Biomedical applications of polymers derived by reversible addition - fragmentation chain-transfer (RAFT)

Adv Drug Deliv Rev. 2015 Aug 30:91:141-52. doi: 10.1016/j.addr.2015.05.016. Epub 2015 Jun 4.

Abstract

RAFT- mediated polymerization, providing control over polymer length and architecture as well as facilitating post polymerization modification of end groups, has been applied to virtually every facet of biomedical materials research. RAFT polymers have seen particularly extensive use in drug delivery research. Facile generation of functional and telechelic polymers permits straightforward conjugation to many therapeutic compounds while synthesis of amphiphilic block copolymers via RAFT allows for the generation of self-assembled structures capable of carrying therapeutic payloads. With the large and growing body of literature employing RAFT polymers as drug delivery aids and vehicles, concern over the potential toxicity of RAFT derived polymers has been raised. While literature exploring this complication is relatively limited, the emerging consensus may be summed up in three parts: toxicity of polymers generated with dithiobenzoate RAFT agents is observed at high concentrations but not with polymers generated with trithiocarbonate RAFT agents; even for polymers generated with dithiobenzoate RAFT agents, most reported applications call for concentrations well below the toxicity threshold; and RAFT end-groups may be easily removed via any of a variety of techniques that leave the polymer with no intrinsic toxicity attributable to the mechanism of polymerization. The low toxicity of RAFT-derived polymers and the ability to remove end groups via straightforward and scalable processes make RAFT technology a valuable tool for practically any application in which a polymer of defined molecular weight and architecture is desired.

Keywords: Biomedical applications; Drug delivery; RAFT; Radical polymerization; Reversible addition-fragmentation chain transfer; Toxicity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Biocompatible Materials / chemistry
  • Drug Delivery Systems*
  • Humans
  • Molecular Weight
  • Polymerization*
  • Polymers / adverse effects
  • Polymers / chemistry*
  • Thiones / chemistry

Substances

  • Biocompatible Materials
  • Polymers
  • Thiones
  • trithiocarbonic acid