Cyclic RGD Conjugated Poly (ethylene glycol)-co-poly (lactic acid) Micelle Enhances Anti-Glioblastoma Effect of Paclitaxel.

Year
2010
Authors
W.Y. Lu, C.Y. Zhan, C. Xie and J. Pan
Institutions
Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, 201203, P.R. China wylu@shmu.edu.cn
Summary

Paclitaxel-loaded RGD-PEG-PLA micelle was developed. It was much effective to the subcutaneous and intracranial glioblastoma models. Glioblastoma multiforme (GBM) is the most frequent primary malignant brain tumors and accounts for approximately 40%. The use of glioblastoma-targeted drug delivery system facilitates efficient delivery of chemotherapeutic agents to malignant gliomas in the central nervous system while minimizing high systemic doses associated with debilitating toxicities. To employ the high binding affinity of a cyclic RGD peptide (c(RGDyK)) with integrin αvβ3 over-expressed on tumor neovasculature and U87MG glioblastoma cells, we prepared paclitaxel-loaded c(RGDyK)-Poly(ethylene glycol)-block-poly(lactic acid) micelle (RGD-PEG-PLA-PTX). Our results suggested that RGD-PEG-PLA-PTX micelle may be a potential drug delivery system in the treatment of integrin αvβ3 over-expressed glioblastoma.