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Review
. 2018 Sep 26;16(10):352.
doi: 10.3390/md16100352.

Addressing the Issue of Tetrodotoxin Targeting

Daria I Melnikova  1   2 , Yuri S Khotimchenko  3   4 , Timur Yu Magarlamov  5   6
Affiliations
Review

Addressing the Issue of Tetrodotoxin Targeting

Daria I Melnikova et al. Mar Drugs. .

Abstract

This review is devoted to the medical application of tetrodotoxin (TTX), a potent non-protein specific blocker of voltage-gated sodium (NaV) channels. The selectivity of action, lack of affinity with the heart muscle NaV channels, and the inability to penetrate the blood⁻brain barrier make this toxin an attractive candidate for anesthetic and analgesic drug design. The efficacy of TTX was shown in neuropathic, acute and inflammatory pain models. The main emphasis of the review is on studies focused on the improvement of TTX efficacy and safety in conjunction with additional substances and drug delivery systems. A significant improvement in the effectiveness of the toxin was demonstrated when used in tandem with vasoconstrictors, local anesthetics and chemical permeation enhancers, with the best results obtained with the encapsulation of TTX in microparticles and liposomes conjugated to gold nanorods.

Keywords: NaV channels; TTX; drug delivery systems; targeted delivery; tetrodotoxin.

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Conflict of interest statement

The authors declare no conflict of interests.

Figures

Figure 1
Figure 1
Molecular targets and principles of action of common anti-pain drugs and tetrodotoxin.
Figure 2
Figure 2
Patents devoted to tetrodotoxin and its analogues in the Google Patents database.
Figure 3
Figure 3
Effect of tetrodotoxin (TTX) co-application and address delivery on its systemic distribution and toxicity.
Figure 4
Figure 4
Influence of the co-application of tetrodotoxin (TTX) with other compounds and drug delivery systems on the therapeutic properties of the toxin.
See this image and copyright information in PMC

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