Tumor regression after intravenous administration of targeted vesicles entrapping the vitamin E α-tocotrienol

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• 作者：Reatul Karim^a ; Sukrut Somani^a ; Majed Al Robaian^a ; Margaret Mullin^b ; Rumelo Amor^a ; Gail McConnell^a ; Christine Dufè ; s^a ; ^{C.Dufes@strath.ac.uk}
• 关键词：Tocotrienol ; Transferrin ; Tumor targeting ; Delivery system ; Cancer therapy
• 刊名：Journal of Controlled Release
• 出版年：2017
• 出版时间：28 January 2017
• 年：2017
• 卷：246
• 期：Complete
• 页码：79-87
• 全文大小：1418 K
• 卷排序：246

文摘

The therapeutic potential of tocotrienol, a member of the vitamin E family of compounds with potent in vitro anti-cancer properties, is limited by its inability to specifically reach tumors following intravenous administration. The purpose of this study is to determine whether a novel tumor-targeted vesicular formulation of tocotrienol would suppress the growth of A431 epidermoid carcinoma and B16-F10 melanoma in vitro and in vivo.In this work, we demonstrated that novel transferrin-bearing multilamellar vesicles entrapping α-T3 resulted in a dramatically improved (by at least 52-fold) therapeutic efficacy in vitro on A431 cell line, compared to the free drug. In addition, the intravenous administration of tocotrienol entrapped in transferrin-bearing vesicles resulted in tumor suppression for 30% of A431 and 60% of B16-F10 tumors, without visible toxicity. Mouse survival was enhanced by > 13 days compared to controls administered with the drug solution only.This tumor-targeted, tocotrienol-based nanomedicine therefore significantly improved the therapeutic response in cancer treatment.