GB2484812A - Composition for reducing hair loss/improving hair condition - Google Patents

Abstract

An oral preparation for maintaining hair growth, strength and condition and reducing hair loss, comprising: - pine bark extract, - caffeine, - curcumin, - resveratrol - horsetail extract - L-cysteine - methylsulphonylmethane - biotin - vitamin B6 P5P - Zinc - Copper - Magnesium The composition may further comprise saw palmetto extract, beta sitosterol, green tea and taurine or iron, vitamin B12, marine cartilage and pantothenic acid.

Description

Complete Supplement Formulae for Maintenance of Hair Growth and Condition The present invention relates to a nutritional supplement for maintaining hair growth and the reduction of hair loss.

Nutrition is a complex subject as the effects of correct nutrition are indirect and slow to appear. This is particularly true for hair which is slow to respond to any form of treatment. Correct nutrition has been shown by many tri&s to be essential for healthy hair growth, and conversely many deficiencies correlate with hair loss. Hair nutrition is therefore a vital part of any treatment regime. A truly systematic and rigorous approach must be taken when formulating a nutritional supplement for hair due the many factors that affect the eventual efficacy of the treatment, The fact that hair growth requires complex nutrients and a ready supply of oxygen is well documented, but often overlooked. Perhaps because the effects are indirect and difficult to measure, comparatively few studies have triaUed ingredients and combinations of ingredients to maintain or promote hair growth.

t is not surprising then that many prior inventors of nutritional supplements have not considered the importance of bioavaUability, balancing elements with shared uptake pathways, and have fai'ed to ensure that no component has a negative effect on the absorption or action of other components in the formula.

Concentration There is a trend among supplement formulators, who are usually food scientists rather than pharmacologists, to include the maximum possib'e level of everything, "bigger is better". It is well known to pharmacologists who study absorption of substances into the body, that this is not necessarily correct. The most common example in hair supplements is saw palmetto. There is strong evidence from tissue sample experiments that saw palmetto inhibits the 5u reductase enzyme responsible for converting testosterone to dihydrotestosterone or "DHT"11. Component analysis shows that certain fatty acids but parUcularly lauric acid and oleic acki are responsible for the activity of saw palmetto121. Saw palmetto extract is a refined version of the whole fruit form, and retains a high percentage of the fatty acid content whilst removing other less useful components. Therefore it is apparent that a significantly lower dose of the extract is required to deliver the same levels of active fatty acids, one calculation estimates that 320mg of extract would have the fatty acid component of 1500mg of the whole fruit form.

An additional consideration is the selective inhibition of the two isoforms of 5o reductase. It has been shown in in vitro tests that both isoforms may be inhibited by lipid-rich saw palmetto extract?1, however there has been no study showing that the whole fruit form has a measurable effect on both isoforms. Of course the whole fruit contains all of the components of the extract and so theoretically would have the same effect, however this has not been proven.

Bloavailability Many common vitamins and all amino acids exist as multiple isomers, however it is rare that both or even all forms are equally available to human metabolism. The chirality of amino acids is well established, as is the dramatic difference between left and right enantiomers in the human body. On the whole, humans can only metabolise left or L enantiomers, such as L-Cysteine. R-Cysteine is not taken up or commonly metabolised, therefore commonly used racemic mixtures of the two forms are only half comprised of useful amino acids.

Vitamins, such as vitamin B6 also have several forms, pyridoxine is the form of vitamin B6 most commonly used in nutritional supplements, however it is not the bio-active form. Instead it must be phosphorylated to become pyridoxal 5 phosphate, which is active as an enzyme cofactor for many reactions, and is important for uptake of other nutrients as well. The phosphorylation reaction to activate pyridoxine takes energy and a certain set of conditions, and therefore not all the pyridoxine taken in a supplement is used. A more efficient alternative would be to use pyridoxal 5 phosphate in the supplement, so the bio-active form is immediately available, requiring no energy, and minimal wastage.

