New Topical Formulation for Use in Alopecia

Abstract

The invention relates to a composition comprising a HIF-1a activity potentiating agent for use in a method of preventing or treating hair loss, wherein the HIF-1a activity potentiating agent is an iron chelator, preferably Deferiprone. The invention further relates to a composition for topical application, comprising a HIF-1a activity potentiating agent that is an iron chelator. Furthermore, the invention relates to a method for cosmetic treatment or prevention of hair loss, comprising topical application of a composition comprising a HIF-1a activity potentiating agent that is an iron chelator to an area of skin.

Claims

1-11. (canceled)

12. A composition for topical application, comprising a HIF-1α activity potentiating agent that is an iron chelator.

13. The composition of claim 12, wherein the HIF-1α activity potentiating agent is selected from the group consisting of Deferiprone, Deferoxamine, sodium gluconate, 2,2′-dipyridyl, Deferasirox, and 3-hydroxy-4-oxo-1(4H)-pyridinealanine.

14. The composition of claim 12, wherein the HIF-1α activity potentiating agent is Deferiprone.

15. The composition of claim 14, comprising Deferiprone at a concentration of 0.001-5.0% w/v.

16. The composition of claim 14, comprising Deferiprone at a concentration of 0.005-2.0% w/v.

17. The composition of claim 14, comprising Deferiprone at a concentration of 0.0101% w/v.

18. A method for prevention of hair loss, comprising topical application to an area of skin in a subject in need thereof, of an amount effective to prevent hair loss of the composition according to claim 12.

19. The method of claim 18, wherein the subject is a human subject, and wherein topical application comprises application to a scalp of the human subject.

20. The method of claim 18, wherein the method: a. supports growth of hair; b. supports growth of transplanted hair; c. supports healing of a hair transplant, by supporting the healing of transplanted skin and/or skin in the area surrounding a hair transplant; d. avoids shedding of hair; and/or e. avoids shedding of transplanted hair, by supporting the healing of transplanted follicular units.

21. The method of claim 18, wherein the composition is applied once a day.

22. The method of claim 18, wherein the composition is in the form of a shampoo, a conditioner, a tonic or a lotion.

23. A method for supporting hair growth, supporting healing of a hair transplant, and/or avoiding shedding of hair, comprising topically administering to a subject in need thereof an amount effective of the composition of claim 12 to support hair growth, support healing of a hair transplant, and/or avoid shedding of hair.

24. The method of claim 23, wherein the subject has received a hair transplant, and the method supports growth of transplanted hair, supports healing of transplanted hair, and/or avoids shedding of transplanted hair.

25. The method of claim 24 wherein the method supports healing of transplanted hair by supporting the healing of transplanted skin and/or skin in the area surrounding a hair transplant.

26. The method of claim 24 wherein the method avoids shedding of transplanted hair by supporting the healing of transplanted follicular units.

Description

BRIEF DESCRIPTION OF DRAWINGS

[0063] FIG. 1: 3D hanging drop culture of DPCs. The DPCs aggregate to stable spheroids over a period of 72 hours. After spheroid formation is complete, the samples are transferred into a 96 well plate for further cultivation and drug exposure.

[0064] FIG. 2: Deferiprone significantly enhances DPC proliferation in a 3D spheroid culture model. (A) Representative images of spheroids stained for newly synthesized cells were taken after drug exposure for 12 hours (left column) and 24 hours (right column) respectively. Scale bars: 200 μm. (B) While Deferiprone treatment left the migratory activity of DPCs in culture unchanged, Minoxidil exposure resulted in a reduction of physiological cell motility demonstrated by a significantly reduced radius of migration around the spheroids after 24 hours. (C) Evaluating the synthesis of new daughter cells demonstrated a significantly enhanced proliferative activity for both Minoxidil and Deferiprone.

