Flamel Technologies

Stéphanie Angot

You-Ping Chan

Olivier Breyne

Gérard Soula

The invention relates to novel materials based on biodegradable polyamino acids, particularly useful for the vectorisation of active principals (PA). The invention further relates to novel, pharmaceutical, cosmetic, dietary or phytosanitary compositions. The invention provides novel polymeric raw material, for use in the vectorisation of PA and with an optimal match for all the requirements of the type: biocompatibility, biodegradability, stability, ability to easily associate with numerous active principals or to solubilise the same and to liberate said active principals in vivo. Said aim is achieved with polyamino acids comprising aspartic and/or glutamate units, some of which carry at least one graft, characterised in that at least one of said grafts is bonded to an aspartic or glutamate unit by means of an amino acids spacer based on Leu, and/or Ileu, and/or Val, and/or Phe and a hydrophobic group with C6-C30 is connected by an ester bond to the spacer.

Polyamino acids functionalised with at least one hydrophobic group and applications thereof particularly therapeutic applications

The invention concerns novel biodegradable polyaminoacid materials, useful in particular for vectoring active principle(s). The invention also concerns novel pharmaceutical, cosmetic dietetic or phytosanitary compositions based on said polyaminoacids. The invention aims at providing a novel polymer raw material, capable of being used for vectoring active principles and enabling optimal fulfillment of all specified requirements: biocompatibility, biodegradability, easy and inexpensive transformation into particles vectoring active principles, the particles being themselves capable of forming colloidal suspensions, of being easily associated with numerous active principles, and of releasing said active principles in vivo. Therefor, the present invention concerns first of all amphiphilic polyaminoacids comprising aspartic acid units and/or glutamic acid units, characterized in that at least part of said units carry grafts, including at least one alpha-tocopherol motif, for example (polyglutamate or polyaspartate grafted with alpha-tocopherol of synthetic or natural origin).

Polyaminoacids functionalized by alpha tocopherol and uses thereof, particular for therapeutic applications

The invention relates to novel materials based on biodegradable polyamino acids that are useful for vectorizing active principle(s)(AP). The aim of the invention is to supply a new polymeric raw material that is used for vectorizing AP and optimally fulfills all requirements concerning biocompatibility, biodegradability, the ability to be easily associated with numerous active principles or solubilize the active principles and to release the active principles in vivo. Such polymers can also be readily and economically transformed into particles vectorizing active principles according to the grafting rate of the hydrophobic groups, said particles being able to form stable aqueous colloidal suspensions. The aim of the invention is achieved by the inventive amphiphile polyamino acids comprising aspartic and/or glutamic units that carry grafts which encompass at least one hydrophobic unit and are linked to the aspartic and/or glutamic units via a rotula containing two amide functions, more particularly via a spacer of the lysine or ornithine type. The amide functions ensure better stability during hydrolysis than comparable products known in prior art. The invention also relates to new pharmaceutical, cosmetic, dietetic, or phytosanitary compositions based on the inventive polyamino acids.

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Lyons, France

Stéphanie Angot