Preparation, characterization, and cytotoxicity of CPT/Fe₂O₃-embedded PLGA ultrafine composite fibers: a synergistic approach to develop promising anticancer material

Touseef Amna¹, M Shamshi Hassan², Ki-Taek Nam², Yang You Bing³, Nasser AM Barakat², Myung-Seob Khil², Hak Yong Kim<sup>1,2

1</sup>Center for Healthcare Technology Development, ²Department of Organic Materials and Fiber Engineering, Chonbuk National University, Jeonju, Korea; ³Animal Science and Technology College, Henan University of Science and Technology, Luoyang, China

Abstract: The aim of this study was to fabricate camptothecin/iron(III) oxide (CPT/Fe₂O₃)-loaded poly(D,L-lactide-co-glycolide) (PLGA) composite mats to modulate the CPT release and to improve the structural integrity and antitumor activity of the released drug. The CPT/ Fe₂O₃-loaded PLGA ultrafine fibers were prepared for the first time by electrospinning a composite solution of CPT/Fe₂O₃ and neat PLGA (4 weight percent). The physicochemical characterization of the electrospun composite mat was carried out by scanning electron microscopy, energy dispersive X-ray spectroscopy, electron probe microanalysis, thermogravimetry, transmission electron microscopy, ultraviolet-visible spectroscopy, and X-ray diffraction pattern. The medicated composite fibers were evaluated for their cytotoxicity on C2C12 cells using Cell Counting Kit-8 assay (Sigma-Aldrich Corporation, St Louis, MO). The in vitro studies indicated a slow and prolonged release over a period of 96 hours with mild initial burst. Scanning electron microscopy, thermogravimetry, and X-ray diffraction studies confirmed the interaction of CPT/Fe₂O₃ with the PLGA matrix and showed that the crystallinity of CPT decreased after loading. Incorporation of CPT in the polymer media affected both the morphology and the size of the CPT/Fe₂O₃-loaded PLGA composite fibers. Electron probe microanalysis and energy dispersive X-ray spectroscopy results confirmed well-oriented composite ultrafine fibers with good incorporation of CPT/Fe₂O₃. The cytotoxicity results illustrate that the pristine PLGA did not exhibit noteworthy cytotoxicity; conversely, the CPT/Fe₂O₃ composite fibers inhibited C2C12 cells significantly. Thus, the current work demonstrates that the CPT/Fe₂O₃-loaded PLGA composite fibers represent a promising chemotherapeutic system for enhancing anticancer drug efficacy and selectively targeting cancer cells in order to treat diverse cancers.

Keywords: camptothecin, C2C12 cells, Fe₂O₃ nanoparticles, electrospinning, cytotoxicity