Trilysinoyl oleylamide-based cationic liposomes for systemic co-delivery of siRNA and an anticancer drug

Gayong Shim, Su Eun Han, Yong Hee Yu, Sangbin Lee, Han Young Lee, Kwangmeyung Kim, Ick Chan Kwon, Tae Gwan Park, Young Bong Kim, Yong Seok Choi, Chan Wha Kim, Yu Kyoung Oh

Research output: Contribution to journalArticlepeer-review

92 Scopus citations


Oligolysine-based cationic lipid derivatives were synthesized for delivery of siRNA, and formulated into cationic liposomes. Among various oligolysine-based lipid derivatives differing in lysine residue number and lipid moiety, trilysinoyl oleylamide (TLO)-based liposomes (TLOL) showed the highest delivery efficiency combined with minimal cytotoxicity. Delivery of siRNA using TLOL silenced target genes both in vitro and in vivo. In green fluorescent protein (GFP)-expressing tumor tissue, a significant reduction of fluorescence was observed after intratumoral administration of siGFP using TLOL compared with control siGL2. Intravenous administration of siMcl1 employing pegylated TLOL (pTLOL) reduced the expression of human Mcl1 protein in KB-xenografted tumor tissue. Despite the reduction in target protein Mcl1 expression following such systemic delivery, tumor growth was only slightly reduced compared to a siGL2-treated control group. To potentiate the anticancer activity of siMcl1, the anticancer drug suberoylanilide hydroxamic acid (SAHA) was additionally encapsulated in pTLOL. After intravenous administration of siMcl1 using SAHA-loaded pTLOL (pSTLOL), a significant reduction in tumor growth was observed compared to that seen in animals treated with free SAHA or siGL2 complexed with pSTLOL. The results indicate that pTLOL could be further developed as a systemic delivery system for synergistic anticancer siRNA and a drug.

Original languageEnglish
Pages (from-to)60-66
Number of pages7
JournalJournal of Controlled Release
Issue number1
StatePublished - 10 Oct 2011

Bibliographical note

Funding Information:
This work was supported by research grants from the Ministry of Education, Science and Technology ( 2010K-001245 ; 2010K-001356 ), from the Korean Health Technology R&D project, Ministry for Health, Welfare and Family Affairs (Grant No. A092010 ), and from the Bio-Green 21 program (Code No. 20100301-061-200-001-03-00 ), Rural Development Administration, South Korea.


  • Cationic liposome
  • Co-delivery
  • siRNA
  • Suberoylanilide hydroxamic acid
  • Trilysinoyl oleylamide


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