Docetaxel prodrug self-assembled nanosystem: Synthesis, formulation and cytotoxicity. Issue 4 (15th February 2018)

• Record Type: Journal Article
• Authors: Jing, Fanbo; Guo, Qie; Xu, Wen; Qu, Haijun; Sui, Zhongguo
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 4(2018)
• Page Start: 826
• Page End: 830
• Publication Date: 2018-02-15
• Subjects: Docetaxel -- Oleic acid -- Thioether bond -- Self-assembled nanosystem -- Redox-sensitive; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.07.041
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Conventional drug delivery systems of docetaxel (DTX) are challenged with low drug loading efficiency and potential carriers-induced toxicity. In this work, a docetaxel prodrug self-assembled nanosystem was designed and synthesized by conjugating docetaxel with oleic acid (OA) exploring a thioether as the linker, which is redox-sensitive to the redox environment within tumor cells. Notably, the carrier-free nanomedicine which does not need any carrier has obviously high drug loading that reaches 58%. Moreover, the cytotoxicity of DTX-S-OA maintains an equal level with DTX. The novel prodrug conjugate therefore has a promising perspective as carrier-free nanomedicine for cancer therapy due to its high drug loading property, redox-sensitive release and long circulation mechanism.