PEGYLATED POLYASPARTAMIDE–POLYLACTIDE BASED NANOPARTICLES PENETRATING CYSTIC FIBROSIS ARTIFICIAL MUCUS

6533b7d0fe1ef96bd125af18

RESEARCH PRODUCT

PEGYLATED POLYASPARTAMIDE–POLYLACTIDE BASED NANOPARTICLES PENETRATING CYSTIC FIBROSIS ARTIFICIAL MUCUS

Barbara Porsio Gaetano Giammona Gennara Cavallaro Carla Sardo Emanuela Fabiola Craparo

subject

Polymers and Plastics Biocompatibility Polyesters α L-aspartamide Nanoparticle Bioengineering Ibuprofen 02 engineering and technology Respiratory Mucosa 010402 general chemistry 01 natural sciences Cell Line Polyethylene Glycols Biomaterials Rhodamine cystic fibrosis chemistry.chemical_compound polymeric nanoparticles cystic fibrosis α β-poly(N-2-hydroxyethyl)-D L-aspartamide Materials Chemistry Copolymer Organic chemistry Humans Derivatization β-poly(N-2-hydroxyethyl)-D polymeric nanoparticles; cystic fibrosis; α; β-poly(N-2-hydroxyethyl)-D; L-aspartamide 021001 nanoscience & nanotechnology Mucus 0104 chemical sciences Mucus polymeric nanoparticles chemistry Settore CHIM/09 - Farmaceutico Tecnologico Applicativo PEGylation Nanoparticles 0210 nano-technology Peptides Ethylene glycol Nuclear chemistry

description

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.

year	journal	country	edition	language
2016-02-11

10.1021/acs.biomac.5b01480 http://hdl.handle.net/11386/4728412