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Effect of PEGylation on Ligand-Targeted Magnetoliposomes: A Missed Goal

Estelrich, Joan, Busquets, Maria Antònia, del Carmen Morán, María·2017·ACS Omega
DOI 10.1021/acsomega.7b00778PMC PMC6044770
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Abstract

We tested the targeting efficiency of magnetoliposomes (MLPs) labeled with tripeptide arginine-glycine-aspartic acid (RGD) on two types of cells: HeLa cells expressing RGD receptors and 3T3 cells lacking RGD receptors. The targeting ability of RGD-MLPs was compared to that of bare MLPs and MLPs stabilized with poly(ethylene glycol) (PEG). Cellular internalization of these liposomes was determined by flow cytometry and confocal microscopy, which showed that both types of cells took up more nontargeting MLPs than targeting RGD-MLPs or PEG-MLPs, with PEG-MLPs showing the lowest degree of internalization. The presence of specific receptors on HeLa cells did not facilitate the binding of RGD-MLPs, probably due to the presence of PEG chains on the liposomal surface. The polymer increases the circulation time of the liposomes in the organism but reduces their interactions with cells. Despite the localization of the RGD peptide on the tip of PEG in RGD-MLPs, the interaction between the liposome and cell was still limited. To avoid this drawback, targeting drug delivery systems can be prepared with two types of PEG: one of a short length to enable biocompatibility and the other of a longer chain to carry the ligand.

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Metadata

Authors
Estelrich, J., Busquets, M. A., & del Carmen Morán, M.
Affiliations
Universitat de Barcelona , ; Avda. Joan XXIII, 27-31 , , Catalonia,
ORCID
Busquets, Maria Antònia
Venue
ACS Omega
Publisher
American Chemical Society (ACS)
Published
2017-10-09
Volume
2
Issue
10
Pages
6544-6555
ISSN
2470-1343
DOI
10.1021/acsomega.7b00778
PMC
PMC6044770
Cited by
17
References
1
Language
en
Licence
pubs.acs.org/page/policy/authorchoice_termsofuse.html (vor)
Funders
Generalitat de Catalunya (2014SGR227)

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