Anti-Cancer Activity Based on the High Docetaxel Loaded Poly(2-Oxazoline)s Micelles

Int J Nanomedicine. 2021 Apr 9:16:2735-2749. doi: 10.2147/IJN.S298093. eCollection 2021.

Abstract

Purpose: Nanocarriers, with a high drug loading content and good safety, to achieve desirable therapeutic effect are always the goals for industry and research.

Methods and results: In the present study, we developed a docetaxel loaded poly-2-oxazoline polymer micellar system which employed poly-2-butyl-2 oxazoline and poly-2-methyl-2 oxazoline as the hydrophobic chain and hydrophilic chain, respectively. This micellar system achieves a high load up to 25% against the docetaxel, and further demonstrates an IC50 as low as 40% of the commercialized docetaxel injection in vitro and a double maximum tolerated dose in MCF-7 cells in vivo.

Conclusion: The high drug loading content, superior safety, and considerable anti-cancer activity make this newly developed docetaxel loaded poly(2-oxazoline) micelle go further in future clinical research.

Keywords: anti-cancer activity; docetaxel; high loading; micelle; poly(2-oxazoline)s.

MeSH terms

  • A549 Cells
  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis
  • Cell Line, Tumor
  • Cell Survival
  • Docetaxel / pharmacology
  • Docetaxel / therapeutic use*
  • Drug Carriers / chemistry
  • Drug Liberation
  • Endocytosis / drug effects
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • MCF-7 Cells
  • Male
  • Maximum Tolerated Dose
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Micelles*
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Oxazoles / chemistry*
  • Particle Size
  • Surface-Active Agents / chemistry
  • Tissue Distribution

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Micelles
  • Oxazoles
  • Surface-Active Agents
  • poly(2-oxazoline)
  • Docetaxel