0000000001218528
AUTHOR
Giovanni Amato
New copolymers graft of α,β-poly(N-2-hydroxyethyl)-d,l-aspartamide obtained from atom transfer radical polymerization as vector for gene delivery
Abstract New cationic α,β-poly(N-2-hydroxyethyl)- d , l -aspartamide (PHEA) graft copolymers were synthesized by ATRP, using diethylamino ethyl methacrylate (DEAEMA) as monomer for polymerization, yielding polycations (PHEA-pDEAEMA) able to condense DNA. Then, consecutive ATRP conditions were set up on PHEA-pDEAEMA to obtain copolymers containing also hydrophilic chains (PHEA-IB-pDMAEMA-pPEGMA) able to improve biocompatibility of polyplexes and to provide them stealth properties. Agarose gel studies showed that the copolymers effectively condensed plasmid DNA to form polyplexes. Light scattering studies were used to analyze the size and the ζ -potential of these polyplexes, showing that cop…
NANOTECHNOLOGIES FOR BIOMEDICAL APLICATIONS
NUOVI COPOLMERI BIOCOMPATIBILI A BASE DI POLI-IDROSSIETILASPARTAMMIDE PER IL NONVIRAL GENE DELIVERY
PHEA-graft-polybutylmethacrylate copolymer microparticles for delivery of hydrophobic drugs.
Abstract Polymeric microparticles encapsulating two model hydrophobic drugs, beclomethasone dipropionate (BDP) and flutamide (FLU) were prepared by using the high pressure homogenization-solvent evaporation method starting from a oil-in-water emulsion. For the preparation of polymeric microparticles a α,β-poly(N-2-hydroxyethyl)- d , l -aspartamide (PHEA) graft copolymer with comb like structure was properly synthesized via grafting from atom transfer radical polymerization (ATRP) technique, by using two subsequent synthetic steps. In the first step a polymeric multifunctional macroinitiator was obtained by the conjugation of a proper number of 2-bromoisobutyryl bromide (BIB) residues to the…
PHEA-graft-polymethacrylate supramolecular aggregates for protein oral delivery
Abstract Salmon calcitonin (sCT) is characterized by a poor oral availability. A new copolymer, β-poly(N-2-hydroxyethyl)-graft-{N-2-ethylene[2-poly(methacrylic acid sodium salt)isobutyrate]}- d , l -aspartamide (PHEA-IB-p(MANa + )), was designed for the oral administration of sCT through the formation of supramolecular aggregates (SAs) based on electrostatic interactions. Several sCT/PHEA-IB-p(MANa + ) weight ratios were characterized by turbidimetry, DLS, zeta potential, and microscopy analysis. After the incubation of sCT/PHEA-IB-p(MANa + ) complex with digestive enzymes, 10% (w/w) of loaded sCT was released in the native form. In vitro investigation was carried out to determine the copol…
Evaluation of thermoresponsive properties and biocompatibility of polybenzofulvene aggregates for leuprolide delivery
Abstract In this study, a polybenzofulvene derivative named poly-6-MOEG-9-BF3k, was evaluated as polymeric material for the production of injectable thermoresponsive nano-aggregates able to load low molecular weight peptidic drug, like the anticancer leuprolide. Thermoresponsive behavior of poly-6-MOEG-9-BF3k was studied in aqueous media by evaluating scattering intensity variations by means of DLS in function of temperature. Zeta potential measurements and SEM observations were also carried out. Moreover, critical aggregation temperature of the poly-6-MOEG-9-BF3k polymer was evaluated by pyrene fluorescence analysis. Then, the ability of prepared thermoresponsive aggregates to protect this…
Synthesis and characterization of polyaspartamide copolymers obtained by ATRP for nucleic acid delivery
Abstract Nucleic acid molecules such as small interfering RNAs (siRNAs) and plasmidic DNAs (pDNAs) have been shown to have the potential to be of therapeutic value in different human diseases. Their practical use is however compromised by the lack of appropriate release systems. Delivered as naked molecules, siRNAs/pDNAs are rapidly degraded by extracellular nucleases thus considerably reducing the amount of molecule which can reach the target cells. Additionally, the anionic charge of the phosphate groups present on the siRNAs/pDNAs backbone, disfavors the interaction with the negatively charged surface of the cell membrane. In this paper we describe the generation of a novel polymer able …
HYDROPHOBIC POLYMER COATED SUPERPARAMAGNETIC NANOPARTICLES FOR ANTICANCER DRUG DELIVERY
HYDROPHOBIC POLYMER COATED SUPERPARAMAGNETI NANOPARTICLES FOR ANTICANCER DRUG DELIVERY LICCIARDI M.1, SCIALABBA C.1, AMATO G.1, CAVALLARO G.1, GIAMMONA G.1,2 1Dipartimento di Scienze e Tecnologie Molecolari e Biomolecolari (STEMBIO), University of Palermo, via Archirafi 32, 90123, Palermo, Italy. 2IBF-CNR, via Ugo La Malfa, 153, 90143 Palermo, Italy. Superparamagnetic Fe3O4 nanoparticles have been recently used in drug delivery applications [1-4]. In this study, a novel approach to prepare magnetic polymeric nanoparticles containing superparamagnetic domains and hydrophobic polymeric shell using microemulsion-solvent evaporation method is reported. PHEA-IB-poly(ButMA) copolymer was used as …