Tuesday, September 9, 2014

New Publication utilizes Mal-PEG-PLGA (Polyvivo AI20) and polyaspartic acid to form bone-tissue targeted nanoparticle

PolySciTech (www.polyscitech.com) provides an array of block copolymers as well as reactive intermediates including polyvivo AI20. Recently researchers utilized PolyVivo AI20 (Mal-PEG-PLGA) along with mPEG-PLGA from PolySciTech to generate a nanoparticle sytem which they then conjugated to thiol endcapped polyaspartic acid to form a targeted system for bone-tissue targeting.  This system was validated against osteoblast cells/stem cells as well as ex-vivo tibia sections to show that it provided a non-cytotoxic method for specifically targeting bone tissue.  This method could be used to aid delivery of drugs specifically to bone tissue for treatment of bone diseases. Read more: Jiang, Tao, Xiaohua Yu, Erica J. Carbone, Clarke Nelson, Ho Man Kan, and Kevin W-H. Lo. "Poly aspartic acid peptide-linked PLGA based nanoscale particles: Potential for bone-targeting drug delivery applications." International Journal of Pharmaceutics (2014). http://www.sciencedirect.com/science/article/pii/S0378517314006334

“Abstract: Delivering drugs specifically to bone tissue is very challenging due to the architecture and structure of bone tissue. Poly(lactic-co-glycolic acid) (PLGA)-based nanoparticles (NPs) hold great promise for the delivery of therapeutics to bone tissue. The goal of the present research was to formulate a PLGA-based NP drug delivery system for bone tissue exclusively. Since poly-aspartic acids (poly-Asp) peptide sequence has been shown to bind to hydroxyapatite (HA), and has been suggested as a molecular tool for bone-targeting applications, we fabricated PLGA-based NPs linked with poly-Asp peptide sequence. Nanoparticles made of methoxy – poly(ethylene glycol) (PEG)-PLGA and maleimide-PEG-PLGA were prepared using a water-in-oil-in-water double emulsion and solvent evaporation method. Fluorescein isothiocyanate (FITC)-tagged poly-Asp peptide was conjugated to the surface of the nanoparticles via the alkylation reaction between the sulfhydryl groups at the N-terminal of the peptide and the Cdouble bond; length as m-dashC double bond of maleimide at one end of the polymer chain to form thioether bonds. The conjugation of FITC-tagged poly-Asp peptide to PLGA NPs was confirmed by NMR analysis and fluorescent microscopy. The developed nanoparticle system is highly aqueous dispersible with an average particle size of 80 nm. In vitro binding analyses demonstrated that FITC-poly-Asp NPs were able to bind to HA gel as well as to mineralized matrices produced by human mesenchymal stem cells and mouse bone marrow stromal cells. Using a confocal microscopy technique, an ex vivo binding study of mouse major organ ground sections revealed that the FITC-poly-Asp NPs were able to bind specifically to the bone tissue. In addition, proliferation studies indicated that our FITC-poly-Asp NPs did not induce cytotoxicity to human osteoblast-like MG63 cell lines. Altogether, these promising results indicated that this nanoscale targeting system was able to bind to bone tissue specifically and might have a great potential for bone disease therapy in clinical applications. Keywords: Nanoparticles; Targeted drug delivery; Peptides; Bone diseases”


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