Centre National De La Recherche Scientifique

Université Paris-Saclay

Da Volterra

Other

Assistance Publique-hopitaux De Paris

Université Paris Diderot-Paris 7

Institut Gustave Roussy

Université Paris-Sud 11

Nicolas Tsapis

Elias Fattal

Antoine Andremont

Franceline Reynaud

Helene-Celine Huguet

Laurence Moine

Julien Nicolas

Helene Huguet

Frédéric Deschamps

Alexandre Bordat

Tanguy Boissenot

Thomas Isoardo

Nicolas Huang

Lambros Tselikas

Thierry De Baere

Romain Canioni

Mathilde Lorscheider

Hélène-Céline Huguet

The present invention relates to a water-in-oil emulsion comprising a continuous oil phase and an aqueous phase dispersed in the form of drops, the said aqueous phase comprising polyester-based nanoparticles and at least one therapeutic agent.

Injectable water-in-oil emulsions and uses thereof

The invention relates to new prodrugs of active molecules. These prodrugs allow, in particular, the subcutaneous or intramuscular administration of active molecules of which the subcutaneous or intramuscular administration is problematic or impossible, in particular because of the toxicity at the injection site. The prodrugs according to the invention comprise an active ingredient, covalently linked with a polymer chain, preferably a hydrophilic and/or thermosensitive polymer chain. The invention relates, in particular, to polymeric prodrugs comprising a polymer chain formed at least in part by acrylamide monomer or one of its derivatives, said polymer comprising a proximal part and a terminal part; a first pharmaceutically active molecule covalently coupled to the proximal part of the polymer; possibly a second pharmaceutically active molecule covalently coupled to the terminal part of the polymer.

Polymeric prodrugs and subcutaneous and/or intramuscular administration thereof

The present invention relates to anti-inflammatory drug formulation. Especially, this invention relates to corticosteroid prodrug nanoparticle. In a first aspect, this invention relates to a nanoparticle comprising a therapeutic agent and a surface coating material. The invention also relates to a process of manufacturing at least one nanoparticle of invention. The invention also relates to pharmaceutical composition and pharmaceutical kits.

Nanoparticulate prodrugs

The present invention relates to a galenic form comprising particles capable of specifically adsorbing the undesirable molecules present in the digestive tract, to the method for preparing same and to the use thereof in particular for producing a medicine intended for preventing or treating undesirable effects linked to an imbalance of the intestinal and/or colonic flora that can result for example from treatment with antibiotics.

Galenic form suitable for absorbing, in a specific manner, the undesirable molecules in the digestive tract

Compositions which deliver adsorbents, alone or in combination with active drug 'degrading molecules,' in a site-specific manner to the intestine, and which eliminate or at least lower the concentration of residual unwanted material within the intestine, and methods of treatment using the compositions, are disclosed. The compositions are ideally designed to specifically release the adsorbents in a programmed manner at a specific site of the intestinal tract. Programmed delivery prevents adsorbents from interfering with the normal absorption process of a given molecule after oral absorption, until it reaches the lower part of the small intestine. The compositions can be used to adsorb, and therefore remove, any residual drug, metabolite thereof, or bacterial toxin after oral or parenteral administration which would otherwise cause adverse effects in the lower intestine and/or colon.

Site-specific intestinal delivery of adsorbents, alone or in combination with degrading molecules

Orally administrable, site-specific (colonic), particulate delivery systems including adsorbents are disclosed. When delivered specifically to the colon, they can remove various substances present in, or as they reach, the colon. Methods of treatment using the delivery systems, and methods of preparing the delivery systems, are also disclosed. The particulate delivery systems are based on adsorbent matrices encapsulated into and/or onto particles, which selectively deliver the adsorbents to the colon. Representative drug delivery devices include pectin beads, which can optionally be crosslinked with metal ions such as zinc and/or calcium. The delivery system protects the adsorbent and prevents its adsorbing effect in the upper gastro-intestinal (GI) tract. When the particles are made from pectin, and the beads are administered to the colon, specific pectinolytic enzymes in the colon degrade the pectin, allowing the adsorbent to be released and to be fully active. Antibiotics, toxins, and other absorbable substances present in the colon will then be inactivated by adsorption into or onto the adsorbent.

Colonic delivery of adsorbents

Compositions which deliver adsorbents, alone or in combination with active drug 'degrading molecules,' in a site-specific manner to the intestine, and which eliminate or at least lower the concentration of residual unwanted material within the intestine, are disclosed. Methods of treatment using the compositions are also disclosed. The material to be eliminated can include residual active antibiotics, metabolites, bacterial or other toxins, and drugs which cause side effects in the gastrointestinal tract. The adsorbents can be formulated in capsules, tablets or any acceptable pharmaceutical composition, and are ideally designed to specifically release the adsorbents in a programmed manner at a specific site of the intestinal tract. The programmed delivery prevents adsorbents from interfering with the normal absorption process of a given molecule after oral absorption, until it reaches the lower part of the small intestine. The compositions can be used to adsorb, and therefore remove, any residual drug, metabolite thereof, or bacterial toxin after oral or parenteral administration which would otherwise cause adverse effects in the lower intestine and/or colon.

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Paris, France

Nicolas Tsapis