The Topic of Discussion: Dermatology in Cosmetics
Hydro-lipidic district dystrophia, commonly referred to as "cellulite" or orange peel skin, results from a defective lipid metabolism uneven texture; on palpation subcutaneous nodules are felt and pinching elicits pain. "cellulite" affects mainly wome n (about 80% while men rarely suffer it) and is amplified by female hormones favouring water retention, especially in but-tocks, thighs, legs, abdomen where the muscle is less stimulated and fats deposit easier. A con-nected factor is the hardening of adi pose lobules, typical of buttocks and the back of the thighs which are much more liable to compression due to frequent sitting.
Hereditary tendency might be triggered and bolstered by acquired mistakes like smoking (nicotine is notoriously arterioloconstrictor); wrong dietary habits (some subtances cause irritation of the liver and this reflects on the venous system); low assumpti on of liquids (especially water which would help local detoxication); excessive sun worshipping which induces dilatation of the venous wall re-ducing its elasticity, increasing it permeability and loss of transudate with local impairment.
Various treatments have been proposed and miscellaneous ingredients (e.g. botanical extracts such as Aesculus Hippocastanum, Cola Acuminata, Fucus Vesiculosus, Hedera Helix, etc.; mucopolysac-charides; proteases; saponins; xanthines; polyphenols; vitamins ) have been topically applied in manifold vehicles with controversial results.
A safe and effective solution for the cosmetic treatment of the hydro-lipidic district dystrophia is a low molecular weight organic molecule (Iodotrat) highly water-soluble, purified through recrystallization, highly stable even at > 80° C, at UV and s unlight. Iodotrat does not release iodine and meets the requirements of the Council Directive 76/768/EEC banning the cosmetic use of elemental iodine.
Comprehensive short term (acute oral and i.p. toxicity; eye irritation; acute skin irritation; skin sen-sitization according to Magnusson and Kligman and skin sensitization in man; phototoxicity; photo-allergenicity) and long term (15-week subacute toxici ty; 6-month chronic toxicity; subacute skin irritation; embryotoxicity and teratogenicity; carcinogenicity) toxicity studies were conducted to assess the safety of Iodotrat employed in the manufacture of topical products which by law must not be liable to cause damage to human health when they are applied under normal and reasonable an-ticipated conditions of use. Moreover Iodotrat dose not show any inhibition on specific skin en-zymes.
Idotrat is active at low use levels (0.8% is recommended for dermatological and cosmetic emulsions or gels - 8% in product for iontophoresis and slimming thermal baths) and at the recommended use level its solution has an eudermic pH (5.5). Conversely xan thine derivatives at effective use levels yield high pH values (8-9).
Formulating cosmetic and dermatological emulsions and lotions containing Iodotrat is easy and data on thermo- and fotostability, pH stability range in 18 months, syneresis check following centrifu-gation, thermo-viscosimetric behaviour and control of no-i odine release of model formulations are available.
Iodotrat has no inconvenience while escin can cause hemolysis; theophylline, theobromine, caffeine and aminophylline have a myolitic action and allergic reactions to proteases are reported. Moreover long term safety of some actives needs to be established and monitoring of serum level of xanthines is recommended to avoid serious toxicity.
Its efficacy was validated via histological studies, in vitro testing of enzyme (beta-oxydation cycle) activity and in vivo clinical evaluation.
Skin biopsies indicate a decrease of the inflammatory lymphocyte infiltration with a gradual rever-sal of the interstitial oedema.
Accordingly, accurate controls (i.e. clinical grading of pain intensity and duration, thickness of skin fold, skin roughness, micro- and macronodules) on volunteers confirmed a size reduction of the treated area and an improved skin surface tactility.
Likely mechanism of action of Iodotrat involves its activity on mast cells as described via histologi-cal studies. Mast cells, large cells in connective tissue, release vasoactive chemicals (e.g. histamine, heparin and serotonin) contained in many coarse cytoplasmic granules. In physiological condition the granule migrates to the cell perimeter, its membrane melts with plasma membrane and its con-tent is extruded. Being mainly localized close to blood vessels in the connective tissue, here as-phyctic due to vasosclerotic reaction, both mast cells and their cytoplasmic granules are reduced in the area affected by "cellulite", an definitely irritant disorder. Topical treatment with Iodotrat induces an increase in the number of mast cells and their granules probably thank to an effect mediated through a receptor.
Mast cells activation induces an improvement of blood circulation which sets up lipid motion on the beta-oxydation cycle (degradation pathway of fatty acids).
Indeed the distinctive "cellulite" issue (active liposynthesis combined with an extremely slowed down and incomplete catabolism leading to adipocyte overwhelming, receptor torpidity and reduced syn-thesis of the lipolytic enzymes responsible for the breakdown of triglycerides into glicerin and free fatty acids) is solved.