G. Dollo et al., Endotracheal tube cuffs filled with lidocaine as a drug delivery system: in vitro and in vivo investigations, EUR J PH SC, 13(3), 2001, pp. 319-323
The purpose of this study was to examine if lidocaine diffusion across an e
ndotracheal tube cuff could improve post-operative tolerance, especially so
re throat. The in vitro release of lidocaine from tube cuffs filled with di
fferent lidocaine formulations (base form, hydrochloride form or alkalinize
d lidocaine hydrochloride) was investigated. A preliminary pilot clinical s
tudy in anaesthesia for spine surgery in smoker patients was carried out to
examine the pharmacokinetic (i.e. systemic uptake) and pharmacodynamic eff
ects (i.e. incidence of sore throat) obtained with the endotracheal tube cu
ff filled with Lidocaine solution, compared to cuffs inflated only with air
. From our in vitro experiment, only the hydrophobic neutral base form of l
idocaine was able to diffuse (65.1 +/-1.1% released after 6 h), while for t
he charged hydrochloride form, only a permeation phenomenon occurred concer
ning only 1% of the total drug. Alkalinization of lidocaine hydrochloride (
the only form available as a drug) allows smaller amounts to be used compar
ed to previous published studies (20-40 mg vs. 200-500 mg) and no lag time
for diffusion. Such a system could provide a controlled release reservoir f
or lidocaine to adjacent tracheal tissue. This was shown in our pilot study
with sustained plasmatic profiles and improved tolerance (decreased pain s
cores) in the rank order: air group much less than lidocaine hydrochloride
group < alkalinized lidocaine group. (C) 2001 Elsevier Science B.V. All rig
hts reserved.