Pharmacokinetics and bioequivalence in the pig of two ivermectin feed formulations

Lees, P.; Cheng, Zhangrui; Chambers, Michael; Speirs, G; Hennessy, D.R.; Abbott, E.M.

doi:10.1111/j.1365-2885.2012.01428.x

Cited by 5 publications

(1 citation statement)

References 12 publications

(12 reference statements)

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“…After 0.2 mg/kg oral tablet administration, IVM plasma concentration levels were in agreement with those previously published for piglets. 25,26 IVM was well absorbed and extensively distributed, resulting in higher concentrations in lung tissue than in plasma (see Fig. 2), a pattern already observed in cattle subcutaneously treated with IVM, 17 and confirmed by a recent pharmacokinetic simulation report looking at IVM lung exposure in humans.…”

Section: Discussionsupporting

confidence: 77%

Safety and Pharmacokinetic Assessments of a Novel Ivermectin Nasal Spray Formulation in a Pig Model

Errecalde

Lifschitz

Vecchioli³

et al. 2021

Journal of Pharmaceutical Sciences

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Recently published data indicates that high ivermectin (IVM) concentrations suppress in vitro SARS-CoV-2 replication. Nasal IVM spray administration may contribute to attaining high drug concentrations in nasopharyngeal tissue, a primary site of virus entrance/replication. The safety and pharmacokinetic performances of a novel IVM spray formulation were assessed in a pig model. Piglets received IVM either orally (0.2 mg/kg) or by one or two nasal spray doses. The overall safety, and histopathology of the IVM-spray application site tissues, were assessed. The IVM concentration profiles measured in plasma and respiratory tract tissues after the nasal spray were compared with those achieved after the oral administration. Animals tolerated well the nasal spray formulation. No local/systemic adverse events were observed. After nasal administration, the highest IVM concentrations were measured in nasopharyngeal and lung tissues. The nasal/oral IVM concentration ratios in nasopharyngeal and lung tissues markedly increased by repeating (12 h apart) the spray application. The fast attainment of high and persistent IVM concentrations in nasopharyngeal tissue is the main advantage of the nasal over the oral route. These original results support the undertaking of future clinical trials to evaluate the safety/efficacy of the nasal IVM spray application in the prevention and/or treatment of COVID-19.

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Section: Discussionsupporting

confidence: 77%

Safety and Pharmacokinetic Assessments of a Novel Ivermectin Nasal Spray Formulation in a Pig Model

Errecalde

Lifschitz

Vecchioli³

et al. 2021

Journal of Pharmaceutical Sciences

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show abstract

Efficient weapon for protracted warfare to malaria: A chondroitin sulfate derivates-containing injectable, ultra-long-lasting meshy-gel system

Luo

Zhang

Liu

et al. 2019

Carbohydrate Polymers

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Ivermectin repurposing for COVID-19 therapy: Safety and pharmacokinetic assessment of a novel nasal spray formulation in a pig model

Errecalde¹,

Lifschitz

Vecchioli³

et al. 2020

Preprint

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High ivermectin (IVM) concentrations suppress in vitro SARS-CoV-2 replication. Nasal IVM spray (NIVM spray) administration may contribute to attaining high drug concentrations in nasopharyngeal (NP) tissue, a primary site of virus entrance/replication. The safety and pharmacokinetic performance of a new NIVM spray formulation in a piglet model were assessed. Crossbred piglets (10/12 kg) were treated with either one or two (12 h apart) doses of N IVM spray (2 mg, 1 puff/nostril) or orally (0.2 mg/kg). The overall safety of NIVM-spray was assessed (clinical, haematological, serum biochemical determinations), and histopathology evaluation of the application site tissues performed. The IVM concentration profiles measured in plasma and respiratory tract tissues (nasopharynx and lungs) after the nasal spray treatment (one and two applications) were compared with those achieved after the oral administration. Animals tolerated well the novel NIVM spray formulation. No local/systemic adverse events were observed. After nasal administration, the highest IVM concentrations were measured in NP and lung tissues. Significant increases in IVM concentration profiles in both NPtissue and lungs were observed after the 2 dose nasal administrations. The nasal/oral IVM concentration ratios in NP and lung tissues (at 6 h postdose) markedely increased by repeating the spray application. The fast attainment of high and persistent IVM concentrations in NP tissue is the main advantage of the nasal over the oral route. These original results are encouraging to support the undertaking of further clinical trials to evaluate the safety/efficacy of the nasal IVM spray application in the treatment and/or prevention of COVID-19.

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Pharmacokinetics and bioequivalence in the pig of two ivermectin feed formulations

Cited by 5 publications

References 12 publications

Safety and Pharmacokinetic Assessments of a Novel Ivermectin Nasal Spray Formulation in a Pig Model

Safety and Pharmacokinetic Assessments of a Novel Ivermectin Nasal Spray Formulation in a Pig Model

Efficient weapon for protracted warfare to malaria: A chondroitin sulfate derivates-containing injectable, ultra-long-lasting meshy-gel system

Ivermectin repurposing for COVID-19 therapy: Safety and pharmacokinetic assessment of a novel nasal spray formulation in a pig model

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