EXAMPLE SECTION

Example 1

Preparation of a Topical Hair Tonic Composition

[0065] The present invention is illustrated by the following preparation of a topical hair tonic composition; to which it is of course not limited. The hair tonic is for the purpose of treating hair loss, improve hair quality and regeneration and the take rate after hair transplantation. A HIF-1α activity modulator for use herein is present in the hair tonic composition at a level of from 0.001% to 5% w/v, preferably from 0.005% to 2.0% w/v, more preferably 0.010% to 1.0% w/v.

[0066] In addition to the HIF-1α activity modulator, the hair tonic composition according to the present invention can contain ingredients conventionally used in hair tonic compositions. Examples of such optional ingredients are solvents such as purified water and ethanol; refrigerants such as menthol; humectants such as propylene glycol, glycerin and sorbitol; keratin-solubilizing agents such as lactic acid, resorcinol and salicylic acid; ethers such as polyoxyethylene oleyl ether and polyoxyethylene lauryl ether; vegetable oils such as olive oil and caster oil; higher alcohols such as cetyl alcohol and oleyl alcohol; hydrocarbons such as liquid paraffin and acetene; vitamin; perfumes; coloring agents; and preservatives. If necessary, ingredients for hair tonic preparations such as hormones, germicides, antiphlogistics, scalp-stimulating agents and the like can be incorporated in the hair tonic composition of the present invention. The hair tonic composition according to the present invention can be prepared in accordance with the general process for preparing an ordinary hair tonic composition except that the gibberellin and the optional proteolytic enzyme are incorporated therein.

Example 2

Preparation of a Shampoo Composition

[0067] The present invention is further illustrated by the following preparation of a shampoo composition; to which it is of course not limited. The shampoo is for the purpose of that is used for cleaning hair and also treating hair loss, improve hair quality and regeneration. A HIF-1α activity modulators for use herein is present in the shampoo composition at a level of from 0.001% to 5% w/v, preferably from 0.005% to 2.0% w/v, more preferably 0.010% to 1.0% w/v.

[0068] The shampoo base is a low viscosity solution which includes an anionic or nonionic surfactant. The viscosity of the shampoo base is preferably low enough such that additive ingredients are easily combined with the shampoo base. Typically the shampoo base has a viscosity from about 600 to 800 cps.

[0069] The shampoo base includes a mild detergent to effectively clean hair without damaging or stripping it. The low viscosity shampoo base is combined with a thickening agent and, optionally, one or more hair enhancing additives.

[0070] The shampoo base contains a major amount of water and is clear to opaque. As used herein, “a major amount of water” means that the shampoo base is made of no less than 50% water. Preferably the shampoo base contains about 60-75 wt-% water. The active detergent agent of the shampoo includes an anionic, nonionic, amphoteric or zwitterionic surfactant. A preferred detergent agent includes an anionic surfactant such as sodium lauroyl sarcosinate or N-lauroyl sarcosine. The shampoo base preferably contains about 5-12% wt-% anionic surfactant, more preferably about 8-10 wt-%.

[0071] The shampoo base can also include a specialized nonionic surfactant which can function as a foam stabilizer, viscosity control agent, or a conditioning agent. Where included, the shampoo base preferably contains about 0.5-5.0 wt-% nonionic surfactant, more preferably about 0.75-2.00 wt-%.

[0072] Useful nonionic surfactants include a carboxylic amide nonionic surfactant which is a condensation product of fatty acids and hydroxyalkyl amines, such as mono- and dialkanolamides of C8-C22 fatty acids. An example is mono- or di(C8-C22)alkanolamide. Commercially available, specialized nonionic surfactants suitable for use in the shampoo base include stearamide DEA, lauramide DEA, stearamide MEA, lauramide MEA, lauramide MIPA, myristamide MEA, myristamide MIPA, myristamide DEA, oleamide DEA, oleamide MEA, oleamide MIPA, cocamide DEA, cocamide MIPA, cocamide MEA, and other dialkanolamine and monoalkanolamine condensates.

[0073] Also useful are organic esters that function as nonionic surfactants and emollient esters. These include polyoxyethylene glycol (C7-C20) fatty acid, esters of glycerol, such as PEG-7 glyceryl cocoate, PEG-30 glyceryl cocoate, PEG-12 glyceryl laureate, and PEG-20 glyceryl oleate.

