Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2021 Jun 24;13(13):2083.
doi: 10.3390/polym13132083.

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

Ana María Martínez-Relimpio  1 , Marta Benito  2 , Elena Pérez-Izquierdo  3 , César Teijón  4 , Rosa María Olmo  5 , María Dolores Blanco  5
Affiliations

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

Ana María Martínez-Relimpio et al. Polymers (Basel). .

Abstract

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.

Keywords: BSA/alginate nanocarriers; cell viability; cellular uptake; folate-targeted nanoparticles; paclitaxel.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
TEM micrographs of 30BSA/70ALG (A), 30BSA/70ALG–Fol (B), PTX-loaded 30BSA/70ALG–Fol (C), 50BSA/50ALG (D), 50BSA/50ALG–Fol (E) and PTX-loaded 50BSA/50ALG–Fol (F) nanoparticles.
Figure 2
Figure 2
Cumulative release of PTX from BSA/ALG–Fol nanoparticles.
Figure 3
Figure 3
Quantitative comparison of coumarin-loaded internalized nanoparticles in (a) MCF-7, (b) MDA-MB-231 and (c) HeLa cells. Fluorescence microscopy images of coumarin-loaded internalized nanoparticles 50BSA/50ALG–Fol into MCF-7 (d), MDA-MB-231 (e) and HeLa (f) after 4 h of incubation.
Figure 4
Figure 4
Cell viability of MCF-7, MDA-MB-231 and HeLa cells in the presence of paclitaxel (PTX) in solution and PTX-loaded nanoparticles.
See this image and copyright information in PMC

References

    1. Shah A., Aftab S., Nisar J., Ashiq M.N., Iftikhar F.J. Nanocarriers for targeted drug delivery. J. Drug Deliv. Sci. Technol. 2021;62:102426. doi: 10.1016/j.jddst.2021.102426. - DOI
    1. Barclay T.G., Day C.M., Petrovsky N., Garg S. Review of polysaccharide particle-based functional drug delivery. Carbohydr. Polym. 2019;221:94–112. doi: 10.1016/j.carbpol.2019.05.067. - DOI - PMC - PubMed
    1. Zhang E., Xing R., Liu S., Qin Y., Li K., Li P. Advances in chitosan-based nanoparticles for oncotherapy. Carbohydr. Polym. 2019;222:115004. doi: 10.1016/j.carbpol.2019.115004. - DOI - PubMed
    1. Martínez A.M., Benito M., Pérez E., Teijón J.M., Blanco M.D. The role of anionic polysaccharides in the preparation of nanomedicines with anticancer applications. Curr. Pharm. Des. 2016;22:3364–3379. doi: 10.2174/1381612822666160128145125. - DOI - PubMed
    1. Martínez A., Pérez E., Montero N., Teijón C., Olmo R., Blanco M.D. Alginate-based drug carriers: Recent advances. In: Moore A., editor. Alginic Acid: Chemical Structure, Uses and Health Benefits. Nova Science Publishers, Inc.; Hauppauge, NY, USA: 2015. pp. 15–43.

LinkOut - more resources