Recycling of almond by-products for intestinal inflammation: improvement of physical-chemical, technological and biological characteristics of a dried almond skins extract.

Background: Almond skins are rich in bioactive compounds that undergo oxidation/degradation phenomena and are poorly soluble in water, reducing in vivo absorption and bioavailability, factors that influence the pharmacological activity of an active product. We developed a dried acetonic almond skins extract/cyclodextrin complex to improve extract solubility, dissolution rate and biological activity. Methods: A lyophilized acetonic almond skin extract was produced. To optimize complex formulation, phase solubility studies and complex characterization (absorption studies, differential scanning calorimetry (DSC), morphology, solubility studies) were performed. To evaluate a possible use in hea…

An Alginate/Cyclodextrin Spray Drying Matrix to Improve Shelf Life and Antioxidant Efficiency of a Blood Orange By-Product Extract Rich in Polyphenols: MMPs Inhibition and Antiglycation Activity in Dysmetabolic Diseases

Alginate and β-cyclodextrin were used to produce easily dosable and spray-dried microsystems of a dried blood orange extract with antidysmetabolic properties, obtained from a by-product fluid extract. The spray-dried applied conditions were able to obtain a concentrate dried extract without the loss of AOA and with TPC and TMA values of 35–40% higher than that of the starting material. They were also effective in producing microparticles with 80–100% of encapsulation efficiency. The 2% sodium alginate was capable of improving the extract shelf life, while the beta-cyclodextrin (1 : 1 molar ratio with dried extract) prolonged the extract antioxidant efficiency by 6 hours. The good inhibition…

A novel alpha-amylase-lipase formulation as anti-staling agent in durum wheat bread

The aim of this work has been to evaluate the anti-staling effect exerted by a novel α-amylase-lipase enzyme formulation on durum wheat bread, in comparison with four different commercial amylase preparations and with control without added enzymes. Bread-making trials were carried out at industrial level. Sliced bread, packed under modified atmosphere, was analyzed for texture profile, moisture content, and water activity during 90 days. Crumb sections were submitted to environmental scanning electron microscopy at the end of the storage period. The α-amylase-lipase enzyme preparation showed synergistic interactions in preventing staling. In particular, bread added of these two enzymes in m…

Evaluation of polyalkylcyanoacrylate nanoparticles as a potential drug carrier: preparation, morphological characterization and loading capacity.

Some physicochemical behaviours were investigated of polyethyl- (PECA) and polyisobutylcyanoacrylate (PICA), which, in recent years, have been proposed as nanoparticle colloidal systems for drug carrying. We observed the influence of preparation conditions, such as pH value and surfactant concentration, on parameters such as particle size and polymer molecular weight. Lower operating pH values (0-2) resulted in smaller nanoparticles than those prepared at pH 5.5. The polymer molecular weight was also a function of pH: low molecular weight at low pH and vice-versa. The surfactant concentration positively influenced main particle size and polymer molecular weight. These trends were independen…

New amphiphilic conjugates of mono- and bis(carboxy)-PEG(2,000) polymers with lipoamino acids as surface modifiers of colloidal drug carriers

Kinetics of Molecule Transfer between Lipid Vesicles and β-Cyclodextrins

Abstract We propose a calorimetric method based on the van't Hoff model of depression of the freezing temperature to investigate slow kinetics involving lipid vesicles (liposomes) and drug–β-cyclodextrin (Cyd) complexes. Some nonsteroidal antiinflammatory drugs (NSAIDs) were examined and standard phospholipid liposomes were used in our experiments. Three different kinetic processes were investigated: (a)9Transfer of drugs from water-soluble Cyd-complexes to void liposomes. (b)9Uptake of drugs from the surface of liposomes by free Cyd dissolved in the aqueous phase. (c)9Exchange of drugs from loaded to void vesicles, and the effect of free Cyd in enhancing such a transfer. Most experiments w…

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…

COMPARATIVE-STUDY ON INCLUSION-COMPOUNDS OF 4-BIPHENYLACETIC ACID WITH BETA-CYCLODEXTRIN, HYDROXYPROPYLATED-BETA-CYCLODEXTRINS, AND METHYLATED-BETA-CYCLODEXTRINS

