Xiao-juan Hu,1,* Yang Liu,1,* Xiao-feng Zhou,2,3 Qiao-ling Zhu,1 Yong-yan Bei,1 Ben-gang You,1 Chun-ge Zhang,1 Wei-liang Chen,1 Zhou-li Wang,1 Ai-jun Zhu,1 Xue-nong Zhang,1 Yu-jiang Fan4 1Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou, People's Republic of China; 2College of Radiological Medicine and Protection, Soochow University, People's Republic of China; 3Changshu Hospital of Traditional Chinese Medicine, Changshu, People's Republic of China; 4Department of Clinical Laboratory, Second People's Hospital of Akesu, Akesu, People's Republic of China *These authors contributed equally to this work Abstract: Novel amphiphilic chitosan derivatives (N-caprinoyl-N-trimethyl chitosan [CA-TMC]) were synthesized by grafting the hydrophobic moiety caprinoyl (CA) and hydrophilic moiety trimethyl chitosan to prepare carriers with good compatibility for poorly soluble drugs. Based on self-assembly, CA-TMC can form micelles with sizes ranging from 136 nm to 212 nm. The critical aggregation concentration increased from 0.6 mg · L-1 to 88 mg · L-1 with decrease in the degree of CA substitution. Osthole (OST) could be easily encapsulated into the CA-TMC micelles. The highest entrapment efficiency and drug loading of OST-loaded CA-TMC micelles(OST/CA-TMC) were 79.1% and 19.1%, respectively. The antitumor efficacy results show that OST/CA-TMC micelles have significant antitumor activity on Hela and MCF-7 cells, with a 50% of cell growth inhibition (IC50) of 35.8 and 46.7 µg · mL-1, respectively. Cell apoptosis was the main effect on cell death of Hela and MCF-7 cells after OST administration. The blank micelles did not affect apoptosis or cell death of Hela and MCF-7 cells. The fluorescence imaging results indicated that OST/CA-TMC micelles could be easily uptaken by Hela and MCF-7 cells and could localize in the cell nuclei. These findings suggest that CA-TMC micelles are promising carriers for OST delivery in cancer therapy. Keywords: N-trimethyl chitosan, micelle solubilization, antitumor activity

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efficacy cancer therapy keywords ntrimethyl chitosan drug loading selfassembly cell growth inhibition ic50 catmc chitosan derivatives entrapment efficiency

Hu XJ,Liu Y,Zhou XF,Zhu QL,Bei YY,You BG,Zhang CG,Chen WL,Wang ZL,Zhu AJ,Zhang XN,Fan YJ,.Synthesis and characterization of low-toxicity N-caprinoyl-N-trimethyl chitosan as self-assembled micelles carriers for osthole. 2013 (Issue 1),.

Hu XJ,Liu Y,Zhou XF,Zhu QL,Bei YY,You BG,Zhang CG,Chen WL,Wang ZL,Zhu AJ,Zhang XN,Fan YJ,"Synthesis and characterization of low-toxicity N-caprinoyl-N-trimethyl chitosan as self-assembled micelles carriers for osthole" 2013

Hu XJ,Liu Y,Zhou XF,Zhu QL,Bei YY,You BG,Zhang CG,Chen WL,Wang ZL,Zhu AJ,Zhang XN,Fan YJ,"Synthesis and characterization of low-toxicity N-caprinoyl-N-trimethyl chitosan as self-assembled micelles carriers for osthole"