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载姜黄素的超分子水凝胶经皮给药治疗皮炎。

Transdermal delivery of curcumin-loaded supramolecular hydrogels for dermatitis treatment.

机构信息

School of Biological Science and Technology, University of Jinan, No. 336 West Road of Nanxinzhuang, Shandong Province, 250022, Jinan, China.

出版信息

J Mater Sci Mater Med. 2019 Jan 8;30(1):11. doi: 10.1007/s10856-018-6215-5.

Abstract

Curcumin (CUR) is a hydrophobic polyphenol with anti-inflammatory activity. However, its low water-solubility and poor skin permeation limited its application in the treatment of dermititis. CUR-loaded micelles were prepared using thin membrane hydration method with methoxy poly (ethylene glycol)-block-poly (ε-caprolactone) (MPEG-PCL) as carrier material. The drug loading capacity and encapsulation efficiency were 12.14 ± 0.33 and 93.57 ± 1.67%, respectively. CUR-loaded micelles increased CUR's water-solubility to 1.87 mg/mL, being 1.87 × 10-folds higher than native CUR. CUR-loaded supramolecular hydrogels (CUR-H) were prepared through mixing the CUR-loaded micelles solution with α-cyclodextrin (α-CD) solution. The CUR-H presented continuous dissolution behaviour in aqueous medium for 4.5 h. The ex vivo skin permeation test and confocal fluorescence microscopy evaluation confirmed that CUR-H obviously enhanced skin deposition of CUR without drug flux from skin. In vivo experimental results confirmed that the CUR-H was more effective than dexamethasone ointments against croton oil-induced ear edema. The CUR-H composed of MPEG-PCL and α-CD is a promising formulation for skin inflammatory treatment.

摘要

姜黄素(CUR)是一种具有抗炎活性的疏水性多酚。然而,其低水溶性和差的皮肤渗透性限制了其在治疗皮炎中的应用。采用薄膜水化法,以甲氧基聚乙二醇-嵌段-聚(ε-己内酯)(MPEG-PCL)为载体材料,制备了载姜黄素胶束。载药率和包封率分别为 12.14±0.33%和 93.57±1.67%。载姜黄素胶束将 CUR 的水溶性提高至 1.87mg/mL,是天然 CUR 的 1.87×10 倍。通过将载姜黄素胶束溶液与α-环糊精(α-CD)溶液混合,制备了载姜黄素超分子水凝胶(CUR-H)。CUR-H 在水介质中连续溶解 4.5h。离体皮肤渗透试验和共聚焦荧光显微镜评价证实,CUR-H 明显增加了 CUR 在皮肤中的沉积,而没有药物从皮肤中流出。体内实验结果证实,CUR-H 比地塞米松软膏更能有效对抗巴豆油诱导的耳肿胀。由 MPEG-PCL 和 α-CD 组成的 CUR-H 是一种有前途的皮肤炎症治疗制剂。

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