The standard for azelaic acid in pharma & cosmeticsservice@azelaic.com

Hair care
reactivates hair growth

Which products are used for reactivating hair growth?

The most frequently observed cause of hair loss is genetic: androgenetic alopecia. Common types of hair loss Hair loss may furthermore be caused by hair diseases such as alopecia diffusa (effluvium) whereby the scalp becomes visible due to hair loss, shortage of iron, malfunctioning of thyroid gland, cancer or the use of particular medicines (some oral contraceptives or chemotherapeutic agents), and also psychological artefacts such as trichotillomania, also known as “hair pulling disorder”.

Hair loss is a common problem. Pattern hair loss by age 50 affects about half of all males and a quarter of females. About 2% of people develop alopecia areata at some point in time.

Various stages of hair loss
Various stages of hair loss

Applicability

Products for reactivate hair growth Cosmetic Use Medical Device Use Pharmaceutical Use
Azelaic acid ++ ++ +
Anthralin - - +
Finasteride - - ++
Dutasteride - - ++
Minoxidil - - ++
Spironolacton - - +
Cafeine ++ ++ +
Botanical products + + -
Legend: (++ Strongly recommended / Very suitable) (+ Limited recommended / Suitable) (+/- Limited allowed / Limited suitable) (- Forbidden)

Functionality

Products for reactivate hair growth Cosmetic functionality Medical Device functionality Pharmaceutical functionality
Azelaic acid ++ ++ ++
Anthralin - - +
Finasteride - - ++
Dutasteride - - ++
Minoxidil - - ++
Spironolacton - - +
Cafeine + + +
Botanical products + + -
Legend: (++ Strongly recommended / Very suitable) (+ Limited recommended / Suitable) (+/- Limited allowed / Limited suitable) (- Forbidden)

Adverse effects

Products for reactivate hair growth CMR properties Skin irritation Side effects Exfoliation Photo activity Cytotoxicity
Azelaic acid - +/- - + - -
Anthralin ++ + + - + +
Finasteride ++ +/- + - - +
Dutasteride ++ +/- ++ - - +
Minoxidil + + ++ - +/- ++
Spironolacton ++ - + - +/- +
Cafeine - - - - +/- -
Botanical products +/- - +/- - +/- -
Legend: (++ Very strong effects) (+ Noticable effects) (+/- Hardly noticable) (- Not noticable)

General Product Characteristics

Azelaic acid is a very potent 5-α-reductase inhibitor, type 1. According to Stama-tiadis 5-α-reductase inhibition is already detectable at an azelaic acid concentration as low as 0,2 mMol/l. Inhibition is complete at a concentration of 3 mMol/l, equivalent to ~0,6 mg/l. Stamatiadis also studied the inhibitory effects of zinc sulphate (3-9 mMol/l) using an in vitro assay with 1,2[3H]-testosterone as substrate; also zinc sulphate showed to be a potent 5-α-reductase inhibitor. An additive effect of these two inhibitors was observed. Pyridoxine (vitamin B6) potentiated the inhibitory effect of zinc sulphate, but not of azelaic acid. This observation suggests that different mechanisms are involved. Simultaneous use of the three products showed to be already effective for the treatment of androgenic alopecia, indicative for a powerful synergy.

The powerful combination {azelaic acid + zinc sulphate + vitamin B6} for the treatment of androgenic alopecia is cosmetically suitable contrary to the steroidal and non-steroidal pharmaceutical preparations. In addition, azelaic acid has a superior toxicological profile. Side effects of azelaic acid boil down to the particular cosmetic properties: skin lightening at the site of application, a slight risk of hypertrichosis, and [seldom] slight skin irritation.

Combinations of minoxidil and azelaic acid are commercially available, despite the unwanted side effects of minoxidil. Both products work on the basis of different mechanisms of action in preventing baldness. The combination of the two would work more effectively than either alone. Commercial products contain up to 15% azelaic acid and 5% minoxidil. These high concentrations are explained because of the poor bioavailability of especially minoxidil. Lower but equally effective preparations can be made using transdermal preparations based on phosphatidylcholine-based organogels, to be mentioned organogels containing azelaic acid and caffeine

Anthralin is used for the treatment of long-term psoriasis. It is chemically described as 1,8-dihydroxyanthron and is found in goa powder. Goa powder, also named Bahia powder, comes from the araroba tree (Andira araroba). At present anthralin is produced artificially. Anthralin is also used to promote hair growth, but there are sincere concerns on the safety of the product. Insufficient toxicological information is available, both for application against psoriasis and for hair growth stimulation.

Finasteride is probably the most effective medication proven for the treatment of androgenic alopecia. It is prescribed for males with a genetic predisposition of male-pattern baldness. Finasteride is a 5-α-reductase type II inhibitor, approved by the FDA, for the treatment of enlarged prostate glands.

A side effect of the medication with finasteride was decreased hair loss and often also hair re-growth. In 1998 finasteride was also approved for anti-baldness treatment. Finasteride is marketed by Merck as Proscar for prostate treatment and Propecia for hair loss treatment.

