Preparation and characterization of anionic pullulan thermoassociative nanoparticles for drug delivery.

Thermoassociative nanoparticles were obtained through the crosslinking reaction of periodate oxidized carboxymethyl pullulan with two difunctional Jeffamines: ED-600 and ED-2003. The nanoparticles were characterized through (1)H NMR spectra; their particle size, determined by dynamic light scattering (DLS) presented a bimodal distribution, with dimensions varying as a function of amount and type of crosslinking agent used; transmission electron microscopy photos confirmed the spherical shape of the nanoparticles and their dimensions determined by DLS. Their amphiphilic character was evidenced by retention of the dyes: hydrophobic (Rose Bengal), amphiphilic (Brilliant Blue) and hydrophilic (Vitamin B12). The thermosensitive properties, more pronounced for ED-2003 crosslinked nanoparticles, were evidenced through absorbance variation, fluorescence and DLS measurements as a temperature function. The nanoparticles retain important amounts of anionic (diclofenac: 40-80 mg/g), cationic (methylene blue: 70-125 mg/g) and hydrophobic (alpha-tocopherol: 220-350 mg/g) drugs. The in vitro characterization of the drug-polymer conjugates recommends the synthesized nanoparticles as supports for drug delivery.

Bioactive cotton fabrics containing chitosan and biologically active substances extracted from plants.

The paper studies the obtaining of bioactive textiles using chitosan-coated fabrics, in which biologically active substances contained by Viola Tricolor (VT) - an extract of three Viola species (Violaceae) - were immobilized. Chitosan was applied on cotton fabric or on chemically modified cotton (having reactive -CHO or carboxymethyl groups), as tripolyphosphate (TPP) crosslinked fine particles, or by use of glutaraldehyde crosslinking agent. The amount of VT retained on the fabrics was found to depend on the procedure of chitosan application on the cotton. The obtained bioactive textiles are expected to have antioxidant activity due to the biologically active substances from VT; they can be used for obtaining clothes for people with allergies or other skin problems, assuring a controlled release of biomolecules. The study focuses on the in vitro release of VT retained on the fabrics, as well as on its antioxidant activity.

New multifunctional textile biomaterials for the treatment of leg venous insufficiency.

Acryloyl monomers have been synthesized by reaction of beta-cyclodextrin and troxerutin with acryloyl chloride and grafted on a knitted material obtained from polyamide 6.6 and polyurethane fibers. Polyamide grafted with beta-cyclodextrin derivative binds troxerutin as a physical complex. The obtained biomaterials have been tested in vivo on rats for their ability to deliver troxerutin (a flebotonic drug) to different skin areas (epidermis, dermis and vascular wall). The results showed that the new synthesized materials can act as multifunctional bioactive textiles that can display both compression (given by the textile material) and sustained venotonic and haemostatic properties (given by the troxerutin delivered from biomaterial to the skin).

Bile acid sequestrants based on cationic dextran hydrogel microspheres. 2. Influence of the length of alkyl substituents at the amino groups of the sorbents on the sorption of bile salts.

Cationic dextran hydrogel microspheres with pendant quaternary ammonium groups having alkyl substituents (C(2)-C(12)) at quaternary nitrogen were synthesized. The in vitro sorption of sodium salts of four bile acids (glycocholic, cholic, taurocholic, and deoxycholic acids) with these hydrogels was studied as a function of substituent alkyl chain length and bile acid hydrophobicity. Sorption experiments were performed in phosphate buffer solutions (pH 7.4) containing one bile salt (individual sorption) or mixtures of several bile salts (competitive sorption). Parameters for individual sorption were calculated taking into consideration the stoichiometric and cooperative binding of bile salts to oppositely charged polymer hydrogels. The results show that the increase in the length of the alkyl chain of the substituent leads to an increase in both ionization constant K(0) and overall stability constant of binding K, but decreases the cooperativity parameter u. The competitive sorption studies indicate that the hydrogels display a good affinity for both dihydroxylic and trihydroxylic bile salts. The molar ratio of maximum amounts bound for the two types of bile acid is 2 to 1, which is much lower than those reported for other cationic polymers recommended as bile acid sequestrants. The binding constants for the sorption of bile salts by some dextran hydrogels are 20-30 times higher than those obtained for cholestyramine under similar sorption conditions.

Sodium cholate sorption on cationic dextran hydrogel microspheres. 1. Influence of the chemical structure of functional groups.

New hydrogel microspheres based on crosslinked dextran, containing pendant quaternary ammonium groups with different chemical structures have been synthesized and tested as possible bile acid sorbents The in vitro sodium cholate sorption by these hydrogels has been followed in the absence or in the presence of competing anions The sorption results have indicated a strong influence of the chemical structure of functional groups on both the affinity and selectivity towards cholate ions. The best sorption performances were obtained with hydrogels having in the structure of functional groups an alkyl substituent with the length higher than C(8).

Aminated polysaccharides as bile acid sorbents: in vitro study.

Dextran, pullulan, and microcrystalline cellulose were cross-linked with 1-chloro-2,3-epoxypropane and reacted with N-(1-chloroethyl)-N,N-diethylamine or N-glycidyl-N,N,N-trialkylammonium chloride in order to obtain sorbents containing tertiary amino and/or quaternary ammonium groups. In vitro equilibrium sorption of cholic acid on these sorbents was studied in comparison with Cholestyramine, and in vitro dissociation of ionic complexes of cholic acid-sorbents was determined under dynamic conditions. The sorption capacity and the affinity of these sorbents for cholic acid were investigated in relation to the nature of the polymeric support, the swelling porosity of sorbent, the basicity of amino groups, and the nature of the substituents at the nitrogen atom. The maximum sorption capacity increases with the increase in amino group content, their basicity, and the length of alkyl substituents at the nitrogen atom. The affinity for cholic acid of all polysaccharide-based sorbents is higher than that of Cholestyramine. Dextran-based sorbents display the highest sorption affinity. It was found that there exists an optimum swelling porosity for the polysaccharide sorbents to attain the highest affinity for cholic acid. The dissociation rate of ionic complexes depends also on the nature of the polysaccharide and the swelling porosity and its lower for sorbents with higher sorption affinity.

Antioxidant action of a new flavonic derivative in acute carbon tetrachloride intoxication.

The antioxidant potential of a new flavonic derivative named conventionally theophylline-rutoside [TR-1722] was estimated by the measurement of G-6-Pase activity (marker enzyme for the endoplasmic reticulum), catalase activity (enzyme involved in the antioxidant defence process), and total -SH groups from the hepatic homogenate, using CCl4 as a free radical generating model. To show changes in the permeability of the hepatocyte membrane, the activity of lactate dehydrogenase (LDH) in plasma was determined. The obtained results suggest that TR-1722 acts by curtailing both lipid peroxidation and alkylation processes.