Cholic acid-based novel micellar nanoplatform for delivering FDA-approved taxanes

Nanomedicine (Lond). 2017 May;12(10):1153-1164. doi: 10.2217/nnm-2017-0361. Epub 2017 Apr 27.

Abstract

Aim: To structurally modify our existing cholic acid (CA)-based telodendrimer (TD; PEG5K-CA8) for effective micellar nanoencapsulation and delivery of the US FDA-approved members of taxane family.

Materials & methods: Generation of hybrid TDs was achieved by replacing four of the eight CAs with biocompatible organic moieties using solution-phase peptide synthesis. Drug loading was done using the standard evaporation method.

Results: Hybrid TDs can generate micelles with narrow size distributions, low critical micelle concentration values (1-6 μM), better hematocompatibility and lack of in vitro cytotoxicity.

Conclusion: Along with PEG5K-CA8, CA-based hybrid nanoplatform is the first of its kind that can stably encapsulate all three FDA-approved taxanes with nearly 100% efficiency up to 20% (w/w) loading.

Keywords: cabazitaxel; cholic acid; docetaxel; drug delivery; micelle; nanoparticle; paclitaxel; taxane; telodendrimer.

MeSH terms

  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / pharmacology
  • Bridged-Ring Compounds / administration & dosage
  • Cell Line, Tumor
  • Cholic Acid / chemistry*
  • Docetaxel
  • Drug Carriers / chemistry*
  • Humans
  • Micelles*
  • Nanoparticles / chemistry*
  • Neoplasms / drug therapy
  • Paclitaxel / administration & dosage
  • Taxoids / administration & dosage*
  • Taxoids / pharmacology

Substances

  • Antineoplastic Agents
  • Bridged-Ring Compounds
  • Drug Carriers
  • Micelles
  • Taxoids
  • Docetaxel
  • taxane
  • Cholic Acid
  • Paclitaxel