Entrapping bupivacaine-loaded emulsions in a crosslinked-hydrogel increases anesthetic effect and duration in a rat sciatic nerve block model

2020 ◽  
Vol 588 ◽  
pp. 119703
Author(s):  
Brett Davis ◽  
Sierra Erickson ◽  
Susan Wojtalewicz ◽  
Andrew Simpson ◽  
Cameron Metcalf ◽  
...  
2020 ◽  
Vol 45 (6) ◽  
pp. 412-418
Author(s):  
Cheng Zhou ◽  
Lei Tang ◽  
Qinqin Yin ◽  
Linghui Yang ◽  
Deying Gong ◽  
...  

Background and objectiveLong-acting nociceptive-selective regional anesthesia has remained an elusive clinical goal. We aspired to identify a novel compound that would produce nociceptive-selective regional anesthesia through the transient receptor potential vanilloid 1 (TRPV1) channels.MethodsWe designed and synthesized a novel compound (LL-a) that penetrates the cell membrane through TRPV1 channels and binds to voltage-gated sodium channels. The regional anesthetic effect of LL-a was evaluated in a rodent sciatic nerve block model. Electrophysiological recording was applied to test the inhibition of LL-a on voltage-gated sodium channel currents.ResultsLL-a inhibited sodium channel currents on the dorsal root ganglion neurons of mice and this action was diminished by TRPV1 channel knockout. In a sciatic nerve block model of a rat, 0.2% and 0.4% (w/v) LL-a produced selective sensory block with median (IQR) durations of 42.0 (24.0, 48.0) and 72.0 (69.0, 78.0) hours, respectively. No motor block was found for 0.2% LL-a. 0.4% LL-a produced a motor block with a median (IQR) duration of 3.0 (0.0, 6.0) hours. This selective sensory block was not observed on TRPV1 knockout mice. As a positive control, 0.5% and 0.75% levobupivacaine produced a non-selective sciatic nerve block with median (IQR) durations of 2.8 (2.6, 2.8) and 3.8 (3.8, 4.8) hours, respectively. No systemic or local irritation was observed during injection of LL-a and sensory and motor function completely recovered for all the animals.ConclusionsLL-a is a potential novel local anesthetic for long-lasting nociceptive-selective analgesia.


Author(s):  
Ahmet Ozkan ◽  
Sedat Akbas ◽  
Mehmet Durak ◽  
Mehmet Erdogan ◽  
Hakan Parlakpinar ◽  
...  

2013 ◽  
Vol 74 ◽  
pp. 74-78 ◽  
Author(s):  
Mehmet Ali Erdogan ◽  
Alaaddin Polat ◽  
Aytac Yucel ◽  
Mustafa Said Aydogan ◽  
Hakan Parlakpinar ◽  
...  

2006 ◽  
Vol 31 (1) ◽  
pp. 14-18 ◽  
Author(s):  
Y KAU ◽  
Y HUNG ◽  
A ZIZZA ◽  
D ZURAKOWSKI ◽  
W GRECO ◽  
...  

2006 ◽  
Vol 31 (1) ◽  
pp. 14-18 ◽  
Author(s):  
Yi-Chuan Kau ◽  
Yu-Chun Hung ◽  
Anthony M. Zizza ◽  
David Zurakowski ◽  
William R. Greco ◽  
...  

2007 ◽  
Vol 32 (4) ◽  
pp. 288-295 ◽  
Author(s):  
Yu-Chun Hung ◽  
Chia-Ying Chen ◽  
Philipp Lirk ◽  
Chi-Fei Wang ◽  
Jen-Kun Cheng ◽  
...  

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