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用于靛玉红类似物透皮递送的混合胶束制剂。

A Mixed Micellar Formulation for the Transdermal Delivery of an Indirubin Analog.

作者信息

Seo Seol Hwa, Kim Eunhwan, Joo Yechan, Lee Juseung, Oh Kyung Taek, Hwang Sung-Joo, Choi Kang-Yell

机构信息

Department of Biotechnology, College of Life Science and Biotechnology, Yonsei University, Seoul 03722, Korea.

College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Seoul 21983, Korea.

出版信息

Pharmaceutics. 2020 Feb 19;12(2):175. doi: 10.3390/pharmaceutics12020175.

Abstract

Indirubin is an active component of Dang Gui Long Hui Wan, which has been used in traditional Chinese medicine to treat inflammatory diseases as well as for the prevention and treatment of human cancer, such as chronic myeloid leukemia. The therapeutic effects of indirubin analogs have been underestimated due to its poor water solubility and low bioavailability. To improve the solubility and bioavailability of indirubin analogs, we prepared a mixed micellar formulation with Kolliphor® EL and Tween 80 as surfactants, and PEG 400 as a co-surfactant, followed by complexation with (2-hydroxyproply)-β-cyclodextrin at appropriate ratios. Overall, improving the solubility and skin penetration of indirubin analogs can increase clinical efficacy and provide maximum flux through the skin.

摘要

靛玉红是当归龙荟丸的一种活性成分,该丸剂在传统中药中用于治疗炎症性疾病以及预防和治疗人类癌症,如慢性粒细胞白血病。由于靛玉红类似物的水溶性差和生物利用度低,其治疗效果一直被低估。为了提高靛玉红类似物的溶解度和生物利用度,我们制备了一种以科丽素®EL和吐温80为表面活性剂、聚乙二醇400为助表面活性剂的混合胶束制剂,然后以适当比例与(2-羟丙基)-β-环糊精络合。总体而言,提高靛玉红类似物的溶解度和皮肤渗透性可提高临床疗效并使经皮通量最大化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24d1/7076637/d2562fc54632/pharmaceutics-12-00175-g001.jpg

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