연구논문 : 인공피부모델을 이용한 트라넥삼산 제형의 피부투과도 및 자극 평가

The skin permeability of active ingredient is one of the most important issues for designing transdermal administration form. At the same time, the formulation should be non-irritant to skin. To evaluate skin permeability and irritancy, various methods have been proposed and ex vivo skin is the tool recommended by regulators. However its use is time consuming and requires numerous human donors. Owing to the similarity to real skin, reconstructed human epidermis model have been recognized as a useful tool. We simultaneously evaluated the permeability and irritancy of tranexamic acid in transdermal formulation using the KeraskinTM of MCTT, a three-dimensional reconstructed human epidermis. We applied 4 transdermal formulations to the KeraskinTM and after incubation for 6 hr, culture medium was collected. KeraskinTM was washed five times with DPBS and MTT assay was performed for measuring cell viability. The collected medium was analyzed by HPLC-MS/MS to determine the tranexamic acid concentration. Cell viability was calculated through dividing with the absorbance of MTT formazan of AHA/BHA non-containing vehicle group. No significant differences were found in four groups. The concentration of tranexamic acid in culture medium was determined by HPLCMS/MS; 11.0 ± 2.5μg/mL in tranexamic acid in AHA/BHA non-containing formulation, 24.6 ± 3.8μg/mL in tranexamic acid in AHA/BHA containing formulation and not detected in vehicle groups. These findings demonstrated that reconstructed human epidermis can be used for the simultaneous evaluation of the skin permeability and irritancy of transdermal drug and cosmetic ingredients or products.