pH-Responsive PEGylated nanoparticles based on amphiphilic polyaspartamide: preparation, physicochemical characterization and in vitro evaluation

A series of amphiphilic graft copolymers based on polyaspartamide were synthesized by successive aminolysis reactions of polysuccinimide using 2‐diisopropylaminoethyl (DIP), O‐(2‐aminoethyl)‐O′‐methylpolyethylene glycol (PEG) and lauryl amine as pH‐sensitive, hydrophilic and hydrophobic groups, resp...

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Bibliographic Details
Published in:Polymer international 2013-08, Vol.62 (8), p.1218-1224
Main Authors: Moon, Jong Rok, Jeon, Young Sil, Zrinyi, Miklos, Kim, Ji-Heung
Format: Article
Language:English
Subjects:
Aminoacid polymers
amphiphilic
Applied sciences
Derivatives
Dipping
drug delivery
Exact sciences and technology
Nanocomposites
Nanomaterials
nanoparticle
Nanoparticles
Nanostructure
Physicochemistry of polymers
polyaspartamide
Self assembly
stimuli-responsive
Synthetic biopolymers
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Summary:A series of amphiphilic graft copolymers based on polyaspartamide were synthesized by successive aminolysis reactions of polysuccinimide using 2‐diisopropylaminoethyl (DIP), O‐(2‐aminoethyl)‐O′‐methylpolyethylene glycol (PEG) and lauryl amine as pH‐sensitive, hydrophilic and hydrophobic groups, respectively. The pH‐dependent self‐assembly behavior of the aqueous copolymer solution was investigated. Nano‐aggregation, which was induced by a hydrophilic/hydrophobic shift of the DIP group in solution, occurred at a pH in the vicinity of the pKa of the DIP group. The mean diameter of the nano‐aggregate could be modulated by changing the compositions of both pendants. The mean diameter of the nanoparticles increased with increasing solution pH from 6.5 to 8. The dissolution of paclitaxel into these amphiphilic nanoparticles was attempted and the pH‐dependent release behavior was examined using a solvent‐casting method. The results showed a significantly faster release of paclitaxel at pH = 6.5, which is a tumoral acidic pH, than at neutral physiological pH. These pH‐sensitive PEGylated polyaspartamide derivatives have potential use as a tumor‐targeting delivery system. Amphiphilic graft copolymers based on polyaspartamide with diisopropylamine and PEG pendants were synthesized and the pH‐dependent self‐assembly behavior of the aqueous copolymer solution was investigated. Paclitaxel was incorporated into these amphiphilic copolymer nanoparticles and the pH‐dependent release behavior was examined.
ISSN:0959-8103
1097-0126
DOI:10.1002/pi.4412