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Open AccessArticle

Combination Formulation of Tetrodotoxin and Lidocaine as a Potential Therapy for Severe Arrhythmias

by Bihong Hong 1,2,*,†, Jianlin He 1,2,†, Qingqing Le 1,2, Kaikai Bai 1,2, Yongqiang Chen 1,3 and Wenwen Huang 1,2
1
Third Institute of Oceanography, Ministry of Natural Resources, Xiamen 361005, China
2
Technical Innovation Center for Utilization of Marine Biological Resources, Ministry of Natural Resources, Xiamen 361005, China
3
College of Food and Biological Engineering, Jimei University, Xiamen 361021, China
*
Author to whom correspondence should be addressed.
They contributed equally to this work.
Mar. Drugs 2019, 17(12), 685; https://doi.org/10.3390/md17120685
Received: 14 November 2019 / Revised: 30 November 2019 / Accepted: 3 December 2019 / Published: 5 December 2019
Severe arrhythmias—such as ventricular arrhythmias—can be fatal, but treatment options are limited. The effects of a combined formulation of tetrodotoxin (TTX) and lidocaine (LID) on severe arrhythmias were studied. Patch clamp recording data showed that the combination of LID and TTX had a stronger inhibitory effect on voltage-gated sodium channel 1.5 (Nav1.5) than that of either TTX or LID alone. LID + TTX formulations were prepared with optimal stability containing 1 μg of TTX, 5 mg of LID, 6 mg of mannitol, and 4 mg of dextran-40 and then freeze dried. This formulation significantly delayed the onset and shortened the duration of arrhythmia induced by aconitine in rats. Arrhythmia-originated death was avoided by the combined formulation, with a decrease in the mortality rate from 64% to 0%. The data also suggests that the anti-arrhythmic effect of the combination was greater than that of either TTX or LID alone. This paper offers new approaches to develop effective medications against arrhythmias. View Full-Text
Keywords: Tetrodotoxin; lidocaine; combination preparation; arrhythmia; freeze dried powder Tetrodotoxin; lidocaine; combination preparation; arrhythmia; freeze dried powder
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Hong, B.; He, J.; Le, Q.; Bai, K.; Chen, Y.; Huang, W. Combination Formulation of Tetrodotoxin and Lidocaine as a Potential Therapy for Severe Arrhythmias. Mar. Drugs 2019, 17, 685.

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