The enzyme 5-α-reductase is responsible for the conversion of testosterone into dihydrotestosterone (DHT). For males that are subject to genetic predisposition for hair loss DHT assumes responsibility for the hair follicle to enter the telogen state. Finasteride inhibits 5-α-reductase, so many of the follicles that would have quit instead continue to produce new hairs. The limitation is that the treatment must be continued to be used; if treatment is discontinued baldness returns, although this may take considerable time. Finasteride is exclusively approved for males only; it is not suitable for (pregnant) females and may cause male foetus to develop ambiguous genitals; female foetuses are not affected. Finasteride may lead to multiple sexual disorders, eventually impotence.

As an extension of finasteride dutasteride has been developed. Like finasteride it is also an anti-androgen and is also used to treat an enlarged prostate; it also inhibits 5-α-reductase. Dutasteride is expected to be effective for the treatment of androgenic alopecia. However, the side effects are more sincere than in the case of finasteride.

Both finasteride and dutasteride are pharmaceutical products and shall by no means be used in personal care & cosmetic products and medical devices.

Minoxidil was originally developed for the treatment of high blood pressure, but it was also observed that it affected hair growth. Contrary to finasteride & dutasteride minoxidil has no hormonal activity. Minoxidil is, however, not allowed in personal care & cosmetic preparations as well as in medical devices; minoxidil is considered to be a pharmaceutical product

A disadvantage of minoxidil is the fact that newly formed hairs frequently stay in the “vellus” phase: short and fine, soft and usually not pigmented hairs

Minoxidil

Minoxidil has a number of side effects: acne, headache/migraine, heart palpitations and irregular heart beat and (unwanted) blood pressure lowering. Minoxidil shall not be used by lactating females. The mode of action of minoxidil is yet unknown

Spironolactone is a potassium-sparing diuretic that prevents from absorbing too much salt and keeps the potassium levels from getting too low. It is also used for the treatment of acne, hirsutism and androgenic alopecia. Spironolactone is for females what finasteride for males is.

The efficacy of spironolactone is rather limited indeed, and hair regrowth is merely a side effect of the diuretic activity. The side effects may be quite sincere indeed. The product shall by no means be part of personal care & cosmetic products and medical devices.

Androgenetic alopecia is hereditary and androgen-dependent. Currently only oral finasteride and topical minoxidil are approved for pharmaceutical treatment of androgenetic alopecia. Recently caffeine has been shown to have beneficial effects in patients suffering from androgenetic alopecia. The proposed mechanism includes phosphodiesterase inhibition rather than inhibition of 5-α-reductase thereby increasing cAMP levels in cells and promoting cell proliferation by stimulating cell metabolism (T.W.Fischer, U.C.Hipler, P.Elsner, Effect of caffeine and testosterone on the proliferation of human hair follicles in vitro. Int.J.Dermatol., 46,27,(2007)).

The combination of caffeine with azelaic acid shall be mentioned as a powerful method to treat androgenic alopecia, with the advantage that both caffeine and azelaic acid are recognised personal care &cosmetic ingredients that also may be used in medical devices.

There are not to many cosmetically allowed products that inhibit 5-α-reductase; saw palmetto (INCI: Sabal Serrulata/Serenoa Repens) is an example. The applicable part of saw palmetto is the ripe fruit. The lipid fraction of the volatile oil and fatty oils contains constituents active in treating benign prostatic hyperplasia (BPH), for which saw palmetto is recommended. Saw palmetto has a proven positive track record for hair (re)growth preparations because of its potential to inhibit 5-α-reductase. The high content phytosterols (ß-sitosterol, stigmasterol, lupeol, lupenone & cycloartenol).

Some other botanical products are also claimed to inhibit 5-α-reductase, but there is insufficient proof of their activity. Examples are Ganoderma lucidum (reishi mushroom), that lives on the oil palm (Elaeis guineensis); ganoderic acid & ganoderol B are believed to be the active species.

Ganoderol B has been described as a potent anti-androgen. Ganoderol B has recently also received quite a bit of attention for the treatment of diabetes mellitus type II. It is a α-glucosidase inhibitor that prevents digestion of carbohydrates.

Also alfalfa (Medicago sativa), the Japanese pagoda tree (Sophora japonica), red clover (Trifolium pratense) and the often praised Indian mulberry (noni fruit; Morinda citrifolia) have been reported to exhibit 5-α-reductase inhibition properties. Although the inhibitory effect has been clearly demonstrated its efficacy is quite variable indeed due to seasonal variation and frequently a high degree of adulteration of the extracts. Furthermore, many of those extracts also contain isoflavones (genistein, daidzein, biochanin, formonometin, etc., either as the glycosides or the aglycons) that exhibit estrogenic properties.

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Types
Types
  • Azepur99® Cosmetic Grade
  • Azepur99® Pharma Grade
Packaging
Packaging
  • In HDPE Drum of 10 kg
Delivery
Delivery
  • DAP
  • CIP airport