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

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

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

Colombo, G Bortolotti, F Chiapponi, V Buttini, F Sonvico, F

Invernizzi, R Quaglia, F Danesino, C Pagella, F Russo, P Bettini, R Colombo, P Rossi, A

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Publication Type:: Journal Article
Citation:: International Journal of Pharmaceutics, 2016, 514 (1), pp. 229 - 237
Issue Date:: 2016-11-30

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Field	Value	Language
dc.contributor.author	Colombo, G	en_US
dc.contributor.author	Bortolotti, F	en_US
dc.contributor.author	Chiapponi, V	en_US
dc.contributor.author	Buttini, F	en_US
dc.contributor.author	Sonvico, F https://orcid.org/0000-0001-7372-1456	en_US
dc.contributor.author	Invernizzi, R	en_US
dc.contributor.author	Quaglia, F	en_US
dc.contributor.author	Danesino, C	en_US
dc.contributor.author	Pagella, F	en_US
dc.contributor.author	Russo, P	en_US
dc.contributor.author	Bettini, R	en_US
dc.contributor.author	Colombo, P	en_US
dc.contributor.author	Rossi, A	en_US
dc.date.available	2016-07-01	en_US
dc.date.issued	2016-11-30	en_US
dc.identifier.citation	International Journal of Pharmaceutics, 2016, 514 (1), pp. 229 - 237	en_US
dc.identifier.issn	0378-5173	en_US
dc.identifier.uri	http://hdl.handle.net/10453/118428
dc.description.abstract	© 2016 The Authors 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.	en_US
dc.relation.ispartof	International Journal of Pharmaceutics	en_US
dc.relation.isbasedon	10.1016/j.ijpharm.2016.07.002	en_US
dc.subject.classification	Pharmacology & Pharmacy	en_US
dc.subject.mesh	Nasal Mucosa	en_US
dc.subject.mesh	Animals	en_US
dc.subject.mesh	Rabbits	en_US
dc.subject.mesh	Humans	en_US
dc.subject.mesh	Epistaxis	en_US
dc.subject.mesh	Telangiectasia, Hereditary Hemorrhagic	en_US
dc.subject.mesh	Thalidomide	en_US
dc.subject.mesh	beta-Cyclodextrins	en_US
dc.subject.mesh	Drug Carriers	en_US
dc.subject.mesh	Powders	en_US
dc.subject.mesh	Administration, Intranasal	en_US
dc.subject.mesh	Chemistry, Pharmaceutical	en_US
dc.subject.mesh	Solubility	en_US
dc.title	Nasal powders of thalidomide for local treatment of nose bleeding in persons affected by hereditary hemorrhagic telangiectasia	en_US
dc.type	Journal Article
utslib.citation.volume	1	en_US
utslib.citation.volume	514	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Graduate School of Health
utslib.copyright.status	closed_access
pubs.issue	1	en_US
pubs.publication-status	Published	en_US
pubs.volume	514	en_US

Abstract:

© 2016 The Authors 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.

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http://hdl.handle.net/10453/118428