Nasal powders of thalidomide for local treatment of nose bleeding in persons affected by hereditary hemorrhagic telangiectasia

G. Colombo, F. Bortolotti, V. Chiapponi, F. Buttini, F. Sonvico, R. Invernizzi, F. Quaglia, C. Danesino, F. Pagella, P. Russo, R. Bettini, P. Colombo, A. Rossi

Research output: Contribution to journalArticlepeer-review

Abstract

In this work nasal powder formulations of thalidomide were designed and studied to be used by persons affected by hereditary hemorrhagic telangiectasia as a complementary anti-epistaxis therapy, with the goal of sustaining the effect obtained with thalidomide oral treatment after its discontinuation for adverse effects. Three nasal powders were prepared using as carriers β-CD or its more hydrophilic derivatives such as hydropropyl-β-CD and sulphobutylether-β-CD and tested with respect to technological and biopharmaceutical features after emission with active and passive nasal powder devices. For all formulated powders, improved dissolution rate was found compared to that of the raw material, making thalidomide promptly available in the nasal environment at a concentration favouring an accumulation in the mucosa. The very limited transmucosal transport measured in vitro suggests a low likelihood of significant systemic absorption. The topical action on bleeding could benefit from the poor absorption and from the fact that about 2–3% of the thalidomide applied on the nasal mucosa was accumulated within the tissue, particularly with the β-CD nasal powder.

Original languageEnglish
Pages (from-to)229-237
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume514
Issue number1
DOIs
Publication statusPublished - Nov 30 2016

Keywords

  • Cyclodextrins
  • Mucoadhesion
  • Nasal devices
  • Nasal powders
  • Telangiectasia
  • Thalidomide

ASJC Scopus subject areas

  • Pharmaceutical Science

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