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  • Title: In-vivo pharmacokinetics, tissue distribution and anti-tumour effect of hydroxycamptothecin delivered in oil-in-water submicron emulsions.
    Author: Zhao YX, Liu DX, Liang WQ, Ye ZW.
    Journal: J Pharm Pharmacol; 2012 Jun; 64(6):783-91. PubMed ID: 22571256.
    Abstract:
    OBJECTIVES: The aim of this study was to investigate the pharmacokinetics, tissue distribution and anti-tumour effect of hydroxycamptothecin submicron emulsions (HCPT-SEs). METHODS: HCPT-SEs or HCPT injection (HCPT-I) was administered intravenously into the tail vein of rats or S180 tumour-bearing mice. KEY FINDINGS:   HCPT-SEs increased the plasma concentration of HCPT compared with HCPT-I at all time points. The AUC(0-∞) , elimination half-life and mean residence time of anionic submicron emulsions containing HCPT (HCPT-ASEs) and cationic submicron emulsions containing HCPT (HCPT-CSEs) were significantly greater than those of HCPT-I (P  <0.01). Especially, a prolonged elimination half-life was found for HCPT-CSEs. HCPT-CSEs and HCPT-ASEs resulted in a 7.9-fold and 3.1-fold increase in AUC(0-6h) of tumour compared with HCPT-I, respectively. The targeting efficiency (T(e) ) of HCPT-ASEs and HCPT-CSEs indicated their selectivity to tumour and the T(e) of HCPT-CSEs was significantly higher than that of HCPT-ASEs (P<0.01). The anti-tumour effect studies showed that HCPT-SEs improved the therapeutic efficiency of HCPT compared with HCPT-I. The percentage of tumour growth suppression rate of mice treated with HCPT-CSEs (2.0 mg HCPT eq./kg) increased 2.1 fold compared with that of HCPT-I. CONCLUSIONS: Submicron emulsions can alter the pharmacokinetic characteristics and tissue distribution of HCPT, and enhance tumour targeting and anti-tumour activity.
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