Dual Acid-Responsive Micelle-Forming Anticancer Polymers as New Anticancer Therapeutics

Autor: Dongwon Lee, Yerang Kim, Gilson Khang, Byungkuk Kim, Sanga Park, Eun-Sun Lee
Rok vydání: 2013
Předmět:
Zdroj: Advanced Functional Materials. 23:5091-5097
ISSN: 1616-301X
DOI: 10.1002/adfm201300871
Popis: Cinnamaldehyde, a major active compound of cinnamon, is known to induce apoptotic cell death in numerous human cancer cells. Here, dual acid-responsive polymeric micelle-forming cinnamaldehyde prodrugs, poly[(3-phenylprop-2-ene-1,1-diyl)bis(oxy)bis(ethane-2,1-diyl)diacrylate]-co-4,4’(trimethylene dipiperidine)-co-poly(ethylene glycol), termed PCAE copolymers, are reported. PCAE is designed to incorporate cinnamaldehyde via acid-cleavable acetal linkages in its pH-sensitive hydrophobic backbone and self assemble to form stable micelles which can encapsulate camptothecin (CPT). PCAE self assembles to form micelles which release CPT and cinnamaldehyde in pH-dependent manners. PCAE micelles induce apoptotic cell death through the generation of intracellular reactive oxygen species (ROS) and exert synergistic anticancer effects with a payload of CPT in vitro and in vivo model of SW620 human colon tumor-bearing mice. It is anticipated that dual acid-sensitive micelle-forming PCAE with intrinsic anticancer activities has enormous potential as novel anticancer therapeutics.
Databáze: OpenAIRE