RIPL peptide (IPLVVPLRRRRRRRRC)-conjugated liposomes for enhanced intracellular drug delivery to hepsin-expressing cancer cells
DC Field | Value | Language |
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dc.contributor.author | Kang, Min Hyung | - |
dc.contributor.author | Park, Min Jung | - |
dc.contributor.author | Yoo, Hyun Joon | - |
dc.contributor.author | Hyuk, Kwon Yie | - |
dc.contributor.author | Lee, Sang Gon | - |
dc.contributor.author | Kim, Sung Rae | - |
dc.contributor.author | Yeom, Dong Woo | - |
dc.contributor.author | Kang, Myung Joo | - |
dc.contributor.author | Choi, Young Wook | - |
dc.date.available | 2019-03-08T21:38:25Z | - |
dc.date.issued | 2014-08 | - |
dc.identifier.issn | 0939-6411 | - |
dc.identifier.issn | 1873-3441 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/11975 | - |
dc.description.abstract | Background: To facilitate selective drug delivery to hepsin (Hpn)-expressing cancer cells, the RIPL peptide (IPLVVPLARRARRRRC; 16mer; 2.1 kDa) was synthesized as a novel cell penetrating/homing peptide (CPHP) and conjugated to a liposomal carrier. Methods: RIPL peptide-conjugated liposomes (RIPL-Lipo) were prepared by conjugating RIPL peptides to maleimide-derivatized liposomal vesicles via the thiol-maleimide reaction. Vesicle size and zeta potential were examined using a Zetasizer. Intracellular uptake specificity of the RIPL peptide, or RIPL-Lipo, was assessed by measuring mean fluorescence intensity (MFI) after treatment with a fluorescent marker in various cell lines: SK-OV-3, MCF-7, and LNCaP for Hpn(+); DU145, PC3, and HaCaT for Hpn(). FITC-dextran was used as a model compound. Selective translocational behavior of RIPL-Lipo to LNCaP cells was visualized by fluorescence microscopy and confocal laser scanning microscopy. Cytotoxicities of the RIPL peptide and RIPL-Lipo were evaluated by WST-1 assay. Results: RIPL peptides exhibited significant Hpn-selectivity. RIPL-Lipo systems were of positively charged nanodispersion (165 nm in average; 6-24 mV depending on RIPL conjugation ratio). RIPL-Lipo with the conjugation of 2300 peptide molecules revealed the greatest MFI in all cell lines tested. Cellular uptake of RIPL-Lipo increased by 20- to 70-fold in Hpn(+) cells, and 5- to 7-fold in Hpn() cells, compared to the uptake of FITC-dextran. Cytosolic internalization of RIPL-Lipo was time-dependent: bound instantly; internalized within 30 mm; distributed throughout the cytoplasm after 1 h. Cytotoxicities of RIPL peptide (up to 50 mu M) and RIPL-Lipo (up to 10%) were minor (cell viability >90%) in LNCaP and HaCaT cells. Conclusion: By employing a novel CPHP, the RIPL-Lipo system was successfully developed for Hpn-specific drug delivery. (C) 2014 Elsevier B.V. All rights reserved. | - |
dc.format.extent | 11 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | ELSEVIER SCIENCE BV | - |
dc.title | RIPL peptide (IPLVVPLRRRRRRRRC)-conjugated liposomes for enhanced intracellular drug delivery to hepsin-expressing cancer cells | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.ejpb.2014.03.016 | - |
dc.identifier.bibliographicCitation | EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, v.87, no.3, pp 489 - 499 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000340141600008 | - |
dc.identifier.scopusid | 2-s2.0-84904263868 | - |
dc.citation.endPage | 499 | - |
dc.citation.number | 3 | - |
dc.citation.startPage | 489 | - |
dc.citation.title | EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS | - |
dc.citation.volume | 87 | - |
dc.type.docType | Article | - |
dc.publisher.location | 네델란드 | - |
dc.subject.keywordAuthor | Liposome | - |
dc.subject.keywordAuthor | Cell penetrating/homing peptide | - |
dc.subject.keywordAuthor | Intracellular delivery | - |
dc.subject.keywordAuthor | Polyarginine | - |
dc.subject.keywordAuthor | IPL | - |
dc.subject.keywordAuthor | Targeting | - |
dc.subject.keywordAuthor | Hepsin | - |
dc.subject.keywordPlus | ARGININE-RICH PEPTIDES | - |
dc.subject.keywordPlus | PENETRATING PEPTIDES | - |
dc.subject.keywordPlus | CELLULAR-UPTAKE | - |
dc.subject.keywordPlus | PROSTATE-CANCER | - |
dc.subject.keywordPlus | IN-VIVO | - |
dc.subject.keywordPlus | MEMBRANE ANTIGEN | - |
dc.subject.keywordPlus | MAMMALIAN-CELL | - |
dc.subject.keywordPlus | TAT PEPTIDE | - |
dc.subject.keywordPlus | NANOPARTICLES | - |
dc.subject.keywordPlus | THERAPY | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | sci | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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