Cell-Penetrating Peptide and Transferrin Co-Modified Liposomes for Targeted Therapy of Glioma
Glioma is one of the most aggressive and common malignant brain tumors. Due to the presence of the blood-brain barrier (BBB), the effectiveness of therapeutics is greatly affected. In this work, to develop an efficient anti-glioma drug with targeting and which was able to cross the BBB, cell-penetra...
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MDPI AG
2019-09-01
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author | Xi Wang Yarong Zhao Shiyan Dong Robert J. Lee Dongsheng Yang Huan Zhang Lesheng Teng |
author_facet | Xi Wang Yarong Zhao Shiyan Dong Robert J. Lee Dongsheng Yang Huan Zhang Lesheng Teng |
author_sort | Xi Wang |
collection | DOAJ |
description | Glioma is one of the most aggressive and common malignant brain tumors. Due to the presence of the blood-brain barrier (BBB), the effectiveness of therapeutics is greatly affected. In this work, to develop an efficient anti-glioma drug with targeting and which was able to cross the BBB, cell-penetrating peptides (R8) and transferrin co-modified doxorubicin (DOX)-loaded liposomes (Tf-LPs) were prepared. Tf-LPs possessed a spherical shape and uniform size with 128.64 nm and their ξ-potential was 6.81 mV. Tf-LPs were found to be stable in serum within 48 h. Uptake of Tf-LPs in both U87 and GL261 cells was analyzed by confocal laser scanning microscopy and by flow cytometry. Tf-LPs were efficiently taken up by both U87 and GL261 cells. Moreover, Tf-LPs exhibited sustained-release. The cumulative release of DOX from Tf-LPs reached ~50.0% and showed excellent anti-glioma efficacy. Histology of major organs, including brain, heart, liver, spleen, lungs and kidney, and the bodyweight of mice, all indicated low toxicity of Tf-LPs. In conclusion, Tf-LPs showed great promise as an anti-glioma therapeutic agent. |
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spelling | doaj.art-ec56afd0dbab44a7875ed0fa8d13e7c92022-12-22T03:35:20ZengMDPI AGMolecules1420-30492019-09-012419354010.3390/molecules24193540molecules24193540Cell-Penetrating Peptide and Transferrin Co-Modified Liposomes for Targeted Therapy of GliomaXi Wang0Yarong Zhao1Shiyan Dong2Robert J. Lee3Dongsheng Yang4Huan Zhang5Lesheng Teng6School of Life Sciences, Jilin University, Changchun 130012, ChinaSchool of Life Sciences, Jilin University, Changchun 130012, ChinaSchool of Life Sciences, Jilin University, Changchun 130012, ChinaDivision of Pharmaceutics and Pharmacology, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USADepartment of Chemistry and Pharmacy, Zhuhai College of Jilin University, Zhuhai 519041, ChinaSchool of Life Sciences, Jilin University, Changchun 130012, ChinaSchool of Life Sciences, Jilin University, Changchun 130012, ChinaGlioma is one of the most aggressive and common malignant brain tumors. Due to the presence of the blood-brain barrier (BBB), the effectiveness of therapeutics is greatly affected. In this work, to develop an efficient anti-glioma drug with targeting and which was able to cross the BBB, cell-penetrating peptides (R8) and transferrin co-modified doxorubicin (DOX)-loaded liposomes (Tf-LPs) were prepared. Tf-LPs possessed a spherical shape and uniform size with 128.64 nm and their ξ-potential was 6.81 mV. Tf-LPs were found to be stable in serum within 48 h. Uptake of Tf-LPs in both U87 and GL261 cells was analyzed by confocal laser scanning microscopy and by flow cytometry. Tf-LPs were efficiently taken up by both U87 and GL261 cells. Moreover, Tf-LPs exhibited sustained-release. The cumulative release of DOX from Tf-LPs reached ~50.0% and showed excellent anti-glioma efficacy. Histology of major organs, including brain, heart, liver, spleen, lungs and kidney, and the bodyweight of mice, all indicated low toxicity of Tf-LPs. In conclusion, Tf-LPs showed great promise as an anti-glioma therapeutic agent.https://www.mdpi.com/1420-3049/24/19/3540cell-penetrating peptidestargetinggliomablood-brain barrier |
spellingShingle | Xi Wang Yarong Zhao Shiyan Dong Robert J. Lee Dongsheng Yang Huan Zhang Lesheng Teng Cell-Penetrating Peptide and Transferrin Co-Modified Liposomes for Targeted Therapy of Glioma Molecules cell-penetrating peptides targeting glioma blood-brain barrier |
title | Cell-Penetrating Peptide and Transferrin Co-Modified Liposomes for Targeted Therapy of Glioma |
title_full | Cell-Penetrating Peptide and Transferrin Co-Modified Liposomes for Targeted Therapy of Glioma |
title_fullStr | Cell-Penetrating Peptide and Transferrin Co-Modified Liposomes for Targeted Therapy of Glioma |
title_full_unstemmed | Cell-Penetrating Peptide and Transferrin Co-Modified Liposomes for Targeted Therapy of Glioma |
title_short | Cell-Penetrating Peptide and Transferrin Co-Modified Liposomes for Targeted Therapy of Glioma |
title_sort | cell penetrating peptide and transferrin co modified liposomes for targeted therapy of glioma |
topic | cell-penetrating peptides targeting glioma blood-brain barrier |
url | https://www.mdpi.com/1420-3049/24/19/3540 |
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