Kwankaew Jutatip, Phimnuan Preeyawass, Wanauppathamkul Sombat, Viyoch Jarupa
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Center of Excellence for Innovation in Chemistry, Naresuan University, Phitsanulok, 65000 Thailand (J.K., P.P., J.V.), and International Laboratories Corp. Ltd., Sadhupradist Road, Chongnonsi, Yannawa, Bangkok, 10120 Thailand (S.W.).
J Cosmet Sci. 2017 Jul/Aug;68(4):257-269.
heartwood extract contains the bioactive compound artocarpin which exhibits melanogenesis inhibitory activity. However, the extract has poor solubility which affects the skin permeability of the compound. A chitosan hydrogel patch incorporating heartwood extract was formulated to enhance the delivery of an amount of artocarpin sufficient for depigmenting the skin. The extract was prepared as an o/w microemulsion before blending with an aqueous solution of chitosan. The hydrogel patch was formulated by blending in a 1:1 ratio by weight of 4% w/w chitosan solution and 0.04% w/w extract microemulsion which provides optimal values of the mechanical properties of the patch. The release of artocarpin from the formulated patch (artocarpin content, 0.07 mg/cm) exhibited two phases; the rapid rate (0-15 min) averaged 0.73 µg/min/mm, and the slow rate (15-240 min) averaged 0.02 µg/min/mm. The formulated patches significantly improved the hyperpigmented area of the subjects after 3 weeks of application. No adverse events were observed. The results indicate that the formulated chitosan hydrogel patch delivers an effective amount of incorporated artocarpin depigmenting action.
心材提取物含有具有黑素生成抑制活性的生物活性化合物波罗蜜木素。然而，该提取物的溶解度较差，这影响了该化合物的皮肤渗透性。制备了一种含有心材提取物的壳聚糖水凝胶贴剂，以增强足以使皮肤色素脱失的一定量波罗蜜木素的递送。在与壳聚糖水溶液混合之前，将提取物制备成水包油型微乳剂。通过将4% w/w壳聚糖溶液和0.04% w/w提取物微乳剂按重量比1:1混合来制备水凝胶贴剂，这为贴剂提供了最佳的机械性能值。从制备的贴剂（波罗蜜木素含量为0.07 mg/cm）中释放波罗蜜木素呈现两个阶段；快速阶段（0 - 15分钟）平均为0.73 µg/分钟/毫米，缓慢阶段（15 - 240分钟）平均为0.02 µg/分钟/毫米。在应用3周后，制备的贴剂显著改善了受试者的色素沉着过度区域。未观察到不良事件。结果表明，制备的壳聚糖水凝胶贴剂递送了有效量的掺入的具有色素脱失作用的波罗蜜木素。
