Long circulating poly(ethylene glycol)-decorated lipid nanocapsules deliver docetaxel to solid tumors

Pharm Res. 2006 Apr;23(4):752-8. doi: 10.1007/s11095-006-9662-5. Epub 2006 Mar 24.

Abstract

Purpose: The purpose of this study was to evaluate the ability of poly(ethylene glycol)-coated lipid nanocapsules (LN) to deliver the highly potent hydrophobic anticancer drug docetaxel to solid tumors.

Methods: Docetaxel-loaded nanocapsules (80-120 nm) were produced by a solvent-free phase inversion process and were coated with polyethylene glycol distearoylphosphatidylethanolamine conjugate by a postinsertion step. In vivo studies were conducted in mice bearing subcutaneously implanted C26 colon adenocarcinoma to assess the pharmacokinetics and biodistribution of both the drug and LN.

Results: Incorporation of docetaxel into the LN dramatically increased the drug's biological half-life while providing substantial accumulation at the tumoral site. The pharmacokinetics and biodistribution pattern were found to depend on the specific surface area and shell composition of the nanocapsules.

Conclusion: This study demonstrates that docetaxel physically entrapped into a lipid colloidal drug carrier can be efficiently targeted to neoplastic tissues.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / administration & dosage*
  • Antineoplastic Agents, Phytogenic / pharmacokinetics*
  • Area Under Curve
  • Capsules
  • Cell Line, Tumor
  • Docetaxel
  • Drug Carriers
  • Drug Delivery Systems
  • Excipients
  • Female
  • Half-Life
  • Humans
  • Lipids
  • Mice
  • Mice, Inbred BALB C
  • Neoplasm Transplantation
  • Neoplasms, Experimental / metabolism*
  • Particle Size
  • Polyethylene Glycols
  • Taxoids / administration & dosage*
  • Taxoids / pharmacokinetics*
  • Tissue Distribution

Substances

  • Antineoplastic Agents, Phytogenic
  • Capsules
  • Drug Carriers
  • Excipients
  • Lipids
  • Taxoids
  • Docetaxel
  • Polyethylene Glycols