title: Tamoxifen-loaded nanoparticles based on a novel mixture of biodegradable polyesters: characterization and in vitro evaluation as sustained release systems.
abstract: Nanoparticles (NP) from mixtures of two poly(D,L-lactide-co-caprolactone) (PLC) copolymers, PLC 40/60 and PLC 86/14, with poly(D,L-lactide) (PDLLA) and PCL were prepared: PLC 40/60-PCL (25:75), PLC 86/14-PCL (75:25) and PLC 86/14-PLA (75:25). Tamoxifen was loaded with encapsulation efficiency between 65% and 75% (29.9-36.3 µg TMX/ mg NP). All selected systems showed spherical shape and nano-scale size. TMX-loaded NPs were in the range of 293-352 nm. TMX release from NP took place with different profiles depending on polymeric composition of the particles. After 60 days, 59.81% and 82.65% of the loaded drug was released. The cytotoxicity of unloaded NP in MCF7 and HeLa cells was very low. Cell uptake of NP took place in both cell types by unspecific internalization in a time dependent process. The administration of 6 and 10 µm TMX by TMX-loaded NP was effective on both cellular types, mainly in MCF7 cells.
authors.affiliation: Polymeric Materials Group for the Controlled Release of Bioactive Compounds in Biomedicine, Departamento de Bioquímica y Biología Molecular, Facultad de Medicina, Universidad Complutense de Madrid, Madrid-28040, Spain.
authors.forename: Elena
authors.initials: E
authors.lastname: Pérez
authors.forename: Marta
authors.initials: M
authors.lastname: Benito
authors.forename: César
authors.initials: C
authors.lastname: Teijón
authors.forename: Rosa
authors.initials: R
authors.lastname: Olmo
authors.forename: José M
authors.initials: JM
authors.lastname: Teijón
authors.forename: M Dolores
authors.initials: MD
authors.lastname: Blanco
mesh_terms: D018931:Antineoplastic Agents, Hormonal / Q000008:administration & dosage; D001672:Biocompatible Materials / Q000737:chemistry; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems; D005260:Female; D006367:HeLa Cells; D006801:Humans; D008422:Materials Testing; D008855:Microscopy, Electron, Scanning; D053769:Nanocapsules / Q000737:chemistry / Q000648:ultrastructure; D036103:Nanotechnology; D011091:Polyesters / Q000737:chemistry; D013629:Tamoxifen / Q000008:administration & dosage*
chemical_list: D018931:Antineoplastic Agents, Hormonal; D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D053769:Nanocapsules; D011091:Polyesters; D013629:Tamoxifen; C062968:lactide-caprolactone copolymer