[0074] Another useful nonionic surfactant is a polyoxyethylene glycol (PEG) ether of the diester of methyl glucose and a fatty acid. Examples of such PEG compounds include PEG-120 methyl glucose dioleate, PEG-20 methyl glucose distearate, PEG-80 methyl glucose laureate, and PEG-20 methyl glucose sesquistearate.

[0075] The shampoo base can also include a cationic polymer, such as quaternary ammonium salt, to provide substantive conditioning, detangling and improved wet and dry compatibility. Examples of useful quaternary ammonium salts include polymeric quaternary ammonium salts, also referred to as “polyquaterniums” (i.e., -6, -7, -10, -11, -16), cetrimonium chloride and steartrimonium chloride. The shampoo base can include about 0.2-2.0 wt-%, preferably about 0.5-1.0 wt-%, of a quaternary ammonium salt.

[0076] Other additives can be included in the shampoo base in lesser, but effective, amounts. Useful additives include a chelating or sequestering agent such as disodium EDTA, tetrasodium EDTA, citric acid or lactic acid. A chelating or sequestering agent is typically added to stabilize the composition. Preferably about 0.001-0.75 wt-%, more preferably about 0.03-0.25 wt-%, is added to the shampoo base. Other additives include germicidal preservative agents such as methylchloroisothiazolinone, methylisothiazolinone, phenoxyethanol, esters of parabenzoic acid, diazolidinyl urea, and imidazolidinyl urea. Preferably, the preservative is added in an effective germicidal amount, typically about 0.05-1.25 wt-%. Other additives include an antioxidant such as ascorbic acid or BHA to inhibit deterioration, typically included at about 0.001-0.5 wt-%. An appropriate amount of natural or synthetic fragrance can also be added for aesthetic purposes. An opacifying agent such as glycol. Stearate or glycol distearate can be included at about 0.5-1.25 wt-% to give the shampoo an opaque or pearlescent appearance.

[0077] The shampoo base typically includes about 60-75 wt-% water, about 5-12 wt-% anionic surfactant, about 1-10 wt-% nonionic surfactant, about 0.2-2.0 wt-% of a quaternary ammonium salt and about 0.5-2.0 wt-% of an amphoteric or zwitterionic surfactant. Optionally, the shampoo base includes minor, but effective, amounts of a germicidal preservative agent, sequestering agent, antioxidant, or fragrance.

ITEMS

[0078] 1. A composition for preventing or treating loss of hair on a scalp of a human being in the form of a shampoo, conditioner, tonic or lotion, comprising a suitable HIF-1α activity potentiating agent, such as an iron chelator, a hypoxia mimetic, a HIF hydroxylase inhibitors or HIF-1α stabilizing compound.

[0079] 2. A composition for supporting the healing of hair transplants and the skin in the area of the transplant, avoid shedding as a side effect of the treatment and supporting the growth of the transplanted hair in the form of a shampoo, conditioner, tonic or lotion, comprising a suitable HIF-1α activity potentiating agent, such as an iron chelator, a hypoxia mimetic, a HIF hydroxylase inhibitors or HIF-1α stabilizing compound.

[0080] 3. The composition of item 1 or 2, wherein the HIF-1α activity potentiating agent is present at a concentration of 0.1% to 50.0% volume/volume.

[0081] 4. The composition of item 1 or 2, wherein the HIF-1α activity potentiating agent is Deferoxamine.

[0082] 5. The composition of item 1 or 2, wherein the HIF-1α activity potentiating agent is Deferiprone.

[0083] 6. The composition of item 1 or 2, wherein the HIF-1α activity potentiating agent is sodium gluconate.

[0084] 7. A composition for preventing or treating loss of hair on a scalp of a human being according to item 1 or 2 or a kit comprising said composition for cosmetic applications such as such as cleaning, nourishing, strengthening and repairing the hair.

[0085] 8. A composition for preventing or treating loss of hair on a scalp of a human being according to item 1 or 2 or a kit comprising said composition for use in therapy.