Effect of Tetrodotoxin Pellets in a Rat Model of Postherpetic Neuralgia

Hong, Bihong; Sun, Jia; Zheng, Honghua; Le, Qingqing; Wang, Changsen; Bai, Kaikai; He, Jianlin; He, Huanghuang; Dong, Yanming

doi:10.3390/md16060195

Cited by 24 publications

(41 citation statements)

References 35 publications

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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%

“…(n = 6, mean ± SD). Reproduced from Bihong Hong et al[16], which is licensed under a Creative Commons Attribution-(CC BY 4.0) International License.…”

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confidence: 99%

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Analgesia Effect of Enteric Sustained-Release Tetrodotoxin Pellets in the Rat

Hong

Sun

et al. 2020

Pharmaceutics

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Tetrodotoxin (TTX) was identified as a latent neurotoxin that has a significant analgesia effect. It was rapidly absorbed and excreted in rat after intramuscular (i.m.) injection. To maintain the effect, frequent injections were required. The enteric sustained-release TTX pellets with sucrose pellets as a drug carrier was prepared by fluidized bed spray irrigation, coated in sequence with Eudragit NE30D as a sustained-release layer, hydroxypropyl methylcellulose (HPMC) as a barrier layer and Eudragit L30D-55 as an enteric coating. TTX in the pellets could be sustained released for 12 h in dissolution test. In vivo, TTX pellets reached Cmax at 5 h, and t1/2 was 14.52 ± 2.37 h after intragastrically (i.g.) administration in rat. In acetic acid induced writhing test in rat, the pellets at the dosages of 20, 40, 60 and 80 μg·kg−1 produced analgesic effect at about 1.5 h to 9 h and the strongest effect was at about 3 h to 6 h. Simultaneously, the LD50 of the enteric sustained-release TTX pellets was 840.13 μg·kg−1, and the ED50 was about 30 μg·kg−1. Thus, the therapeutic index was about 25. The enteric sustained-release TTX pellets with absolute analgesia effect and greatly enhanced safety was prepared.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Analgesia Effect of Enteric Sustained-Release Tetrodotoxin Pellets in the Rat

Hong

Sun

et al. 2020

Pharmaceutics

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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%

Can bioactive peptides of Lagocephalus sceleratus be evaluated in the functional food industry

Çavaş¹,

Bilgin²,

Yılmaz-Abeşka³

2020

biost

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Observations of Lessepsian migrant Lagocephalus sceleratus has been increasing along the Turkish coastline. Because of its toxins, it is known as a poisonous fish and not recommended to consume. To overcome this problem, an in silico-based biotechnological approach is proposed to evaluate the bioactive peptides from this species. The bioactive peptide contents of cytochrome oxidase subunit 1 in L. sceleratus with BIOPEP parameters were investigated in this study. The results show that there are many bioactive peptides such as the peptides with DPP-IV, ACE, alphaglucosidase inhibition activities, antioxidant and antiamnestic and their levels are comparable in well-consumed species such as Gallus gallus domesticus and Bos taurus. In conclusion, after removal of the toxin, the biomass of the L. sceleratus can be used to produce bioactive peptides for the production of functional foods which will be very important for food industry to provide multi-functional properties to foods. The paper can be used as a model methodology to exploit new bioactive peptides when new proteins are explored from L. sceleratus.

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“…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%

Investigation of the Size Distribution for Diffusion-Controlled Drug Release From Drug Delivery Systems of Various Geometries

Spiridonova

Tverdokhlebov

Anissimov

2019

Journal of Pharmaceutical Sciences

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Various Drug Delivery Systems (DDSs) are often used in modern medicine to achieve controlled and targeted drug release. Diffusional release of drugs from DDSs is often the main mechanism, especially at early times. Generally, average dimensions of DDS are used to model the drug release, but our recent work on drug release from fibers demonstrated that taking into account diameter distribution is essential. This work systematically investigated the effect of size distribution on diffusional drug release from DDSs of various geometric forms such as membranes, fibers and spherical particles. The investigation clearly demonstrated that the size distribution has the largest effect on the drug release profiles from spherical particles compared to other geometric forms. Published experimental data for drug release from polymer micro-and nanoparticles were fitted and the diffusion coefficients were determined assuming reported radius distributions. Assuming the average radius when fitting the data leads to up to 5 times underestimation of the diffusion coefficient of drug in the polymer.

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Effect of Tetrodotoxin Pellets in a Rat Model of Postherpetic Neuralgia

Cited by 24 publications

References 35 publications

Analgesia Effect of Enteric Sustained-Release Tetrodotoxin Pellets in the Rat

Analgesia Effect of Enteric Sustained-Release Tetrodotoxin Pellets in the Rat

Can bioactive peptides of Lagocephalus sceleratus be evaluated in the functional food industry

Investigation of the Size Distribution for Diffusion-Controlled Drug Release From Drug Delivery Systems of Various Geometries

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