LDL-conjugated to GM1 micelles incorporating anticancer drugs to improve tumor cell uptake

Objective(s): The role of lipoproteins (LDL) as active molecules with preferential tumor interaction, but limited drug delivery capacity, has been previously reported. On the other hand, in a previous report, we demonstrated the high capacity of monosialogangliosides (GM1) micelles as drug transport...

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Main Authors: Ariel Gustavo Garro, Roxana Valeria Alasino, Victoria Leonhard, Valeria Heredia, Dante Miguel Beltramo
Format: Article
Language:English
Published: Mashhad University of Medical Sciences 2021-04-01
Series:Nanomedicine Journal
Subjects:
Online Access:https://nmj.mums.ac.ir/article_17560_287fbe222676e43be5a9c85a85d09ec6.pdf
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author Ariel Gustavo Garro
Roxana Valeria Alasino
Victoria Leonhard
Valeria Heredia
Dante Miguel Beltramo
author_facet Ariel Gustavo Garro
Roxana Valeria Alasino
Victoria Leonhard
Valeria Heredia
Dante Miguel Beltramo
author_sort Ariel Gustavo Garro
collection DOAJ
description Objective(s): The role of lipoproteins (LDL) as active molecules with preferential tumor interaction, but limited drug delivery capacity, has been previously reported. On the other hand, in a previous report, we demonstrated the high capacity of monosialogangliosides (GM1) micelles as drug transporters. Materials and Methods: In this work, GM1 was loaded with high doses of oncologic drugs such Paclitaxel or Doxorubicin and binded to LDL lipoproteins to form GM1-drug-LDLwater soluble complex. Evidence suggests that both, hydrophobic and electrostatic forces, participate in the interaction, regulated by conditions such as pH, temperature and ionic strength.Results: Results of DLS and TEM show that GM1-LDL complexes are considerably larger than the sum of their individual compounds, with a high charge of electronegative surface (-55.9 mV). In addition, the cytotoxic effect on cell cultures is greater when drugs are contained in GM1-LDL complexes than when loaded in GM1 micelles. Conclusion: The results suggest the participation of active energy-dependent mechanism in the uptake of GM1-LDL drug, probably linked to the LDL receptor by the tumor cells. However, we could not confirm that the transport through LDL receptors is the only one that participates in the cellular uptake of the micelles.
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spelling doaj.art-caaf12954e1d402dbf2853a194de1cf22022-12-21T23:26:51ZengMashhad University of Medical SciencesNanomedicine Journal2322-30492322-59042021-04-018210611610.22038/nmj.2021.08.00317560LDL-conjugated to GM1 micelles incorporating anticancer drugs to improve tumor cell uptakeAriel Gustavo Garro0Roxana Valeria Alasino1Victoria Leonhard2Valeria Heredia3Dante Miguel Beltramo4Centro de Excelencia en Productos y Procesos de Córdoba (CEPROCOR), Córdoba, ArgentinaCentro de Excelencia en Productos y Procesos de Córdoba (CEPROCOR), Córdoba, ArgentinaCentro de Excelencia en Productos y Procesos de Córdoba (CEPROCOR), Córdoba, ArgentinaCentro de Excelencia en Productos y Procesos de Córdoba (CEPROCOR), Córdoba, ArgentinaCentro de Excelencia en Productos y Procesos de Córdoba (CEPROCOR), Córdoba, ArgentinaObjective(s): The role of lipoproteins (LDL) as active molecules with preferential tumor interaction, but limited drug delivery capacity, has been previously reported. On the other hand, in a previous report, we demonstrated the high capacity of monosialogangliosides (GM1) micelles as drug transporters. Materials and Methods: In this work, GM1 was loaded with high doses of oncologic drugs such Paclitaxel or Doxorubicin and binded to LDL lipoproteins to form GM1-drug-LDLwater soluble complex. Evidence suggests that both, hydrophobic and electrostatic forces, participate in the interaction, regulated by conditions such as pH, temperature and ionic strength.Results: Results of DLS and TEM show that GM1-LDL complexes are considerably larger than the sum of their individual compounds, with a high charge of electronegative surface (-55.9 mV). In addition, the cytotoxic effect on cell cultures is greater when drugs are contained in GM1-LDL complexes than when loaded in GM1 micelles. Conclusion: The results suggest the participation of active energy-dependent mechanism in the uptake of GM1-LDL drug, probably linked to the LDL receptor by the tumor cells. However, we could not confirm that the transport through LDL receptors is the only one that participates in the cellular uptake of the micelles.https://nmj.mums.ac.ir/article_17560_287fbe222676e43be5a9c85a85d09ec6.pdfgm1-ldlmicellesnanodeliveryoncological drugslipoproteins
spellingShingle Ariel Gustavo Garro
Roxana Valeria Alasino
Victoria Leonhard
Valeria Heredia
Dante Miguel Beltramo
LDL-conjugated to GM1 micelles incorporating anticancer drugs to improve tumor cell uptake
Nanomedicine Journal
gm1-ldl
micelles
nanodelivery
oncological drugs
lipoproteins
title LDL-conjugated to GM1 micelles incorporating anticancer drugs to improve tumor cell uptake
title_full LDL-conjugated to GM1 micelles incorporating anticancer drugs to improve tumor cell uptake
title_fullStr LDL-conjugated to GM1 micelles incorporating anticancer drugs to improve tumor cell uptake
title_full_unstemmed LDL-conjugated to GM1 micelles incorporating anticancer drugs to improve tumor cell uptake
title_short LDL-conjugated to GM1 micelles incorporating anticancer drugs to improve tumor cell uptake
title_sort ldl conjugated to gm1 micelles incorporating anticancer drugs to improve tumor cell uptake
topic gm1-ldl
micelles
nanodelivery
oncological drugs
lipoproteins
url https://nmj.mums.ac.ir/article_17560_287fbe222676e43be5a9c85a85d09ec6.pdf
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