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LOW-DIMENSIONAL SOLIDS AND MOLECULAR CRYSTALS

Design of guaiazulene derivatives-conjugated podophyllotoxin nano-prodrug toward anticancer drug delivery

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Pages 100-108 | Published online: 25 Mar 2022
 

Abstract

In nanoparticle-based drug delivery systems, dispersion stability is one of the most significant factors controlling drug efficacy and side effects. Herein, we synthesized guaiazulene derivatives-conjugated podophyllotoxin prodrugs and fabricated their nanoparticles (GA-CN-PPT nano-prodrugs). GA-CN-PPT nano-prodrugs were obtained with a size of about 100 nm and possessed high dispersion stability. The cytotoxicity was tunable by changing the length of the carbon chain linker. Notably, the release rate of PPT was the key factor for the anticancer activity of GA-CN-PPT nano-prodrugs. The nano-prodrugs could serve as a promising template for developing a novel delivery system using nano-prodrugs.

Additional information

Funding

This study was supported by JSPS Grants-in-Aid for Scientific Research (No. 19K15690, and No. 19H02785), the Cooperative Research Program of “Network Joint Research Center for Materials and Devices”, and the Research Program of “Dynamic Alliance for Open Innovation Bridging Human, Environment and Materials” in “Network Joint Research Center for Materials and Devices”.

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