Heparin-coated dendronized hyperbranched polymers for antimalarial targeted delivery

San Anselmo, María ; Lantero, Elena ; Avalos-Padilla, Yunuen ; Bouzón-Arnáiz, Inés ; Ramírez, Miriam ; Postigo, Alejandro (Universidad de Zaragoza) ; Serrano, José Luis (Universidad de Zaragoza) ; Sierra, Teresa ; Hernández-Ainsa, Silvia (Universidad de Zaragoza) ; Fernàndez-Busquets, Xavier

Resumen: The rampant evolution of resistance in Plasmodium to all existing antimalarial drugs calls for the development of improved therapeutic compounds and of adequate targeted delivery strategies for them. Loading antimalarials in nanocarriers specifically targeted to the parasite will contribute to the administration of lower overall doses, with reduced side effects for the patient, and of higher local amounts to parasitized cells for an increased lethality toward the pathogen. Here, we report the development of dendronized hyperbranched polymers (DHPs), with capacity for antimalarial loading, that are coated with heparin for their specific targeting to red blood cells parasitized by Plasmodium falciparum. The resulting DHP–heparin complexes exhibit the intrinsic antimalarial activity of heparin, with an IC50 of ca. 400 nM, added to its specific targeting to P. falciparum-infected (vs noninfected) erythrocytes. DHP–heparin nanocarriers represent a potentially interesting contribution to the limited family of structures described so far for the loading and targeted delivery of current and future antimalarial compounds.

Idioma: Inglés

DOI: 10.1021/acsapm.2c01553

Año: 2022

Publicado en: ACS applied polymer materials 5, 1 (2022), 381-390
ISSN: 2637-6105

Factor impacto JCR: 5.0 (2022)

Categ. JCR: POLYMER SCIENCE rank: 16 / 85 = 0.188 (2022) - Q1 - T1
Categ. JCR: MATERIALS SCIENCE, MULTIDISCIPLINARY rank: 117 / 343 = 0.341 (2022) - Q2 - T2

Factor impacto CITESCORE: 6.7 - Materials Science (Q1) - Chemistry (Q1) - Chemical Engineering (Q2)

Factor impacto SCIMAGO: 0.999 - Organic Chemistry (Q1) - Process Chemistry and Technology (Q1) - Polymers and Plastics (Q1)

Financiación: info:eu-repo/grantAgreement/ES/DGA-FSE/E47-20R
Financiación: info:eu-repo/grantAgreement/ES/MCIU/BES-2016-078774
Financiación: info:eu-repo/grantAgreement/ES/MCIU-FEDER/RTI2018-094579-B-I00
Financiación: info:eu-repo/grantAgreement/ES/MICINN/CEX2018-000806-S
Financiación: info:eu-repo/grantAgreement/ES/MICINN/PID2021-126132NB-I00

Tipo y forma: Artículo (Versión definitiva)

Área (Departamento): Área Química Orgánica (Dpto. Química Orgánica)