References of "Riva, Raphaël"
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See detailMetal-free synthesis of a glucosamine labeled amphiphilic polymer for drug delivery applications
Riva, Raphaël ULg; Boyère, Cécric; Debuigne, Antoine ULg et al

Poster (2014, May 19)

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See detailDrug delivery systems based on PEO-b-polyphosphate copolymers
Vanslambrouck, Stéphanie ULg; Clément, Benoit; Riva, Raphaël ULg et al

Poster (2014, May)

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See detailElaboration of drug nanocarriers based on a glucosamine labeled amphiphilic polymer
Boyère, Cédric; Duhem, N; Debuigne, Antoine ULg et al

in Polymer Chemistry (2014), 5(8), 3030-3037

A new functional polymer micelle with high loading efficiency of a poorly soluble drug was made of biocompatible and/or biosourced compounds, i.e. cholesterol-poly(ethylene glycol)-glucosamine (Chol-PEG ... [more ▼]

A new functional polymer micelle with high loading efficiency of a poorly soluble drug was made of biocompatible and/or biosourced compounds, i.e. cholesterol-poly(ethylene glycol)-glucosamine (Chol-PEG-GlcNH2). A synthesis strategy combining enzymatic and metal-free click chemistry was developed in order to meet the increasingly stringent requirements of biomedical applications. After the self-assembly of the Chol-PEG-GlcNH2 amphiphilic polymer in water, the presence of glucosamine at the micelle surface confers an active targeting moiety to the nanocarriers whereas protonation of the peripheral primary amine delay their aggregation. The complete characterization of this novel functional amphiphilic bioconjugate is presented as well as its aqueous solution behaviour and encapsulation efficiency using ketoconazole as a model hydrophobic drug. [less ▲]

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See detailChitosan nanoparticles for siRNA delivery: Optimizing formulation to increase stability and efficiency
Ragelle, Héloïse; Riva, Raphaël ULg; Vandermeulen, G. et al

in Journal of Controlled Release (2014), 176

This study aims at developing chitosan-based nanoparticles suitable for an intravenous administration of small interfering RNA (siRNA) able to achieve (i) high gene silencing without cytotoxicity and (ii ... [more ▼]

This study aims at developing chitosan-based nanoparticles suitable for an intravenous administration of small interfering RNA (siRNA) able to achieve (i) high gene silencing without cytotoxicity and (ii) stability in biological media including blood. Therefore, the influence of chitosan/tripolyphosphate ratio, chitosan physicochemical properties, PEGylation of chitosan as well as the addition of an endosomal disrupting agent and a negatively charged polymer was assessed. The gene silencing activity and cytotoxicity were evaluated on B16 melanoma cells expressing luciferase. We monitored the integrity and the size behavior of siRNA nanoparticles in human plasma using fluorescence fluctuation spectroscopy and single particle tracking respectively. The presence of PEGylated chitosan and poly(ethylene imine) was essential for high levels of gene silencing in vitro. Chitosan nanoparticles immediately released siRNA in plasma while the inclusion of hyaluronic acid and high amount of poly(ethylene glycol) in the formulation improved the stability of the particles. The developed formulations of PEGylated chitosan-based nanoparticles that achieve high gene silencing in vitro, low cytotoxicity and high stability in plasma could be promising for intravenous delivery of siRNA. [less ▲]

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See detailDevice-based controlled local delivery of anastrozol into peritoneal cavity: in vitro and in vivo evaluation
Krier, Fabrice ULg; Riva, Raphaël ULg; Defrère, Sylvie et al

in Journal of Drug Delivery Science and Technology [=JDDST] (2014), 24(2), 198-204

Local treatment using drug loaded implants allows decreasing seric concentrations of the active ingredient with the purpose of limiting side effects and reaching perfect observance. Nowadays, some ... [more ▼]

Local treatment using drug loaded implants allows decreasing seric concentrations of the active ingredient with the purpose of limiting side effects and reaching perfect observance. Nowadays, some diseases are already treated with implants, but generally, by subcutaneous or intra vaginal implantation. In this work, a new implant device dedicated to the intra-peritoneal cavity was developed. For this purpose, a core-membrane polymer implant was selected. We propose an original method to determine the most appropriate membrane to control the release based on the use of Franz cells. The ability of the implant to release a constant quantity of an active ingredient will be assessed by testing implants in vitro. Finally, intra peritoneal cavity and subcutaneous in vivo implantation has been achieved in order to confirm the controlled and local release of the active ingredient. [less ▲]

