Abstract | BACKGROUND: METHODS:
SV119 was covalently linked with polyethylene glycol-dioleyl amido aspartic acid conjugate (PEG-DOA) to generate a novel functional lipid, SV119-PEG-DOA. This lipid was utilized for the preparation of targeted liposomes to enhance their uptake by cancer cells. Liposomes with various SV119 densities (0, 1, 3, and 5 mole%) were prepared and their cellular uptake was investigated in several tumor cell lines. In addition, doxorubicin (DOX) was loaded into the targeted and unmodified liposomes, and the cytotoxic effect on the DU-145 cells was evaluated by MTT assay. RESULTS:
Liposomes with or without SV119-PEG-DOA both have a mean diameter of approximately 90 nm and a neutral charge. The incorporation of SV119-PEG-DOA significantly increased the cellular uptake of liposomes by the DU-145, PC-3, A549, 201T, and MCF-7 tumor cells, which was shown by fluorescence microscopy and the quantitative measurement of fluorescence intensity. In contrast, the incorporation of SV119 did not increase the uptake of liposomes by the normal BEAS-2B cells. In a time course study, the uptake of SV119 liposomes by DU-145 cells was also significantly higher at each time point compared to the unmodified liposomes. Furthermore, the DOX-loaded SV119 liposomes showed significantly higher cytotoxicity to DU-145 cells compared to the DOX-loaded unmodified liposomes. CONCLUSION:
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Authors | Yifei Zhang, Yixian Huang, Peng Zhang, Xiang Gao, Robert B Gibbs, Song Li |
Journal | International journal of nanomedicine
(Int J Nanomedicine)
Vol. 7
Pg. 4473-85
( 2012)
ISSN: 1178-2013 [Electronic] New Zealand |
PMID | 22927761
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, U.S. Gov't, Non-P.H.S.)
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Chemical References |
- Antineoplastic Agents
- Azabicyclo Compounds
- Carbamates
- Ligands
- Liposomes
- Receptors, sigma
- Rhodamines
- SV119
- sigma-2 receptor
- Polyethylene Glycols
- Doxorubicin
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Topics |
- Antineoplastic Agents
(chemistry, pharmacokinetics, pharmacology)
- Azabicyclo Compounds
(chemistry, pharmacokinetics)
- Carbamates
(chemistry, pharmacokinetics)
- Cell Line, Tumor
- Cell Survival
(drug effects)
- Doxorubicin
(chemistry, pharmacokinetics, pharmacology)
- Humans
- Ligands
- Liposomes
(chemistry, pharmacokinetics, pharmacology)
- Particle Size
- Polyethylene Glycols
(chemistry)
- Receptors, sigma
(metabolism)
- Rhodamines
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