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首页> 外文期刊>Acta pharmaceutica: a quarterly journal of Croatian Pharmaceutical Society and Slovenian Pharmaceutical Society, dealing with all branches of pharmacy and allied sciences >Enhanced delivery of etoposide to Dalton's lymphoma in mice through polysorbate 20 micelles.
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Enhanced delivery of etoposide to Dalton's lymphoma in mice through polysorbate 20 micelles.

机译：依托泊苷通过聚山梨酯20胶束向小鼠道尔顿淋巴瘤的递送增强。

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The study evaluates the possibility of enhancing uptake of etoposide (topoisomerase II inhibitor) by tumor when delivered through polysorbate 20 micelles. The micelle formation was ascertained by determining the critical micellar concentration (CMC) with a du Nouy ring tensiometer and by size measurement using dynamic light scattering. Addition of 5% ethanol decreased the CMC of Polysorbate 20 (from 5.0 x 10(-5) to 4.54 x 10(-5) mol L(-1)). Etoposide (ET) and etoposide loaded polysorbate 20 micelles (EPM) were radiolabeled with (99m)Tc by the reduction method using stannous chloride. Labeling parameters were optimized to obtain high labeling efficiency. The diethylenetriaminepentaacetic acid and cysteine challenge tests showed very low transchelation of (99m)Tc-ET and (99m)Tc-EPM complexes indicating their in vitro stability. The complexes also exhibited serum stability assessed by ascending thin layer chromatography. Subcutaneous injection of EPM resulted in significantly higher tumor uptake ( 100 folds compared to ET 6 h post injection) (p < 0.001) and prolonged tumor retention. Tumor uptake was also confirmed by gamma imaging studies. EPM exhibited relatively high brain concentrations ( 7 fold 24 h post injection) compared to ET, suggesting the potential use of EPM in the treatment of brain malignancies.
机译：该研究评估了通过聚山梨醇酯20胶束递送时，肿瘤增强依托泊苷（拓扑异构酶II抑制剂）摄取的可能性。通过使用du Nouy环张力计确定临界胶束浓度（CMC）并通过使用动态光散射的尺寸测量来确定胶束的形成。添加5％乙醇会降低聚山梨酯20的CMC（从5.0 x 10（-5）降至4.54 x 10（-5）mol L（-1））。依托泊苷（ET）和负载依托泊苷的聚山梨酯20胶束（EPM）通过氯化亚锡的还原方法用（99m）Tc进行放射性标记。优化了标记参数以获得高标记效率。二亚乙基三胺五乙酸和半胱氨酸激发试验表明，（99m）Tc-ET和（99m）Tc-EPM复合物的转运非常低，表明它们的体外稳定性。该复合物还显示出通过上升薄层色谱法评估的血清稳定性。皮下注射EPM导致明显更高的肿瘤吸收（与注射后6 h的ET相比高100倍）（p <0.001）和延长的肿瘤保留。 γ摄取成像研究也证实了肿瘤吸收。与ET相比，EPM表现出相对较高的脑部浓度（注射后24小时7倍），表明EPM在治疗脑恶性肿瘤方面具有潜在的用途。

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