Sterically polymer-based liposomal complexes with dual-shell structure for enhancing the siRNA delivery

Shuian Yin Lin, Wei Yu Zhao, Hsieh Chih Tsai, Wei Hsin Hsu, Chun Liang Lo*, Ging Ho Hsiue

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

26 Scopus citations

Abstract

The sterically polymer-based liposomal complexes (SPLexes) were formed by cationic polymeric liposomes and pH-sensitive diblock copolymer were studied for their capabilities in improving the stability with high efficiency of siRNA delivery. The SPLexes were formed a dual-shelled structure and uniform size distribution. The PEGylated outer shell could mitigate the phagocytosis and reduce the cytotoxicity. Moreover, the folated SPLexes improved 42.9× accumulation in vitro and 1.7× tumor uptake in vivo in contrast with nonfolated SPLexes. The protonated copolymer at low pH would improve the siRNA released into cytoplasm following SPLexes fusion with the endo/lysosome membrane and inhibited the protein expression to 75.6 ± 4.5% efficiently. Results of this study significantly contribute to efforts to develop lipoplexes based siRNA delivery systems.

Original languageEnglish
Pages (from-to)664-675
Number of pages12
JournalBiomacromolecules
Volume13
Issue number3
DOIs
StatePublished - 12 Mar 2012

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