Preparation and tumor targeting of NGR-SWCNTs-paclitaxel / 中国药学杂志

ABSTRACT

OBJECTIVE: To investigate the best method for preparing NGR-SWCNTs-paclitaxel and observe its targeting efficiency. 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 12; Poloxamerl88-phenylalanine was 73; 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.