Sterically stabilized RIPL peptide-conjugated nanostructured lipid carriers: Characterization, cellular uptake, cytotoxicity, and biodistributionopen access
- Authors
- Kim, Chang Hyun; Sung, Si Woo; Lee, Eun Seok; Kang, Tae Hoon; Yoon, Ho Yub; Goo, Yoon Tae; Cho, Ha Ra; Kim, Dong Yoon; Kang, Myung Joo; Choi, Yong Seok; Lee, Sangkil; Choi, Young Wook
- Issue Date
- Dec-2018
- Publisher
- MDPI AG
- Keywords
- nanostructured lipid carrier; RIPL peptide; cellular uptake; steric stabilization; cytotoxicity; biodistribution
- Citation
- Pharmaceutics, v.10, no.4
- Journal Title
- Pharmaceutics
- Volume
- 10
- Number
- 4
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/3213
- DOI
- 10.3390/pharmaceutics10040199
- ISSN
- 1999-4923
- Abstract
- As a platform for hepsin-specific drug delivery, we previously prepared IPLVVPLRRRRRRRRC peptide (RIPL)-conjugated nanostructured lipid carriers (RIPL-NLCs) composed of Labrafil® M 1944 CS (liquid oil) and Precirol® ATO 5 (solid lipid). In this study, to prevent the recognition by the mononuclear phagocyte system, polyethylene glycol (PEG)-modified RIPL-NLCs (PEG-RIPL-NLCs) were prepared using PEG3000 at different grafting ratios (1, 5, and 10 mole %). All prepared NLCs showed a homogeneous dispersion (130–280 nm), with zeta potentials varying from −18 to 10 mV. Docetaxel (DTX) was successfully encapsulated in NLCs: encapsulation efficiency (93–95%); drug-loading capacity (102–109 µg/mg). PEG-RIPL-NLCs with a grafting ratio of 5% PEG or higher showed significantly reduced protein adsorption and macrophage phagocytosis. The uptake of PEG(5%)-RIPL-NLCs by cancer cell lines was somewhat lower than that of RIPL-NLCs because of the PEG-induced steric hindrance; however, the uptake level of PEG-RIPL-NLCs was still greater than that of plain NLCs. In vivo biodistribution was evaluated after tail vein injection of NLCs to normal mice. Compared to RIPL-NLCs, PEG(5%)-RIPL-NLCs showed lower accumulation in the liver, spleen, and lung. In conclusion, we found that PEG(5%)-RIPL-NLCs could be a promising nanocarrier for selective drug targeting with a high payload of poorly water-soluble drugs. © 2018 by the authors. Licensee MDPI, Basel, Switzerland.
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