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Antitumoral activity of L-ascorbic acid-poly- D,L-(lactide-co-glycolide) nanoparticles containing violacein.

Martins D, Frungillo L, Anazzetti MC, Melo PS, Durán N - Int J Nanomedicine (2010)

Bottom Line: It has been demonstrated that tumoral cells have a higher uptake of ascorbic acid compared to normal cells.Violacein loading efficiency was determined as 32% +/- 1% and this drug was gradually released from nanoparticles at different rates depending on the composition of the release media.In addition, this system was observed to be 2 x more efficient as an antitumoral compared with free violacein.

View Article: PubMed Central - PubMed

Affiliation: Institute of Chemistry, Biological Chemistry Laboratory, Universidade Estadual de Campinas-UNICAMP, Campinas, SP, Brazil.

ABSTRACT
It has been demonstrated that tumoral cells have a higher uptake of ascorbic acid compared to normal cells. This differential characteristic can be used as a way to improve the specificity of antitumoral compounds if combined with polymeric drug delivery systems. The aim of this study was to prepare, characterize and evaluate the antitumoral activity of poly- D,L-(lactide-co-glycolide) 50:50 loading the antitumoral compound violacein and capped with L-ascorbic acid. Nanoparticles were prepared using the nanoprecipitation method and morphologically characterized by scanning electron microscopy (SEM). The average diameter and Zeta potential were determined by photon correlation spectroscopy method (PCS), and assays were carried out to determine the content of ascorbic acid and in vitro drug release kinetics. The antitumoral activity of this system was also evaluated against HL-60 cells by tetrazolium reduction assay. Nanoparticles with size distribution between 300-400 nm and strong negative outer surface (-40 mV) were obtained by this method. Analysis of ascorbic acid content showed that this compound was mainly localized on the external surface of nanoparticles. Violacein loading efficiency was determined as 32% +/- 1% and this drug was gradually released from nanoparticles at different rates depending on the composition of the release media. In addition, this system was observed to be 2 x more efficient as an antitumoral compared with free violacein.

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Release kinetics profile free or NP-AA-violacein in ethanol-buffer ethanol-buffer (A) or surfactant-buffer (B) solutions.Notes: (●) free violacein in ethanol-PBS solution; (○) NP-AA-violacein in ethanol-PBS solution; (▪) free violacein in Tween-PBS solution (□) NP-AA-violacein in Tween-PBS solution.Abbreviations: NP-AA, nanopatide-asconbic acid; PBS, Phosphate buffered saline.
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f3-ijn-5-077: Release kinetics profile free or NP-AA-violacein in ethanol-buffer ethanol-buffer (A) or surfactant-buffer (B) solutions.Notes: (●) free violacein in ethanol-PBS solution; (○) NP-AA-violacein in ethanol-PBS solution; (▪) free violacein in Tween-PBS solution (□) NP-AA-violacein in Tween-PBS solution.Abbreviations: NP-AA, nanopatide-asconbic acid; PBS, Phosphate buffered saline.

Mentions: No differences of the dissolution profile of free violacein in surfactant-buffer or ethanol-buffer solutions were observed (Figure 3). In terms of violacein release kinetics of nanoparticles, an initial burst of release in three hours of analysis was observed (about 40% and 60% for surfactant-buffer and ethanol- buffer solutions, respectively), followed by a gradual release until 36 hours and reaching a cumulative release of 80% of the initial content at 72 hours of analysis (Figure 3). Moreover, a significant difference was observed in the release kinetics profile of this system depending on the composition of the analysis solution. The release rates in ethanol-buffer media was observed to be faster compared to the surfactant-buffer solution.


Antitumoral activity of L-ascorbic acid-poly- D,L-(lactide-co-glycolide) nanoparticles containing violacein.

Martins D, Frungillo L, Anazzetti MC, Melo PS, Durán N - Int J Nanomedicine (2010)

Release kinetics profile free or NP-AA-violacein in ethanol-buffer ethanol-buffer (A) or surfactant-buffer (B) solutions.Notes: (●) free violacein in ethanol-PBS solution; (○) NP-AA-violacein in ethanol-PBS solution; (▪) free violacein in Tween-PBS solution (□) NP-AA-violacein in Tween-PBS solution.Abbreviations: NP-AA, nanopatide-asconbic acid; PBS, Phosphate buffered saline.
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Related In: Results  -  Collection

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getmorefigures.php?uid=PMC2819901&req=5

f3-ijn-5-077: Release kinetics profile free or NP-AA-violacein in ethanol-buffer ethanol-buffer (A) or surfactant-buffer (B) solutions.Notes: (●) free violacein in ethanol-PBS solution; (○) NP-AA-violacein in ethanol-PBS solution; (▪) free violacein in Tween-PBS solution (□) NP-AA-violacein in Tween-PBS solution.Abbreviations: NP-AA, nanopatide-asconbic acid; PBS, Phosphate buffered saline.
Mentions: No differences of the dissolution profile of free violacein in surfactant-buffer or ethanol-buffer solutions were observed (Figure 3). In terms of violacein release kinetics of nanoparticles, an initial burst of release in three hours of analysis was observed (about 40% and 60% for surfactant-buffer and ethanol- buffer solutions, respectively), followed by a gradual release until 36 hours and reaching a cumulative release of 80% of the initial content at 72 hours of analysis (Figure 3). Moreover, a significant difference was observed in the release kinetics profile of this system depending on the composition of the analysis solution. The release rates in ethanol-buffer media was observed to be faster compared to the surfactant-buffer solution.

Bottom Line: It has been demonstrated that tumoral cells have a higher uptake of ascorbic acid compared to normal cells.Violacein loading efficiency was determined as 32% +/- 1% and this drug was gradually released from nanoparticles at different rates depending on the composition of the release media.In addition, this system was observed to be 2 x more efficient as an antitumoral compared with free violacein.

View Article: PubMed Central - PubMed

Affiliation: Institute of Chemistry, Biological Chemistry Laboratory, Universidade Estadual de Campinas-UNICAMP, Campinas, SP, Brazil.

ABSTRACT
It has been demonstrated that tumoral cells have a higher uptake of ascorbic acid compared to normal cells. This differential characteristic can be used as a way to improve the specificity of antitumoral compounds if combined with polymeric drug delivery systems. The aim of this study was to prepare, characterize and evaluate the antitumoral activity of poly- D,L-(lactide-co-glycolide) 50:50 loading the antitumoral compound violacein and capped with L-ascorbic acid. Nanoparticles were prepared using the nanoprecipitation method and morphologically characterized by scanning electron microscopy (SEM). The average diameter and Zeta potential were determined by photon correlation spectroscopy method (PCS), and assays were carried out to determine the content of ascorbic acid and in vitro drug release kinetics. The antitumoral activity of this system was also evaluated against HL-60 cells by tetrazolium reduction assay. Nanoparticles with size distribution between 300-400 nm and strong negative outer surface (-40 mV) were obtained by this method. Analysis of ascorbic acid content showed that this compound was mainly localized on the external surface of nanoparticles. Violacein loading efficiency was determined as 32% +/- 1% and this drug was gradually released from nanoparticles at different rates depending on the composition of the release media. In addition, this system was observed to be 2 x more efficient as an antitumoral compared with free violacein.

Show MeSH