6533b835fe1ef96bd129ed3d

RESEARCH PRODUCT

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

Gennara CavallaroGaetano GiammonaEmanuela Fabiola CraparoBarbara PorsioDaniela TrioloCalogero Fiorica

subject

Surface PropertieAnti-Inflammatory AgentsBiocompatible MaterialsMucin permeation02 engineering and technologyPharmacology030226 pharmacology & pharmacyMicelleAntioxidantsDrug Delivery Systems0302 clinical medicineNanoparticleColloid and Surface ChemistryCopolymerDrug CarrierLungMicellesmedia_commonCell uptakeBiocompatible MaterialDrug CarriersLipoic acidThioctic AcidChemistryBeclomethasoneSurfaces and InterfacesGeneral Medicinerespiratory systemEthylenediamines021001 nanoscience & nanotechnologyPolyaspartamideAnti-Inflammatory AgentDrug deliveryPeptideAntioxidant0210 nano-technologyDrug carrierSurfaces and InterfaceHumanBiotechnologyDrugBiocompatibilitySurface PropertiesCell Survivalmedia_common.quotation_subjectEthylenediamineBronchi03 medical and health sciencesMicroscopy Electron TransmissionPolymeric micelleHumansSurface chargeParticle SizePhysical and Theoretical ChemistryEpithelial CellEthanolEpithelial CellsMicroscopy FluorescenceSettore CHIM/09 - Farmaceutico Tecnologico ApplicativoNanoparticlesNanocarriersPeptidesDrug Delivery SystemNuclear chemistrySustained releaseMicelle

description

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.

yearjournalcountryeditionlanguage
2017-03-01
10.1016/j.colsurfb.2016.11.025http://hdl.handle.net/10447/248383