Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization

Among the different ways to reduce the secondary effects of antineoplastic drugs in cancer treatment, the use of nanoparticles has demonstrated good results due to the protection of the drug and the possibility of releasing compounds to a specific therapeutic target. The α-isoform of the folate rece...

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Main Authors: Ana María Martínez-Relimpio, Marta Benito, Elena Pérez-Izquierdo, César Teijón, Rosa María Olmo, María Dolores Blanco
Format: Article
Language:English
Published: MDPI AG 2021-06-01
Series:Polymers
Subjects:
Online Access:https://www.mdpi.com/2073-4360/13/13/2083
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author Ana María Martínez-Relimpio
Marta Benito
Elena Pérez-Izquierdo
César Teijón
Rosa María Olmo
María Dolores Blanco
author_facet Ana María Martínez-Relimpio
Marta Benito
Elena Pérez-Izquierdo
César Teijón
Rosa María Olmo
María Dolores Blanco
author_sort Ana María Martínez-Relimpio
collection DOAJ
description Among the different ways to reduce the secondary effects of antineoplastic drugs in cancer treatment, the use of nanoparticles has demonstrated good results due to the protection of the drug and the possibility of releasing compounds to a specific therapeutic target. The α-isoform of the folate receptor (FR) is overexpressed on a significant number of human cancers; therefore, folate-targeted crosslinked nanoparticles based on BSA and alginate mixtures and loaded with paclitaxel (PTX) have been prepared to maximize the proven antineoplastic activity of the drug against solid tumors. Nanometric-range-sized particles (169 ± 28 nm–296 ± 57 nm), with negative Z-potential values (between −0.12 ± 0.04 and −94.1± 0.4), were synthesized, and the loaded PTX (2.63 ± 0.19–3.56 ±0.13 µg PTX/mg Np) was sustainably released for 23 and 27 h. Three cell lines (MCF-7, MDA-MB-231 and HeLa) were selected to test the efficacy of the folate-targeted PTX-loaded BSA/ALG nanocarriers. The presence of FR on the cell membrane led to a significantly larger uptake of BSA/ALG–Fol nanoparticles compared with the equivalent nanoparticles without folic acid on their surface. The cell viability results demonstrated a cytocompatibility of unloaded nanoparticle–Fol and a gradual decrease in cell viability after treatment with PTX-loaded nanoparticle–Fol due to the sustainable PTX release.
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spelling doaj.art-911c0909e0cd43f68a27aab79899ec182023-11-22T01:38:23ZengMDPI AGPolymers2073-43602021-06-011313208310.3390/polym13132083Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro CharacterizationAna María Martínez-Relimpio0Marta Benito1Elena Pérez-Izquierdo2César Teijón3Rosa María Olmo4María Dolores Blanco5Facultad de Ciencias Experimentales, Universidad Francisco de Vitoria, Pozuelo de Alarcón, 28223 Madrid, SpainFundación San Juan de Dios, Centro de Ciencias de la Salud San Rafael, Universidad de Nebrija, Paseo de La Habana, 70, 28036 Madrid, SpainDepartment of Health Sciences, Faculty of Biomedical and Health Sciences, Universidad Europea de Madrid, Urbanización El Bosque, Calle Tajo, s/n, 28670 Villaviciosa de Odón, SpainNursing Department, Faculty of Nursing, Physiotherapy and Podiatry, Universidad Complutense de Madrid, 28040 Madrid, SpainDepartment of Biochemistry and Molecular Biology, Faculty of Medicine, Universidad Complutense de Madrid, 28040 Madrid, SpainDepartment of Biochemistry and Molecular Biology, Faculty of Medicine, Universidad Complutense de Madrid, 28040 Madrid, SpainAmong the different ways to reduce the secondary effects of antineoplastic drugs in cancer treatment, the use of nanoparticles has demonstrated good results due to the protection of the drug and the possibility of releasing compounds to a specific therapeutic target. The α-isoform of the folate receptor (FR) is overexpressed on a significant number of human cancers; therefore, folate-targeted crosslinked nanoparticles based on BSA and alginate mixtures and loaded with paclitaxel (PTX) have been prepared to maximize the proven antineoplastic activity of the drug against solid tumors. Nanometric-range-sized particles (169 ± 28 nm–296 ± 57 nm), with negative Z-potential values (between −0.12 ± 0.04 and −94.1± 0.4), were synthesized, and the loaded PTX (2.63 ± 0.19–3.56 ±0.13 µg PTX/mg Np) was sustainably released for 23 and 27 h. Three cell lines (MCF-7, MDA-MB-231 and HeLa) were selected to test the efficacy of the folate-targeted PTX-loaded BSA/ALG nanocarriers. The presence of FR on the cell membrane led to a significantly larger uptake of BSA/ALG–Fol nanoparticles compared with the equivalent nanoparticles without folic acid on their surface. The cell viability results demonstrated a cytocompatibility of unloaded nanoparticle–Fol and a gradual decrease in cell viability after treatment with PTX-loaded nanoparticle–Fol due to the sustainable PTX release.https://www.mdpi.com/2073-4360/13/13/2083folate-targeted nanoparticlesBSA/alginate nanocarrierspaclitaxelcellular uptakecell viability
spellingShingle Ana María Martínez-Relimpio
Marta Benito
Elena Pérez-Izquierdo
César Teijón
Rosa María Olmo
María Dolores Blanco
Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization
Polymers
folate-targeted nanoparticles
BSA/alginate nanocarriers
paclitaxel
cellular uptake
cell viability
title Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization
title_full Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization
title_fullStr Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization
title_full_unstemmed Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization
title_short Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization
title_sort paclitaxel loaded folate targeted albumin alginate nanoparticles crosslinked with ethylenediamine synthesis and in vitro characterization
topic folate-targeted nanoparticles
BSA/alginate nanocarriers
paclitaxel
cellular uptake
cell viability
url https://www.mdpi.com/2073-4360/13/13/2083
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