caa a22 4500 44531222X CHVBK 20180317142634.0 cr unu---uuuuu 170323e20110701xx s 000 0 eng 10.1007/s11095-011-0403-z doi (NATIONALLICENCE)springer-10.1007/s11095-011-0403-z Surface Characterisation of Bioadhesive PLGA/Chitosan Microparticles Produced by Supercritical Fluid Technology [Elektronische Daten] [Luca Casettari, Enzo Castagnino, Snjezana Stolnik, Andrew Lewis, Steven Howdle, Lisbeth Illum] ABSTRACT: Purpose: Novel biodegradable and mucoadhesive PLGA/chitosan microparticles with the potential for use as a controlled release gastroretentive system were manufactured using supercritical CO2 (scCO2) by the Particle Gas Saturated System (PGSS) technique (also called CriticalMixTM). Methods: Microparticles were produced from PLGA with the addition of mPEG and chitosan in the absence of organic solvents, surfactants and crosslinkers using the PGSS technique. Microparticle formulations were morphologically characterized by scanning electron microscope; particle size distribution was measured using laser diffraction. Microparticle surface was analyzed using X-ray photoelectron spectroscopy (XPS) and time-of-flight secondary ion mass spectrometry (ToF-SIMS) to evaluate the presence of chitosan on the surface. Mucoadhesiveness of the microparticles was evaluated in vitro using a mucin assay employing two different kinds of mucin (Mucin type III and I-S) with different degrees of sialic acid contents, 0.5-1.5% and 9-17%, respectively. Results: The two analytical surface techniques (XPS and ToF-SIMS) demonstrated the presence of the chitosan on the surface of the particles (<100μm), dependent on the polymer composition of the microparticles. The interaction between the mucin solutions and the PLGA/chitosan microparticles increased significantly with an increasing concentration of mucin and chitosan. Conclusions: The strong interaction of mucin with the chitosan present on the surface of the particles suggests a potential use of the mucoadhesive carriers for gastroretentive and oral controlled drug release. Springer Science+Business Media, LLC, 2011 chitosan nationallicence controlled release nationallicence mucoadhesive nationallicence PLGA nationallicence ToF-SIMS nationallicence XPS nationallicence ASES : aerosol solvent extraction system nationallicence BSA : bovine serum albumin nationallicence CAN-BD : supercritical carbon dioxide assistednebulisation with a bubble dryer nationallicence FAT : fixed analyzer transmission nationallicence GAS : gas anti-solvent nationallicence mPEG : methoxy polyethylene glycol nationallicence PAS : periodic acid-Schiff nationallicence PCA : precipitation with a compressed fluid anti-solvent nationallicence PEO : polyethylene oxide nationallicence PGSS : particle gas saturated system nationallicence PLA : polylactic acid nationallicence PLGA : poly(lactic-co-glycolic acid) nationallicence PSD : particle size distribution nationallicence RESS : rapid expansion from a supercritical solution nationallicence RESOLV : rapid expansion of a supercritical solution into a liquid solvent nationallicence SAA : supercritical assisted atomization nationallicence SAS : supercritical anti-solvent nationallicence scCO2 : supercritical carbon dioxide nationallicence SCF : supercritical fluid nationallicence SEDS : solution enhanced dispersion of solids nationallicence TMC : N-trimethyl chitosan nationallicence ToF-SIMS : time-of-flight secondary ion mass spectrometry nationallicence VMD : volume-averaged mean diameter nationallicence XPS : X-ray photoelectron spectroscopy nationallicence Casettari Luca Department of Drug and Health Sciences, University of Urbino "Carlo Bo”, Urbino P.zza Rinascimento 6, 61029, Urbino, Italy aut Castagnino Enzo Department of Drug and Health Sciences, University of Urbino "Carlo Bo”, Urbino P.zza Rinascimento 6, 61029, Urbino, Italy aut Stolnik Snjezana Drug Delivery and Tissue Engineering Division, School of Pharmacy, University of Nottingham, NG7 2RD, Nottingham, UK aut Lewis Andrew Critical Pharmaceuticals Limited, BioCity, Pennyfoot Street, NG1 1GF, Nottingham, UK aut Howdle Steven School of Chemistry, University of Nottingham, NG7 2RD, Nottingham, UK aut Illum Lisbeth Critical Pharmaceuticals Limited, BioCity, Pennyfoot Street, NG1 1GF, Nottingham, UK aut Pharmaceutical Research Springer US; http://www.springer-ny.com 28/7(2011-07-01), 1668-1682 0724-8741 28:7<1668 2011 28 11095 https://doi.org/10.1007/s11095-011-0403-z text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s11095-011-0403-z text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Casettari Luca Department of Drug and Health Sciences, University of Urbino "Carlo Bo”, Urbino P.zza Rinascimento 6, 61029, Urbino, Italy aut NATIONALLICENCE 700 1- Castagnino Enzo Department of Drug and Health Sciences, University of Urbino "Carlo Bo”, Urbino P.zza Rinascimento 6, 61029, Urbino, Italy aut NATIONALLICENCE 700 1- Stolnik Snjezana Drug Delivery and Tissue Engineering Division, School of Pharmacy, University of Nottingham, NG7 2RD, Nottingham, UK aut NATIONALLICENCE 700 1- Lewis Andrew Critical Pharmaceuticals Limited, BioCity, Pennyfoot Street, NG1 1GF, Nottingham, UK aut NATIONALLICENCE 700 1- Howdle Steven School of Chemistry, University of Nottingham, NG7 2RD, Nottingham, UK aut NATIONALLICENCE 700 1- Illum Lisbeth Critical Pharmaceuticals Limited, BioCity, Pennyfoot Street, NG1 1GF, Nottingham, UK aut NATIONALLICENCE 773 0- Pharmaceutical Research Springer US; http://www.springer-ny.com 28/7(2011-07-01), 1668-1682 0724-8741 28:7<1668 2011 28 11095 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer