Amoxicillin-loaded polyethylcyanoacrylate nanoparticles: influence of PEG coating on the particle size, drug release rate and phagocytic uptake.

Polyethyleneglycol (PEG)-coated polyethylcyanoacrylate (PECA) nanoparticles loaded with amoxicillin were prepared and the influence of the PEG coating on the particle size, zeta potential, drug release rate and phagocytic uptake by murine macrophages was studied. Experimental results show that this colloidal drug delivery system could be useful for intravenous or oral administration. The profile of amoxicillin release from PECA nanoparticles system was studied under various conditions similar to those of some corporeal fluids. In all these experiments, amoxicillin release in the free form was studied by HPLC analysis. Experimental results showed that at pH 7.4 drug release rises when molecu…

Solid lipid nanoparticles containing vancomycin: preparation, characterization and in vitro anti-Staphylococcus aureus biofilms activity

Coagulase-negative staphylococci and Staphylococcus aureus are the most common cause of nosocomial infections and can induce a wide spectrum of diseases associated with remarkable morbidity and mortality. Biofilms of staphylococci are intrinsically resistant to conventional antibiotics and, being commonly associated with implanted medical device, such as catheters and vascular grafts, have the potential to cause blood-stream infections. The paper describes the preparation and characterization of vancomycin-loaded Solid Lipid Nanoparticles (SLNs) and in vitro studies of the inhibition of Staphylococcus aureus ATCC 29213 biofilms in the presence of this nanoparticle system. Methods. The vanco…

Una soluzione oleosa capace di prevenire la formazione di biofilm di Listeria monocytogenes

La Listeria monocytogenes è un batterio patogeno che può causare gastroenteriti lievi o gravi infezioni del sangue e del sistema nervoso, con tassi di mortalità tra il 20% e il 67%. È trasmesso all'uomo prevalentemente attraverso il cibo e può colpire le donne in gravidanza causando l’aborto. La malattia causata da questo batterio ha il nome di listeriosi e appartiene al gruppo di patologie definibili come “tossinfezioni alimentari”. Diversi focolai di listeriosi, associati con i prodotti alimentari “pronti da mangiare”, sono stati attribuiti a una combinazione di contaminazione di L. monocytogenes, durante la lavorazione e la successiva crescita nei prodotti durante lo stoccaggio. Oltre a …

ChemInform Abstract: Reaction of 2-Acetyltetralone with Some Esters of Benzoic Acid.

In order to investigate the pharmacological screening of a number of pyran-4-ones their synthesis by cyclization with sulphuric acid of the corresponding 1,3,5-triketones has been carried out with high yields. In the course of preparation of the latter the reaction of 2-acetyltetralone with some esters of benzoic acid derivatives has been studied and in particular, for a number of them, an interesting nucleophilic substitution of a chlorine atom with an alkoxy group on a benzenic nucleus has been evidenced.

Oregano essential oils activity against Listeria monocitogenes biofilms

SOLID LIPID NANOPARTICLES (SLN) AS DRUG CARRIERS FOR NEUROPROTECTIVE AGENTS: PREPARATION, CHARACTERIZATION AND RELEASE STUDIES

Solid lipid nanoparticles containing tamoxifen characterization and in vitro antitumoral activity.

Solid lipid nanoparticles (SLNs) containing tamoxifen, a nons- teroidal antiestrogen used in breast cancer therapy, were prepared by microemulsion and precipitation techniques. Tamoxifen loaded SLNs seem to have dimensional properties useful for parenteral administration, and in vitro plasmatic drug release studies demon- strated that these systems are able to give a prolonged release of the drug in the intact form. Preliminary study of antiproliferative ac- tivity in vitro, carried out on MCF-7 cell line (human breast cancer cells), demonstrated that SLNs, containing tamoxifen showed an antitumoral activity comparable to free drug. The results of char- acterization studies and of in vitro …

Ocular tolerability and in vivo bioavailability of poly(ethylene glycol) (PEG)-coated polyethyl-2-cyanoacrylate nanosphere-encapsulated acyclovir.

