAPaclitaxel (Taxol®), is a drug used to treat ovarian, breast, lung and bladder cancer. However, the low solubility of this drug in water is a major limitation in its clinical use. One strategy to overcome this limitation would be to encapsulate paclitaxel in polymeric microspheres that are biocompatible and can be used as drug carriers. The aim of this study was to use the bioresorbable, biocompatible copolymer poly-L-co-D,L-lactic acid (PLDLA) in the 70:30 rate to produce and characterize microspheres containing paclitaxel. The simple emulsion technique was used to obtain spherical microspheres that were studied by scanning electron microscopy (SEM) and atomic force microscopy (AFM). The average size of PLDLA microspheres without and with paclitaxel was 10.3 ± 1.7 μm and 12.7 ± 1.3 μm, respectively, as determined by laser light scattering (LLS). Differential scanning calorimetry (DSC) showed that pure paclitaxel had an endothermic peak corresponding to a melting point of 220 °C, which indicated its crystalline nature. The same peak was observed in a physical mixture of PLDLA + paclitaxel in which both components were present in the same proportions used to prepare the microspheres . In contrast, this peak was not observed for the drug, indicating that paclitaxel did not crystallize in PLDLA microspheres. Differential scanning calorimetry (DSC) indicated that paclitaxel was homogeneously dispersed in the PLDLA microspheres, the incorporation of paclitaxel into the microspheres did not alter the thermal properties of PLDLA. The Fourier transform infrared spectroscopy (FTIR) analysis seems to indicate the absence of chemical interaction between polymer and drugs in microspheres and the presence of drugs as a molecular dispersion in the polymer matrix. The efficiency of paclitaxel encapsulation in PLDLA microspheres was 98.0 ± 0.3%, as assessed by high performance liquid chromatography (HPLC). A kinetic study of drug release in vitro using HPLC showed an initial burst release followed by a slower release characteristic of large diameter distribution systems. PLDLA microspheres released 90 ± 4% of the drug over a 30-day period. These findings indicate that PLDLA microspheres are promising carriers for paclitaxel, with a potential for future applications in drug delivery systems.ABM, ABC, ABPol2014-06-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S1516-14392014000300016Materials Research v.17 n.3 2014reponame:Materials research (São Carlos. Online)instname:Universidade Federal de São Carlos (UFSCAR)instacron:ABM ABC ABPOL10.1590/S1516-14392014005000028info:eu-repo/semantics/openAccessMartins,Kelly F.Messias,André D.Leite,Fábio L.Duek,Eliana A.R.eng2014-06-18T00:00:00Zoai:scielo:S1516-14392014000300016Revistahttp://www.scielo.br/mrPUBhttps://old.scielo.br/oai/scielo-oai.phpdedz@power.ufscar.br1980-53731516-1439opendoar:2014-06-18T00:00Materials research (São Carlos. Online) - Universidade Federal de São Carlos (UFSCAR)false
dc.title.none.fl_str_mv Preparation and characterization of paclitaxel-loaded PLDLA microspheres
title Preparation and characterization of paclitaxel-loaded PLDLA microspheres
spellingShingle Preparation and characterization of paclitaxel-loaded PLDLA microspheres
Martins,Kelly F.
chemotherapy
microspheres
paclitaxel
PLDLA
title_short Preparation and characterization of paclitaxel-loaded PLDLA microspheres
title_full Preparation and characterization of paclitaxel-loaded PLDLA microspheres
title_fullStr Preparation and characterization of paclitaxel-loaded PLDLA microspheres
title_full_unstemmed Preparation and characterization of paclitaxel-loaded PLDLA microspheres
title_sort Preparation and characterization of paclitaxel-loaded PLDLA microspheres
author Martins,Kelly F.
author_facet Martins,Kelly F.
Messias,André D.
Leite,Fábio L.
Duek,Eliana A.R.
author_role author
author2 Messias,André D.
Leite,Fábio L.
Duek,Eliana A.R.
author2_role author
author
author
dc.contributor.author.fl_str_mv Martins,Kelly F.
Messias,André D.
Leite,Fábio L.
Duek,Eliana A.R.
dc.subject.por.fl_str_mv chemotherapy
microspheres
paclitaxel
PLDLA
topic chemotherapy
microspheres
paclitaxel
PLDLA
description Paclitaxel (Taxol®), is a drug used to treat ovarian, breast, lung and bladder cancer. However, the low solubility of this drug in water is a major limitation in its clinical use. One strategy to overcome this limitation would be to encapsulate paclitaxel in polymeric microspheres that are biocompatible and can be used as drug carriers. The aim of this study was to use the bioresorbable, biocompatible copolymer poly-L-co-D,L-lactic acid (PLDLA) in the 70:30 rate to produce and characterize microspheres containing paclitaxel. The simple emulsion technique was used to obtain spherical microspheres that were studied by scanning electron microscopy (SEM) and atomic force microscopy (AFM). The average size of PLDLA microspheres without and with paclitaxel was 10.3 ± 1.7 μm and 12.7 ± 1.3 μm, respectively, as determined by laser light scattering (LLS). Differential scanning calorimetry (DSC) showed that pure paclitaxel had an endothermic peak corresponding to a melting point of 220 °C, which indicated its crystalline nature. The same peak was observed in a physical mixture of PLDLA + paclitaxel in which both components were present in the same proportions used to prepare the microspheres . In contrast, this peak was not observed for the drug, indicating that paclitaxel did not crystallize in PLDLA microspheres. Differential scanning calorimetry (DSC) indicated that paclitaxel was homogeneously dispersed in the PLDLA microspheres, the incorporation of paclitaxel into the microspheres did not alter the thermal properties of PLDLA. The Fourier transform infrared spectroscopy (FTIR) analysis seems to indicate the absence of chemical interaction between polymer and drugs in microspheres and the presence of drugs as a molecular dispersion in the polymer matrix. The efficiency of paclitaxel encapsulation in PLDLA microspheres was 98.0 ± 0.3%, as assessed by high performance liquid chromatography (HPLC). A kinetic study of drug release in vitro using HPLC showed an initial burst release followed by a slower release characteristic of large diameter distribution systems. PLDLA microspheres released 90 ± 4% of the drug over a 30-day period. These findings indicate that PLDLA microspheres are promising carriers for paclitaxel, with a potential for future applications in drug delivery systems.
publishDate 2014
dc.date.none.fl_str_mv 2014-06-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S1516-14392014000300016
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S1516-14392014000300016
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/S1516-14392014005000028
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv text/html
dc.publisher.none.fl_str_mv ABM, ABC, ABPol
publisher.none.fl_str_mv ABM, ABC, ABPol
dc.source.none.fl_str_mv Materials Research v.17 n.3 2014
reponame:Materials research (São Carlos. Online)
instname:Universidade Federal de São Carlos (UFSCAR)
instacron:ABM ABC ABPOL
instname_str Universidade Federal de São Carlos (UFSCAR)
instacron_str ABM ABC ABPOL
institution ABM ABC ABPOL
reponame_str Materials research (São Carlos. Online)
collection Materials research (São Carlos. Online)
repository.name.fl_str_mv Materials research (São Carlos. Online) - Universidade Federal de São Carlos (UFSCAR)
repository.mail.fl_str_mv dedz@power.ufscar.br
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