Minghetti Paola, Casiraghi Antonella, Cilurzo Francesco, Gambaro Veniero, Montanari Luisa
Istituto di Chimica Farmaceutica e Tossicologica P. Pratesi, Via Mangiagalli 14, 20133 Milano, Italy.
Nat Prod Commun. 2009 Jan;4(1):133-7.
The antimicrobial, antifungal and anti-inflammatory properties of tea tree oil (TTO), the essential oil of Melaleuca alternifolia are well documented. In order to optimize its therapeutic activity, TTO patches were designed. The aim of this work was the formulation of monolayer patches containing TTO. Moreover, the performance of oleic acid (OA) as a skin penetration enhancer in patches was evaluated. Terpinen-4-ol (T4OL), the main component of TTO, was the marker used to evaluate TTO skin permeability. The permeation study was performed through human epidermis by using Franz diffusion cells. Patches were prepared by using methacrylic copolymers, Eudragit E100 (EuE100) or Eudragit NE (EuNE), and a silicone resin, BioPSA7-4602 (Bio-PSA). TTO and OA contents were fixed at 10% w/w and 3% w/w, respectively. The patches were prepared by a casting method and characterised in terms of T4OL content and skin permeability. All the selected polymers were suitable as the main component of the patch matrix. Since the main critical issue in the use of TTO is related to its toxicity after absorption, the local administration of TTO can take advantage of the use of patches based on EuE100 because of the high retained amount and the low permeation of T4OL. In this matrix, OA slightly increased the T4OL retained amount, improving the efficacy and safety of TTO patches.
互叶白千层精油茶树油(TTO)的抗菌、抗真菌和抗炎特性已有充分记载。为了优化其治疗活性,设计了TTO贴片。这项工作的目的是制备含TTO的单层贴片。此外,还评估了油酸(OA)作为贴片中皮肤渗透促进剂的性能。TTO的主要成分萜品-4-醇(T4OL)是用于评估TTO皮肤渗透性的标志物。使用Franz扩散池通过人表皮进行渗透研究。贴片采用甲基丙烯酸共聚物、Eudragit E100(EuE100)或Eudragit NE(EuNE)以及硅树脂BioPSA7-4602(Bio-PSA)制备。TTO和OA的含量分别固定为10% w/w和3% w/w。贴片采用浇铸法制备,并根据T4OL含量和皮肤渗透性进行表征。所有选定的聚合物都适合作为贴片基质的主要成分。由于使用TTO的主要关键问题与其吸收后的毒性有关,基于EuE100的贴片可用于TTO的局部给药,因为T4OL的保留量高且渗透性低。在这种基质中,OA略微增加了T4OL的保留量,提高了TTO贴片的疗效和安全性。