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Electrospun Composite Nanofibers Based on PLA/Artesunate-loaded Citrate-functionalized Hydroxyapatite for Boosting in vitro Anticancer Efficacy and Drug Delivery of Artesunate

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Abstract

The development of a facile method for preparing electrospun artesunate-loaded inorganic/organic composite nanofiber drug delivery systems will significantly enhance the therapeutic applications of artesunate as a novel anticancer medication. Herein, artesunate- loaded citrate-functionalized hydroxyapatite nanorods (ART@Cit-HAp NRs) were prepared, and then encapsulated into PLA nanofibers (ART@Cit-HAp NRs/PLA composite nanofibers) via the electrospinning method. The produced Cit-HAp NRs, ART@Cit-HAp NRs and ART@Cit-HAp NRs/PLA composite nanofibers were characterized using a variety of comprehensive techniques. Electrospun PLA nanofibers have a smooth surface and a homogeneous diameter without any grains on the surface. The as-prepared citrate functionalized hydroxyapatite nanorods showed the high drug-loading efficiency of ∼92 %. The mechanism of pseudo-second-order adsorption is the most prominent model for ART adsorption on Cit-HAp NRs. The in vitro ART release from the composite nanofibers (ART@Cit-HAp NRs/PLA composite nanofibers) was investigated and compared to ART@Cit-HAp NRs under different pH conditions. The ART released from the ART@Cit-HAp NRs/PLA composite nanofibers in a sustained, slow rate was in contrast to Cit-HAp NRs and dependent on the pH of the medium. The in vitro antitumor activity of nanoformulations were evaluated on two colon cancer (CaCo-2 and HCT 116) cell lines. The findings revealed that ART@Cit-HAp NRs/PLA composite nanofibers demonstrated higher anti-proliferating activity compared to free ART, and the pH-triggered release of ART@Cit-HAp NRs/PLA composite nanofibers are interesting prospects for colon cancer treatment.

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Correspondence to Nehal Salahuddin or Maged El-Kemary.

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Salahuddin, N., Ibrahim, E.M. & El-Kemary, M. Electrospun Composite Nanofibers Based on PLA/Artesunate-loaded Citrate-functionalized Hydroxyapatite for Boosting in vitro Anticancer Efficacy and Drug Delivery of Artesunate. Fibers Polym 23, 3415–3426 (2022). https://doi.org/10.1007/s12221-022-4017-3

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