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Stabilized Polymer Micelles for the Development of IT-147, an Epothilone D Drug-Loaded Formulation

Adam Carie1, Bradford Sullivan1, Tyler Ellis1

  • 1Intezyne Technologies, 3720 Spectrum Blvd. Ste. 104, Tampa, FL, USA.

Journal of Drug Delivery
|January 4, 2017
PubMed

Insights

Epothilone D shows cancer-fighting potential but has safety issues. Encapsulating it in polymer micelles (IT-147) improves drug delivery, enhancing efficacy and reducing toxicity for better cancer treatment.

Area of Science:

  • Oncology
  • Nanotechnology
  • Drug Delivery

Background:

  • Epothilones, like Epothilone D, are potent microtubule-stabilizing agents with anticancer activity.
  • Clinical trials of Epothilone D were halted due to dose-limiting toxicities and poor plasma stability.
  • Encapsulation in nanocarriers offers a strategy to improve Epothilone D's therapeutic index.

Purpose of the Study:

  • To develop a novel formulation of Epothilone D using stabilized polymer micelles.
  • To enhance the safety and efficacy of Epothilone D through improved drug delivery.
  • To create a formulation (IT-147) that increases tumor accumulation and reduces systemic toxicity.

Main Methods:

  • Designed and synthesized a library of triblock copolymers for micelle formulation.
  • Characterized the Epothilone D-loaded micelles (IT-147) for size, drug loading, and release kinetics.
  • Evaluated the pharmacokinetic profile and toxicity of IT-147 compared to free Epothilone D in preclinical models.

Main Results:

  • IT-147 achieved high drug loading efficiency (>90%) and a particle size of 75 nm.
  • The formulation demonstrated pH-dependent release of Epothilone D.
  • IT-147 significantly increased Epothilone D plasma exposure (6-fold) and exhibited a higher no-observed-adverse-effect level (NOAEL) compared to the free drug.

Conclusions:

  • Stabilized polymer micelles (IT-147) represent a promising platform for delivering Epothilone D.
  • IT-147 enhances Epothilone D's pharmacokinetic profile and safety, potentially overcoming previous clinical limitations.
  • This formulation offers a safer and more effective approach for Epothilone D-based cancer therapy.

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