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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