Acyclovir-loaded polyethyl-2-cyanoacrylate (PECA) nanospheres were prepared by an emulsion polymerization process in the micellar phase and characterized. The influence of the presence of nonionic surfactant as well as other substances [i.e., 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) and poly(ethylene glycol) (PEG)], on formulation parameters and loading capacity was investigated. In particular, the presence of PEG resulted in an increase of mean size and size distribution. To obtain PEG-coated PECA nanospheres with a mean size of200 nm, Pluronic F68 at concentrations1.5% (w/v) should be used during preparation. The presence of PEG also resulted in a change in zeta potential, from -25…

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…

Solid Lipid Nanoparticles Containing Vancomycin

Staphylococci coagulase-negative and Staphylococcus aureus are the most common cause of nosocomial infections and can induce a wide spectrum of diseases associated with remarkable morbidity and mortality. Biofilms of staphylococci are intrinsically resistant to conventional antibiotics and, being commonly associated with implanted medical device, such as catheters and vascular grafts, have the potential to cause blood-stream infections. In recent years increasing attention has been addressed to Solid Lipid Nanoparticles (SLNs), thanks to their biodegradability and ability to entrap a variety of biologically active compounds, in the area of modified drug delivery technology in the attempt to…

Reaction of 2-acetyltetralone with some esters of benzoic acid

In order to investigate the pharmacological screening of a number of pyran-4-ones their synthesis by cyclization with sulphuric acid of the corresponding 1,3,5-triketones has been carried out with high yields. In the course of preparation of the latter the reaction of 2-acetyltetralone with some esters of benzoic acid derivatives has been studied and in particular, for a number of them, an interesting nucleophilic substitution of a chlorine atom with an alkoxy group on a benzenic nucleus has been evidenced.

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…

Coupling of the antiviral agent zidovudine to polyaspartamide and in vitro drug release studies.

A macromolecular prodrug of the known antiretroviral agent zidovudine and alpha, beta-poly(N-2-hydroxyethyl)-DL-aspartamide (PHEA) was synthesized. A succinic spacer was present between the polymer and the drug, and 1,1'-carbonyldiimidazole was used as the coupling agent. In vitro drug release studies at pH 1.1, 5.5 and 7.4 indicated that limited amounts of intact drug were released from the conjugate. At pH 1.1 and 7.4 succinylzidovudine was released, and this was hydrolysed to give free zidovudine. In the presence of alpha-chymotrypsin, zidovudine was released preferentially in comparison with the succinyl derivative. The amounts of released zidovudine and succinylzidovudine were greater …

ATTIVITÀ ANTIBATTERICA DI UNA SOLUZIONE OLEOSA: possibili applicazioni nell’industria alimentare per la prevenzione della formazione di biofilm

Le malattie che derivano dal consumo di alimenti hanno sempre minacciato la salute umana. Oggi il loro aumento è diventato un problema per salute pubblica, emergente in tutto il mondo. Molte di queste malattie sono state associate alla presenza di biofilm batterici, comunità microbiche complesse, nell’industria alimentare. Il biofilm è diventato un grosso problema per l’industria della lavorazione del pesce, del latte e derivati, del pollame, della carne e dei cibi “pronti da mangiare”, perché, in seguito alla sua formazione, i batteri a esso associati sono particolarmente resistenti agli agenti antimicrobici e alle operazioni di pulizia. Anche se fino ad oggi sono ancora utilizzate, e sono…

Hydrophilic and Hydrophobic Polymeric Derivatives of Anti-Inflammatory Agents Such as Alclofenac, Ketoprofen, and Ibuprofen

Macromolecular prodrugs of a hydrophilic polymer [α,β-poly( N- hydroxyethyl)-DL-aspartamide (PHEA)] was used as a drug carrier. Three poly- (HEA)-NSAID adducts were studied: poly(HEA)-Alclofenac, poly(HEA)-Keto profen, and poly(HEA)-Ibuprofen. Prodrugs with different drug content were synthesized both as water-soluble and water-insoluble agents. Hydrolysis of water-soluble adducts in a simulated gastric juice was studied.