AbstractThe inclusion behavior of Hydroxypropyl-β-Cyclodextrin (HP-β-Cyd) and of methylated-β-Cyclodextrins, heptakis-(2,6-di-O-methyl)-β-Cyclodextrin (DM-β-Cyd) and heptakis-(2,3,6-tri-O-methyl)-β-Cyclodextrin (TM-β-Cyd), in solution and solid state was compared with that of natural β-Cyclodextrin (β-Cyd) using an anti-inflammatory drug, 4-biphenylacetic acid (BPAA), as a guest molecule. The solubility of BPAA with β-Cyd and β-Cyd derivatives in aqueous solution were determined. Stability constants were calculated by phase solubility method at various pH values and temperatures. The formation of inclusion complexes with β-Cyd and β-Cyd derivatives in the solid slate were confirmed by infra…

Nanocomplexes for gene therapy of respiratory diseases: Targeting and overcoming the mucus barrier

Gene therapy, i.e. the delivery and expression of therapeutic genes, holds great promise for congenital and acquired respiratory diseases. Non-viral vectors are less toxic and immunogenic than viral vectors, although they are characterized by lower efficiency. However, they have to overcome many barriers, including inflammatory and immune mediators and cells. The respiratory and airway epithelial cells, the main target of these vectors, are coated with a layer of mucus, which hampers the effective reaching of gene therapy vectors carrying either plasmid DNA or small interfering RNA. This barrier is thicker in many lung diseases, such as cystic fibrosis. This review summarizes the most impor…

Effect of?-cyclodextrin complexation on the photohaemolitic activity induced by Ketoprofen and Naproxen sensitization

Red blood cell lysis photosensitized by two non-steroidal anti-inflammatory drugs Naproxen (NAP) and Ketoprofen (KPF) was investigated in the presence of β-cyclodextrin (β-Cyd). The photohaemolysis was inhibited by the addition of β-Cyd both for NAP and, to a lesser extent, for KPF. The protective action was found only in a restricted range of concentration of β-Cyd. Higher amounts of β-Cyd interfered with the resistance of the cell to the osmotic shock induced by the photosensitization process. The complexing action of β-Cyd was ascertained through UV-vis absorption spectroscopy, induced circular dichroism and emission spectroscopy. The isolated complexes Naproxen-β-Cyd (NAP-β-Cyd) and Ket…

Preparation and physico-chemical study of inclusion complexes between idebenone and modified beta-cyclodextrins

The inclusion properties of modifiedβ-cyclodextrins (trimethyl-β-cyclodextrin, dimethyl-β-cyclodextrin and hydroxypropyl-β-cyclodextrin) towards idebenone were compared with naturalβ-cyclodextrin. The inclusion complexes were prepared by different methods (coprecipitation, kneading, and freeze-drying) and characterized by differential scanning calorimetry, X-ray diffractometry, UV, CD and NMR spectroscopy. The results obtained by CD and NMR spectroscopy indicate a different orientation of idebenone in dimethyl-β-cyclodextrin with respect to other cyclodextrins. Stability constants of the complexes were determined in water at various temperatures and consequently thermodynamic parameters wer…

Live nativity and brucellosis, Sicily.

To the Editor: Worldwide, brucellosis remains a major zoonosis and an important cause of travel-associated illness (1). Brucellosis is transmitted to humans through the consumption of infected, unpasteurized, animal-milk products; direct contact with infected animal parts; or inhalation of infected aerosolized particles. We report an outbreak of brucellosis in a small village of the Ionic coast of Messina province (eastern Sicily). In 2003, health authorities in the Messina province were notified of 29 cases of brucellosis; 18 of the patients were members of 9 different families. All patients had observed a Nativity pantomime that used live animals and was organized by the local population.…

INTERACTION OF MACROMOLECULAR PRO-DRUGS WITH LIPID MODEL MEMBRANE - CALORIMETRIC STUDY OF 4-BIPHENYLACETIC ACID LINKED TO ALPHA,BETA-POLY(N-HYDROXYETHYL)-DL-ASPARTAMIDE INTERACTING WITH PHOSPHATIDYLCHOLINE VESICLES

