Effect of chitosan and thiolated chitosan coating on the inhibition behaviour of PIBCA nanoparticles against intestinal metallopeptidases

Surface modified nanoparticles composed of poly(isobutylcyanoacrylate) (PIBCA) cores surrounded by a chitosan and thiolated chitosan gel layer were prepared and characterized in previous works. The presence of such biopolymers on the nanoparticle surface conferred those nanosystems interesting characteristics that might partially overcome the gastrointestinal enzymatic barrier, improving the oral administration of pharmacologically active peptides. In the present work, the antiprotease behaviour of this family of core–shell nanoparticles was in vitro tested against two model metallopeptidases present in the gastrointestinal tract (GIT): Carboxypeptidase A -CP A- (luminal protease) and Leucine Aminopeptidase M -LAP M- (membrane protease). As previous step, the zinc-binding capacity of these nanoparticles was evaluated. Interestingly, an improvement of both the zinc-binding capacity and the antiprotease effect of chitosan was observed when the biopolymers (chitosan and thiolated chitosan) were used as coating component of the core–shell nanoparticles, in comparison with their behaviour in solution, thanks to the different biopolymer chains rearrangement. The presence of amino, hydroxyl and thiol groups on the nanoparticle surface promoted zinc binding and hence the inhibition of the metallopeptidases analysed. On the contrary, the occurrence of a cross-linked structure in the gel layer surrounding the PIBCA cores of thiolated formulations, due to the formation of interchain and intrachain disulphide bonds, partially limited the inhibition of the proteases. The low accessibility of cations to the active groups of the cross-linked polymeric shell was postulated as a possible explanation of this behaviour. Results obtained in this work make this family of surface-modified nanocarriers promising candidates for the successfull administration of pharmacologically active peptides and proteins by the oral route.     

A Topological Criterion for the Existence of Half-Bound States

The following theorem is proved: if (M⁴ⁿ⁺¹,g) is a completeRiemannian manifold and M is an oriented hypersurface partitioningM and with non-zero signature, then the spectrum of the Hodge–deRhamLaplacian is [0,]. This result is obtained by a new Callias-typeindex. This new formula links half-bound harmonic forms (thatis, nearly L² but not in L²) with the signature of .     

Gaussian estimates and L p -boundedness of Riesz means

We show that suitable upper estimates of the heat kernel are sufficient to imply the L ^p boundedness of several families of operators associated with the Schr?dinger group in various situations. This generalizes results by Sj?strand and others in the Euclidean case, and by Alexopoulos in the case of Lie groups and Riemannian manifolds. RID="*" ID="*"Research partially supported by the European Commission (European TMR Network "Harmonic Analysis" 1998-2001, Contract ERBFMRX-CT97-0159).     

Structure of 9,10-di(9,9-dioctylfluorenyl)anthracene in the solid and in solution

A new example of magnetic nonequivalence of chemically equivalent atoms is identified from the proton and carbon resonance spectra of 9,10-di(9,9-dioctylfluorenyl)anthracene with the aid of its conformation in the crystalline state. Molecular modeling suggests that it has a similar conformation in solution.     

Etude comparative des proprietes magnetiques des oxydes lamellaires ACrO2 (A = Li,Na, K)—I: Etude par effet Mössbauer de LiCrO2 dope par le fer

A Mössbauer study of the dimensionality of magnetic interactions in the layer oxide LiCr_0.99Fe_0.01O₂ shows a 2-D behaviour.     

Étude de la dissipation d'énergie dans la fission de 234u à l'aide de la réaction 233U(d,pf)

The energy balance in the fission of ²³⁴U has been investigated on the basis of experimental results from the ²³³U(d, pf) reaction. Taking into account the neutron evaporation we have deduced the total kinetic energy and excitation energy distributions of the primary fragments as functions of the excitation energy of the fissioning nucleus. The neutron evaporation temperatures have been adjusted so as to reproduce the average value and width of the measured kinetic energy distributions for each fragmentation. Excitation energy distributions of the fragments have been deduced. The data are discussed in the framework of the liquid-drop model with shell corrections. Evidence for energy dissipation in the fission of ²³⁴U, involving drastic changes in the scission configuration, is shown for some fragmentation modes.     

Reduction of β-ketosulfoxides : a highly efficient asymmetric synthesis of both enantiomers of methyl carbinols from the corresponding esters

It is shown that reductions of β-ketosulfoxides of identical chirality (R) at sulfur, lead to reduction products of opposite stereochemistry according to the reducing agent used. The high enantiomeric excesses obtained (80 to 100%) provide a general route to both enantiomers of methylcarbinols from the corresponding esters.     

Symetries isometriques applications a la dualite des espaces reticules

We show that ifE is a non-reflexive Banach lattice, there exists for everyn a dual of finite even order ofE which contins isometicallyl _n ^/l . We show that itE is a Banach lattice which is isometric to the dual of a Banach spaceX, then the order intervals are σ (E, X)-compact. We prove then that under various conditions, a Banach lattice which is a dual as a Banach space, is a dual as a Banach lattice. In particular, this is true when the predual ofE is unique.