1. Academic Validation
  2. Biodegradable poly(D,L-lactide-co-glycolide)/poly(L-γ-glutamic acid) nanoparticles conjugated to folic acid for targeted delivery of doxorubicin

Biodegradable poly(D,L-lactide-co-glycolide)/poly(L-γ-glutamic acid) nanoparticles conjugated to folic acid for targeted delivery of doxorubicin

  • Mater Sci Eng C Mater Biol Appl. 2017 Jul 1:76:743-751. doi: 10.1016/j.msec.2017.03.145.
Laura Jaimes-Aguirre 1 Enrique Morales-Avila 2 Blanca E Ocampo-García 3 Luis Alberto Medina 4 Gustavo López-Téllez 5 Brenda V Gibbens-Bandala 1 Vanessa Izquierdo-Sánchez 6
Affiliations

Affiliations

  • 1 Universidad Autónoma del Estado de México, Facultad de Química Toluca, Mexico.
  • 2 Universidad Autónoma del Estado de México, Facultad de Química Toluca, Mexico. Electronic address: [email protected].
  • 3 Instituto Nacional de Investigaciones Nucleares, Departamento de Materiales Reactivos Ocoyoacac, Mexico.
  • 4 Instituto de Física, Universidad Nacional Autónoma de México, Ciudad de México 04510, México; Mexico Unidad de Investigación Biomédica en Cáncer INCan/UNAM, Instituto Nacional de Cancerología, Ciudad de México 14080, México.
  • 5 Universidad Autónoma del Estado de Mexico, Centro Conjunto de Investigación en Química Sustentable UAEM/UNAM, Mexico.
  • 6 Instituto de Física, Universidad Nacional Autónoma de México, Ciudad de México 04510, México.
Abstract

A novel targeted drug delivery nanoparticle system based on poly(D,L-lactide-co-glycolide) acid (PLGA) for delivery of doxorubicin (DOX) was developed. DOX-PLGA NPs were obtained by the emulsification-solvent evaporation technique. Then, their surface was modified with poly(L-γ-glutamic acid) (γ-PGA) and finally conjugated to modified folic acid (FA) as a targeting ligand. The surface modification and FA conjugation were followed by UV-Vis and FT-IR spectroscopies. Morphology was observed by TEM/SEM. Particle size, PDI and zeta potential were measured using DLS studies. Encapsulation and loading efficiencies, and DOX release kinetics were determined. Specific uptake and cell viability of DOX-PLGA/γ-PGA-FA NPs were tested in HeLa cells. Quasi-spherical nanoparticles with a particle size lower than 600nm (DLS) were obtained. Spectroscopic techniques demonstrated the successful surface modification with γ-PGA and FA conjugation. Release profile of DOX-PLGA/γ-PGA-FA NPs showed a release of 55.4±0.6% after seven days, in an acidic environment. HeLa cells exhibited a decrease in viability when treated with DOX-PLGA/γ-PGA-AF NPs, and cellular uptake was attributed to FA receptor-mediated endocytosis. These results suggest that DOX-PLGA/γ-PGA-FA NPs are a potential targeted drug carrier for further applications in Cancer therapy.

Keywords

Folic acid; Multimeric FA nanoparticles; PLGA nanoparticles; Sustained-release system; Targeted drug delivery.

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