2018
DOI: 10.3390/md16060195
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Effect of Tetrodotoxin Pellets in a Rat Model of Postherpetic Neuralgia

Abstract: Postherpetic neuralgia (PHN) is nerve pain caused by a reactivation of the varicella zoster virus. Medications are used to reduce PHN but their use is limited by serious side effects. Tetrodotoxin (TTX) is a latent neurotoxin that can block neuropathic pain, but its therapeutic index is only 3–5 times with intravenous or intramuscular injection. Therefore, we prepared oral TTX pellets and examined their effect in a rat model of PHN induced by resiniferatoxin (RTX). Oral TTX pellets were significantly effective… Show more

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Cited by 25 publications
(41 citation statements)
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“…Previously, the pharmacokinetic profile of the immediate-release TTX pellets was studied by our group with the dose of 100 µg/kg [16], which was well-tolerated on rat, and TTX concentrations in plasma were included in the limit of quantification. Comparing the dissolution curves of the immediate-release and sustained-release TTX pellets, 150 µg/kg was used in this study to ensure the quantification of TTX in plasma.…”
Section: Discussionmentioning
confidence: 99%
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“…Previously, the pharmacokinetic profile of the immediate-release TTX pellets was studied by our group with the dose of 100 µg/kg [16], which was well-tolerated on rat, and TTX concentrations in plasma were included in the limit of quantification. Comparing the dissolution curves of the immediate-release and sustained-release TTX pellets, 150 µg/kg was used in this study to ensure the quantification of TTX in plasma.…”
Section: Discussionmentioning
confidence: 99%
“…administration was included in this paper to calculate absolute bioavailability of the sustained-release TTX pellets. Additionally, in another study that we've conducted [16], the immediate-release TTX pellets was orally administrated to SD rats, in which the T max was 2 h, t 1/2 was 3.23 h and the F was 6.7%. In the current study, the T max was 5 h, t 1/2 was 14.52 h and the F was 9.7% for the sustained-release TTX pellets (Table 5), indicating a significant improvement of TTX retention in the body.…”
Section: Discussionmentioning
confidence: 99%
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“…However, it must be noted that TTX should be removed from L. sceleratus based products for possible human consumption because of its toxic effects on human metabolism. Alternatively, TTX containing formulas like in Hong et al 2018 andHong et al 2019 may be prepared to evaluate the biomass of the species (for therapeutic purposes).…”
Section: Discussionmentioning
confidence: 99%
“…In addition, it should be noted that the authors of [33] provided the MATLAB program code for the implementation of their model. That model [33] was subsequently successfully applied in practice in work [34] for investigation of effect of tetrodotoxin pellets in a rat model of postherpetic neuralgia. These mathematical models described the drug release from an ensemble of coated pellets and capsules, with the release described by empirical functions or by ordinary differential equations.…”
Section: Introductionmentioning
confidence: 99%