CRGD-functionalized mPEG-PLGA-PLL nanoparticles for imaging and therapy of breast cancer

Shanghai Cancer Institute, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, No.25, Lane 2200, Xietu Road, Shanghai 200032, PR China.
Biomaterials (Impact Factor: 8.56). 07/2012; 33(28):6739-47. DOI: 10.1016/j.biomaterials.2012.06.008
Source: PubMed


Cyclic peptide (arginine-glycine-aspartic-glutamic-valine acid, cRGD)-modified monomethoxy (polyethylene glycol)-poly (D,L-lactide-co-glycolide)-poly (L-lysine) nanoparticles (mPEG-PLGA-PLL-cRGD NPs) with antitumor drug Mitoxantrone (DHAQ) or fluorescence agent Rhodamine B (Rb) encapsulated in their interior were prepared. The remarkable features of the mPEG-PLGA-PLL-cRGD NPs are the effective improvement for the cytotoxicity and uptake of the cell in vitro, and the significant enhancement of delivery ability for DHAQ or Rb in vivo. As a consequence, an excellent therapeutic efficiency for cancer is obtained, demonstrating the mPEG-PLGA-PLL-cRGD NPs play a key role in enhancing cancer therapeutic efficiency.

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    • "Although chemotherapeutic agents are stabilized in the PLA matrix against dissolution by hydrophobic interaction, and drug release kinetics is controlled by matrix degradation [3], surface active agents are used to prevent NPs aggregation , reduce the initial burst release, or improve the cell uptake of NPs [14] [15] [16] [17]. These active agents include amphiphilic PEG-based copolymers [18] [19], biomolecules such as vitamin E [16], peptides [20] [21], and proteins [22]. These modifiers not only stabilize NPs against aggregation and improve cell uptake, but also they affect the drug safety profile including immunogenicity and systemic toxicity [23]. "
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