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Colloidal suspension of submicronic particles for carrying active principles and their mode of preparation

a technology of carrier particles and colloidal suspensions, which is applied in the field of colloidal suspensions of carrier particles, can solve the problems of disclosing the use of copolymers, and achieve the effect of high bioavailability of ap and easy and economical production

Inactive Publication Date: 2008-01-17
FLAMEL TECHNOLOGIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009] 1 The first specification sought for the CP would be that the polymer constituting the CP is biocompatible, capable of elimination (by excretion) and / or biodegradable, and particularly that it is metabolized to products that are non-toxic to the organism. In addition, the biodegradation in the organism should be of a sufficiently short duration.
[0161] Given the nanometric size of the particles, the suspension can be filtered on sterilization filters, enabling sterile injectable medicinal liquids to be obtained easily and at lower cost. The ability, afforded by the invention, to control the particle size and reach Dh values of between 25 and 100 nm is an important asset.

Problems solved by technology

However, FR-A-2 746 035 does not disclose the use of the copolymers by themselves as a nanoparticulate pharmaceutical system for carrying AP.

Method used

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  • Colloidal suspension of submicronic particles for carrying active principles and their mode of preparation

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Poly(Leucine / Methyl Glutamate) Block Copolymer

[0183] The techniques used to polymerize NCA to polymers with block or random structures are known to those skilled in the art and are described in detail in the work by H. R. KRICHELDORF entitled “α-Amino acid N-carboxy anhydrides and related heterocycles”, Springer Verlag (1987). The synthesis of one such polymer is specified below.

[0184] Synthesis of poly(Leu)40poly(GluOMe)80: 10 g of NCA-GluOMe are solubilized in 150 ml of NMP at 60° C. 5 ml of a solution of 0.91 g of benzylamine in 50 ml of NMP are added all at once to the monomer. After 1 h, 14.1 g of NCA-Leu, previously solubilized in 20 ml of NMP, are added. Polymerization continues for a further 3-4 h.

[0185] Sampling of the reaction medium affords the following characterizations: Yield: 90%. Composition by 1H NMR (TFA-d): 66 mol % of GluOMe. Reduced viscosity (0.5% of TFA at 25° C.): 0.4 dl / g. Molecular weight by GPC: 20,000 g / mol.

example 2

Aminolysis of Poly(Leucine / Methyl Glutamate) Block Copolymer with Hydroxyethylamine

[0186] 10 g of hydroxyethylamine are added all at once to the NMP solution of polymer prepared according to Example 1. The medium is heated to 80° C. and kept at this temperature for 2 days. 150 ml of water are then added to the polymer solution, which is then purified by a dialysis step to ensure removal of the excess amine and the NMP. Finally, the particles are isolated by lyophilization.

[0187] Yield: quantitative. 1H NMR (TFA-d): 8% of residual methoxy (3.5 ppm); 92% of hydroxyethylglutamine. Composition by 1H NMR (TFA-d): 34% of Leu. Particle size (light scattering, QLS mode): 100 nm.

example 3

Demonstration of Nanoparticles by Light Scattering (LS) and Transmission Electron Microscopy (TEM)

[0188] 10 mg of particles of polymer 1 are suspended in 10 ml of water or an aqueous solution of salt. This solution is then introduced into a Coulter granulometer (or laser diffractometer). The results of particle size analysis of the different products tested are shown in Table 1 below.

TABLE 1Measurement of the size of the CPExamplePolymerSize (nm)2poly[(Leu)0.66]-poly[(Gln-N-100hydroxyethyl)0.37]x block copolymer

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Abstract

The invention concerns a suspension of biocompatible particles for carrying active principles. Said carrier particles are based on a double-block hydrophilic neutral polyaminoacid / hydrophobic neutral polyaminoacid copolymer. Said hydrophilic neutral polyaminoacid / hydrophobic neutral polyaminoacid particles are capable of combining in colloidal suspension in non-dissolved state, at least an active principle and of releasing same, in particular in vivo, in prolonged and / or delayed delivery. The invention also concerns a powdery solid from which are derived the carrier particles and the preparation of said solid and of said suspension of active principle based on hydrophilic neutral polyaminoacids / hydrophobic neutral polyaminoacids. Said carrier particles form spontaneously and in the absence of surfactants or organic solvents, stable aqueous suspensions. The invention also concerns the carrier particles in dry form, the method for preparing them, and pharmaceutical compositions (in dry form or suspension) comprising said carrier particles associated with an active principle.

Description

TECHNICAL FIELD [0001] The present invention relates to the field of carrier particles (CP) that are useful for the administration of active principles (AP). The latter are preferably drugs or nutriments for administration to an animal or human organism by the oral or nasal, vaginal, ocular, subcutaneous, intravenous, intramuscular, intradermal, intra-peritoneal, intracerebral, parenteral or other route. However, they can also be cosmetic products or plant health products such as herbicides, pesticides, insecticides, fungicides, etc. In terms of their chemical nature, the AP to which the invention relates more particularly, but without implying a limitation, are e.g. proteins, glycoproteins, peptides, polysaccharides, lipopolysaccharides, oligo-nucleotides, polynucleotides and organic molecules. [0002] The present invention relates more precisely to colloidal suspensions of carrier particles, advantageously of the submicron type, that are based on polyamino acids (PAA). [0003] The p...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C08G69/08A61K47/42A61K8/02A61K8/04A61K8/11A61K8/64A61K8/72A61K9/10A61K9/14A61K9/51A61K9/66A61K38/28A61K45/00A61Q19/00B01J13/00
CPCA61K8/11A61K9/5138B01J13/0021A61K2800/413A61Q19/00A61K9/5146A61K47/30
Inventor BRYSON, NATHANSOULA, GERARD
Owner FLAMEL TECHNOLOGIES
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