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See detailChitosan: a versatile platform for pharmaceutical applications
Riva, Raphaël ULg; Jérôme, Christine ULg

in Material Matters: Chemistry Driving Performance (2014), 9(3), 95-98

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See detailReversibly cross-linked polymer micelle as smart drug dellivery device
Lecomte, Philippe ULg; Riva, Raphaël ULg; Cajot, Sébastien et al

Conference (2013, November 20)

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See detailDrug delivery systems based on amphiphilic polyphosphate-copolymers
Vanslambrouck, Stéphanie ULg; Clement, Benoît ULg; Riva, Raphaël ULg et al

Poster (2013, September 18)

Thanks to their biocompatibility, biodegradability and their structure similar to natural biomacromoleculesn such as nucleic acids, polyphosphates (PPhos) are of prime interest as biomaterials. In ... [more ▼]

Thanks to their biocompatibility, biodegradability and their structure similar to natural biomacromoleculesn such as nucleic acids, polyphosphates (PPhos) are of prime interest as biomaterials. In contrast to poly--caprolactone and polylactides, PPhos properties and functionality are easily tuned via the nature of the pendant group of the starting cyclic monomer. For example, by varying the length of the alkyl chain the hydrophobicity of the PPhos can be adjusted. In this work, an efficient organo-catalytic system was developed to synthesize a series of amphiphilic diblock copolymers, i.e. poly(ethylene oxide)-b-polyphosphate (PEO-b-PPhos) by ring-opening polymerization of cyclic phosphates. This novel approach prevents metallic residues to polute the final product, and which is highly desirable when biomedical applications are foreseen. For drug delivery application, the micellization of these novel diblock copolymers in aqueous media was investigated, as well as, encapsulation of an hydrophobic drug. Data on, the influence of the polyphosphate nature of the polymer on drug loading will be presented. [less ▲]

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See detailTailor made amphiphilic copolymers for the design of smart drug delivery systems
Riva, Raphaël ULg; Cajot, Sébastien; Jérôme, Christine ULg

Conference (2013, August 21)

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See detailDevice-based controlled local delivery for the treatment of peritoneal pathologies
Riva, Raphaël ULg; Krier, Fabrice; Defrère, Sylvie et al

Poster (2013, August 18)

This contribution aims at reporting the developpment of a controlled drug delivery system (DDS) dedicated to the treatment of intra-peritoneal pathologies, especially endometriosis. At present time ... [more ▼]

This contribution aims at reporting the developpment of a controlled drug delivery system (DDS) dedicated to the treatment of intra-peritoneal pathologies, especially endometriosis. At present time, endometriosis is generally treated by daily oral absorption of drug with the purpose to improve the life quality of patients by the reduction of the pain caused by endometrial lesions. Nevertheless, deleterious side-effects, mainly infertility, are observed as a consequence of the important amount of absorbed active principle. One main advantage of controlled drug delivery devices, e.g. polymer implants, is to maintain sustained drug release over a prolonged period of time thereby eliminating fluctuations in the drug plasma concentration. Moreover, DDS allows a local release of the drug at a specific area, which significantly decreases the active principle concentration in the body and limits side-effects. The peritoneal cavity is a convenient site for the implantation of a DDS against endometriosis because large parts of lesion are localized in this region. At our knowledge, no application of an implant dedicated to the treatment of endometriosis is reported in the literature, whereas the local controlled release of an active principle presents several advantages compared to systemic administration. In this study, anastrozole (2,2’-[5-1H-1,2,4-triazole-1-yl-methyl)-1,3-phenylene]bis(2-methylpropiononitrile)), a well-known aromatase-inhibiting drug, was selected as active molecule. Typically, two non-biodegradable polymers were tested for the elaboration of an anastrozole loaded intra-peritoneal implant, namely polydimethylsiloxane (PDMS) and poly(ethylene-co-vinyl acetate) (EVA). As preliminary research, the ‘in vivo’ biocompatibility of PDMS and EVA in the intra-peritoneal cavity was confirmed by implantation of PDMS and EVA rod-shaped implants in rats. The kinetic of release was determined ‘in vitro’ and confirmed ‘in vivo’. Besides, the efficiency of the implants was improved by the addition of a polymer membrane, which allowed a controlled release of anastrozole over a period of 400 days. [less ▲]

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See detailNovel functional degradable block copolymers for the building of reactive micelles
Cajot, Sébastien; Lecomte, Philippe ULg; Jérôme, Christine ULg et al

in Polymer Chemistry (2013), 4(4), 1025-1037

Amphiphilic biocompatible copolymers are promising materials for the elaboration of nanosystems for drug delivery applications. This paper aims at reporting on the synthesis of new functional amphiphilic ... [more ▼]

