title: Polymeric drug delivery micelle-like nanocarriers for pulmonary administration of beclomethasone dipropionate.
abstract: In this paper, the potential of novel polymeric micelles as drug delivery systems for Beclomethasone Dipropionate (BDP) administration into the lung is investigated. These nanostructures are obtained starting from α,β-poly(N-2-hydroxyethyl)-d,l-aspartamide (PHEA), which was subsequently functionalized with O-(2-aminoethyl)-O'-methylpolyethylenglycole (PEG2000), ethylenediamine (EDA) and lipoic acid (LA), obtaining PHEA-PEG2000-EDA-LA graft copolymer. Empty and drug-loaded micelles possess adequate chemical-physical characteristics for pulmonary administration such as spherical shape, slightly positive surface charge and mean size of about 200nm. Besides, BDP-loaded micelles, obtained with a Drug Loading equal to 5wt%, result to be stable in physiological-mimicking media, protecting the drug from hydrolysis and giving a sustained drug release profile. Moreover, the micelle-like structure and surface characteristics seems to improve drug permeation through the mucus layer. Finally, it is also demonstrated that BDP-loaded PHEA-PEG2000-EDA-LA micelles are able to increase cell uptake of BDP of about 44wt% compared to Clenil®on 16-HBE cells and possess an higher biocompatibility in comparison with the same commercial formulation.
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Laboratory of Biocompatible Polymers, University of Palermo, Via Archirafi, 32, 90129 Palermo, Italy.
authors.forename: D
authors.initials: D
authors.lastname: Triolo
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Laboratory of Biocompatible Polymers, University of Palermo, Via Archirafi, 32, 90129 Palermo, Italy.
authors.forename: E F
authors.initials: EF
authors.lastname: Craparo
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Laboratory of Biocompatible Polymers, University of Palermo, Via Archirafi, 32, 90129 Palermo, Italy.
authors.forename: B
authors.initials: B
authors.lastname: Porsio
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Laboratory of Biocompatible Polymers, University of Palermo, Via Archirafi, 32, 90129 Palermo, Italy.
authors.forename: C
authors.initials: C
authors.lastname: Fiorica
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Laboratory of Biocompatible Polymers, University of Palermo, Via Archirafi, 32, 90129 Palermo, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Giammona
authors.affiliation: Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Laboratory of Biocompatible Polymers, University of Palermo, Via Archirafi, 32, 90129 Palermo, Italy. Electronic address: gennara.cavallaro@unipa.it.
authors.forename: G
authors.initials: G
authors.lastname: Cavallaro
mesh_terms: D000893:Anti-Inflammatory Agents / Q000008:administration & dosage*; D000975:Antioxidants / Q000737:chemistry; D001507:Beclomethasone / Q000008:administration & dosage*; D001672:Biocompatible Materials; D001980:Bronchi / Q000166:cytology; D002470:Cell Survival; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D004847:Epithelial Cells / Q000166:cytology; D000431:Ethanol / Q000737:chemistry; D005029:Ethylenediamines / Q000737:chemistry; D006801:Humans; D008168:Lung / Q000187:drug effects*; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D008856:Microscopy, Fluorescence; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D010455:Peptides / Q000737:chemistry; D013499:Surface Properties; D008063:Thioctic Acid / Q000737:chemistry
chemical_list: D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D001672:Biocompatible Materials; D004337:Drug Carriers; D005029:Ethylenediamines; D008823:Micelles; D010455:Peptides; C008965:alpha,beta-poly((2-hydroxyethyl)-aspartamide); D000431:Ethanol; C031234:ethylenediamine; D008063:Thioctic Acid; D001507:Beclomethasone
keywords: Cell uptake; Lipoic acid; Mucin permeation; Polyaspartamide; Polymeric micelles; Sustained release