Kitagawa Shuji, Inoue Kana, Teraoka Reiko, Morita Shin-ya
Kobe Pharmaceutical University, Kobe 658-8558, Japan.
Chem Pharm Bull (Tokyo). 2010 Mar;58(3):398-401. doi: 10.1248/cpb.58.398.
To improve the efficiency of the intradermal delivery of genistein and other two isoflavones (daidzein and biochanin A), we tried to clarify the usefulness of microemulsion by in vitro study on excised guinea pig dorsal skin and Yucatan micropig skin. Using microemulsion consisting of isopropyl myristate (IPM), 150 mM NaCl solution, Tween 80 and ethanol as a vehicle, the solubility of all the isoflavones markedly increased and significant amounts of isoflavones were delivered to the skin. The effect of water-in-oil (w/o)-type microemulsion D was larger than that of oil-in-water (o/w)-type microemulsion A. Among three isoflavones tested, the increase of genistein was most marked on both solubility and skin accumulation. Genistein retained in the skin significantly inhibited lipid peroxidation in vitro dose-dependently. Furthermore, pretreatment of guinea pig dorsal skin with genistein containing gel-like microemulsion D prevented UV irradiation-induced erythema formation. These findings indicate the potential use of w/o-type microemulsion for the delivery of genistein to protect skin against UV-induced oxidative damage.
为提高染料木黄酮及其他两种异黄酮（大豆苷元和鹰嘴豆芽素A）皮内给药的效率，我们通过对豚鼠背部离体皮肤和尤卡坦小型猪皮肤进行体外研究，试图阐明微乳剂的效用。以肉豆蔻酸异丙酯（IPM）、150 mM氯化钠溶液、吐温80和乙醇组成的微乳剂作为载体，所有异黄酮的溶解度均显著增加，且大量异黄酮被输送至皮肤。油包水（w/o）型微乳剂D的效果大于水包油（o/w）型微乳剂A。在所测试的三种异黄酮中，染料木黄酮在溶解度和皮肤蓄积方面的增加最为显著。皮肤中留存的染料木黄酮在体外剂量依赖性地显著抑制脂质过氧化。此外，用含染料木黄酮的凝胶状微乳剂D预处理豚鼠背部皮肤可预防紫外线照射引起的红斑形成。这些发现表明，w/o型微乳剂在输送染料木黄酮以保护皮肤免受紫外线诱导的氧化损伤方面具有潜在用途。
