# name
ImmunoPEGliposomes for the targeted delivery of novel lipophilic
                drugs to red blood cells in a falciparum malaria murine model

# metadata.dc.description.abstract[].value
Most drugs currently entering the clinical pipeline for severe
                malaria therapeutics are of lipophilic nature, with a relatively
                poor solubility in plasma and large biodistribution volumes. Low
                amounts of these compounds do consequently accumulate in
                circulating Plasmodium-infected red blood cells, exhibiting
                limited antiparasitic activity. These drawbacks can in principle
                be satisfactorily dealt with by stably encapsulating drugs in
                targeted nanocarriers. Here this approach has been adapted for
                its use in immunocompetent mice infected by the Plasmodium
                yoelii 17XL lethal strain, selected as a model for human blood
                infections by Plasmodium falciparum. Using immunoliposomes
                targeted against a surface protein characteristic of the murine
                erythroid lineage, the protocol has been applied to two novel
                antimalarial lipophilic drug candidates, an aminoquinoline and
                an aminoalcohol. Large encapsulation yields of >90% were
                obtained using a citrate-buffered pH gradient method and the
                resulting immunoliposomes reached in vivo erythrocyte targeting
                and retention efficacies of >80%. In P. yoelii-infected mice,
                the immunoliposomized aminoquinoline succeeded in decreasing
                blood parasitemia from severe to uncomplicated malaria parasite
                densities (i.e. from >/=25% to ca. 5%), whereas the same
                amount of drug encapsulated in non-targeted liposomes had no
                significant effect on parasite growth. Pharmacokinetic analysis
                indicated that this good performance was obtained with a rapid
                clearance of immunoliposomes from the circulation (blood
                half-life of ca. 2 h), suggesting a potential for improvement of
                the proposed model.

# metadata.dc.relation.isformatof[].value
Reproducció del document publicat a:
                http://dx.doi.org/10.1016/j.biomaterials.2017.08.020

# metadata.dc.source[].value
Articles publicats en revistes (ISGlobal)

# metadata.dc.title[].value
ImmunoPEGliposomes for the targeted delivery of novel lipophilic
                drugs to red blood cells in a falciparum malaria murine model