Buranajaree Supasiri, Donsing Piyaporn, Jeenapongsa Rattima, Viyoch Jarupa
Faculty of Pharmaceutical Sciences and Center of Excellence for Innovation in Chemistry, Naresuan University, Phitsanulok, 65000 Thailand.
J Cosmet Sci. 2011 Jan-Feb;62(1):1-14.
Melasma hyperpigmentation is an acquired disorder predominantly affecting the female population. The present study was conducted to determine the potential of a botanical extract to reduce observable hyperpigmentation. The extract from heartwood of Artocarpus incisus was formulated into nanoemulsions, and the depigmenting efficacy of the formulated nanoemulsion was determined in vivo. HPLC analysis showed that the extract contained artocarpin in an amount of 44.5 ± 0.1% w/w. The extract exhibited melanogenesis inhibition with an IC(50) value of 30.2 ± 2.4 mg/ml, while kojic acid, a well known lightening agent, exhibited an IC(50) of 51.4 ± 5.1 mg/ml. The nanoemulsion containing the extract was then formulated and prepared by the phase inversion technique. The concentration of the extract used was about six times its IC(50). The optimal formula containing 0.02% w/w extract, 41.6% w/w isopropyl myristate, 0.03% w/w α-tocopherol, 5% w/wglyc-eryl monostearate (co-emulsifier), 8% w/w ceteareth-10 (emulsifier), 0.05% triethanolamine, 0.03% w/w carbopol 940, and water adjusted to 100% w/w provided a homogeneous o/w emulsion with a droplet size of 325 ± 15 nm and a polydispersity of 0.31 ± 0.02. The depigmenting efficacy was then observed following topical application of the formulated nanoemulsion to UVB-stimulated hyperpigmented dorsal skin of C57BL/6 mice. A strongly visible decrease in hyperpigmentation was observed after six weeks of treatment with the formulated nanoemulsion. The degree of pigmentation decreased after the application was 84 ± 4 units, while that after the application of the extracted prepared into solution was 51 ± 3 units. The applied areas would return to their original color after treatment was stopped for four weeks.
黄褐斑色素沉着是一种主要影响女性群体的后天性疾病。本研究旨在确定一种植物提取物减少可见色素沉着的潜力。将面包树心材提取物制成纳米乳剂，并在体内测定其美白功效。高效液相色谱分析表明，该提取物中面包果精的含量为44.5±0.1%（w/w）。该提取物对黑色素生成的抑制IC50值为30.2±2.4mg/ml，而著名的美白剂曲酸的IC50值为51.4±5.1mg/ml。然后通过相转变技术制备含该提取物的纳米乳剂。所用提取物的浓度约为其IC50的6倍。最佳配方包含0.02%（w/w）提取物、41.6%（w/w）肉豆蔻酸异丙酯、0.03%（w/w）α-生育酚、5%（w/w）单硬脂酸甘油酯（助乳化剂）、8%（w/w）鲸蜡硬脂醇聚醚-10（乳化剂）、0.05%三乙醇胺、0.03%（w/w）卡波姆940，加水至100%（w/w），得到均匀的水包油型乳剂，液滴尺寸为325±15nm，多分散性为0.31±0.02。然后将制备好的纳米乳剂局部应用于经紫外线B照射产生色素沉着的C57BL/6小鼠背部皮肤，观察其美白功效。用制备好的纳米乳剂治疗六周后，色素沉着明显减轻。应用纳米乳剂后色素沉着程度降低了84±4个单位，而应用提取物溶液后为51±3个单位。停止治疗四周后，用药部位会恢复到原来的颜色。
