Liposomal butamben gel formulations: toxicity assays and topical anesthesia in an animal model

J Liposome Res. 2017 Mar;27(1):74-82. doi: 10.3109/08982104.2016.1160924. Epub 2016 Apr 28.

Abstract

The aim of this study was to evaluate the in vitro cytotoxicity and the in vivo analgesic effect and local toxicity of the local anesthetic butamben (BTB) encapsulated in conventional or elastic liposomes incorporated in gel formulations. The results showed that both gel formulations of liposomal BTB reduced the cytotoxicity (p < 0.001; one-way ANOVA/Tukey's test) and increased the topical analgesic effect (p < 0.05; one-way ANOVA/Tukey's test) of butamben, compared to plain BTB gel. The gel formulations presented good rheological properties, and stability assays detected no differences in physicochemical stability up to 30 d after preparation. Moreover, histological assessment revealed no morphological changes in rat skin after application of any of the gel formulations tested.

Keywords: Butamben; liposomes; local anesthetics; topical anesthesia.

MeSH terms

  • 3T3 Cells
  • Administration, Topical
  • Anesthesia, Local / adverse effects*
  • Animals
  • Benzocaine / administration & dosage
  • Benzocaine / analogs & derivatives*
  • Benzocaine / chemistry
  • Benzocaine / toxicity
  • Cell Survival / drug effects
  • Cells, Cultured
  • Disease Models, Animal*
  • Gels / administration & dosage
  • Gels / chemistry
  • Gels / toxicity*
  • Injections, Intraperitoneal
  • Liposomes / administration & dosage
  • Liposomes / chemistry
  • Liposomes / toxicity*
  • Mice
  • Mice, Inbred BALB C
  • Rats
  • Rats, Wistar

Substances

  • Gels
  • Liposomes
  • butamben
  • Benzocaine