0000000000122015
AUTHOR
Vincenzo Tomarchio
New hydrogel matrices based on chemical crosslinked α,β -polyas parthydrazide: Synthesis, characterization and in vivo biocompatibility studies
New swellable micromatrices of α,β-polyasparthydrazide (PAHy) crosslinked with glutaraldehyde were prepared. The effect of crosslinking agent concentration was evaluated. In particular, crosslinking density affected aqueous dynamic swelling and glass-transition temperature of the material. The structure of prepared networks was also studied by scanning electron microscopy and X-ray analysis. Finally, biocompatibility of PAHy derivatives was investigated in vivo by subcutaneous implantation and in oral administration to laboratory animals.
Swellable microparticles containing Suprofen: evaluation of in vitro release and photochemical behaviour
Suprofen, an anti-inflammatory drug was incorporated in polymer networks based on biocompatible macromolecules, such as alpha,beta-polyasparthydrazide (PAHy) and alpha,beta-poly(N-hydroxyethyl)-DL-aspartamide (PHEA) crosslinked by glutaraldehyde or gamma-rays, respectively. Swelling tests carried out in aqueous media showed that pH value affects the swelling degree of the prepared hydrogels. In vitro release tests were performed in simulated gastrointestinal fluids (pH 1/6.8) using the pH variation method and in phosphate-buffered saline, pH 7.4. Experimental data indicated that Suprofen was released in a sustained way both from PAHy and PHEA microparticles. Further, incorporation of Suprof…
Effect of pH on the transfer kinetics of an anti-inflammatory drug from polyaspartamide hydrogels to a lipid model membrane
Abstract The release of a nonsteroidal anti-inflammatory drug (NSAID), 4-biphenylacetic acid (BPAA), from α,β-poly( N -hydroxyethyl)- dl -aspartamide (PHEA) hydrogels was tested at different pHs (4 and 7.4) by measuring the drug transfer from loaded hydrogel to dimyristoylphosphatidylcholine (DMPC) liposomes (multilamellar vesicles, MLV), chosen as a biomembrane model. This drug transfer was compared with the transfer from powdered drug and with drug classical. The perturbing effect of pure BPAA on the thermotropic behaviour of DMPC liposomes, in terms of transition temperature shift (Δ T m ) and enthalpy changes (Δ H ), was analysed at different pHs (4 and 7.4) by differential scanning cal…
Synthesis and characterization of water-swellable?,?-polyasparthydrazide derivatives
α, β-polyasparthydrazide (PAHy) was crosslinked by glutaraldehyde to form water-swellable materials possessing a three-dimensional molecular network. Different crosslinking degrees were prepared varying glutaraldehyde/PAHy ratio and samples containing 5-fluorouracil were obtained by incorporating the drug into the polymer networks during the crosslinking reaction. All samples were characterized by swelling tests, thermal, x-ray and SEM analysis. Their microstructure was observed through scanning electron microscopy. Furthermore, for samples containing the anticancer drug,in vitro release studies were performed in pH 7.4 buffer solution.
A Hydrogel Based on a Polyaspartamide: Characterization and Evaluation of In-vivo Biocompatibility and Drug Release in the Rat
Abstract This paper deals with the characterization of a new microparticulate hydrogel obtained by gamma irradiation of α,β-poly[N-(2-hydroxyethyl)-dl-aspartamide] (PHEA). When enzymatic digestion of PHEA hydrogel was evaluated using various concentrations of pepsin and α-chymotrypsin no degradation occurred within 24 h. In-vivo studies showed that this new material is biocompatible after oral administration to rats. PHEA hydrogel was also studied as a system for delivery of diflunisal, an anti-inflammatory drug. In-vitro release studies in simulated gastrointestinal juice (pH 1 or 6.8) showed that most of the drug was released at pH 6.8. In-vivo studies indicated that diflunisal-loaded PHE…
Preparation, characterization and in vitro antimicrobial activity of ampicillin-loaded polyethylcyanoacrylate nanoparticles.
In this paper, the experimental conditions for preparing ampicillin-loaded polyethylcyanoacrylate (PECA) nanoparticles are described. The effects of drug concentration and surfactant type in the polymerization medium on the particle size distribution and loading capacity were studied. The results of these studies show that only the type of surfactant has an impact on the nanoparticle dimensions. The release rate of ampicillin from PECA nanoparticles at pH 7.4 (extracellular value pH) performed either with and without esterases, show that the drug release is considerably increased in the presence of these exzymes. The results of drug release study at pH 1.1 (simulated gastric juice) are very…
α,β-Poly(N-Hydroxyethyl)-DL-Aspartamide Hydrogels as Drug Delivery Devices
α,β-poly(N-hydroxyethyl)-DL-aspartamide (PHEA) was exposed to gamma radiation to obtain micromatrices able to swell in an aqueous medium. Crosslinked PHEA was loaded with an anti-inflammatory drug, 4-biphenylacetic acid (BPAA) and the drug dispersion in the network was investigated by X-ray analysis. The BPAA loaded PHEA microparticles were also characterized by dimensional analysis, which showed the presence of quasispherical shapes. The drug release from PHEA hydrogel was studied in vitro in a pH 1.1 (simulated gastric juice) and in a pH 7.4 buffer solution, respectively. The experimental data indicate that an anomalous delivery occurs, but Fickian diffusion through swollen PHEA hydrogel…
Glycidyl methacrylate derivatization of α,β-poly(N-hydroxyethyl)-dl-aspartamide and α,β-polyasparthydrazide
Abstract α,β-Poly(N-hydroxyethyl)- dl -aspartamide (PHEA) and α,β-polyasparthydrazide (PAHy) are two synthetic macromolecules having many potential applications in the field of biomedical sciences. This paper describes the functionalization of PHEA and PAHy with glycidyl methacrylate (GMA), in order to introduce pendant double bonds in their chains. Derivatized PHEA and PAHy (samples PHG and PAG, respectively) at various GMA content have been obtained and characterized. It has been shown that the derivatization reaction can be controlled by varying some parameters as solvent, catalyst, pH, GMA concentration and reaction time. As expected, PAHy reacted more rapidly and more extensively than …