Bioactive vesicles from saccharide- and hexanoyl-modified poly(l-lysine) copolypeptides and evaluation of the cross-linked vesicles as carriers of doxorubicin for controlled drug release

Yun Chiao Huang, Marannu Arham, Jeng Shiung Jan

研究成果: Article同行評審

21 引文 斯高帕斯(Scopus)

摘要

We report the synthesis and self-assembly of an amphiphilic glycopolypeptide through the conjugation of both lactobionolactone, a model targeted ligand to HepG2 liver cells, and hexanoyl groups onto poly(l-lysine) (PLL). The self-assembled glycopolypeptide vesicles were stabilized via genipin-cross-link and evaluated as cell-targeted carriers. The experimental data revealed that the saccharide and hexanoyl substitution can regulate the amphiphilic nature and chain conformation of the glycopolypeptide, and subsequently the size of the assembled vesicles. Taking the advantages of the glycopolypeptide vesicles including stable structure, pH-responsiveness, and cell-targeting ability, the glycopolypeptide was employed for drug encapsulation, i.e. doxorubicin (Dox). A high Dox loading level (45 wt.%) can be achieved with the aid of sonication as a pH gradient was applied between the outside and inside of the vesicles. The cross-linked, vesicles loaded with Dox exhibited noticeable pH-sensitive behavior with accelerated Dox release at acidic condition due to the protonation of amino groups and the release rate can be controlled by the genipin to amine feed ratio. The cytocompatibility of the polypeptide was improved upon grafting the saccharide group and cross-link. The Dox-loaded vesicles exhibited a comparable cytotoxicity with respect to free Dox against HepG2 liver cells. These results point to a potential of novel glycopolypeptide vesicles with cross-linkable membrane to be carriers for the delivery of bioactive agents.

原文English
頁(從 - 到)726-737
頁數12
期刊European Polymer Journal
49
發行號3
DOIs
出版狀態Published - 2013 三月

All Science Journal Classification (ASJC) codes

  • Physics and Astronomy(all)
  • Polymers and Plastics
  • Organic Chemistry
  • Materials Chemistry

指紋 深入研究「Bioactive vesicles from saccharide- and hexanoyl-modified poly(l-lysine) copolypeptides and evaluation of the cross-linked vesicles as carriers of doxorubicin for controlled drug release」主題。共同形成了獨特的指紋。

引用此