Mangiferin and Hesperidin Transdermal Distribution and Permeability through the Skin from Solutions and Honeybush Extracts (Cyclopia sp.)-A Comparison Ex Vivo Study.

Polyphenolic compounds-mangiferin and hesperidin-are, among others, the most important secondary metabolites of African shrub Cyclopia sp. (honeybush). The aim of this study was to compare the percutaneous absorption of mangiferin and hesperidin from solutions (water, ethanol 50%, (v/v)) and extracts obtained from green and fermented honeybush (water, ethanol 50%, (v/v)). Research was performed with the Bronaugh cells, on human dorsal skin. The mangiferin and hesperidin distributions in skin layers (stratum corneum, epidermis, and dermis) and in acceptor fluid (in every 2, 4, 6, and 24 h) were evaluated by HPLC-Photodiode Array Coulometric and Coulometric Electrochemical Array Detection. The transdermal distribution of hesperidin was also demonstrated by fluorescence microscopy. Results indicated that mangiferin and hesperidin were able to cross the stratum corneum and penetrate into the epidermis and dermis. An advantage of hesperidin penetration into the skin from the water over ethanol solution was observed (451.02 ± 14.50 vs. 357.39 ± 4.51 ng/cm2), as well as in the mangiferin study (127.56 ± 9.49 vs. 97.23 ± 2.92 ng/cm2). Furthermore, mangiferin penetration was more evident from nonfermented honeybush ethanol extract (189.85 ± 4.11 ng/cm2) than from solutions. The permeation of mangiferin and hesperidin through the skin to the acceptor fluid was observed regardless of whether the solution or the honeybush extract was applied. The highest ability to permeate the skin was demonstrated for the water solution of hesperidin (250.92 ± 16.01 ng/cm2), while the hesperidin occurring in the extracts permeated in a very low capacity. Mangiferin from nonfermented honeybush ethanol extract had the highest ability to permeate to the acceptor fluid within 24 h (152.36 ± 8.57 ng/cm2).

Transdermal transport of collagen and hyaluronic acid using water in oil microemulsion.

Collagen and hyaluronic acid (HA) are biopolymers that affect the appearance and condition of the skin. Delivery of these compounds into the skin is highly challenging since have a number of disadvantageous properties, such as high molecular weight and hydrophilicity. Here, we evaluated the transdermal penetration of low and high molecular weight collagen and HA from microemulsions. A number of microemulsion formulations, differing in the content of polymers and surfactants (i.e. penetration promoters), were used for the permeation study. In addition, a correlation was made between the composition of these microemulsions and the polymers transport efficiency. The results indicate that, microemulsions enable transdermal permeation of collagen and HA. The concentration of polymers and the solubilization capacity of microemulsions had the greatest influence on the permeation. Surprisingly, the molecular weight of polymers and the content of other components affected the size of microemulsion particles, and thus these parameters had an indirect influence on the permeation process. This study demonstrated therefore the potential therapeutic use of microemulsion with collagen and HA in improving and regenerating the barrier of aged or diseased skin.

The effect of mangiferin on skin: Penetration, permeation and inhibition of ECM enzymes.

Mangiferin (2-C-ß-D-glucopyranosyl-1,3,6,7-tetrahydroxyxanthone) is a polyphenol with strong antioxidant properties. Mangiferin is obtained from the mango tree (Mangifera indica L., Anacardiaceae). It has been proven that mangiferin exhibits many pharmacological activities. The aim of this study was to analyze the penetration of mangiferin into the human skin and through the skin. According to our knowledge, skin penetration and permeation studies of mangiferin have not been analyzed so far. Additionally, the influence of mangiferin on two Extracellular Matrix Enzymes (ECM): collagenase and elastase, was evaluated for the first time. It has been indicated that mangiferin is able to permeate the stratum corneum and penetrate into the epidermis and dermis in comparable amounts. For confirmation of the obtained results, fluorescence microscopy was successfully utilized. The analysis revealed the capability of mangiferin to reversibly inhibit elastase and collagenase activity. The mechanism of mangiferin interaction with both enzymes was estimated as a noncompetitive inhibition.

Commentary to the article "Human skin penetration of the major components of Australian tea tree oil applied in its pure form and as a 20% solution in vitro".

This note summarises recent studies on skin penetration of terpinen-4-ol, which is the main component of tea tree oil [S.E. Cross, M. Russell, I. Southwell, M.S. Roberts, Human skin penetration of the major components of Australian tea tree oil applied in its pure form and as a 20% solution in vitro, Eur. J. Pharm. Biopharm. doi: 10.1016/j.ejpb.2007.10.002 (in press)]. The influence of different experimental models on obtained skin penetration results is discussed.