Pan-In Porntip, Wongsomboon Atthakorn, Kokpol Chayada, Chaichanawongsaroj Nuntaree, Wanichwecharungruang Supason
Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok, Thailand.
Technopreneurship and Innovation Management Program, Graduate School, Chulalongkorn University, Bangkok, Thailand.
J Pharmacol Sci. 2015 Dec;129(4):226-32. doi: 10.1016/j.jphs.2015.11.005. Epub 2015 Nov 19.
Although entrapment of nanoparticles of appropriate sizes at hair follicles has been clarified, there is no report on specific clinical application of this finding. Since sebaceous gland is associated with hair follicle, we hypothesize that effective acne vulgaris treatment/prevention can be achieved by depositing anti-acne agent in nanoparticle form at the hair follicles. Challenge of this strategy, however, lies at the finding of effective anti-acne particles with minimal skin irritation. Here using cellulose-based nanoparticles as nano-reservoir and α-mangostin (an active component isolated from the edible Garcinia mangostana Linn. fruit) as anti-acne agent, we prepare nanoparticles highly loaded with α-mangostin. Ability of the obtained particles to sustained release α-mangostin into synthetic sebum is demonstrated. The obtained mangostin particles are verified for their insignificant skin irritation through the two-week, twice-daily open application test in 20 healthy human volunteers. Excellent entrapment and sustainment of the mangostin nanoparticles at the hair follicles are elucidated in six human volunteers by detecting the presence of α-mangostin at the roots of hairs pulled from the treated skin area. The 4-week-randomized, double-blind, placebo-controlled, split-face study in 10 acne patients indicates significant improvement in acne vulgaris condition on the side twice daily applied with mangostin nanoparticles.
尽管毛囊对合适尺寸纳米颗粒的截留作用已得到阐明，但关于这一发现的具体临床应用尚无报道。由于皮脂腺与毛囊相关，我们推测通过在毛囊处沉积纳米颗粒形式的抗痤疮剂可实现寻常痤疮的有效治疗/预防。然而，该策略的挑战在于找到对皮肤刺激性最小的有效抗痤疮颗粒。在此，我们以纤维素基纳米颗粒作为纳米储库，以α-山竹素（从可食用的山竹果中分离出的一种活性成分）作为抗痤疮剂，制备了高负载α-山竹素的纳米颗粒。证明了所得颗粒将α-山竹素持续释放到合成皮脂中的能力。通过在20名健康人类志愿者中进行为期两周、每日两次的开放性应用试验，验证了所得山竹素颗粒对皮肤的刺激性极小。通过检测从治疗皮肤区域拔出的毛发根部α-山竹素的存在，在6名人类志愿者中阐明了山竹素纳米颗粒在毛囊处的良好截留和维持效果。在10名痤疮患者中进行的为期4周的随机、双盲、安慰剂对照、半脸研究表明，每天两次涂抹山竹素纳米颗粒的一侧寻常痤疮状况有显著改善。
