10.1021/acsnano.8b05408.s001
Christopher Weldon
Christopher
Weldon
Tianjiao Ji
Tianjiao
Ji
Minh-Thuy Nguyen
Minh-Thuy
Nguyen
Alina Rwei
Alina
Rwei
Weiping Wang
Weiping
Wang
Yi Hao
Yi
Hao
Chao Zhao
Chao
Zhao
Manisha Mehta
Manisha
Mehta
Bruce Y. Wang
Bruce Y.
Wang
Jonathan Tsui
Jonathan
Tsui
Robert
P. Marini
Robert
P.
Marini
Daniel S. Kohane
Daniel S.
Kohane
Nanoscale
Bupivacaine Formulations To Enhance the
Duration and Safety of Intravenous Regional Anesthesia
American Chemical Society
2018
anesthetic
dose
M-Bup
anesthesia
safety
Intravenous Regional Anesthesia Intravenous
rat tail vein IVRA model
postoperative pain relief
L-Bup
Nanoscale Bupivacaine Formulations
100 nm liposomal bupivacaine
tourniquet removal
2018-10-23 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Nanoscale_Bupivacaine_Formulations_To_Enhance_the_Duration_and_Safety_of_Intravenous_Regional_Anesthesia/7358720
Intravenous
regional anesthesia (IVRA; Bier block) is commonly
used to anesthetize an extremity for surgery. Limitations of the procedure
include pain from the required tourniquet, the toxicity that can occur
from systemic release of local anesthetics, and the lack of postoperative
pain relief. We hypothesized that the nanoencapsulation of the local
anesthetic would prolong local anesthesia and enhance safety. Here,
we developed an ∼15 nm micellar bupivacaine formulation (M-Bup)
and tested it in a rat tail vein IVRA model, in which active agents
were restricted in the tail by a tourniquet for 15 min. After tourniquet
removal, M-Bup provided local anesthesia for 4.5 h, which was two
times longer than that from a larger dose of free bupivacaine. Approximately
100 nm liposomal bupivacaine (L-Bup) with the same drug dose as M-Bup
did not cause anesthesia. Blood levels of bupivacaine after tourniquet
removal were lower in animals receiving M-Bup than L-Bup or free bupivacaine,
demonstrating enhanced safety. Tissue reaction to M-Bup was benign.