Surface-Modification of RIPL Peptide-Conjugated Liposomes to Achieve Steric Stabilization and pH Sensitivity
- Authors
- Kwon, Yie Hyuk; Shin, Taek Hwan; Jang, Moon Ho; Yoon, Ho Yub; Kang, Min Hyung; Kang, Myung Joo; Choi, Young Wook
- Issue Date
- Feb-2017
- Publisher
- AMER SCIENTIFIC PUBLISHERS
- Keywords
- Liposome; RIPL Peptide; Oligopeptide; pH Sensitivity; Targeting; Surface Modification; Cell Uptake; Hepsin; Nanocarrier
- Citation
- JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY, v.17, no.2, pp 1008 - 1017
- Pages
- 10
- Journal Title
- JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
- Volume
- 17
- Number
- 2
- Start Page
- 1008
- End Page
- 1017
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/4850
- DOI
- 10.1166/jnn.2017.12670
- ISSN
- 1533-4880
1533-4899
- Abstract
- We have previously demonstrated that RIPL peptide-conjugated liposomes (RIPL-L) exhibited high hepsin (HPN) selectivity and enhanced intracellular drug delivery. In this study, surface modification of RIPL-L was performed to reduce plasma protein adsorption and off-target effects. For steric stabilization, distearoyl phosphatidylethanolamine (DSPE)-polyethylene glycol (PEG)(2000) was used (5% molar ratio to total lipid) to prepare PEG-RIPL-L. Further, pH-sensitive oligopeptides [(HD)(4) or (HE)(4)] were coupled to shield the RIPL polyarginine moiety, yielding (HD)(4)/PEG-RIPL-L and (HE)(4)/PEG-RIPL-L. All liposomal vesicles had a narrow and homogenous size distribution of approximately 140-150 nm, with zeta potentials varying from - 15 to 36 mV. Increased plasma stability was observed upon quantifying the protein adsorbed onto liposomes by using a micro bicinchoninic acid assay. The (HD)(4) - and (HE)(4)-coupling capacity of PEG-RIPL-L was investigated by measuring the amount of oligopeptide involved in transient ionic complexation (TIC-oligopep) and zeta potential changes. As the molar ratio of (HD)(4) and (HE)(4) increased, TIC-oligopep increased and zeta potential decreased. (HE)(4)/PEG-RIPL-L were pH- sensitive, producing 1.6-fold greater cellular uptake of FITC-dextran by LNCaP cells at pH 6.8 than at pH 7.4. This result suggested that (HE)(4)/PEG-RIPL-L might provide a sterically stabilized, pH-sensitive drug carrier for HPN-specific cancer targeting.
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