262598-45-8Relevant articles and documents
Synthesis and evaluation of water-soluble docetaxel prodrugs-docetaxel esters of malic acid
Du, Wenting,Hong, Lan,Yao, Tongwei,Yang, Xiaochun,He, Qiaojun,Yang, Bo,Hu, Yongzhou
, p. 6323 - 6330 (2007)
The synthesis of docetaxel esters of malic acid is described. These compounds were found to have greatly improved water solubility and are stable in solution at neutral pH. The C2′ modified compounds 2a-c and 3a-c behave as prodrugs, that is, docetaxel is
MODIFIED DRUGS FOR USE IN LIPOSOMAL NANOPARTICLES
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Paragraph 0270; 0342-0344, (2018/08/25)
Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.