Bioavailability is not just controUed by isomeric forms. Nutrient uptake is complex, and there are many surprising instances where one nutrient is dramatically affected either negatively or positively, by a completely different nutrient in the formula. Pyridoxal 5 phosphate increases L-cysteine incorporation into keratin51, therefore a combination of the two would be beneficial for hair strength. Also interesting are the studies showing that both green tea and saw palmetto inhibit the absorption of iron. Whilst the mechanism for this is not entirely described, it is thought to be due to the concentrations of tannic acids in both16. Tannic acid levels are not significantly reduced when they are used in their purified extract form.

Therefore a formula must be designed so not only are bioavailable forms used, but the whole formula is studied for negative interactions and targeted towards a particular concern.

Balance Unfortunately a formula containing all of the nutrients necessary without a single negative interaction is rarely possible. Therefore balance is essential, especially where nutrients compete for uptake via the same pathways.

Balance is not simply a matter of including every competing element at the same percentage. Certain nutrients will compete more successfully than others, and all elements for healthy hair are necessary at different levels. The ion uptake channel for copper, zinc and magnesium ions is a useful illustration as the balance between the three competing elements is fine, and taking too much of one will decrease the other two. It has been shown that copper, zinc, and magnesium separately are all important for hair growth. As well as their role in nutrition and enzyme action, Copper and zinc have also both been shown to inhibit So reductase, although zinc has only been proven to inhibit the type 1 isoform found in skin not hair 7'8k Magnesium deficiency has been shown to correlate with certain diffuse alopedas in women91, but the precise cause has not been established.

However it would not be correct to create a supplement with more copper, slightly less zinc, and lower magnesium content due to their relative importance. In fact as magnesium is required at higher levels around the body comparatively it should be included at a higher dose, followed by zinc, and then copper which is useful even at low levels.

Component Synergy Whilst competition is important, it is also vital to consider the opposite possibility in complex formulae. Combinations of nutrients may improve the results of the two nutrients separately, such as the combination of curcumin and resveratrol. Resveratrol has been extensively studied both as an anti.inflammatory and anti-angiogenic agent, however results have been limited. Curcumin has also not lived up to initial promise as an anti-inflammatory. However it has been shown that the two work synergistically in a cancer model1101 to decrease inflammation.

Correct synergy can even result in a measurable effect where neither ingredient was effective separately. L-cysteine and pantothenic acid can be useful as they are incorporated into keratin; pantothenic acid in particular is very common in the form of panthenol, the conditioning agent. A combination of the two has been suggested by in vitro tests to help increase hair repair and keratinocyte proliferation11'121 which the two individually do not.

There are also several obvious examples where two ingredients act together, and these should not be ignored. For instance it is well known that vitamin Bi 2 and iron are both necessary for erythrocyte formation, and hence oxygen circulation, so it is important that a supplement contain both to significantly help this process.

Circulation An often overlooked factor to consider is the circulation of oxygen and nutrients to the hair. Even a perfectly balanced supplement would not be effective if there was no blood flow to the hair. Many believe that several forms of hair oss are caused or exacerbated by a deficient blood supply to the hair follicle, and so it is possible that nutrients from a supplement could not reach the follicle in useful quantities. Therefore it may be beneficial to increase the circulation. This can be achieved through topical treatments that stimulate nitric oxide production or angiogenesis. However a simpler solution may be to include a stimulant like taurine or caffeine to increase bloodflow around the entire body.

The stimulatory effects of caffeine and taurine on nutrient uptake and metabolism may also be beneficial. An added consideration is the possible effect of caffeine upon DHT and hair loss. Caffeine has been shown by several studies to reduce hair loss caused by DHT, the in vivo studies were successful topically1. Taurine has also been shown by in vitro testing to protect the hair from TGFI3-1 induced apoptosi&141.

Gender and Causation Whilst an ideal supplement would alleviate all known causes of hair loss and improve hair condition uniformly on any consumer, due to the competition mentioned above, and other practical considerations such as the size of a tablet, this is not possible. Therefore the cause of hair loss must be considered, and as many likely causes targeted as possible.

