1a.Department of Pathophysiology, School of Basic Medical Sciences, 1b.School of Pharmaceutical Sciences, Zhengzhou 450001, China; 2.The Fifth Affiliated Hospital of Zhengzhou University, Zhengzhou 450001, China
Abstract��
To investigate the best method for preparing NGR-SWCNTs-paclitaxel and observe its targeting efficency. METHODS SWCNTs-paclitaxel was prepared by solution mixing, and then conjugated with NGR to obtain a novel paclitaxel delivery system:NGR-SWCNTs-paclitaxel. Taking loading efficiency and encapsulate efficiency as index,studied the influential factors of the preparation of NGR-SWCNTs-paclitaxel by surfactant��times and frequency of probe sonography, quantity of carbon nano tube. The drug concentration in different tissue were detected by high performance liquid chromatography(HPLC).The targeting efficiency were used to evaluate the tissue targeting of NGR-SWCNTs-paclitaxel, SWCNTs-paclitaxel and paclitaxel.RESULTS SWCNTs-paclitaxel was prepared by SWCNTs-paclitaxel was 1��2; Poloxamer188-phenylalanine was 7��3;probe sonography 600 W,15 times. SWCNTs-paclitaxel conjugated with NGR formed NGR-SWCNTs-paclitaxel . Its loading efficiency was (83.9±2.7)% and encapsulate efficiency was (69.3±1.5)%. The Zeta potential was(-22.6±1.5)mV, partical size was about(182.1±2.4)nm. The AUC of NGR-SWCNTs-paclitaxel and SWCNTs-paclitaxel in mice slpeen��liver��lung and tumor were increased obviously compared with paclitaxel(P<0.05,P<0.01).The targeting efficiency of SWCNTs-paclitaxel and NGR-SWCNTs-paclitaxel in heart and kidney were decreased(P<0.05), and in tumor the targeting efficiency was 6.78% and 21.33% separately, the difference was significantly(P<0.01). CONCLUSION The preparation of NGR-SWCNTs- paclitaxel was practicable by solution mixing. The loading efficiency and encapsulate efficiency of NGR-SWCNTs-paclitaxel are higher. NGR-SWCNTs-paclitaxel can enhance tumor targeting of paclitaxel obviously.
ZHANG Yan-Yan-a,
FU Xu-Dong-,
LIU Kang-Dong-a etc
.Preparation and Tumor Targeting of NGR-SWCNTs-Paclitaxel[J] Chinese Pharmaceutical Journal, 2013,V48(20): 1748-1754
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2013, Vol. 48 
