Microparticles with cyclodextrins having a dual level of encapsulation

Patent metadata

Field	Value
Publication number	US-2016175229-A1
Application number	US-201414896943-A
Country	US
Kind code	A1
Filing date	Jun 16, 2014
Priority date	Jun 14, 2013
Publication date	Jun 23, 2016
Grant date	—

Abstract

Microparticles include a solid and porous matrix which includes at least one biocompatible polymer. The matrix includes, within its pores, water and at least one inclusion complex formed between a cyclodextrin and at least one first active ingredient. The microparticle is characterized in that the first active ingredient is selected in the group constituted by cosmetic active ingredients and dermatological active ingredients for topical use and in that the microparticle further includes at least one second cosmetic or dermatological active ingredient for topical use which is not in the form of an inclusion complex with the cyclodextrin.

First claim

1 . A microparticle which includes a solid and porous matrix, said matrix comprising at least one biocompatible polymer and including, within its pores, water and at least one inclusion complex formed between a cyclodextrin and at least one first active ingredient, wherein the first active ingredient is selected in the group constituted by cosmetic active ingredients and dermatological active ingredients for topical use and said microparticle further comprises at least one second cosmetic or dermatological active ingredient for topical use which is not in the form of an inclusion complex with the cyclodextrin.

2 . The microparticle according to claim 1 , wherein the pores that the matrix includes are closed.

3 . The microparticle according to claim 1 , wherein said second ingredient is a hydrophilic active ingredient which is contained in the pores of the and/or a second hydrophobic active which is matrix and/or a second hydrophobic active ingredient which is solubilized in the matrix.

4 . The microparticle according to claim 1 , wherein it comprises a plurality of inclusion complexes formed from a plurality of cyclodextrins which are identical or different from each other and a plurality of first active ingredients which are identical or different from each other.

5 . The microparticle according to claim 1 , wherein the first active ingredient and the second active ingredient are cosmetic ingredients which are selected in the group constituted by the active ingredients having an anti-ageing effect, an anti-wrinkle effect, an anti-redness effect, a moisturizing effect, a soothing effect, a brightening effect, a plumping effect or still a purifying effect.

6 . The microparticle according to claim 1 , wherein the first active ingredient is selected in the group constituted by hesperidin, the hesperidin derivatives, the lipoic acid and the lipoic acid derivatives.

7 . The microparticle according to claim 1 , wherein the second active ingredient is selected in the group constituted by tocopherol acetate, the pyrrolidone carboxylic acid, caffeine, amino acids, peptides, oligosaccharides, polysaccharides, menthol, methyl nicotinate, unsaturated fatty acids, retinol, tocopherol and their derivatives.

8 . An aqueous suspension, wherein it comprises microparticle according to claim 1 .

9 . The aqueous suspension according to claim 8 , wherein it further comprises at least one third active ingredient selected in the group constituted by cosmetic active ingredients and dermatological active ingredients for topical use.

10 . A cosmetic or dermatological composition for topical use, wherein it comprises at least microparticles according to claim 1 .

11 . A cosmetic or dermatological composition for topical use, wherein it comprises at least one aqueous suspension according to claim 8 .

12 . A method for producing microparticle according to claim 3 , wherein it comprises the following steps consisting in:
a) preparing a first aqueous solution which comprises at least one first active ingredient selected in the group constituted by the cosmetic active ingredients and the dermatological active ingredients for topical use, and at least one cyclodextrin, the amounts of the first active ingredient and the cyclodextrin being determined so that the first active ingredient and the cyclodextrin form an inclusion complex, said first aqueous solution further comprises at least one second active ingredient, in the case where the second ingredient is a hydrophilic ingredient; b) preparing a second organic solution which comprises at least one organic solvent and at least one biocompatible polymer, the organic solvent solubilizing the biocompatible polymer, said second organic solution further comprises at least one second active ingredient, in the case where the second active ingredient is a hydrophobic ingredient; c) introducing the first aqueous solution in the second organic solution and stirring this set, which set results from the combination of these two solutions, so as to obtain an aqueous-in-organic type emulsion; d) introducing this emulsion which has been obtained upon completion of step c) in a third aqueous solution and stirring this set, which set results from the combination of the emulsion and the third solution, so as to obtain an aqueous-in-organic-in-aqueous type double emulsion; e) extracting the organic solvent by means of a water-soluble organic co-solvent; f) evaporating the organic solvents and co-solvents, so as to obtain an aqueous suspension of the microparticles; g) optionally, recovering the microparticles.

Assignees

• Lca Dermatech
• Centre Nat Rech Scient
• Univ Claude Bernard Lyon

Inventors

• Delalande Charlotte
• Burtin Frédéric
• Chevalier Yves
• Bolzinger Marie-Alexandrine
• Pelletier Jocelyne

Classifications

• A61K8/0287

  the particulate containing a solid-in-solid dispersion · CPC title

• A61K8/678

  Tocopherol, i.e. vitamin E · CPC title

• C08B37/0015

  Inclusion compounds, i.e. host-guest compounds, e.g. polyrotaxanes · CPC title

• A61K8/602

  Glycosides, e.g. rutin · CPC title

• A61K2800/56

  Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms · CPC title