Science
Mechanism of Action
Tioxolone acts as a prodrug, undergoing cleavage within the active site of carbonic anhydrase II to yield 4-mercaptobenzene-1,3-diol. This active metabolite then binds to the zinc active site of metalloenzyme carbonic anhydrase I (CAI), exhibiting potent inhibition with a Ki of 91 nM. In dermatological applications, this translates to the inhibition of enzymes critical for sebum production and inflammatory responses, conferring anti-acne, anti-inflammatory, anti-bacterial (against Gram-positive, Gram-negative, and M. tuberculosis), anti-mycotic (against dermatophytes, yeasts, and molds), cytostatic, and anti-psoriatic benefits. It also has specific claims for regulating skin oiliness.
Research
Clinical Evidence
Low confidenceN/A
Transparency
Dusting Analysis
No data available to suggest Tioxolone is commonly dusted or to establish effective dusting thresholds.
The Formula
Formulation
Stability
Tioxolone powder should be stored at -20°C for up to 3 years or 4°C for 2 years. When in solvent, it maintains stability at -80°C for 2 years or -20°C for 1 year, provided repeated freeze-thaw cycles are meticulously avoided. Due to the hygroscopic nature of DMSO, utilizing freshly opened solvent is recommended for optimal solubility. While primarily oil-soluble, with reported water solubility as low as 0.67 mg/mL (requiring ultrasonication) or up to 9005 mg/L in some estimates, it can be dissolved in DMSO (≥ 100 mg/mL) and ethanol (34 mg/mL). Achieving aqueous concentrations of ≥ 2.5 mg/mL is possible through the use of co-solvents like PEG300 and Tween80 in saline. Heating and/or sonication significantly aid dissolution. Tioxolone is implied to be unstable in alkaline solutions.
Conflicts
- Alkaline solutions
Safety
Safety Profile
Tioxolone is classified with GHS hazard statements: H302 (Harmful if swallowed), H315 (Causes skin irritation), H319 (Causes serious eye irritation), and H335 (May cause respiratory irritation), featuring a 'Warning' signal word and 'Irritant (GHS07)' pictogram. Oral toxicity data shows an LD50 (oral-rat) of 633 mg/kg, and inhalation toxicity an LC50 (inhalation-rat) of 3710 mg/m3. There are documented reports of contact dermatitis, and it is categorized as a contact irritant or corrosive substance to eyes, skin, and mucous membranes. Its WGK Germany rating is 3.
Your Skin
Skin Compatibility
Our Assessment
Verdict
While offering potent anti-acne, oil-regulating, and antimicrobial benefits for specific skin concerns, Tioxolone's high irritancy potential and lack of a CIR safety review necessitate extreme caution in formulation and application.
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