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2016 ; 514
(1
): 229-237
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English Wikipedia
Nasal powders of thalidomide for local treatment of nose bleeding in persons
affected by hereditary hemorrhagic telangiectasia
#MMPMID27863666
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
Int J Pharm
2016[Nov]; 514
(1
): 229-237
PMID27863666
show ga
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 ?-CD or its more
hydrophilic derivatives such as hydropropyl-?-CD and sulphobutylether-?-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 ?-CD nasal
powder.