Biovector Therapeutics, S.a.

Kobo Products, Inc.

Kobo Products S.a.r.l.

A Et S Biovecteurs

Pascal E Delrieu

Li Ding

Daniel Samain

Ignacio De Miguel

Monique Cervilla

Karim Ioualalen

Valerie Rieumajou

Laurent Imbertie

Jaouad Meniali

Didier Betbeder

Roger Kravtzoff

Michel Major

Frederique Nguyen

Joelle Gibilaro

Fr&eacute;d&eacute;rique N'guyen

Nadine Candelotto

Roselyne Dirson

Corinne Soler

Nadine Soulet

Igancio De Miguel

Corinne Segreto

Gel particles or beads can be prepared by forming a hot aqueous solution of a gelling agent, and discharging the hot gelling agent solution through a discharge orifice into a cold moving stream of hydrophobic liquid so that the gelling agent solution cools rapidly and good quality gel particles coalesce in the cold hydrophobic liquid stream. The cold hydrophobic liquid stream can be contained in a conduit so that the cold hydrophobic liquid stream moves past the discharge orifice and exerts a force on hot solution in the discharge orifice, the force acting to withdraw the hot solution from the discharge orifice. Optionally, the gel particles can be crushable gel beadsformed of an agar complex providing cosmetic, pharmaceutical, etc. delivery vehicles for topical delivery of biologically or cosmetically active agents. Preferred agar beadsare complexes of a continuous phase of agar gelin a self-supporting solid or semi-solid form with a restraining polymer. Various active agentsmay be bound to restraining polymer, for, example ascorbic acid, lactic acid or papain.

Cosmetic particulate gel carriers for topically applied active agents

A synthetic particulate vector comprising a non-liquid hydrophilic nucleus which does not have an external lipid layer grafted thereon. A method for preparing a particulate vector by encapsulating an ionizable active principle, vectors obtainable through said method, and pharmaceutical, cosmetological or food compositions containing such vectors are also disclosed.

Synthetic particulate vectors and preparation process

Crushable gel beads,formed of an agar complex provide novel cosmetic, pharmaceutical, etc. delivery vehicles for topical delivery of biologically or cosmetically active agents. Preferred agar beads,are complexes of a continuous phase of agar gel,in a self-supporting solid or semi-solid form with a restraining polymer,Entrapped in and dispersed randomly throughout each agar bead,is a water-soluble, preferably polar, restraining polymer,preferably a quaternized cationic polymer, such as polyquaternium 24 or steardimonium hydroxyethylcellulose. Various active agents,may be bound to restraining polymer,for example ascorbic acid, lactic acid or papain. Methods of manufacture are also described.

Agar gel bead composition and method

A biodegradable particulate vector for transporting biologically active molecules is prepared containing a nucleus formed of a cross-linked polysaccharide or oligosaccharide matrix having grafted ionic ligands, a layer of fatty acid compounds covalently bonded to the nucleus and a layer of phospholipids hydrophobically bonded to the layer of fatty acid compounds. Dextran, cellulose or starch may be cross-linked with epichlorohydrin to form a cross-linked polysaccharide matrix. Ionic ligands may be grafted using an acidic compound such as succinic acid, phosphoric acid or phosphorous oxychloride, or a basic compound such as choline, hydroxycholine, 2-(dimethylamino)ethanol or 2-(dimethylamino) ethylamine fastened onto the grafted acidic compound. Phosphoric acid or phosphorous oxychloride in one step provide both cross-linking and ionic ligands. Co-cross-linking can be obtained using a protein such as keratin, collagen or elastase. The vector may be prepared by reacting succinic acid monochloride with a cross-linked polysaccharide matrix to graft succinic acid onto the matrix to form the nucleus having ionic ligands, grinding the nucleus to a size between 10 .mu.nm and 10 .mu.m, drying, coupling fatty acid compounds to the nucleus and hydrophobically bonding phospholipids to the fatty acid compounds. After coupling the fatty acid compounds and before bonding the phospholipids, a molecule having biological activity may be added. The succinic acid monochloride is preferably prepared by reacting succinic acid dichloride with free succinic acid to form pure crystalline succinic acid monochloride.

Biodegradable particulate vector for transporting molecules having

A protective cosmetic particulate gel delivery system for a topically applied active agent employs an agar gel and a restraining polymer to retain the actve agent in the gel. The particles have an average particle diameter of at least 0.05 mm while the restraining polymer has a molecular weight of at least 50,000 daltons and has retention groups to bind the active agent. The restraining polymers can be selected from the group consisting of polyquaternium 24, laurdimonium hydroxyethylcellulose, cocodimonium hydroxyethylcellulose, steardimonium hydroxyethylcellulose, quaternary ammonium substituted water-soluble polysaccharides, alleyl quaternary celluloses and polypeptides having or provided with retention groups to retain the active agent. The gel particles of the invention are manually crushable on the skin to increase the surface area of the gel particle material and expose the restraining polymer to the skin or other body surface for release of the active agent. The delivery system can be incorporated in multiphase cosmetic formulations such as gels, creams and lotions.

Cosmetic particulate gel delivery system and method of preparing complex

Lecithin-type liposomes are stabilized with quaternized alkyated polymers, such as steardimonium hydroxyethylcellulose, to provide excellent stability for cosmetic and pharmaceutical formulations. Temperature, storage, solvent, and acidity stability are described. The stabilized liposomes can serve as vectors for alpha-hydroxy acids and showed no aggregation even after 4 months of storage at pH 2.

Stabilized liposomes

A biodegradable particulate vector for transporting biologically active molecules is prepared containing a nucleus for containing a biologically active molecule, a first layer of fatty acid compounds covalently bonded to the nucleus and a second layer of phospholipids hydrophobically bonded to the first layer. The nucleus is between 10 nm and 10 .mu.m in size and is formed of a cross-linked polysaccharide or oligosaccharide matrix onto which ionic ligands are uniformly grafted. The cross-linked polysaccharide may be dextran, cellulose or starch cross-linked with epichlorohydrin. The ligand may be an acidic compound selected from succinic acid, phosphoric acid, citric acid, glycine, alanine, glutamic acid and aspartic acid, or a basic compound such as choline, hydroxycholine, 2-(dimethylamino)ethanol or 2-(dimethylamino)ethylamine fastened onto the matrix via the acidic compound. The polysaccharide or oligosaccharide may be co-cross-linked with a protein such as keratin/collagen or elastase. The vector may be prepared by reacting succinic acid monochloride in aqueous solution with a cross-linked polysaccharide or oligosaccharide matrix to graft succinic acid onto the matrix to form the nucleus, grinding the nucleus to a size between 10 nm and 10 .mu.m, drying the ground nucleus, coupling fatty acid compounds to the nucleus to form a first layer and hydrophobically bonding phospholipids to the first layer to form a second layer. The succinic acid monochloride is preferably prepared by reacting succinic acid dichloride with free succinic acid to form pure crystalline succinic acid monochloride.

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Castanet Tolosan, France

Pascal E Delrieu