Tuesday, March 4, 2014

PLGA-PEG-COOH precursor for targeted cancer therapy

PolySciTech (www.polyscitech.com) provides PLGA-PEG-COOH precursors (e.g. PolyVivo AI34) for a variety of modifications and targeted delivery applications. Recently similar polymers have been utilized to generate dual-targeted nanoparticles by conjugating an Asn-Gly-Arg peptide endcap. Read more at: Gupta, Madhu, Gousia Chashoo, Parduman Raj Sharma, Ajit Kumar Saxena, Prem Narayan Gupta, Govind Prasad Agrawal, and Suresh Prasad Vyas. "Dual Targeted Polymeric Nanoparticles Based on Tumor Endothelium and Tumor Cells for Enhanced Antitumor Drug Delivery." Molecular pharmaceutics (2014).http://pubs.acs.org/doi/abs/10.1021/mp400404p

“Abstract: Some specific types of tumor cells and tumor endothelial cells represented CD13 proteins and act as receptors for Asn-Gly-Arg (NGR) motifs containing peptide. These CD13 receptors can be specifically recognized and bind through the specific sequence of cyclic NGR (cNGR) peptide and presented more affinity and specificity toward them. The cNGR peptide was conjugated to the poly(ethylene glycol) (PEG) terminal end in the poly(lactic-co-glycolic) acid PLGA-PEG block copolymer. Then, the ligand conjugated nanoparticles (cNGR-DNB-NPs) encapsulating docetaxel (DTX) were synthesized from preformed block copolymer by the emulsion/solvent evaporation method and characterized for different parameters. The various studies such as in vitro cytotoxicity, cell apoptosis, and cell cycle analysis presented the enhanced therapeutic potential of cNGR-DNB-NPs. The higher cellular uptake was also found in cNGR peptide anchored NPs into HUVEC and HT-1080 cells. However, free cNGR could inhibit receptor mediated intracellular uptake of NPs into both types of cells at 37 and 4 °C temperatures, revealing the involvement of receptor-mediated endocytosis. The in vivo biodistribution and antitumor efficacy studies indicated that targeted NPs have a higher therapeutic efficacy through targeting the tumor-specific site. Therefore, the study exhibited that cNGR-functionalized PEG-PLGA-NPs could be a promising approach for therapeutic applications to efficient antitumor drug delivery. Keywords: cyclic NGR; CD13 receptor; nanoparticles; solid tumor; docetaxel”
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