Formulation and pharmacokinetic evaluation of tetracycline-loaded solid lipid nanoparticles for subcutaneous injection in mice

Chem Pharm Bull (Tokyo). 2011;59(2):260-5. doi: 10.1248/cpb.59.260.

Abstract

The aim of this work was to prepare tetracycline-loaded solid lipid nanoparticles (Tet-SLN), and to evaluate the potential of these colloidal carriers for subcutaneous injection. Tet-SLN was prepared by microemulsion method and the preparation conditions were optimized by ternary phase diagram. At optimized process conditions, lyophilized Tet-SLN showed spherical particles with a mean diameter of 87.2±46.9 nm and a negative zeta potential of -6.69 mV, up to 1.7% tetracycline drug content was achieved after loading. In vitro release test showed a biphasic release profile for Tet-SLN and more than 80% of the drug was liberated from Tet-SLN in 48 h. After subcutaneous injection of Tet-SLN to mice, a considerable sustained release was observed; tetracycline in blood could be detected lasting 36 h, and lower concentrations of tetracycline in all tissues tested compared to the free tetracycline solution were observed. In conclusion, Tet-SLN can be prepared well by microemulsion method and subcutaneous injection of SLN provide a new perspective for drug sustained release.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Drug Evaluation, Preclinical / methods
  • Injections, Subcutaneous
  • Lipids
  • Male
  • Mice
  • Nanoparticles / administration & dosage*
  • Random Allocation
  • Tetracycline / administration & dosage*
  • Tetracycline / pharmacokinetics*
  • Tissue Distribution / drug effects
  • Tissue Distribution / physiology

Substances

  • Lipids
  • Tetracycline