For some, particularly men, DHT is a major cause of hair loss. There is a certain amount of inflammation and oxidative damage associated with this form of hair loss.

Therefore one possible aspect should aim to reduce DHT levels, prevent DHT from acting, and prevent inflammation and oxidative damage at the same time. Keratin components and other nutrients may be useful to prevent deficiencies and encourage natural growth.

For others, mostly women, DHT is less important. lt is more common for female hair loss to be caused by iron or another deficiency, although there are also inflammatory aspects to these types of hair loss as well. Therefore an alternative aspect would not focus on anti-DHT agents, (particularly as some prevent iron absorption) but would focus on mineral and keratin component supplementation with similar levels of anti-inflammatory and antioxidant molecules.

Statement of the lnvention

From the research above, a specific combination of ingredients has been selected from the plethora of available ingredients and combinations to give a holistic solution for a variety of causes of hair loss in men and women.

The core of the invention is: Pine bark extract rich in proanthocyanidins which promote hair growth for men and women. Other sources such as grape seed exist, but pine bark is preferred as having high proanthocyanidin levels, wide availability, and a very low allergic response rate.

Caffeine which increases ingredient circulation and prevents DHT from acting on the hair follicle. Particularly importantly for women it does this without changing hormone levels, unlike other options such as saw palmetto, uva ursi, pygeum africanum and others.

Curcumin & Resveratrol in combination have powerful anti-inflammatory and antioxidant effects and unlike many antioxidants such as ascorbic acid, remain stable for prolonged periods of time.

Horsetail extract is an antioxidant and also a source of silica, which helps create smoother hair.

L-cysteine is a vital amino acid for keratin formation, unlike many amino acids it also creates stronger hair through the increased number of disulphide bonds.

Methylsulfonylmethane is a source of sulphur which helps form stronger hair.

Methylsulfonylmethane is a preferred source of sulphur as it is more readily bioavailable than other organic sulphur sources like chondroitin.

Biotin is another key component of strong and smooth hair.

Vitamin B6 P5P increases the uptake of several nutrients such as L-cysteine and is the only active form of Vitamin B6, there are 6 other forms available.

Zinc, Copper and Magnesium will prevent deficiencies which can all cause hair loss.

Each has benefits for hair growth but all need to be taken together, as taking just one may reduce serum levels of the others.

In addition, the following ingredients may be considered to make a supplement more

suitable for men.

Saw palmetto extract is a well-supported DHT inhibitor for men, unlike the whole fruit form and many other "DHT inhibitors" the extract inhibits both forms of 5 alpha reductase.

Beta sitosterol is another anti-DHT ingredient, but as it may work in a subtly different way from saw palmetto the two would be more effective in combination. Beta sitosterol could be used in the form of avocado, wheat germ, or rice, but a purer phytosterol extract is preferred.

Green tea is not a preferred antioxidant or DHT inhibitor in a formulation for women because it blocks iron absorption, however in combination with other antioxidants and anti-DHT agents it would have an additional effect.

Taurine is a very useful addition for male hair loss specifically as it alleviates the effects of TOF-beta, a cytokine responsible for causing hair to fafl out. This cytokine is stimulated by DHT, and so using Taurine in combination with DHT inhibitors will provide a broader spectrum of protection.

Alternatively, the following ingredients may be considered to make a supplement more

suitable for women.

Iron & Vitamin B12 are extremely important as anaemia is a common cause of poor hair condition and hair loss in women. It is not as prevalent as in men. Whilst iron is more commonly given as a single supplement, the two should improve erythropoiesis in a synergistic fashion.

Pantothenic acid improves hair condition independently, and in combination with L-cysteine alleviates certain forms of alopecia common in women.

Marine cartilage has been regarded by other inventors simply as another source of sulphur, similar to methylsulfonylmethane, however more recent research shows it stimulates hair growth -which methylsulfonylmethane alone does not, therefore it is a beneficial addition to a female formula.

