Evaluation of PEG-b-polycarbonates self-assemblies containing azobenzene or coumarin moieties as nanocarriers using paclitaxel as a model hydrophobic drug

Abstract

The work assesses the performance of nanocarriers from amphiphilic block copolymers with functional azobenzene or coumarin moieties for delivery of paclitaxel. Placlitaxel was encapsulated by the nanoprecipitation method. Characterisations were performed by DLS, TEM, Zeta potential and HPLC. Cell viability was investigated in HeLa and Huh-5-2-cell lines. Coumarin-containing polymeric micelles (D_h = 26 ± 2 nm, PDI = 0.28, ζ = ‒22.9 ± 3.6 mV) with 11.2 ± 0.5%w/w drug loading showed enhanced cytotoxicity in HeLa cells (IC50 < 0.02 nM) compared to free paclitaxel (IC50 = 0.17 ± 0.02 nM). Azobenzene-containing polymeric vesicles (D_h = 390 ± 20 nm, PDI = 0.24, ζ = ‒33.2 ± 5.0 mV) with a 6.8 ± 0.4%w/w drug loading showed increased cytotoxicity under 530 nm light (IC50 = 0.0114 ± 0.00033 nM) in HeLa cells due to a stimulated delivery of paclitaxel. Effectivity of these block copolymers as paclitaxel nanovectors and light stimulated release has been demonstrated.

Keywords:

• Block copolymers
• self-assembly
• nanocarriers
• drug loading
• paclitaxel
• light-stimulated

Acknowledgements

Authors would like to acknowledge the use of Servicio General de Apoyo a la Investigación-SAI, Universidad de Zaragoza and of Centro de Química y Materiales de Aragón-CEQMA, Universidad de Zaragoza-CSIC.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This research was funded by the Ministerio de Economía y Competitividad (MINECO)-FEDER, Spain, under the project grant number MAT2017-84838-P (L.O., M.P., Programa Excelencia), Fondo Social Europeo and Gobierno de Aragon-FEDER [E47_17R and B25_17R, FEDER 2014–2020 ‘Construyendo Europa desde Aragón’], Fondo de Investigaciones Sanitarias from Instituto de Salud Carlos III and European Union (ERDF/ESF, ‘Investing in your future’) [PI15/00663 and PI18/00349 to O.A.], Centro de Investigación Biomédica en Red en Enfermedades Hepáticas y Digestivas (CIBERehd) to O.A.