title: PEGylated versus non-PEGylated magnetic nanoparticles as camptothecin delivery system.
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.
authors.affiliation: INSTM and Dipartimento di Scienze Chimiche e Geologiche. Università di Cagliari, Italy ; Departamento de Sistemas Físicos, Químicos y Naturales. Universidad Pablo de Olavide, Sevilla, Spain.
authors.forename: Paula M
authors.initials: PM
authors.lastname: Castillo
authors.affiliation: Centro Andaluz de Biología del Desarrollo (CABD-CSIC-Universidad Pablo de Olavide), Sevilla, Spain.
authors.forename: Mario
authors.initials: M
authors.lastname: de la Mata
authors.affiliation: INSTM and Dipartimento di Scienze Chimiche e Geologiche. Università di Cagliari, Italy.
authors.forename: Maria F
authors.initials: MF
authors.lastname: Casula
authors.affiliation: Centro Andaluz de Biología del Desarrollo (CABD-CSIC-Universidad Pablo de Olavide), Sevilla, Spain.
authors.forename: José A
authors.initials: JA
authors.lastname: Sánchez-Alcázar
authors.affiliation: Departamento de Sistemas Físicos, Químicos y Naturales. Universidad Pablo de Olavide, Sevilla, Spain.
authors.forename: Ana P
authors.initials: AP
authors.lastname: Zaderenko
keywords: camptothecin; cancer therapy; iron oxide superparamagnetic nanoparticles; polyethylene glycol