title: Nano-engineering of 5-fluorouracil-loaded magnetoliposomes for combined hyperthermia and chemotherapy against colon cancer.
abstract: The present investigation aimed to develop magnetoliposome nanoparticles loaded with 5-fluorouracil by following a reproducible thin film hydration technique. The physicochemical characterization (including electron microscopy analysis, dynamic light scattering, infrared spectrometry, X-ray diffractometry, electrophoresis, and surface thermodynamics) suggested that superparamagnetic magnetite nuclei were successfully embedded into a multilamellar lipid vesicle. Magnetic responsiveness of these nanocomposites was quantitatively analyzed by determining the hysteresis cycle and qualitatively confirmed by microscopic visualizations. A high frequency alternating electromagnetic field was further used to define their heating properties. The absence of cytotoxicity in human colon fibroblast CCD-18 and in human colon carcinoma T-84 cell lines and excellent hemocompatibility of these core/shell particles were demonstrated. Additionally, 5-fluorouracil incorporation was investigated by two procedures: (i) entrapment into the nanoparticulate matrix and (ii) surface deposition onto already formed magnetoliposome particles. The former method reported greater drug loading values and a sustained release profile. Interestingly, 5-fluorouracil release was also triggered by the heating properties of the nanoparticles (hyperthermia-triggered drug release). Hence, we put forward that magnetoliposome particles hold important properties, that is, magnetically targeted delivery, hyperthermia inducing capability, high 5-fluorouracil loading capability, and hyperthermia-triggered burst drug release, suggestive of their potential for a combined antitumor therapy against colon cancer.
authors.affiliation: Department of Pharmacy and Pharmaceutical Technology, University of Granada, Spain.
authors.forename: Beatriz
authors.initials: B
authors.lastname: Clares
authors.forename: Rafael A
authors.initials: RA
authors.lastname: Biedma-Ortiz
authors.forename: Eva
authors.initials: E
authors.lastname: Sáez-Fernández
authors.forename: José C
authors.initials: JC
authors.lastname: Prados
authors.forename: Consolación
authors.initials: C
authors.lastname: Melguizo
authors.forename: Laura
authors.initials: L
authors.lastname: Cabeza
authors.forename: Raúl
authors.initials: R
authors.lastname: Ortiz
authors.forename: José L
authors.initials: JL
authors.lastname: Arias
mesh_terms: D000328:Adult; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D003110:Colonic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D016503:Drug Delivery Systems; D055590:Electromagnetic Phenomena; D005260:Female; D005347:Fibroblasts / Q000187:drug effects / Q000378:metabolism; D005472:Fluorouracil / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006979:Hyperthermia, Induced / Q000379:methods; D008081:Liposomes; D008280:Magnetics; D058185:Magnetite Nanoparticles; D008875:Middle Aged
chemical_list: D000964:Antimetabolites, Antineoplastic; D003692:Delayed-Action Preparations; D008081:Liposomes; D058185:Magnetite Nanoparticles; D005472:Fluorouracil
keywords: 5-Fluorouracil; Colon cancer; Combined cancer therapy; Hyperthermia; Magnetic drug targeting; Magnetoliposome; Temperature-triggered drug release