Reductive degradation of poly(ethylene oxide)-S-S-poly([varepsilon]-caprolactone) assemblies for drug and siRNA delivery

• Published in: Molecular therapy 2012-09, Vol.20 (9), p.62-62
• Main Authors: Oltra, Nuria Sancho, Rajagopal, Karthikan, Discher, Dennis E
• Format: Article
• Language: English
• ISSN: 1525-0016; 1525-0024

Worm-like micelles from amphiphilic diblock copolymers represent a very attractive structure for drug delivery due to both high drug loading per carrier and longer in vivo circulation times compared to spherical assemblies.[1,2] The performance of polymeric carriers can in principle be enhanced by the introduction of functionalities responsive to disease environments such as a reductive environment found in tumors. Here, we describe a diblock copolymer containing a disulfide group connecting both blocks of poly(ethylene oxide)-S-S-poly([varepsilon]-caprolactone), or PEO-S-S-PCL which self-assembles into worm-like micelles and undergoes degradation under reducing conditions. Besides the delivery of hydrophobic drugs and the attachment of Near-Infrared dyes useful for in vivo imaging, this system can also be used to deliver siRNA by incorporating an oligonucleotide-S-S-PCL block copolymer in the assembly. The applicability of such a drug-delivery vehicle is significantly broadened b y such responsive functionality.