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

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 × more efficient as an antitumoral compared with free violacein.

Antitumor activity of silver nanoparticles in Dalton’s lymphoma ascites tumor model

“…Compounds possessing antiangiogenic properties are known for their potential ability to block the activity of abnormally expressed signaling proteins, such as Ras and Akt, cytokine-based therapies, DNA-or proteinbased vaccines against specific tumor markers, and tyrosine kinase inhibitors which exhibit a consistent antitumor effect. 33 In this study, AgNPs of size 50 nm at a concentration of 500 nM had cytotoxic effects on DLA tumor cells under in vitro conditions as well as in an in vivo tumor model.…”

Bactericidal Application and Cytotoxic Activity of Biosynthesized Silver Nanoparticles with an Extract of the Red Seaweed Pterocladiella capillacea on the HepG2Cell Line

“…Devi and Valentin Bhimba (2012) reported that the cytotoxic effect is inversely proportional to the size of AgNPs. Martins et al (2010) explained that the cytotoxic effect of silver is the result of active physicochemical interaction of silver atoms with the functional groups of intracellular proteins as well as with the nitrogen bases and phosphate groups in DNA. Sriram et al (2010) demonstrated that AgNPs serve as antitumor agents by decreasing progressive development of tumor cells.…”

Potential applications of violacein: a microbial pigment

“…Ascorbic acid was used since tumor cells have a higher uptake of this acid compared to normal cells. The antitumoral activity of this system was twofold more efficient against HL60 cells compared with free violacein (Martins et al, 2010b).…”