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

W.Y. Lu, C.Y. Zhan, C. Xie and J. Pan

Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, 201203, P.R. China  wylu@shmu.edu.cn 

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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.

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