In one aspect, the invention provides a preparation for maintaining hair growth, strength and/or condition; and/or the reduction of hair loss. The preparation in this aspect comprises all of the ingredients in set "a" in combination with either of the ingredient sets "b" or c", yet not both "b" and "c": a) 50mg of pine bark extract 50mg of caffeine 50mg of curcumin 100mg of resveratrol 30mg of horsetail extract 100mg of L-cysteine 150mg of methylsulfonylmethane I mg of biotin 2.8mg of vitamin 86 P5P 30mg of zinc 4mg of copper 150mg of magnesium b) 320mg of saw palmetto extract 50mg of beta sitosterol 200mg of green tea 100mg of taurine c) 48mg of iron 1 2pg of vitamin 812 12mg of pantothenic acid 640mg of marine cartilage n a preferred embodiment, any one or more of the quantities may be varied by as much as -i-I-30%. In a more greatly preferred embodiment, any one or more of the quantities may be varied by as much as +1-20%.

n a second aspect, the invention provides a preparation for maintaining hair growth, strength and condition; and/or the reduction of hair loss. The preparation in this aspect comprises all of the ingredients: 320mg of saw palmetto extract 50mg of pine bark extract 50mg of beta sitosterol 50mg of caffeine (a'so promoting circulation) 200mg of green tea (also an anti-oxidant) 50mg of curcumin (in combination with resveratroi) 100mg of resveratrol (in combination with curcumin) 30mg of horsetail extract (also a source of silica) 100mg of L-cysteine 150mg of methylsulfonylmethane I mg of biotin 2.8mg of vitamin B6 P5P 100mg of taurine 30mg of zinc 4mg of copper 150mg of magnesium In a preferred embodiment, any one or more of the quantities may be varied by as much as +1-30%. in a more greatly preferred embodiment, any one or more of the quantities may be varied by as much as +1-20%.

In a third aspect, the invention provides a preparation for maintaining hair growth, strength and condition; and/or the reduction of hair loss. The preparation in this aspect comprises all of the ingredients: 48mg of iron I2pg of vitamin B12 640mg of marine cartilage 100mg of L-cysteine 12mg of pantothenic acid 150mg of methylsuifonylmethane 1 mg of biotin 100mg of horsetail extract 50mg of curcumin 100mg of resveratrol 2.8 mg of vitamin B6 P5P 50mg of caffeine 50mg of pine bark extract 30mg of zinc 4 mg of copper 150mg of magnesium In a preferred embodiment, any one or more of the quantities may be varied by as much as +1-30%. ln a more greatly preferred embodiment, any one or more of the quantities may be varied by as much as +1-20%.

In any of the above aspects, the preparation may be in the form of one or more tablets, Uquid, powder or encapsulated powder and may be taken orally. The preparation may be mixed with other powders or liquids prior to ingestion. The preparation may be taken as two or more parts at substantially different times of the day and/or night, and composition of each part may differ from the others.

The preparation may contain at least one inactive ingredient such as maltodextrose, magnesium stearate, silicon dioxide, microcrystalline cellulose, and/or stearic acid.

The preparation may have a therapeutic effect. The preparation may reduce or prevent the action of factors such as hormones which may promote hair loss. The preparation may be used as part of a programme to reduce hair loss, maintain or improve hair growth, and/or enhance hair strength, shine and condition. Programme in this case is accepted to mean either repeated use of this invention alone, or use of the invention in conjunction with other treatment options such as minoxidil, finasteride, dutasteride, spironolatone, ketoconazole, thymic peptides, copper peptides, growth factors, platelet rich plasma therapy, hair transplantation, restricted or planned diet, shampoos and/or conditioners. Any and all of these examples can be used in combination.

References 1. Marks L. S., et aL, Tissue effects of saw palmetto and finasteride: use of biopsy cores for in situ quantification of prostatic androgens. Urology, 2001. 57(5): p. 999-1005.

2. Abe M., et al. Pharmacologically relevant receptor binding characteristics and 5alpha-reductase inhibitory activity of free Fatty acids contained in saw palmetto extracL Bbbgical and Pharmacological Bulletin, 2009. 32(4): p. 646-650.

