title: Engineering of Δ9-tetrahydrocannabinol delivery systems based on surface modified-PLGA nanoplatforms.
abstract: The objective of this work is to develop a nanoplatform that can potentiate the oral administration of Δ9-tetrahidrocannabinol, a highly lipophilic active agent with very promising antiproliferative and antiemetic activities. To that aim, colloidal carriers based on the biodegradable and biocompatible poly(D,L-lactide-co-glycolide) were investigated. Such delivery systems were prepared by nanoprecipitation, and nanoparticle engineering further involved surface modification with a poly(ethylene glycol), chitosan, or poly(ethylene glycol)-chitosan shells to assure the greatest uptake by intestinal cells and to minimize protein adsorption. Characterization of the nanoplatforms included particle geometry (size and shape), electrophoretic properties (surface charge). Δ9-tetrahydrocannabinol vehiculization capabilities (loading and release), blood compatibility, and cellular uptake and cytotoxicity. Results were satisfactorily used to define the optimum engineering conditions to formulate surface modified nanoparticles for the efficient oral administration of Δ9-tetrahydrocannabinol. To the best of our knowledge, this is the first time that biocompatible polymeric nanoparticles have been formulated for Δ9-tetrahydrocannabinoldelivery.
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/ Prof. García González, n°2, 41012 Sevilla, Spain. Electronic address: luciamartin@us.es.
authors.forename: Lucía
authors.initials: L
authors.lastname: Martín-Banderas
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/ Prof. García González, n°2, 41012 Sevilla, Spain.
authors.forename: Inmaculada
authors.initials: I
authors.lastname: Muñoz-Rubio
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/ Prof. García González, n°2, 41012 Sevilla, Spain.
authors.forename: Josefa
authors.initials: J
authors.lastname: Álvarez-Fuentes
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/ Prof. García González, n°2, 41012 Sevilla, Spain.
authors.forename: Matilde
authors.initials: M
authors.lastname: Durán-Lobato
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Granada, Campus Universitario de Cartuja, s/n, 18071 Granada, Spain.
authors.forename: José L
authors.initials: JL
authors.lastname: Arias
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/ Prof. García González, n°2, 41012 Sevilla, Spain.
authors.forename: Ma Ángeles
authors.initials: MÁ
authors.lastname: Holgado
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Sevilla, C/ Prof. García González, n°2, 41012 Sevilla, Spain.
authors.forename: Mercedes
authors.initials: M
authors.lastname: Fernández-Arévalo
mesh_terms: D048271:Chitosan / Q000737:chemistry; D013759:Dronabinol / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D004337:Drug Carriers; C118638:glycol-chitosan; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D013759:Dronabinol; D048271:Chitosan
keywords: Blood compatibility; Cannabinoids; Cellular uptake; Cytotoxicity; PLGA nanoparticles; Surface functionalization; Δ(9)-Tetrahydrocannabinol