PMID- 29962407 OWN - NLM STAT- MEDLINE DCOM- 20181024 LR - 20191210 IS - 1347-5215 (Electronic) IS - 0918-6158 (Linking) VI - 41 IP - 7 DP - 2018 TI - Development of a Screening System for Targeting Carriers Using Peptide-Modified Liposomes and Tissue Sections. PG - 1107-1111 LID - 10.1248/bpb.b18-00151 [doi] AB - 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 alpha(v)beta(3)-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. FAU - Negishi, Yoichi AU - Negishi Y AD - Department of Drug Delivery and Molecular Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences. FAU - Hamano, Nobuhito AU - Hamano N AD - Department of Drug Delivery and Molecular Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences. FAU - Sato, Hinako AU - Sato H AD - Department of Drug Delivery and Molecular Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences. FAU - Katagiri, Fumihiko AU - Katagiri F AD - Department of Clinical Biochemistry, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences. FAU - Takatori, Kyohei AU - Takatori K AD - Department of Drug Delivery and Molecular Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences. FAU - Endo-Takahashi, Yoko AU - Endo-Takahashi Y AD - Department of Drug Delivery and Molecular Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences. FAU - Kikkawa, Yamato AU - Kikkawa Y AD - Department of Clinical Biochemistry, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences. FAU - Nomizu, Motoyoshi AU - Nomizu M AD - Department of Clinical Biochemistry, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences. LA - eng PT - Evaluation Study PT - Journal Article PL - Japan TA - Biol Pharm Bull JT - Biological & pharmaceutical bulletin JID - 9311984 RN - 0 (Antineoplastic Agents) RN - 0 (Integrin alphaVbeta3) RN - 0 (Ligands) RN - 0 (Liposomes) RN - 0 (Oligopeptides) RN - 0 (aspartyl-phenylalanyl-lysyl-leucyl-phenylalanyl-alanyl-valyl-tyrosyl-isoleucyl-lysyl-tyrosyl-arginine) SB - IM MH - Animals MH - Antineoplastic Agents/administration & dosage MH - Cell Line, Tumor MH - Chemistry, Pharmaceutical/*methods MH - Drug Delivery Systems/*methods MH - High-Throughput Screening Assays/*methods MH - Human Umbilical Vein Endothelial Cells MH - Humans MH - Integrin alphaVbeta3/metabolism MH - Ligands MH - Liposomes MH - Male MH - Mice MH - Mice, Inbred BALB C MH - Mice, Inbred C57BL MH - Nanoparticles/*chemistry MH - Neoplasms/drug therapy MH - Oligopeptides/chemistry MH - Xenograft Model Antitumor Assays OTO - NOTNLM OT - C16Y peptide OT - drug delivery system OT - nano carrier OT - screening array EDAT- 2018/07/03 06:00 MHDA- 2018/10/26 06:00 CRDT- 2018/07/03 06:00 PHST- 2018/07/03 06:00 [entrez] PHST- 2018/07/03 06:00 [pubmed] PHST- 2018/10/26 06:00 [medline] AID - 10.1248/bpb.b18-00151 [doi] PST - ppublish SO - Biol Pharm Bull. 2018;41(7):1107-1111. doi: 10.1248/bpb.b18-00151.