3. lehló C., et aL Human prostatic steroid 5 alpha -reductase iso forms--a comparative study of selective inhibitors. Journal of Steroid Biochemistry and Molecular Biology, 1995. 54(5-6): p.273-279.

4. Combs, G. F. The Vitamins: Fundamental Aspects in Nutrition and Health.

Elsevier, 2008.

5. D'Agostini F., et al., Chemoprevention of smoke-induced alopecia in mice by oral administration of L-cystine and vitamin 86. Journal of Dermatological Science, 2007. 46(3): p. 189-1 98.

6. Miller L.G., Herbal medicinals: selected clinical considerations focusing on known or potential drug-herb interactions. Archives of Internal Medicine, 1998. 158(20): p. 2200-2211.

7. Sugimoto Y., et al., Cations inhibit specifically type 15 alpha-reductase found in human skin. Journal of Investigative Dermatology, 1995. 104(5): p. 775-778.

8. Om A.S., Chung K.W., Dietary zinc deficiency alters 5 alpha-reduction and aromatization of testosterone and androgen and estrogen receptors in rat liver.

Journal of Nutrition,1996. 126(4): p. 842-848.

9. Tataru A., Nicoara E., Idiopathic diffuse alopecias in young women correlated with hypomagnesemia. Jorunal of the European Academy of Dermatology and Venereology, 2004. 18(3): p. 393-394.

10. Aftab N., Vieira A., Antioxidant activities of curcumin and combinations of this curcuminoid with other phytochemicals. Phytotherapy Research, 2010. 24(4): p. 500-502.

11. Budde J. et at. Systemic therapy of diffuse effluvium and hair structure damage.

Der Hautarzt, 1993. 44(6): p. 380384.

12. Obrigkeit D.H, et ak, Xenobiotics in vitro: the influence of L-cystine, pantothenat, and miliacin on metabolic and proliferative capacity of keratinocytes. Cutaneous and Ocular Toxicology, 2006. 25(1): p. 13-22.

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International Journal of Cosmetic Science, 2006. 28(4): p. 289-298.

Claims (12)

1. Claims 1. A preparation to be taken orally for maintaining hair growth, strength and condition; and/or the reduction of hair loss consisting of the following ingredients: 50mg of pine bark extract 50mg of caffeine 50mg of curcumin 100mg of resveratrol 30mg of horsetail extract 100mg of L-cysteine 1 50mg of methylsulfonylmethane 1 mg of biotin 2.8mg of vitamin B6 P5P 30mg of zinc 4mg of copper 150mg of magnesium Any one or more of the quantities may be varied by approximately +1-20%.
2. 2. The preparation of claim 1, further consisting of the following ingredients: 320mg of saw palmetto extract 50mg of beta sitosterol 200mg of green tea 100mg of taurine Any one or more of the quantities may be varied by approximately +/-20%.
3. 3. A preparation of claim 1, further consisting of the following ingredients: 48mg of iron 1 2pg of vitamin 812 640mg of marine cartilage 12mg of pantothenic acid Any one or more of the quantities may be varied by approximately +1-20%.
4. 4. The preparation of any of claims 1-3 wherein the preparation is in the form of one or more tablets to be taken orafly.
5. 5. The preparation of any of ciaims 1-3 wherein the preparation is in the form of a powder to be taken orafly.
6. 6. The preparation of claim 5 wherein the preparation in the form of a powder is encapsulated.
7. 7. The preparation any of claims 1-3 wherein the preparation is in the form of a liquid to be taken orally.
8. 8. The preparation of any of claims 6, 7 and 8 wherein the powder or liquid are mixed with other powders or liquids prior to ingestion.
9. 9. The preparation of any of the above claims wherein the preparation is ingested in two or more parts at substantially different times of the day.
10. 10. Use of the preparation of any of the above claims as part of a programme to reduce hair loss.
11. 11. Use of the preparation of any of the above claims as part of a programme to maintain hair growth.
12. 12. Use of the preparation of any of the above claims as part of a programme to maintain hair strength, shine and/or condition.