A dual‑targeting liposome conjugated with transferrin and arginine‑glycine‑aspartic acid peptide for glioma‑targeting therapy

Qin,Li; Wang,Cheng‑Zheng; Fan,Hui‑Jie; Zhang,Chong‑Jian; Zhang,Heng‑Wei; Lv,Min‑Hao; Cui,Shu‑De

doi:10.3892/ol.2014.2449

A dual‑targeting liposome conjugated with transferrin and arginine‑glycine‑aspartic acid peptide for glioma‑targeting therapy

Authors:
- Li Qin
- Cheng‑Zheng Wang
- Hui‑Jie Fan
- Chong‑Jian Zhang
- Heng‑Wei Zhang
- Min‑Hao Lv
- Shu‑De Cui
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Affiliations: Department of Breast, Henan Cancer Hospital, Affiliated Cancer Hospital of Zhengzhou University, Zhengzhou, Henan 450008, P.R. China, Department of Breast, Henan Cancer Hospital, Affiliated Cancer Hospital of Zhengzhou University, Zhengzhou, Henan 450008, P.R. China, Department of Oncology, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan 450052, P.R. China
Published online on: August 14, 2014 https://doi.org/10.3892/ol.2014.2449
Pages: 2000-2006

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Abstract

The treatment of a brain glioma remains one of the most difficult challenges in oncology. In the present study a delivery system was developed for targeted drug delivery across the blood‑brain barrier (BBB) to the brain cancer cells. A cyclic arginine‑glycine‑aspartic acid (RGD) peptide and transferrin (TF) were utilized as targeting ligands. Cyclic RGD peptides are specific targeting ligands of cancer cells and TFs are ligands that specifically target the BBB and cancer cells. Liposome (LP) was used to conjugate the cyclic RGD and TFs to establish the brain glioma cascade delivery system (RGD/TF‑LP). The LPs were prepared by the thin film hydration method and physicochemical characterization was conducted. In vitro cell uptake and three‑dimensional tumor spheroid penetration studies demonstrated that the system could target endothelial and tumor cells, as well as penetrate the tumor cells to reach the core of the tumor spheroids. The results of the in vivo imaging further demonstrated that the RGD/TF‑LP provided the highest brain distribution. As a result, the paclitaxel‑loaded RGD/TF‑LP presents the best antiproliferative activity against C6 cells and tumor spheroids. In conclusion, the RGD/TF‑LP may precisely target brain glioma, which may be valuable for glioma imaging and therapy.

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