Polysorbate 80 coated poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) micelles for paclitaxel delivery

Int J Pharm. 2012 Sep 15;434(1-2):1-8. doi: 10.1016/j.ijpharm.2012.05.015. Epub 2012 May 15.

Abstract

In this article, polysorbate 80 coated poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) (PCEC) micelles were successfully prepared for paclitaxel (PTX) delivery. The particle size distribution, morphology, drug loading, encapsulation efficiency and sustained release profile of the micelles were studied in detail. The safety of the micelle formulation was evaluated by MTT assay on HEK293 cells. And the encapsulated PTX in the micelles remained potent antitumor effect on C6 glioma cells. The pharmacokinetic study showed that the PCEC micelles coated with polysorbate 80 altered the biodistribution pattern and increased PTX concentration in the brain significantly compared to the uncoated micelles and the free drug after intravenous injection. The results indicated that polysorbate 80 coated PCEC micelles might be a candidate for PTX delivery for brain tumor chemotherapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / administration & dosage*
  • Antineoplastic Agents, Phytogenic / pharmacokinetics
  • Antineoplastic Agents, Phytogenic / toxicity
  • Brain / metabolism
  • Brain Neoplasms / drug therapy
  • Delayed-Action Preparations
  • Drug Carriers / chemistry
  • Drug Delivery Systems*
  • HEK293 Cells
  • Humans
  • Injections, Intravenous
  • Male
  • Micelles
  • Paclitaxel / administration & dosage*
  • Paclitaxel / pharmacokinetics
  • Paclitaxel / toxicity
  • Particle Size
  • Polyesters / chemistry
  • Polyethylene Glycols / chemistry
  • Polysorbates / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Tissue Distribution
  • Toxicity Tests

Substances

  • Antineoplastic Agents, Phytogenic
  • Delayed-Action Preparations
  • Drug Carriers
  • Micelles
  • Polyesters
  • Polysorbates
  • poly(epsilon-caprolactone)-poly(oxyethylene)-poly(epsilon-caprolactone)
  • Polyethylene Glycols
  • Paclitaxel