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Self-defensive nano-assemblies from camptothecin-based antitumor drugs 5th China-Europe Symposium on Biomaterials in Regenerative Medicine(CESB 2015)Hangzhou,China April 7–10,2015 被引量:1

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摘要 Camptothecin(CPT)-based drugs always undergo the reversible,pH-dependent lactone ring-opening reaction,yielding the inactive but toxic carboxylate form.Self-assembly strategy provides an effective route for preserving their bio-stability.In this article,nano-sized self-assemblies from CPTbased antitumor drugs were simply built up by directly diluting the stock dimethylsulfoxide solutions of(S)-(t)-CPT,(S)-10-hydroxyl camptothecin and carboxylic CPT with water/phosphatebuffered saline solution.Because of their different molecular structures in A-ring or modification on the 20-OH group,CPT self-assembled into helical nano-ribbons,whereas 10-hydroxycamptothecin and carboxylic CPT self-aggregated into flat nano-ribbons and cylindric nano-rods,respectively.Attractively,the self-assembly of CPT-based drugs could occur within 1 min at a low concentration of 1×10^(-5)M.Adopting the J-type self-aggregation,self-assemblies were stable in aqueous solution and could effectively protect the CPT-based drugs from hydrolysis,which thereby kept their bioactivity for tumor therapy.
出处 《Regenerative Biomaterials》 SCIE 2015年第3期159-166,共8页 再生生物材料(英文版)
基金 This work was supported by the National Natural Science Foundation of China(51125014,51233003 and 21474077) the Ministry of Science and Technology of China(2011CB606202).
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