A detachable coating of cholesterol-anchored PEG improves tumor targeting of cell-penetrating peptide-modified liposomes
Cell-penetrating peptides (CPPs) have been widely used to enhance the membrane translocation of various carriers for many years, but the non-specificity of CPPs seriously limits their utility in vivo. In this study, cholesterol-anchored, reduction-sensitive PEG (first synthesized by our laboratory)...
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| Format: | Article |
| Language: | English |
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Elsevier
2014-02-01
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| Series: | Acta Pharmaceutica Sinica B |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211383513001093 |
| _version_ | 1819263934025170944 |
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| author | Jie Tang Li Zhang Han Fu Qifang Kuang Huile Gao Zhirong Zhang Qin He |
| author_facet | Jie Tang Li Zhang Han Fu Qifang Kuang Huile Gao Zhirong Zhang Qin He |
| author_sort | Jie Tang |
| collection | DOAJ |
| description | Cell-penetrating peptides (CPPs) have been widely used to enhance the membrane translocation of various carriers for many years, but the non-specificity of CPPs seriously limits their utility in vivo. In this study, cholesterol-anchored, reduction-sensitive PEG (first synthesized by our laboratory) was applied to develop a co-modified liposome with improved tumor targeting. Following optimization of the formulation, the in vitro and in vivo properties of the co-modified liposome were evaluated. The co-modified liposome had a much lower cellular uptake and tumor spheroid uptake, but a much higher tumor accumulation compared to CPP-modified liposome, indicating the non-specific penetration of CPPs could be attenuated by the outer PEG coating. With the addition of exogenous reducing agent, both the in vitro and in vivo cellular uptake was markedly increased, demonstrating that the reduction-sensitive PEG coating achieved a controllable detachment from the surface of liposomes and did not affect the penetrating abilities of CPPs. The present results demonstrate that the combination of cholestervsitive PEG and CPPs is an ideal alternative for the application of CPP-modified carriers in vivo. |
| first_indexed | 2024-12-23T20:21:28Z |
| format | Article |
| id | doaj.art-6ee62495c65644d78f8d7193d29b0519 |
| institution | Directory Open Access Journal |
| issn | 2211-3835 2211-3843 |
| language | English |
| last_indexed | 2024-12-23T20:21:28Z |
| publishDate | 2014-02-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Acta Pharmaceutica Sinica B |
| spelling | doaj.art-6ee62495c65644d78f8d7193d29b05192022-12-21T17:32:31ZengElsevierActa Pharmaceutica Sinica B2211-38352211-38432014-02-0141677310.1016/j.apsb.2013.12.004A detachable coating of cholesterol-anchored PEG improves tumor targeting of cell-penetrating peptide-modified liposomesJie TangLi ZhangHan FuQifang KuangHuile GaoZhirong ZhangQin HeCell-penetrating peptides (CPPs) have been widely used to enhance the membrane translocation of various carriers for many years, but the non-specificity of CPPs seriously limits their utility in vivo. In this study, cholesterol-anchored, reduction-sensitive PEG (first synthesized by our laboratory) was applied to develop a co-modified liposome with improved tumor targeting. Following optimization of the formulation, the in vitro and in vivo properties of the co-modified liposome were evaluated. The co-modified liposome had a much lower cellular uptake and tumor spheroid uptake, but a much higher tumor accumulation compared to CPP-modified liposome, indicating the non-specific penetration of CPPs could be attenuated by the outer PEG coating. With the addition of exogenous reducing agent, both the in vitro and in vivo cellular uptake was markedly increased, demonstrating that the reduction-sensitive PEG coating achieved a controllable detachment from the surface of liposomes and did not affect the penetrating abilities of CPPs. The present results demonstrate that the combination of cholestervsitive PEG and CPPs is an ideal alternative for the application of CPP-modified carriers in vivo.http://www.sciencedirect.com/science/article/pii/S2211383513001093Cell penetrating peptideReduction-sensitive PEGTumor targetingCholesterolLiposome |
| spellingShingle | Jie Tang Li Zhang Han Fu Qifang Kuang Huile Gao Zhirong Zhang Qin He A detachable coating of cholesterol-anchored PEG improves tumor targeting of cell-penetrating peptide-modified liposomes Acta Pharmaceutica Sinica B Cell penetrating peptide Reduction-sensitive PEG Tumor targeting Cholesterol Liposome |
| title | A detachable coating of cholesterol-anchored PEG improves tumor targeting of cell-penetrating peptide-modified liposomes |
| title_full | A detachable coating of cholesterol-anchored PEG improves tumor targeting of cell-penetrating peptide-modified liposomes |
| title_fullStr | A detachable coating of cholesterol-anchored PEG improves tumor targeting of cell-penetrating peptide-modified liposomes |
| title_full_unstemmed | A detachable coating of cholesterol-anchored PEG improves tumor targeting of cell-penetrating peptide-modified liposomes |
| title_short | A detachable coating of cholesterol-anchored PEG improves tumor targeting of cell-penetrating peptide-modified liposomes |
| title_sort | detachable coating of cholesterol anchored peg improves tumor targeting of cell penetrating peptide modified liposomes |
| topic | Cell penetrating peptide Reduction-sensitive PEG Tumor targeting Cholesterol Liposome |
| url | http://www.sciencedirect.com/science/article/pii/S2211383513001093 |
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