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Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/134979
Micelle carriers based on dendritic macromolecules containing bis-MPA and glycine for antimalarial drug delivery
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Abstract
Biomaterials for antimalarial drug transport still need
to be investigated in order to attain nanocarriers that can
tackle essential issues related to malaria treatment, e.g.
complying with size requirements and targeting specificity for
their entry into Plasmodium-infected red blood cells (pRBCs),
and limiting premature drug elimination or drug resistance
evolution. Two types of dendritic macromolecule that can form
vehicles suitable for antimalarial drug transport are herein
explored. A new hybrid dendritic-linear-dendritic block
copolymer based on Pluronic\xC2\xAE F127 and amino terminated
2,2'-bis(glycyloxymethyl)propionic acid dendrons with a
poly(ester amide) skeleton (HDLDBC-bGMPA) and an amino
terminated dendronized hyperbranched polymer with a polyester
skeleton derived from 2,2'-bis(hydroxymethyl)propionic acid
(DHP-bMPA) have provided self-assembled and unimolecular
micelles. Both types of micelle carrier are biocompatible and
exhibit appropriate sizes to enter into pRBCs. Targeting studies
have revealed different behaviors for each nanocarrier that may
open new perspectives for antimalarial therapeutic approaches.
Whereas DHP-bMPA exhibits a clear targeting specificity for
pRBCs, HDLDBC-bGMPA is incorporated by all erythrocytes. It has
also been observed that DHP-bMPA and HDLDBC-bGMPA incorporate
into human umbilical vein endothelial cells with different
subcellular localization, i.e. cytosolic and nuclear,
respectively. Drug loading capacity and encapsulation
efficiencies for the antimalarial compounds chloroquine,
primaquine and quinacrine ranging from 30% to 60% have been
determined for both carriers. The resulting drug-loaded
nanocarriers have been tested for their capacity to inhibit
Plasmodium growth in in vitro and in vivo assays.
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MARTÍ COMA-CROS, Elisabet, et al. Micelle carriers based on dendritic macromolecules containing
bis-MPA and glycine for antimalarial drug delivery. Biomaterials science. 2019. Vol. 7, num. 4, pags. 1661-1674. ISSN 2047-4830. [consulted: 11 of August of 2026]. Available at: https://hdl.handle.net/2445/134979