Addressing the Issue of Tetrodotoxin Targeting
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...
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| Format: | Article |
| Language: | English |
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MDPI AG
2018-09-01
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| Series: | Marine Drugs |
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| Online Access: | http://www.mdpi.com/1660-3397/16/10/352 |
| _version_ | 1798035104538296320 |
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| author | Daria I. Melnikova Yuri S. Khotimchenko Timur Yu. Magarlamov |
| author_facet | Daria I. Melnikova Yuri S. Khotimchenko Timur Yu. Magarlamov |
| author_sort | Daria I. Melnikova |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-11T20:53:34Z |
| format | Article |
| id | doaj.art-41293e052acb494c818ecbbc4ff048c2 |
| institution | Directory Open Access Journal |
| issn | 1660-3397 |
| language | English |
| last_indexed | 2024-04-11T20:53:34Z |
| publishDate | 2018-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Marine Drugs |
| spelling | doaj.art-41293e052acb494c818ecbbc4ff048c22022-12-22T04:03:46ZengMDPI AGMarine Drugs1660-33972018-09-01161035210.3390/md16100352md16100352Addressing the Issue of Tetrodotoxin TargetingDaria I. Melnikova0Yuri S. Khotimchenko1Timur Yu. Magarlamov2National Scientific Center of Marine Biology, Far Eastern Branch, Russian Academy of Sciences, Vladivostok 690041, RussiaNational Scientific Center of Marine Biology, Far Eastern Branch, Russian Academy of Sciences, Vladivostok 690041, RussiaNational Scientific Center of Marine Biology, Far Eastern Branch, Russian Academy of Sciences, Vladivostok 690041, RussiaThis 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.http://www.mdpi.com/1660-3397/16/10/352tetrodotoxinTTXNaV channelstargeted deliverydrug delivery systems |
| spellingShingle | Daria I. Melnikova Yuri S. Khotimchenko Timur Yu. Magarlamov Addressing the Issue of Tetrodotoxin Targeting Marine Drugs tetrodotoxin TTX NaV channels targeted delivery drug delivery systems |
| title | Addressing the Issue of Tetrodotoxin Targeting |
| title_full | Addressing the Issue of Tetrodotoxin Targeting |
| title_fullStr | Addressing the Issue of Tetrodotoxin Targeting |
| title_full_unstemmed | Addressing the Issue of Tetrodotoxin Targeting |
| title_short | Addressing the Issue of Tetrodotoxin Targeting |
| title_sort | addressing the issue of tetrodotoxin targeting |
| topic | tetrodotoxin TTX NaV channels targeted delivery drug delivery systems |
| url | http://www.mdpi.com/1660-3397/16/10/352 |
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