PUBLICATION

Aspartic acid based modified PLGA-PEG nanoparticles for bone targeting: in vitro and in vivo evaluation

Authors
Fu, Y.C., Fu, T.F., Wang, H.J., Lin, C.W., Lee, G.H., Wu, S.C., Wang, C.K.
ID
ZDB-PUB-140723-4
Date
2014
Source
Acta biomaterialia   10(11): 4583-96 (Journal)
Registered Authors
Fu, Tzu-Fun, Lee, Gang-Hui
Keywords
Aspartic acid, Bone targeting, Drugs delivery, Nanoparticle, PLGA-PEG
MeSH Terms
  • Adsorption
  • Animals
  • Aspartic Acid/chemical synthesis
  • Aspartic Acid/chemistry*
  • Aspartic Acid/pharmacology
  • Bone and Bones/drug effects
  • Bone and Bones/metabolism*
  • Cell Survival/drug effects
  • Drug Delivery Systems*
  • Durapatite/chemistry
  • Endocytosis/drug effects
  • Larva/drug effects
  • Mice, Inbred BALB C
  • Minerals/metabolism
  • Nanoparticles/chemistry*
  • Nanoparticles/ultrastructure
  • Particle Size
  • Polyethylene Glycols/chemical synthesis
  • Polyethylene Glycols/chemistry*
  • Polyethylene Glycols/pharmacology
  • Polyglactin 910/chemical synthesis
  • Polyglactin 910/chemistry*
  • Polyglactin 910/pharmacology
  • Proton Magnetic Resonance Spectroscopy
  • Rats
  • Spectrometry, Mass, Electrospray Ionization
  • Static Electricity
  • Time Factors
  • Tissue Distribution/drug effects
  • Zebrafish
PubMed
25050775 Full text @ Acta Biomater
Abstract
Nanoparticles (NPs) that target bone tissue were developed using PLGA-PEG (poly(lactic-co-glycolic acid)-polyethylene glycol) diblock copolymers and bone targeting moieties based on aspartic acid, (Asp)n (1, 3). These NPs are expected to enable the transport of hydrophobic drugs. The molecular structures were examined by (1)H NMR or identified using mass spectrometry and FT-IR spectra. The NPs were prepared using the water miscible solvent displacement method, and their size characteristics were evaluated using TEM and dynamic light scattering. The bone targeting potential of the NPs was evaluated in vitro using hydroxyapatite affinity assays and in vivo using fluorescent imaging in zebrafish and rats. We confirmed that the average particle size of the NPs was smaller than 200 nm and that the dendritic Asp3 moiety of the PLGA-PEG-Asp3 NPs exhibited the best apatite mineral binding ability. The preliminary in vivo bone affinity assays in zebrafish and rats indicated that the PLGA-PEG-ASP3 NPs may display increased bone-targeting efficiency compared with other PLGA-PEG based NPs that lack a dendritic Asp3 moiety. These NPs may act as a delivery system for hydrophobic drugs, warranting further evaluation for the treatment of bone disease.
Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping