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.
Cintia Maria Saia Cereda  1 ,  Viviane Aparecida Guilherme  1 ,  Melissa Inger Alkschbirs  2 ,  Rui Barbosa de Brito Junior  3 ,  Giovana Radomille Tofoli  3 ,  Michelle Franz-Montan  4 ,  Daniele Ribeiro de Araujo  5 ,  Eneida de Paula  1
Affiliations
  • 1. a Department of Biochemistry and Tissue Biology , Institute of Biology, State University of Campinas , Campinas, São Paulo , Brazil.
  • 2. b Department of Physical Chemistry , Institute of Chemistry, State University of Campinas , Campinas, São Paulo , Brazil.
  • 3. c Department of Molecular Biology , São Leopoldo Mandic Dental Research Institute , Campinas, São Paulo , Brazil.
  • 4. d Department of Physiological Sciences , Piracicaba Dental School, State University of Campinas , Piracicaba, São Paulo , Brazil , and.
  • 5. e Federal University of ABC, Human and Natural Sciences Center , Santo André, São Paulo , Brazil.
PMID: 27126194 DOI: 10.3109/08982104.2016.1160924
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.
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