25905-73-1Relevant articles and documents
Docetaxel prodrug self-assembled nanosystem: Synthesis, formulation and cytotoxicity
Jing, Fanbo,Guo, Qie,Xu, Wen,Qu, Haijun,Sui, Zhongguo
, p. 826 - 830 (2018)
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.
Disulfide bond bridged docetaxel-fatty acid prodrugs and self-assembled nanoparticles thereof
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Paragraph 0037-0038, (2021/04/07)
According to the invention, a series of reduction-sensitive disulfide bond bridged docetaxel fatty acid prodrugs are designed and synthesized. The series of prodrugs can be self-assembled into a nano drug delivery system through a one-step nano precipitation method. The nano drug delivery system has the following advantages that: docetaxel is prepared into a disulfide bond connected prodrug, so that the system toxicity of a docetaxel parent drug is reduced, the parent drug can be specifically released in a high reduction environment in tumor cells, and the effects of synergy and toxicity reduction are achieved; the drug loading capacity is high, the use of a solubilizer with higher toxicity is avoided, and the tolerance and the compliance of a patient are expected to be improved; through the one-step nano precipitation method, the preparation process is simple, and large-scale production is easy; the nanoparticles are small and uniform in particle size and are easily enriched at a tumor part through an EPR effect; and surface modification is easy, and removal of a reticuloendothelial system can be slowed down through modification of PEG modification.
Facile synthesis of lysophospholipids containing unsaturated fatty acid chains
Hopper, Darrin W.,Catalano, John G.,Macdonald, Timothy L.
, p. 7871 - 7874 (2007/10/03)
The efficient synthesis of polyunsaturated phospholipids is challenging due to the sensitivity of the unsaturated moiety to the conditions employed in phosphate ester deprotection. We discuss here three independent methods that resolve this issue and enable the synthesis of a series of unsaturated lysophosphatidic acid mimics for the development of a more comprehensive understanding of the structure-activity relationship in this series.
