Azeco Cosmeceuticals

Question: You kindly sent us a sample of Azepur 99 over a year ago and we have been testing it for re- ducing hair loss with some success. We would like to develop a product using it so can I please ask a few questions? What is the most effective level of use for treating androgenic alopecia? We have so far put the Azelic acid into propylene glycol and glycerine with some ethanol, but this can be too heavy. What is the best mixture to use as a carrier? Do you have a sample formulation available as a guide? We intend to carry out our development over the next few months, so can I please request two further samples to be sent to me – otherwise I am happy to buy a small quantity for development purposes. Answer This answer relates to azelaic acid for the treatment of androgenic alopecia. To give a certified answer to your question is impossi - ble: by all means, it all depends on the bio-availability of azelaic acid how effective the product will be. If you would be able to make 100% of the amount of azelaic acid bio-available you would need a concentration of 1,0-1,5% calculated on the basis of a gel-like preparation. 1. Add 2% ethoxydiglycol. This is a superb solvent for azelaic acid and improves the dryness of the product when applied to the scalp. Ethoxydiglycol enables transdermal transport in the follicle, with a high degree of efficacy. For personal care & cosmetic products a maximum of ethoxydiglycol of 2,6% applies. This is not applicable for medical devices, given the “mode of action” of the medical device has been properly defined and that the consumer product is not subject to cytotoxicity. Ethoxydiglycol is supplied by Gattefosse as Transcutol CG. 2. Cytotoxicity can be suppressed by using 5% betaine (trimethylglycine), supplied by Dupont under the tradename Genenca- re OSMS BA. 3. It would properly better to use Zemea (INCI: propanediol; chemical name 1,3-propylene glycol). This product reduces the skin irritation induced by 1,2-propylkene glycol. Zemea is commercially made available by Dupont. 4. A system as applicable to your wishes is best thickened by 2-3% hydroxypropylcellulose (HPC). This polymer does not give a resident feel on the scalp. To prepare a gel the polymer shall first be dissolved in the final HPC before adding other products to be dissolved to avoid dissolution competition. HPC is commercially made available by Ashland as Klucel. The current system based on propylene glycol, glycerin & ethanol is rather resident on the scalp indeed, but it is a well-chosen sol- vent for azelaic acid. The system can be greatly improved using the following system:

Let me know if any further questions remain.

Mussenberg 1 • 6049 GZ Roermond • The Netherlands

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