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CAFFEINE
Principal indication: cellulite
PURE ACTIVE A90
Bibliographical summary
 
  • INCI name : CAFFEINE
  • Titrated plant extract of green coffee beans with guaranteed caffeine content (= 60%))
 

Caffeine is an alkaloid from the methylxanthine family found in various foodstuffs, which acts as a stimulant, a psychotropic drug and an aphrodisiac as well as being slightly diuretic.
Caffeine was discovered in 1819 by the German chemist, Friedrich Ferdinand Runge. Caffeine is found in the seeds, leaves and fruit of various plants. It is most commonly consumed in the form of infusions of the beans of the coffee plant or the leaves of the tea plant. Likewise in several foods and beverages containing products from the Cola nut.
It is also a constituent of the insoluble chemicals guaranine and mateine, discovered respectively in the guaraná bean and the yerba maté leaf. In man, caffeine acts as a stimulant for the central nervous system and the cardiovascular system, temporarily alleviating somnolence and increasing the attention span.
In topical applications, caffeine has slimming properties. It has a lipolytic activity on fat cells and an action on the transport of glucose.

  • ACTION MECHANISMS / PROOFS OF EFFECTIVENESS

The action mechanisms of caffeine are manifold and described in various works. Caffeine is used for treating cellulite as it is involved in lipogenesis, lipolysis and the transport of glucose. Lipogenesis is based on the synthesis of triglycerides from fatty acids. LPL (LipoProtein Lipase) catalyzes this reaction. Conversely, lipolysis is the hydrolysis of the triglycerides contained in the adipocyte vacuole into non-esterified fatty acids. It works under the influence of hormone-sensitive lipase (HSL), which is active in its phosphorylated form.

• The action mechanisms of caffeine have been demonstrated in vitro:
Caffeine activates lipolysis in the adipocytes, by inhibiting cAMP phosphodiesterase, the enzyme that converts cAMP (cyclic Adenosine Monophosphate) in its inactive form and the antagonistic effect on the adenosine receptors [1].
Moreover, it inhibits lipogenesis by inhibiting the expression of lipoprotein lipase (LPL) and therefore diminishes its activity on mature adipocytes. The effect is dose-dependent and the optimal concentration is 0.5mM [2].
Finally, it inhibits the transport of glucose stimulated by the insulin in the adipocytes [3].
In vivo, the effectiveness of caffeine has been demonstrated, in combination with ruscogenin and retinol, on the appearance of cellulite [4]. It has been demonstrated that the ideal concentration of caffeine for regular transcutaneous penetration is around 5% [5].
These various mechanisms give caffeine therapeutic properties for the treatment of cellulite. Indeed, cellulite is characterized by a dimpled surface appearance resulting from the development of the volume of adipocytes organized into lobules within the inextensible partitions of connective tissue, which cause the retraction of the epidermis to the deep tissues [6].
The application of caffeine induces lipolysis of the adipocytes and inhibits their lipogenesis, resulting in the reduction in volume of the adipocytes and an improvement in the surface of the skin.

  • OUR EXPERT'S OPINION

This alkaloid molecule is an active of choice in the pharmacopoeia and has given rise to numerous studies. It belongs to the class of methylxanthines with which it shares a range of properties (theophylline, theobromine…). The powerful systemic pharmacological properties were soon noticed: cardiac, pulmonary, central nervous system… Its interest for the skin is more recent (around 30 years) but results, in fact, from the same ubiquitous mechanism, which, by inhibiting the phosphodiesterases, enables a consecutive elevation of the cell cAMP, which is a central messenger in biochemistry.
Caffeine, contrary to other more recent and more specific molecules (IPDE4), has no selectivity for the skin, but offers the advantage of being relatively safe and is approved by a large body of accumulated knowledge.
The increase of cAMP in the skin may synergize other mechanisms like melanogenesis and have regulatory properties on certain inflammations. The same mechanism increases peripheral blood flow and it has often been used in combination with other actives that stimulate the dermis to improve the quality and density of the tissues.
But it is for its action on the adipocyte that claims have most frequently been made. Indeed, by increasing cell lipase, caffeine helps to get rid of triglycerides. Other beneficial actions have now been discovered, alongside the principal effect. In addition, caffeine is a molecule that helps cutaneous diffusion and it has been used as a model in a great many studies. It has a lipophilic-hydrophilic balance that may enable it to be a good reference for studying cutaneous penetration.

Its action in vivo, without managing to be spectacular as regards deep, sclerous fat deposits for various reasons, particularly availability, is appreciable on recent and more moveable fat accumulations.
A great many well controlled, but not always published, studies mention significant losses of approximately 2 cm around the thigh. These results correspond to a 3 mm reduction of the adipose panniculus, which is an appreciable performance on average thicknesses of 2 cm, for example.
The reference concentrations generally range from 3 to 10%, depending on the formula, and a clear saturation of penetration for concentrations above these percentages.
For us, the best "reference to propose" is the concentration of 5% in a hydroalcoholic medium. Measurable results are obtained between 2 to 4 weeks. In our experience, a limit is reached at around 6 weeks. The result must then be maintained (a few applications a week), otherwise a return to the "base" state has been observed in the 3 months following the end of treatment.
The effects of caffeine are "accompanied" in a lot of products on the market, either by synergizing the effect on cAMP with forskolin, or by improving the effects on blood vessel resistance (Ruscus), or by playing on other factors that move the fat (insulin, hormones…) and restructure the dermis (Centella Asiatica).

  • EFFECTIVE DOSE

The body of publications and scientific studies, customary usages of this active and our expert's opinion concur in using Caffeine pure Active at the dose of 2500 mg per bottle.

  • BIBLIOGRAPHICAL REFERENCES

[1] New derivatives of methylxanthine: effect of thiocaffeine, thiothéophilline and 8-phenyltheophylline on lipolysis and on phospho diesterase activities. Scotini E et al. Pharmacol Res Commun, 15(2):131-143. 1983.

[2] Effects of caffeine on lipoprotein lipase gene expression during the adypocyte differentation process. Couturier C et al. Lipids, 33(5): 455-460. 1998.

[3] Inhibitory mechanism of caffeine on insulin-stimulated glucose uptake in adipose cells. Akiba T et al. Biochemical pharmacology, 68(10):1929-1937. 2004.

[4] A double-bind evaluation of the activity of an anti-cellulite product containing retinol, caffeine, and ruscogenine by a combination of several non-invasive method. Bertin C et al. J Cosmet Sci, 52(4):199-210. 2001.

[5] Cellulite et Caféine : percutanée. Etude récentes sur percutaféine.Compte rendu de thérapeutique/T VI/ N° 60/ Fevrier 1988. Belilowski.

[6] L’adipocyte dans une histoire d’amincissant. Franchi J et al. Pathologie Biologie, 51(5) :244-247. 2003.

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