RIPL peptide-conjugated nanostructured lipid carriers for enhanced intracellular drug delivery to hepsin-expressing cancer cells
DC Field | Value | Language |
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dc.contributor.author | Lee, Sang Gon | - |
dc.contributor.author | Kim, Chang Hyun | - |
dc.contributor.author | Sung, Si Woo | - |
dc.contributor.author | Lee, Eun Seok | - |
dc.contributor.author | Goh, Min Su | - |
dc.contributor.author | Yoon, Ho Yub | - |
dc.contributor.author | Kang, Myung Joo | - |
dc.contributor.author | Lee, Sangkil | - |
dc.contributor.author | Choi, Young Wook | - |
dc.date.available | 2019-01-22T14:20:11Z | - |
dc.date.issued | 2018-06 | - |
dc.identifier.issn | 1178-2013 | - |
dc.identifier.issn | 1178-2013 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/1491 | - |
dc.description.abstract | Background: To facilitate selective and enhanced drug delivery to hepsin (Hpn)-expressing cancer cells, RIPL peptide (IPLVVPLRRRRRRRRC, 16-mer)-conjugated nanostructured lipid carriers (RIPL-NLCs) were developed. Methods: NLCs were prepared using a solvent emulsification-evaporation method and the RIPL peptide was conjugated to the maleimide-derivatized NLCs via the thiol-maleimide reaction. Employing a fluorescent probe (DiI), in vitro target-selective intracellular uptake behaviors were observed using fluorescence microscopy and flow cytometry. Separately, docetaxel (DTX) was encapsulated by pre-loading technique, then cytotoxicity and drug release were evaluated. In vivo antitumor efficacy was investigated in BALB/c nude mice with SKOV3 cell tumors after intratumoral injections of different DTX formulations at a dose equivalent to 10 mg/kg DTX. Results: RIPL-NLCs showed positively charged nanodispersion, whereas NLCs were negatively charged. DTX was successfully encapsulated with an encapsulation efficiency and drug loading capacity of 95-98% and 44-46 mu g/mg, respectively. DTX release was diffusion-controlled, revealing the best fit to the Higuchi equation. Cellular uptake of DiI-loaded RIPL-NLCs was 8.3-and 6.2-fold higher than that of DiI-loaded NLCs, in Hpn(+) SKOV3 and LNCaP cells, respectively. The translocation of RIPL-NLCs into SKOV3 cells was time-dependent with internalization within 1 h and distribution throughout the cytoplasm after 2 h. DTX-loaded RIPL-NLCs (DTX-RIPL-NLCs) revealed dose-dependent in vitro cytotoxicity, while drug-free formulations were non-cytotoxic. In SKOV3-bearing xenograft mouse model, DTX-RIPL-NLCs significantly inhibited tumor growth: the inhibition ratios of the DTX solution-treated and DTX-RIPL-NLC-treated groups were 61.4% and 91.2%, respectively, compared to those of the saline-treated group (control). Conclusion: RIPL-NLCs are good candidates for Hpn-selective drug targeting with a high loading capacity of hydrophobic drug molecules. | - |
dc.format.extent | 16 | - |
dc.publisher | DOVE MEDICAL PRESS LTD | - |
dc.title | RIPL peptide-conjugated nanostructured lipid carriers for enhanced intracellular drug delivery to hepsin-expressing cancer cells | - |
dc.type | Article | - |
dc.identifier.doi | 10.2147/IJN.S166021 | - |
dc.identifier.bibliographicCitation | INTERNATIONAL JOURNAL OF NANOMEDICINE, v.13, pp 3263 - 3278 | - |
dc.description.isOpenAccess | Y | - |
dc.identifier.wosid | 000433629500001 | - |
dc.identifier.scopusid | 2-s2.0-85048291276 | - |
dc.citation.endPage | 3278 | - |
dc.citation.startPage | 3263 | - |
dc.citation.title | INTERNATIONAL JOURNAL OF NANOMEDICINE | - |
dc.citation.volume | 13 | - |
dc.type.docType | Article | - |
dc.publisher.location | 뉴질랜드 | - |
dc.subject.keywordAuthor | nanostructured lipid carriers | - |
dc.subject.keywordAuthor | RIPL peptide | - |
dc.subject.keywordAuthor | intracellular delivery | - |
dc.subject.keywordAuthor | docetaxel | - |
dc.subject.keywordAuthor | antitumor efficacy | - |
dc.subject.keywordAuthor | targeting | - |
dc.subject.keywordPlus | IN-VIVO EVALUATION | - |
dc.subject.keywordPlus | MULTIFUNCTIONAL TANDEM PEPTIDE | - |
dc.subject.keywordPlus | PACLITAXEL-LOADED LIPOSOMES | - |
dc.subject.keywordPlus | LUNG-CANCER | - |
dc.subject.keywordPlus | MACROMOLECULAR THERAPEUTICS | - |
dc.subject.keywordPlus | INTRATUMORAL INJECTION | - |
dc.subject.keywordPlus | PENETRATING PEPTIDES | - |
dc.subject.keywordPlus | ORAL BIOAVAILABILITY | - |
dc.subject.keywordPlus | SURFACE MODIFICATION | - |
dc.subject.keywordPlus | NANOPARTICLES | - |
dc.relation.journalResearchArea | Science & Technology - Other Topics | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Nanoscience & Nanotechnology | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | sci | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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