Cosmetic Division, NanoCarrier Co., Ltd., 144-15 Chuo, 226-39 Wakashiba, Kashiwa, Chiba 277-0871, Japan.
Cosmetic Division, NanoCarrier Co., Ltd., 144-15 Chuo, 226-39 Wakashiba, Kashiwa, Chiba 277-0871, Japan.
Int J Pharm. 2018 Dec 20;553(1-2):132-140. doi: 10.1016/j.ijpharm.2018.10.039. Epub 2018 Oct 16.
Polymeric micelles, which form through the self-assembly of poly(ethylene glycol)-poly(amino acid) block copolymers, are systemic nanocarriers in targeted cancer therapy. These micelles can encapsulate therapeutic compounds, such as lipophilic substances, charged compounds, and metal complexes, that have characteristics of increased solubility, sustained release, and improved tissue distribution. However, few studies have been conducted on the local distribution of polymeric micelles. Thus, we evaluated the skin penetration pattern of hydrophobic drugs in polymeric micelles. We revealed that improved water solubility by the encapsulation of the hydrophobic drugs indomethacin and resveratrol in polymeric micelles significantly increased the amount of drugs penetrating into the skin. Moreover, polymeric micelles did not enhance the permeability of drugs. Furthermore, although the polymers remained on or in the stratum corneum, the encapsulated drugs gradually moved deeper into the skin. These results indicate that encapsulated hydrophobic drugs in polymeric micelles can penetrate the living cell layer of the skin without bringing about unexpected side effects associated with other ingredients in the formulation. Thus, polymeric micelles for encapsulating hydrophobic drugs can be used for skin applications.
聚合物胶束通过聚乙二醇-聚氨基酸嵌段共聚物的自组装形成，是靶向癌症治疗中的系统纳米载体。这些胶束可以包裹治疗化合物，如亲脂性物质、带电化合物和金属配合物，具有增加溶解度、持续释放和改善组织分布的特点。然而，关于聚合物胶束的局部分布的研究很少。因此，我们评估了疏水性药物在聚合物胶束中的皮肤渗透模式。我们发现，通过将疏水性药物吲哚美辛和白藜芦醇包封在聚合物胶束中，可显著提高药物进入皮肤的量。此外，聚合物胶束不会增加药物的通透性。而且，尽管聚合物仍留在或位于角质层中，但包封的药物逐渐向皮肤深处移动。这些结果表明，聚合物胶束中包封的疏水性药物可以穿透皮肤的活细胞层，而不会引起配方中其他成分的意外副作用。因此，用于包封疏水性药物的聚合物胶束可用于皮肤应用。
