Evaluation of the permeation of peat substances through human skin in vitro

• Published in: International journal of pharmaceutics 2003-03, Vol.253 (1), p.169-175
• Main Authors: Beer, André-M., Junginger, H.E., Lukanov, J., Sagorchev, P.
• Format: Article
• Language: English
• Subjects: Benzopyrans - isolation & purification; Benzopyrans - pharmacokinetics; Biological and medical sciences; Chromatography, High Pressure Liquid; Fulvic acid; General pharmacology; Humans; Humic Substances - isolation & purification; Humic Substances - pharmacokinetics; In Vitro Techniques; Medical sciences; Muscle Contraction - drug effects; Muscle, Smooth - drug effects; Peat; Permeability; Permeation; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Skin - metabolism; Skin Absorption; Smooth muscles; Soil; Ulmic acid
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/S0378-5173(02)00706-8

Peat and various peat extracts have been successfully applied for a variety of clinical indications. Quite apart from the physico-thermal effects, new studies point towards the so-called “chemical effects” of peat containing substances. These effects include a stimulatory response of the spontaneous contractile activity (SCA) of smooth muscle (SM) tissue. The effects are, however, dependent on the possible permeability of pharmacologically active substances as naturally occurring ingredients of peat. Since peat is a mixture of various products it is necessary to examine the various peat types based upon their biological activity on SM tissue. In order to unequivocally prove the pharmacological activity of cutaneous peat treatment, in vitro permeation measurements of these actives across excised human skin can be used. HPLC analysis revealed that aqueous peat extracts contain up to 18 fractions of water-soluble compounds of fulvic and ulmic acids. These compounds have been found to have a stimulatory response on the contractile activity of SM tissue. In vitro diffusion studies showed that the permeability of these substances across human full thickness skin (thickness: 200 um −1) is highly selective and the resulting stimulatory activity is dependent on the permeated fraction. Especially, the HPLC fractions 7–11 and 14 are able to permeate human skin. Fractions 7–11 show a moderate stimulatory effect of SCA on SM for more than 90 min whereas fraction 14 shows the strongest stimulatory effect which was, however, suppressed after 87 min. These results show that the cutaneous therapy with peat treatment results in transcutaneaous permeation of biologically active fulvic and ulmic acid derivatives explaining the additional “chemical” effect of peat treatment in clinical practice.