Development of electrosprayed artesunate-loaded core–shell nanoparticles

Abstract

Objective: Artesunate (ART) is proven to have potential anti-proliferative activities, but its instability and poor aqueous solubility limit its application as an anti-cancer drug. The present study was undertaken to develop coaxial electrospraying as a novel technique for fabricating nanoscale drug delivery systems of ART as the core–shell nanostructures.

Methods: The core–shell nanoparticles (NPs) were fabricated with coaxial electrospraying and the formation mechanisms of NPs were examined. The physical solid state and drug–polymer interactions of NPs were characterized by X-ray powder diffraction (XRPD) and Fourier transform infrared (FTIR) spectroscopy. The effects of materials and electrospraying process on the particle size and surface morphology of NPs were investigated by scanning electron microscopy (SEM). The drug release from NPs was determined in vitro by a dialysis method.

Results: The ART/poly(lactic-co-glycolic) acid (PLGA) chitosan (CS) NPs exhibited the mean particle size of 303 ± 93 nm and relatively high entrapment efficiency (80.5%). The release pattern showed an initial rapid release within two hours followed by very slow extended release. The release pattern approached the Korsmeyer–Peppas model.

Conclusions: The present results suggest that the core–shell NPs containing PLGA and CS have a potential as carriers in the anticancer drug therapy of ART.

Keywords:

• Artesunate
• chitosan
• coaxial electrospraying
• core–shell nanoparticles
• poly(lactic-co-glycolic) acid

Acknowledgements

The help of Dr. Urve Paaver and Dr. Martin Järvekülg (UT) for SEM measurement and analysis is highly appreciated. Dr. Jaan Aruväli and Prof. Kalle Kirsimäe are acknowledged for their help in conducting the XRPD experiments. Prof. Anne Kahru (National Institute of Chemical Physics and Biophysics) is thanked for providing facilities for zeta potential measurements.

Disclosure statement

The authors report no conflicts of interest.

Novelty statement: In the present study, coaxial electrospraying was used as a novel technique for fabricating core–shell nanoparticles and drug delivery systems of artesunate with a protective PLGA inner layer and functional CS outer layer.

Additional information

Funding

This research work was supported by the European Social Fund (for Doctoral Studies and Internationalisation Programme DoRa T5) [grant number 30.1-6/886], the Estonian Science Foundation [grant number ETF7980] and the Estonian Research Council [grant number IUT34-18]. The Ministry of Education and Research in Estonia is acknowledged for the financial support.