Minoxidil Sulfate vs. Regular Minoxidil: Effectiveness and Carrier Selection for Hair Loss Solutions
Question
Question regarding Minoxidil Sulfate and Clascoterone Formulation
- Effectiveness Comparison: Is
Minoxidil Sulfatemore effective than regularMinoxidilbecause it is already in the active sulfate form? I understand that some people lack the sulfotransferase enzyme (SULT1A1) in their hair follicles, which is necessary to convert regularMinoxidilinto its active form. - Solubility and Carrier Selection: What is the best carrier system or solvent combination to effectively dissolve the following ingredients in a single formulation:
Minoxidil Sulfate(Water-soluble)Clascoterone(Poorly water-soluble)
I am looking for a solution that ensures both ingredients are fully dissolved and can effectively penetrate the skin.
Answer
Minoxidil Sulfate vs. Regular Minoxidil
Minoxidil Sulfate is the active metabolite of regular Minoxidil. For regular Minoxidil to work, it must be converted into Minoxidil Sulfate by the enzyme sulfotransferase (SULT1A1) located in the hair follicles.
- Effectiveness: Research suggests that individuals with low levels of sulfotransferase enzyme activity in their hair follicles may not respond well to regular Minoxidil. Since Minoxidil Sulfate is already in the active form, it bypasses the need for enzymatic conversion, potentially making it more effective for those "non-responders" who lack sufficient enzyme levels.
- Solubility: Unlike regular Minoxidil (which is difficult to dissolve), Minoxidil Sulfate is water-soluble, making it easier to formulate in aqueous solutions.
Clascoterone and Carrier Selection
Clascoterone (Antiandrogen) is a topical androgen receptor inhibitor used for hormonal hair loss and acne. It is generally poorly soluble in water and requires organic solvents for effective delivery.
Recommended Carrier System:
To dissolve both Minoxidil Sulfate (water-soluble) and Clascoterone (solvent-soluble) while ensuring skin penetration, a combination of solvents is typically used:
- Ethoxydiglycol (e.q. Transcutol): An excellent solvent and penetration enhancer that helps move active ingredients into the hair follicle.
- Propylene Glycol (USP): Acts as a co-solvent and humectant to keep the actives in solution on the skin.
- Ethanol: Often used to help dissolve Clascoterone and speed up drying time.
- Purified Water: Necessary to dissolve the Minoxidil Sulfate.
Important Note: Both Minoxidil Sulfate and Clascoterone are classified for research and medical use only (hospitals, clinics, or pharmacies) and are not permitted for use in general cosmetic formulations.