Amphiphilic biocompatible copolymers are promising materials for the elaboration of nanosystems for drug delivery applications. This paper aims at reporting on the synthesis of new functional amphiphilic copolymers based on biocompatible and bioeliminable blocks. Poly(ethylene oxide) was selected as the hydrophilic block, whereas an aliphatic polyester, i.e. poly(epsilon-caprolactone), or a polycarbonate, i.e. poly(trimethylene carbonate), were chosen as the degradable hydrophobic block. In order to allow a post-functionalization of the micelles core, azide groups were introduced on the hydrophobic segment to provide reactivity towards functional alkyne derivatives by the copper azide-alkyne cycloaddition (CuAAC). For this purpose, a functional lactone, i.e. alpha-chloro-epsilon-caprolactone was introduced during the polymerization of the hydrophobic block before being converted into azide on the preformed copolymer. Such reactivity of the block copolymers and their self-assemblies is of prime interest for drugs or fluorescent dyes grafting, so as for micelles cross-linking. The influence of the azides distribution along the degradable block on the micelles post-functionalization ability has been studied by using alkyne bearing fluorescent dyes as model for drugs. The hydrophilicity of the dye on the micelles post-functionalization efficiency has also been investigated. [less ▲]

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See detailFunctional degradable polymers for advanced drug delivery systems
Cajot, Sébastien; Riva, Raphaël ULg; Jérôme, Christine ULg

Conference (2012, September)

Nowadays, polymer micelles have attracted an increasing interest in pharmaceutical research because they could be used as efficient drug delivery systems. Micelles of amphiphilic block copolymers are ... [more ▼]

Nowadays, polymer micelles have attracted an increasing interest in pharmaceutical research because they could be used as efficient drug delivery systems. Micelles of amphiphilic block copolymers are supramolecular core-shell type assemblies of several tens of nanometers in diameter. In principle, the micelle core is usually constructed with biodegradable hydrophobic polymers such as aliphatic polyesters, e.g. poly(ε-caprolactone) (PCL), which serves as a reservoir for the incorporation of various lipophilic drugs. Water soluble poly(ethylene oxide) (PEO) is most frequently used to build the micelle corona because it is very efficient in preventing protein adsorption at surfaces and in stabilizing micelles in the blood compartment, making particles invisible to the body defense system. Even if micelles get a high stability in aqueous media thanks to their low critical micellar concentration, micelle dissociation is not always preserved when they are injected in the blood compartment. A way to provide the micelle stability during their administration is to cross-link them. Different kinds of cross-linked micelles can be investigated depending on the localization of the cross-linking. Shell cross-linked micelles or nanocage structures with a degradable core have the great advantage to reach drug encapsulation with a high loading rate. However, cross-linking the hydrophilic shell may affect the stealthiness of the carrier. Thus, we have designed reversibly cross-linked micelles by introducing the cross-linking bridges in the hydrophobic segment of the block copolymer, rather than in the hydrophilic one, leading so to more internal cross-linking and thus preserving the mobility of the hydrophilic segment. Three different localizations of the cross-linking has been targeted; (i) loose core cross-linking of a core-corona system, (ii) tight core cross-linking of a core-shell-corona system (the shell and the core being both hydrophobic and the corona hydrophilic) and (iii) tight shell cross-linking of a similar core-shell-corona system. To reach this goal, three types of amphiphilic copolymers have been used bearing pendent azide groups in the hydrophobic segment. These copolymers have been obtained by starting the ring-opening polymerization of ε-CL and a functional CL, either as a mixture or sequentially from a poly(ethylene oxide) macroinitiator leading to the three targeted architectures. The azide groups located along the PCL backbone have then been used to cross-link the micelles by the Huisgens cycloaddition with a bis-alkyne cross-linker. The choice of this cross-linker has also taken into account the requirement to make the cross-linking reversible. For that purpose, disulfide bridges have been selected in order to impart reversibility to the cross-linking by intracellular reduction. Indeed, the marked concentration difference of glutathione between extra- and intra-cellular environments has already been used to trigger drug release by intracellular disulfide bond cleavage. Accordingly, a bis-alkyne disulfide molecule has been chosen as cross-linker. The micellization and cross-linking of these amphiphilic azido macromolecules have been studied. The reversibility of the cross-linking in reductive environment and the cross-linked micelles stealthiness have been tested. [less ▲]

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