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Moumoujus

THEOPHYLLINE.

Avoid CAS 58-55-9 / SKIN CONDITIONING, TONIC

Theophylline is a methylxanthine derivative historically recognized for its potential anti-aging and antioxidant properties in skin. Ex vivo studies indicate its ability to boost collagen and antioxidant production, enhance dermal structure, and mitigate cellular damage.

Summary

Skin conditioning Tonic Antioxidant Collagen booster Anti-inflammatory (indirect) Dermal structural support

Science

Mechanism of Action

Theophylline functions as a competitive nonselective phosphodiesterase inhibitor, elevating intracellular cAMP and cGMP, which activates protein kinase A (PKA). It also antagonizes adenosine receptors and activates histone deacetylase. In human skin ex vivo, it stimulates antioxidant metallothionein-1, increases mRNA levels of collagen I and III, stabilizes dermal microfibrils by impacting fibrillin-1, reduces matrix metalloproteinases (MMP-2, MMP-9), and decreases menadione-induced keratinocyte apoptosis. Additionally, it boosts endogenous melatonin production and upregulates keratin 15, a stem cell marker.

Research

Clinical Evidence

Medium confidence
Effective range 0.00018–0.0018%
Optimal

N/A

Key findings

  1. 01 An ex vivo study on human skin demonstrated increased protein expression of antioxidant metallothionein-1, elevated mRNA levels of collagen I and III, enhanced structural stability of dermal microfibrils (fibrillin-1), and decreased MMP-2 and MMP-9 mRNA levels. It also partially counteracted ROS donor effects, reduced menadione-stimulated keratinocyte apoptosis, increased intracutaneous melatonin production, and upregulated keratin 15 expression.
  2. 02 Similar to the 10 µM concentration, this dosage in an ex vivo human skin study showed stimulation of metallothionein-1, increased collagen I and III mRNA, improved dermal microfibril stability, reduced MMP-2 and MMP-9 mRNA, partial antagonism of ROS effects, decreased keratinocyte apoptosis, increased endogenous melatonin, and enhanced keratin 15 expression.

Transparency

Dusting Analysis

Not commonly dusted

Despite historical recognition as a cosmetic agent, Theophylline is currently prohibited in finished cosmetic products within the European Union (effective December 1, 2023). Its primary use today is as a pharmaceutical bronchodilator for respiratory conditions.

The Formula

Formulation

Solubility
Both
Optimal pH N/A
0 7 14

Stability

Theophylline has a pKa of 8.77 at 25 °C. A saturated solution of theophylline sodium glycinate exhibits a pH range of 8.7-9.1. High humidity may impact the stability and drug release characteristics of tablet formulations due to hydration.

Conflicts

  • tannins

Safety

Safety Profile

CIR Status
Theophylline specifically not individually reviewed by CIR; however, its class (methylxanthines) was deemed 'safe in cosmetics' in a broader assessment.
Sensitization risk Unknown

As of December 1, 2023, Theophylline is listed in Annex II of EU Regulation 1223/2009, prohibiting its use in finished cosmetic products in the European Union. The US FDA primarily classifies Theophylline as a bronchodilator drug.

Your Skin

Skin Compatibility

No Normal
No Dry
No Oily
No Sensitive
Irritancy Unknown
Comedogenicity Unknown

Our Assessment

Verdict

Avoid

Despite promising ex vivo data on anti-aging and antioxidant benefits, Theophylline is prohibited in cosmetic products within the European Union, rendering its inclusion in new formulations for a global precision skincare brand unfeasible.

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References

Sources