Reference - Detail
| RRC ID | 44066 |
|---|---|
| Author | Sato Y, Hatakeyama H, Sakurai Y, Hyodo M, Akita H, Harashima H. |
| Title | A pH-sensitive cationic lipid facilitates the delivery of liposomal siRNA and gene silencing activity in vitro and in vivo. |
| Journal | J Control Release |
| Abstract |
Modification of liposomal siRNA carriers with polyethylene glycol, i.e., PEGylation, is a generally accepted strategy for achieving in vivo stability and delivery to tumor tissue. However, PEGylation significantly inhibits both cellular uptake and the endosomal escape process of the carriers. In a previous study, we reported on the development of a multifunctional envelope-type nano device (MEND) for siRNA delivery and peptide-based functional devices for overcoming the limitations and succeeded in the efficient delivery of siRNA to tumors. In this study, we synthesized a pH-sensitive cationic lipid, YSK05, to overcome the limitations. The YSK05-MEND had a higher ability for endosomal escape than other MENDs containing conventional cationic lipids. The PEGylated YSK05-MEND induced efficient gene silencing and overcame the limitations followed by optimization of the lipid composition. Furthermore, the intratumoral administration of the YSK05-MEND resulted in a more efficient gene silencing compared with MENDs containing conventional cationic lipids. Collectively, these data confirm that YSK05 facilitates the endosomal escape of the MEND and thereby enhances the efficacy of siRNA delivery into cytosol and gene silencing. |
| Volume | 163(3) |
| Pages | 267-76 |
| Published | 2012-11-10 |
| DOI | 10.1016/j.jconrel.2012.09.009 |
| PII | S0168-3659(12)00695-5 |
| PMID | 23000694 |
| MeSH | Animals Cell Cycle Proteins / genetics Cell Line, Tumor Endocytosis Erythrocytes / drug effects Erythrocytes / pathology Gene Silencing* HeLa Cells Humans Hydrogen-Ion Concentration Lipids / administration & dosage* Lipids / chemistry Liposomes Male Mice Mice, Inbred BALB C Mice, Inbred ICR Nanostructures / chemistry Neoplasms / metabolism Peptides / chemistry Piperidines / administration & dosage* Piperidines / chemistry Protein Serine-Threonine Kinases / genetics Proto-Oncogene Proteins / genetics RNA, Small Interfering / administration & dosage* |
| IF | 7.727 |
| Times Cited | 154 |
| WOS Category | PHARMACOLOGY & PHARMACY CHEMISTRY, MULTIDISCIPLINARY |
| Altmetric score |
オルトメトリクス指標項目
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| The most frequently cited source | Patent(IFI CLAIMS) |
| Total number of mentions | 27 |
| Altmetric score changes over past 6months | 3.0 |
| Resource | |
| Human and Animal Cells | HeLa(RCB0007) |