A pH- and thermo-responsive poly(amino acid)-based drug delivery system

作者：Liu Na; Li Bingqiang; Gong Chu; Liu Yuan; Wang Yanming; Wu Guolin^*

来源：Colloids and Surfaces B: Biointerfaces , 2015, 136: 562-569.

DOI：10.1016/j.colsurfb.2015.09.057

• Stimuli-responsive
• pH-sensitive
• Thermo-responsive
• Drug delivery
• Poly(amino acid)

A pH- and thermo-responsive poly(amino acid)-based amphiphilic copolymer was developed, functioning as a tumour targeting drug delivery system with good biocompatibility and biodegradability. To provide multi-stimuli sensitivity characteristics to the poly(amino acid)s, the polyaspartamide scaffold has been functionalized with N,N-diisopropylamide groups via aminolysis reaction of polysuccinimide. PEG chains have also been chemically grafted to the poly(amino acid) backbone through acid-labile hydrazone linkages, providing a removable shield for the poly(amino acid) based nanoparticles. Furthermore, doxorubicin was chemically linked to the copolymer chain via hydrazone bonds, acting as the hydrophobic moiety to drive the polymeric self-assembly. Free doxorubicin molecules could be encapsulated into the self-assembled nanoparticles via hydrophobic interactions and molecular pi-pi stacking. The results obtained show that the drug release can be triggered by the temperature with a significantly increased release being observed under acidic conditions. The cytotoxicity behaviour of the copolymers and drug-loaded nanoparticles was investigated in vitro at varying pH values and different temperatures. In doing so, superior characteristics concerning compatibility and anti-cancer activity could be observed.

• 出版日期2015-12-1
• 单位南开大学