Fine-tuning thermoresponsive functional poly(ε-caprolactone)s to enhance micelle stability and drug loading.

Block copolymers synthesized by the ring-opening polymerization of γ-2-[2-(2-methoxyethoxy)ethoxy]ethoxy-ε-caprolactone (MECL), γ-2-methoxyethoxy-ε-caprolactone (MECL), and ε-caprolactone (CL) are reported. Previously, diblock copolymers of PMECL-b-PMECL displayed excellent thermoresponsive tunability (31-43 °C) and self-assembled into micelles with moderate thermodynamic stability. In this report, two strategies are employed to enhance thermodynamic stability of PMECL/PMECL-type block copolymer micelles while maintaining their attractive thermoresponsive qualities: modification of the end group position and alteration of hydrophobic block composition by using both MECL and CL.

Systematic repurposing screening in xenograft models identifies approved drugs with novel anti-cancer activity.

Approved drugs target approximately 400 different mechanisms of action, of which as few as 60 are currently used as anti-cancer therapies. Given that on average it takes 10-15 years for a new cancer therapeutic to be approved, and the recent success of drug repurposing for agents such as thalidomide, we hypothesized that effective, safe cancer treatments may be found by testing approved drugs in new therapeutic settings. Here, we report in-vivo testing of a broad compound collection in cancer xenograft models.

Towards smart polymeric drug carriers: self-assembling γ-substituted polycaprolactones with highly tunable thermoresponsive behavior.

Synthesis and ring opening polymerization of a new γ-substituted ε-caprolactone monomer, γ-(2-methoxyethoxy)-ε-caprolactone is reported. Amphiphilic diblock copolymers comprised of poly[γ-(2-methoxyethoxy)-ε-caprolactone] and thermosensitive poly{γ-2-[2-(2-methoxyethoxy)ethoxy]ethoxy-ε-caprolactone} as the hydrophobic and hydrophilic blocks, respectively, were prepared. The copolymers exhibited fully biodegradable backbones and highly tunable thermoresponsive behavior in the range of 31-43 °C.