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首页> 外文期刊>Biological & pharmaceutical bulletin >Modifying Cationic Liposomes with Cholesteryl-PEG Prevents Their Aggregation in Human Urine and Enhances Cellular Uptake by Bladder Cancer Cells
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Modifying Cationic Liposomes with Cholesteryl-PEG Prevents Their Aggregation in Human Urine and Enhances Cellular Uptake by Bladder Cancer Cells

机译：用胆固醇-PEG改性阳离子脂质体可防止它们在人尿中的聚集并通过膀胱癌细胞增强蜂窝摄取

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摘要

Intravesical drug delivery by cationic liposomes (Cat-LPs) represents a potent nanotechnology for enhancing therapeutic effects against bladder disorders. However, preventing the aggregation of Cat-LPs in urine poses a significant barrier. We report on an examination of the effect of modifying liposomes with polyethylene glycol (PEG) lipids to prevent Cat-LPs from aggregating in human urine. Although Cat-LPs underwent significant aggregation in human urine, introducing 5 mol% of PEG2k lipid or 2 mol% of PEG5k lipid completely inhibited the aggregation of the Cat-LPs. When 2 mol% of PEG2k lipids were introduced, the lipid structures of 1,2-distearoly-sn-glycero-3-phosphoethanolamine (DSPE) and 1,2-distearoyl-sn-glycerol (DSG) greatly prevented aggregation compared with cholesterol. By contrast, when Cat-LPs, after incubation in urine, were exposed to bladder cancer cells, only introducing cholesteryl-PEG into the Cat-LPs showed a significant enhancement in cellular uptake. These results offer the potential for incorporating cholesteryl-PEG into Cat-LPs for achieving both stability in urine and effective cellular uptake.
机译：阳离子脂质体（CAT-LPS）的膀胱内药物递送代表了一种有效的纳米技术，用于增强对膀胱疾病的治疗作用。然而，防止尿液中的猫LP的聚集姿势造成显着的屏障。我们报告了用聚乙二醇（PEG）脂质改性脂质体的效果的检查，以防止猫LPS在人尿中聚集。虽然CAT-LPS在人尿中进行了显着的聚集，但引入5摩尔％的PEG2K脂质或2摩尔％的PEG5K脂质完全抑制了CAT-LP的聚集。当引入2mol％的PEG2K脂质时，与胆固醇相比，1,2- Distearoly-Sn-甘油-3-磷酸乙醇胺（DSPE）和1,2-Distearoyl-Sn-甘油（DSG）的脂质结构大大防止了聚集。相比之下，当尿液尿液孵育后，暴露于膀胱癌细胞，仅将胆固醇-PEG引入CAT-LPS显示出蜂窝摄取的显着增强。这些结果提供了将胆固醇-PEG掺入CAT-LPS的可能性，以实现尿液中稳定性和有效的细胞吸收。

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