Development of a Screening System for Targeting Carriers Using Peptide-Modified Liposomes and Tissue Sections
Open accessAbstract
Liposomes have been used as targeting carriers for drug delivery systems (DDSs), and the carriers are able to be modified with targeting ligands, such as antibodies and peptides. To evaluate the targetability of DDS carriers modified with a targeting ligand, culture cells expressing the targeting molecules as well as small animals are used. Furthermore, in vitro and in vivo screening analyses must be repeatedly performed. Therefore, it is important to establish an easy and high-precision screening system for targeting carriers. With this aim, we focused that whether this ex vivo system could easily support assessment of interaction between targeting ligand and its receptor under physiological environment and further screen the DDS carrier-modified with targeting moiety. We examined targeting ability via in vitro, ex vivo, and in vivo analyses using integrin αvβ3-targeting C16Y-L. For the in vitro analysis, the cellular uptake of C16Y-L was higher than that of control liposomes in colon26 cells. For the ex vivo analysis, we performed an immunohistochemical analysis using colon26 tumor sections. C16Y-L was specifically attached to the tumor sections, as found in the in vitro analysis. Moreover, to evaluate the ex vivo–in vivo correlation, we examined the intratumoral localization of C16Y-L. This result showed that C16Y-L was accumulated not only in the tumor tissue but also in the tumor vasculature after the intravenous injection of C16Y-L, suggesting that the ex vivo peptide-modified liposomal analysis was correlated with the in vivo analysis. Thus, the ex vivo peptide-modified liposomal analysis may be an easy and rapid screening system with high-precision and for consideration in in vivo conditions.
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C16Y-L accumulates in tumor tissues and tumor blood vessels in vivo.
“In vivo studies have found that C16Y-L not only accumulates in tumor tissues, but also in tumor blood vessels.”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [220]
C16Y-L has higher cellular uptake in colon 26 cells than liposomes and specifically attaches to tumor slices.
“Its cellular uptake in colon 26 cells is higher than that of liposomes, and it can specifically attach to tumor slices.”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [220]
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Smart nanoparticles for cancer therapy
Sun, L., Liu, H., Ye, Y., Lei, Y., Islam, R., Tan, S., Tong, R., Miao, Y.-B., & Cai, L. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01642-x · Cited by 1,073 · see citing works
- Authors
- Negishi, Y., Hamano, N., Sato, H., Katagiri, F., Takatori, K., Endo-Takahashi, Y., Kikkawa, Y., & Nomizu, M.
- Affiliations
- Tokyo University of Pharmacy and Life Sciences (JP)
- Department of Drug Delivery and Molecular Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences
- Venue
- Biological and Pharmaceutical Bulletin
- Publisher
- Pharmaceutical Society of Japan
- Published
- 2018-07-01
- Volume
- 41
- Issue
- 7
- Pages
- 1107-1111
- ISSN
- 0918-6158 (ISSN-L)
- 1347-5215
- OpenAlex
- W2810546913
- Cited by
- 8
- References
- 21
- Citations by year
- 2026: 1 · 2025: 3 · 2023: 1 · 2020: 1 · 2019: 2
- FWCI
- 0.24
- Type
- journal article
- Language
- en
- Open access
- diamond
- doi.org
- Locations
- Biological and Pharmaceutical Bulletin (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Ministry of Education, Culture, Sports, Science and Technology
- Japan Society for the Promotion of Science (17K07180)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- integrin αvβ3, tumor vasculature targeting, drug delivery systems, ligand-receptor interactions
- MeSH terms
- Animals, Antineoplastic Agents, Chemistry, Pharmaceutical, Humans, Ligands, Liposomes, Male, Mice, Inbred BALB C, Mice, Inbred C57BL, Neoplasms, Oligopeptides, Drug Delivery Systems, Xenograft Model Antitumor Assays, Integrin alphaVbeta3, Cell Line, Tumor, Mice, Nanoparticles, High-Throughput Screening Assays, Human Umbilical Vein Endothelial Cells
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