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Modifying Cationic Liposomes with Cholesteryl-PEG Prevents Their Aggregation in Human Urine and Enhances Cellular Uptake by Bladder Cancer Cells
| Title: | Modifying Cationic Liposomes with Cholesteryl-PEG Prevents Their Aggregation in Human Urine and Enhances Cellular Uptake by Bladder Cancer Cells |
| Authors: | Nakamura, Takashi Browse this author →KAKEN DB | | Noma, Yosuke Browse this author | | Sakurai, Yu Browse this author | | Harashima, Hideyoshi Browse this author →KAKEN DB |
| Keywords: | cationic lipid | | drug delivery system | | liposome | | pegylation | | urine stability | | nanoparticle |
| Issue Date: | Feb-2017 |
| Publisher: | Pharmaceutical soc japan |
| Journal Title: | Biological & pharmaceutical bulletin |
| Volume: | 40 |
| Issue: | 2 |
| Start Page: | 234 |
| End Page: | 237 |
| Abstract: | 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. |
| Type: | article |
| URI: | http://hdl.handle.net/2115/64963 |
| Appears in Collections: | 薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)
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Submitter: 原島 秀吉
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