title: Pegylated Polyaspartamide-Polylactide-Based Nanoparticles Penetrating Cystic Fibrosis Artificial Mucus.
abstract: Here, the preparation of mucus-penetrating nanoparticles for pulmonary administration of ibuprofen in patients with cystic fibrosis is described. A fluorescent derivative of α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide is synthesized by derivatization with rhodamine, polylactide, and poly(ethylene glycol), to obtain polyaspartamide-polylactide derivatives with different degrees of pegylation. Starting from these copolymers, fluorescent nanoparticles with different poly(ethylene glycol) content, empty and loaded with ibuprofen, showed spherical shape, colloidal size, slightly negative ζ potential, and biocompatibility toward human bronchial epithelial cells. The high surface poly(ethylene glycol) density of fluorescent nanoparticles and poly(ethylene glycol) brush-like conformation assumed on their surface, conferred to pegylated nanoparticles the mucus-penetrating properties, properly demonstrated by assessing their ability to avoid interactions with mucus components and to penetrate cystic fibrosis artificial mucus. Finally, ibuprofen release profile and uptake capacity within human bronchial epithelial cells in the presence of cystic fibrosis artificial mucus showed how these mucus-penetrating nanoparticles could rapidly diffuse through the mucus barrier reaching the mucosal surface, where they could offer a sustained delivery of ibuprofen at the site of disease.
authors: Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università di Palermo , Via Archirafi 32, 90123 Palermo, Italy.
authors: Emanuela Fabiola
authors: EF
authors: Craparo
authors: Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università di Palermo , Via Archirafi 32, 90123 Palermo, Italy.
authors: Barbara
authors: B
authors: Porsio
authors: Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università di Palermo , Via Archirafi 32, 90123 Palermo, Italy.
authors: Carla
authors: C
authors: Sardo
authors: Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università di Palermo , Via Archirafi 32, 90123 Palermo, Italy.
authors: Gaetano
authors: G
authors: Giammona
authors: Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università di Palermo , Via Archirafi 32, 90123 Palermo, Italy.
authors: Gennara
authors: G
authors: Cavallaro
mesh_terms: D002460:Cell Line; D003550:Cystic Fibrosis / Q000378:metabolism; D006801:Humans; D007052:Ibuprofen / Q000008:administration & dosage; D009093:Mucus / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry / Q000378:metabolism*; D010455:Peptides / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D020545:Respiratory Mucosa / Q000187:drug effects / Q000378:metabolism*
chemical_list: D010455:Peptides; D011091:Polyesters; C017645:polyaspartate; D011092:Polyethylene Glycols; C033616:poly(lactide); D007052:Ibuprofen