Development of gold(III) thiosemicarbazonate complex–loaded PLGA nanoparticles: characterization and sustained release studies

The gold(III) complex [AuCl(L 1 )] has been reported as a lead candidate for Chagas’ disease (CD) treatment. However, in order to be effective, the drug must first reach the target tissue and then be delivered in therapeutic amounts. In this context, nanoparticles (NPs) of poly(lactic-co-glycolic ac...

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Veröffentlicht in:Journal of nanoparticle research : an interdisciplinary forum for nanoscale science and technology 2020-11, Vol.22 (11), Article 339
Hauptverfasser: Silva, Raphael T. C., Dalmolin, Luciana F., Moreto, Jéferson A., Oliveira, Carolina G., Machado, Antonio E. H., Lopez, Renata F. V., Maia, Pedro I. S.
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container_title Journal of nanoparticle research : an interdisciplinary forum for nanoscale science and technology
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creator Silva, Raphael T. C.
Dalmolin, Luciana F.
Moreto, Jéferson A.
Oliveira, Carolina G.
Machado, Antonio E. H.
Lopez, Renata F. V.
Maia, Pedro I. S.
description The gold(III) complex [AuCl(L 1 )] has been reported as a lead candidate for Chagas’ disease (CD) treatment. However, in order to be effective, the drug must first reach the target tissue and then be delivered in therapeutic amounts. In this context, nanoparticles (NPs) of poly(lactic-co-glycolic acid) (PLGA) have been developed to be used as delivery systems for [AuCl(L 1 )]. The [AuCl(L 1 )]-PLGA-NPs were prepared via the emulsification and solvent evaporation technique and displayed encapsulation efficiency around 90% with the size range of 275 ± 5 nm, polydispersity index (PDI) around 0.115, and a higher value of zeta potential (− 6.51 ± 0.47 mV) compared to blank NPs (without gold complex), which agree with the formation of a cationic species in solution, as indicated by computational calculations. Additionally, high-resolution images obtained by SEM showed the [AuCl(L 1 )]-PLGA-NPs spherical shape with average sizes close to those analyzed by the DLS technique. Stability studies for the [AuCl(L 1 )]-PLGA-NPs pointed out that no significant changes in relation to size and PDI occur over almost 2 months of storage at 8 °C. The release of the complex from NPs was about 10% in 24 h, followed by a slow release. By means of the Korsmeyer-Peppas model, it was possible to identify the release mechanism as being through diffusion and relaxation of the polymeric matrix. Overall, it has been shown that the PLGA-NPs are promising carriers for delivery of [AuCl(L 1 )] and are recommended to be investigated as formulations for parasite treatment in vivo experiments. Graphical abstract
doi_str_mv 10.1007/s11051-020-05064-6
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C. ; Dalmolin, Luciana F. ; Moreto, Jéferson A. ; Oliveira, Carolina G. ; Machado, Antonio E. H. ; Lopez, Renata F. V. ; Maia, Pedro I. S.</creator><creatorcontrib>Silva, Raphael T. C. ; Dalmolin, Luciana F. ; Moreto, Jéferson A. ; Oliveira, Carolina G. ; Machado, Antonio E. H. ; Lopez, Renata F. V. ; Maia, Pedro I. S.</creatorcontrib><description>The gold(III) complex [AuCl(L 1 )] has been reported as a lead candidate for Chagas’ disease (CD) treatment. However, in order to be effective, the drug must first reach the target tissue and then be delivered in therapeutic amounts. In this context, nanoparticles (NPs) of poly(lactic-co-glycolic acid) (PLGA) have been developed to be used as delivery systems for [AuCl(L 1 )]. The [AuCl(L 1 )]-PLGA-NPs were prepared via the emulsification and solvent evaporation technique and displayed encapsulation efficiency around 90% with the size range of 275 ± 5 nm, polydispersity index (PDI) around 0.115, and a higher value of zeta potential (− 6.51 ± 0.47 mV) compared to blank NPs (without gold complex), which agree with the formation of a cationic species in solution, as indicated by computational calculations. Additionally, high-resolution images obtained by SEM showed the [AuCl(L 1 )]-PLGA-NPs spherical shape with average sizes close to those analyzed by the DLS technique. Stability studies for the [AuCl(L 1 )]-PLGA-NPs pointed out that no significant changes in relation to size and PDI occur over almost 2 months of storage at 8 °C. The release of the complex from NPs was about 10% in 24 h, followed by a slow release. By means of the Korsmeyer-Peppas model, it was possible to identify the release mechanism as being through diffusion and relaxation of the polymeric matrix. Overall, it has been shown that the PLGA-NPs are promising carriers for delivery of [AuCl(L 1 )] and are recommended to be investigated as formulations for parasite treatment in vivo experiments. 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In this context, nanoparticles (NPs) of poly(lactic-co-glycolic acid) (PLGA) have been developed to be used as delivery systems for [AuCl(L 1 )]. The [AuCl(L 1 )]-PLGA-NPs were prepared via the emulsification and solvent evaporation technique and displayed encapsulation efficiency around 90% with the size range of 275 ± 5 nm, polydispersity index (PDI) around 0.115, and a higher value of zeta potential (− 6.51 ± 0.47 mV) compared to blank NPs (without gold complex), which agree with the formation of a cationic species in solution, as indicated by computational calculations. Additionally, high-resolution images obtained by SEM showed the [AuCl(L 1 )]-PLGA-NPs spherical shape with average sizes close to those analyzed by the DLS technique. Stability studies for the [AuCl(L 1 )]-PLGA-NPs pointed out that no significant changes in relation to size and PDI occur over almost 2 months of storage at 8 °C. The release of the complex from NPs was about 10% in 24 h, followed by a slow release. By means of the Korsmeyer-Peppas model, it was possible to identify the release mechanism as being through diffusion and relaxation of the polymeric matrix. Overall, it has been shown that the PLGA-NPs are promising carriers for delivery of [AuCl(L 1 )] and are recommended to be investigated as formulations for parasite treatment in vivo experiments. 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subjects Characterization and Evaluation of Materials
Chemistry and Materials Science
Computer applications
Controlled release
Emulsification
Evaporation
Glycolic acid
Gold
Image resolution
In vivo methods and tests
Inorganic Chemistry
Lasers
Materials Science
Nanoparticles
Nanotechnology
Optical Devices
Optics
Parasites
Photonics
Physical Chemistry
Polydispersity
Polylactide-co-glycolide
Research Paper
Stability analysis
Sustained release
Vector-borne diseases
Zeta potential
title Development of gold(III) thiosemicarbazonate complex–loaded PLGA nanoparticles: characterization and sustained release studies
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