Effect of Various Herbal and Chemical Enhancers on Skin Permeability to Cetirizine: A Study of Changes in Rat Skin Cells

Background: Cetirizine is a second-generation antihistamine with anti-allergy and anti-itching properties. The topical formulation of this medicine is used in androgenic alopecia treatment. Due to the hydrophilic nature of cetirizine, its skin absorption is negligible, so to increase its absorption, various enhancers were examined to see which can be used in the design of a topical formulation.Methods: First, the skin was exposed to enhancers, including eucalyptus, menthol, Tween ۸۰, propylene glycol, and oleic acid, for ۱ or ۲ hours. Then, the permeability parameters of the cetirizine solution and the structural changes of the skin after exposure to enhancers were analyzed by differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR) techniques.Results: The obtained results show that all used enhancers increased the permeability of the drug cetirizine compared to water. Various mechanisms, such as liquefaction of lipids, destruction of lipid structure, and irreversible denaturation of intracellular keratin, are involved in the increase in drug penetration caused by eucalyptus, mint, Tween ۸۰, propylene glycol, and oleic acid.Conclusions: The results showed that among the studied absorption enhancers, eucalyptus and Tween ۸۰ had the strongest, and propylene glycol had the weakest absorption enhancement effect after ۲- and ۱-hour pre-contact, respectively.

کلیدواژه ها:

Enhanced Absorption ، Skin Permeability ، Cetirizine ، DSC ، FT-IR