Abstract
Camptothecin (CPT; (S)-(+)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-(4H,12H)-dione) is a highly cytotoxic natural alkaloid that has not yet found use as chemotherapeutic agent due to its poor water-solubility and chemical instability and, as a consequence, no effective administration means have been designed. In this work, camptothecin has been successfully loaded into iron oxide superparamagnetic nanoparticles with an average size of 14 nm. It was found that surface modification of the nanoparticles by polyethylene glycol enables loading a large amount of camptothecin. While the unloaded nanoparticles do not induce apoptosis in the H460 lung cancer cell line, the camptothecin-loaded nanoparticle formulations exhibit remarkable pro-apoptotic activity. These results indicate that camptothecin retains its biological activity after loading onto the magnetic nanoparticles. The proposed materials represent novel materials based on naturally occurring bioactive molecules loaded onto nanoparticles to be used as chemotherapeutic formulations. The procedure seems apt to be extended to other active molecules extracted from natural products. In addition, these materials offer the potential of being further implemented for combined imaging and therapeutics, as magnetic nanoparticles are known to be multifunctional tools for biomedicine.
Highlights
Camptothecin (CPT) is a quinoline based alkaloid, which exhibits a potent cytotoxic activity against a broad spectrum of tumours [1,2,3]
Superparamagnetic iron oxide nanoparticles (SPION) can be effectively used as contrast agents for magnetic resonance imaging [24,25], as carriers for chemotherapeutic drugs [26,27,28] and to destroy cancer cells by acting as heat mediators in hyperthermia treatments [29,30,31]
Few attempts to develop CPT-delivery systems based on SPION have been reported [32,33,34], and none of them examine their ability to adsorb CPT, nor takes advantage of the Further insights into the crystalline structure were obtained from X-ray diffraction (XRD) patterns
Summary
Camptothecin (CPT) is a quinoline based alkaloid, which exhibits a potent cytotoxic activity against a broad spectrum of tumours [1,2,3]. We report a simple method to synthesise PEG-coated ultrasmall magnetite (USM) nanoparticles, and we examine the ability of both, bare and PEGylated USM nanoparticles, to conjugate CPT.
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