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Polymeric drug delivery micelle-like nanocarriers for pulmonary administration of beclomethasone dipropionate

  • Autori: Triolo, D.; Craparo, E.; Porsio, B.; Fiorica, C.; Giammona, G.; Cavallaro, G.
  • Anno di pubblicazione: 2017
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • Parole Chiave: Cell uptake; Lipoic acid; Mucin permeation; Polyaspartamide; Polymeric micelles; Sustained release; Anti-Inflammatory Agents; Antioxidants; Beclomethasone; Biocompatible Materials; Bronchi; Cell Survival; Drug Carriers; Epithelial Cells; Ethanol; Ethylenediamines; Humans; Lung; Microscopy, Electron, Transmission; Microscopy, Fluorescence; Nanoparticles; Particle Size; Peptides; Surface Properties; Thioctic Acid; Drug Delivery Systems; Micelles; Biotechnology; Surfaces and Interfaces; Physical and Theoretical Chemistry; Colloid and Surface Chemistry
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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 200 nm. Besides, BDP-loaded micelles, obtained with a Drug Loading equal to 5 wt%, 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 44 wt% compared to Clenil®on 16-HBE cells and possess an higher biocompatibility in comparison with the same commercial formulation.