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Mar. Drugs 2018, 16(10), 352;

Addressing the Issue of Tetrodotoxin Targeting

National Scientific Center of Marine Biology, Far Eastern Branch, Russian Academy of Sciences, Vladivostok 690041, Russia
School of Biomedicine, Far Eastern Federal University, Vladivostok 690091, Russia
Author to whom correspondence should be addressed.
Received: 4 September 2018 / Revised: 21 September 2018 / Accepted: 24 September 2018 / Published: 26 September 2018
(This article belongs to the Special Issue Toxins as Marine-Based Drug Discovery)
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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. View Full-Text
Keywords: tetrodotoxin; TTX; NaV channels; targeted delivery; drug delivery systems tetrodotoxin; TTX; NaV channels; targeted delivery; drug delivery systems

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Melnikova, D.I.; Khotimchenko, Y.S.; Magarlamov, T.Y. Addressing the Issue of Tetrodotoxin Targeting. Mar. Drugs 2018, 16, 352.

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