The effect of 4-biphenylacetic acid (BPAA) covalently linked to α,β-poly(N-hydroxyethyl)-dl-aspartamide (PHEA) on the thermotropic properties of dipalmitoylphosphatidylcholine (DPPC) liposomes was investigated by differential scanning calorimetry (DSC). Addition of increasing amounts of PHEA-BPAA adduct to a suspension of phospholipid vesicles modified the thermotropic gel-to-liquid crystalline phase transition by decreasing the enthalpy changes ΔH with concomitant broadening of the peak without variations in the transition temperature (Tm). These effects are interpreted in terms of a deep interaction of BPAA bound to the polymer with the apolar moiety of the lipid bilayer. The amount of dr…

A Novel Artificial Mosaic Generation Technique Driven by Local Gradient Analysis

Art often provides valuable hints for technological innovations especially in the field of Image Processing and Computer Graphics. In this paper we present a novel method to generate an artificial mosaic starting from a raster input image. This approach, based on Gradient Vector Flow computation and some smart heuristics, permit us to follow the most important edges maintaining at the same time high frequency details. Several examples and comparisons with other recent mosaic generation approaches show the effectiveness of our technique.

Pefloxacine mesilate- and ofloxacin-loaded polyethylcyanoacrylate nanoparticles: characterization of the colloidal drug carrier formulation.

The entrapment of fluoroquinolones, perfloxacine mesilate (PFX) and ofloxacin (OFX), in polyalkylcyanoacrylate (PECA) nanoparticles could offer some advantages for their biological application; for examples, increasing their bioavailability, controlling the drug time-release in blood, and reducing the formation of bacterial resistance. To load these two drugs in PECA polymeric bulk, the incorporation or adsorption method was performed. These two methods were capable of influencing nanoparticle size, molecular weight, release profile, and drug–polymer association. The incorporation method, particularly for the OFX system, achieved PECA nanoparticle suspensions with a mean size value three ti…

Preparation and Biological Evaluation of Ethylcellulose Microspheres Containing Tolmetin

AbstractTolmetin microspheres were prepared by the coacervation process from the ethylcellulose. Microspheres were obtained both in presence and without protecting colloids, such as polyisobutilene (PIB) or ethyl-vinylacetate copolimers (EVA). The effect of these agents on the preparation, drug content, wall thickness, surface morphology, drug dissolution arid release from microspheres, were evaluated. The dissolution rate analysis was carried out also in the presence of a surfactant (Tween 80) at different pH values.In addition, microspheres containing Tolmetin as a core material were submitted to biological tests, in comparison with the free drug, to evaluate upon experimental models the …

Calorimetric investigation of the complex formation between surfactants and α-, β- and γ-cyclodextrins

Abstract A calorimetric technique has been used to study complex formation between α-, β- and γ-cyclodextrins (αCD, βCD and γCD) and some surfactants (sodium dodecylsulphate (SDS), hexadecyl trimethylammonium bromide (CTAB) and p-(1,1,3,3-tetramethylbutyl) phenoxypoly(oxyethyleneglycol) (Triton X-100)). The experimental data indicate that some complexes (SDS-αCD, SDS-βCD and CTAB-αCD) are very stable and allow direct determination of their stoichiometry and molar enthalpy of complex formation. Those for other complexes closely fit a model based on an equilibrium reaction between surfactant, cyclodextrin and a single complex. According to the model, data analysis allows determination of the …

5-Fluorouracil: various kinds of loaded liposomes: encapsulation efficiency, storage stability and fusogenic properties

Abstract This paper describes the optimization of 5-fluorouracil (5-FU) loaded liposome formulations. Four different preparation procedures were carried out, obtaining two types of multilamellar vesicles (MLVs), stable plurilamellar vesicles (SPLVs) and large unilamellar vesicles (LUVs). In this study various phospholipids were used to prepare liposomes. The lipid mixtures containing diplamitoylphosphatidylserine seemed the best for biological 5-FU delivery by presenting better encapsulation efficiency parameters, serum and storage stability, and fusogenic properties, which are an important factor prerequisite for in vivo liposome-cell interaction. The presence of cholesterol in the liposom…