Assessment of a liposomal formulation of ivermectin in rabbit after a single subcutaneous administration

Bassissi, Firas; Lespine, Anne; Alvinerie, M.

doi:10.1007/s00436-005-0073-z

Cited by 19 publications

(22 citation statements)

References 35 publications

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“…6, 13 The results of the present study differ from those previously reported for IVM in rabbits. 6 In the previous study IVM was administered at 0.4 mg/kg whereas in this study it was administered at 0.3 mg/kg.…”

Section: Discussioncontrasting

confidence: 99%

“…20 In a previous study, the effect of lipid ingestion on the kinetic disposition of MXD has been investigated in rabbits following oral administration at a dose rate of 0.3 mg/kg. 13 This study suggested that lipid administration increases the systemic availability of oral MXD. However, the plasma availability of MXD after oral administration in the previous study was much lower (C max : 7.44 ng/mL, Previous studies have shown that the plasma disposition of endectocides in different animal species is significantly affected by the solvent vehicle of the drug formulation.…”

Section: Discussionmentioning

confidence: 93%

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Plasma dispositions of ivermectin, doramectin and moxidectin following subcutaneous administration in rabbits

et al. 2010

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This study evaluated the comparative plasma dispositions of ivermectin (IVM), doramectin (DRM) and moxidectin (MXD) following subcutaneous administration in rabbits. Fifteen New Zealand white rabbits were allocated into three groups of five animals each. The animals in each group received IVM, DRM or MXD by subcutaneous injection at a single dose of 0.3 mg/kg. Blood samples were collected at various times between 1 h and 40 days after treatment and the plasma samples were analysed by high-performance liquid chromatography using fluorescence detection. Moxidectin was absorbed faster from the injection site and reached the peak plasma concentration (C max ) significantly earlier than IVM and DRM. There was no significant difference in C max values among the three molecules, whereas the area under the concentration -time curves of DRM (258.40 ng.d/mL) and IVM (191.62 ng.d/mL) was significantly higher than that of MXD (83.17 ng.d/mL). The mean plasma residence time and terminal half-life (t 1/2lz ) were longer for DRM (7.52 and 4.48 days, respectively) and MXD (8.97 and 8.16 days, respectively) compared with IVM (4.73 and 2.75 days, respectively). Considering the pharmacokinetic parameters for the parent molecules, the persistence of DRM and MXD are significantly longer than IVM and this may have a positive effect on their efficacy in rabbits following subcutaneous administration or utility relating to interdosing interval. Avermectins and milbemycins have been used intensively to control parasites of animals, humans and crops worldwide. Both chemical groups are naturally derived 16-membered macrocyclic lactones 1 produced by the soil dwelling actinomycetes, Streptomyces spp. Milbemycins are structurally related to the avermectins and share physicochemical properties with avermectins. Avermectins and milbemycins have excellent activity against nematodes and have systemic activity against several pathogenic ectoparasites of domestic animals at low dosage rates. Due to the high activity of avermectins and milbemycins against both nematodes and arthropods, they are now classified as 'endectocides'.2 The pharmacokinetic behaviour of avermectins and milbemycins is significantly affected by route of administration, formulation of the drug, and interspecies and interindividual variation.2 These anthelmintics are highly lipophilic substances, and are extensively distributed throughout the body and slowly eliminated through tissues such as liver and fat.3 For this reason a larger volume of distribution (V d ) may be obtained for these compounds compared with other anthelmintics. 4 Rabbits are widely used as laboratory animals for animal experiments. Endectocides are used extralabelly to control particularly ectoparasites, such as mite and mange infestations in rabbits.5212 Pharmacokinetic behaviours of endectocides have been extensively studied in different animal species. Although kinetic dispositions of ivermectin (IVM) have been reported previously, 6,13 very little information is available on the plasma pharma...

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Section: Discussioncontrasting

confidence: 99%

Section: Discussionmentioning

confidence: 93%

Plasma dispositions of ivermectin, doramectin and moxidectin following subcutaneous administration in rabbits

et al. 2010

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“…This suggested that SPC-SDC-MMs containing IVM could reach the bloodstream by the lymphatic pathway, which depended on the lymph node chains that absorbed the drug from the injection site. Also, the IVM injection demonstrated a slow and prolonged process of absorption due to the precipitation of the drug at the site of injection (Bassissi et al, 2006). Despite the difference in the absorption process, the two formulations shared similar pharmacokinetic profiles in rabbits.…”

Section: Discussionmentioning

confidence: 98%

“…One of the main goals of modern antiparasite chemotherapy is to optimize drugs to the pathogen and minimize side effects by innovative formulations to enhance the antihelmintic efficacy (Bassissi et al, 2006). Studies showed that the PC-BC-MMs system had great potential to improve the solubility of poorly soluble drug, particularly the lipophilic drugs.…”

Section: Discussionmentioning

confidence: 99%

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Subcutaneously injected ivermectin-loaded mixed micelles: formulation, pharmacokinetics and local irritation study

Dong

Lian

et al. 2014

Drug Delivery

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Clinical application of ivermectin (IVM) is limited by several unfavorable properties, induced by its insolubility in water. Slight differences in formulation may change the plasma pharmacokinetics and efficacy. In this study, an IVM-loaded Soy phosphatidylcholine-sodium deoxycholate mixed micelles (IVM-SPC-SDC-MMs) were developed to improve its aqueous solubility, aiming to make it more applicable for clinical use. First, IVM-SPC-SDC-MMs were prepared using the co-precipitation method. After formulation optimization, the particle size was 9.46 ± 0.16 nm according to dynamic light scattering. The water solubility of IVM in SPC-SDC-MMs (4.79 ± 0.02 mg/mL) was improved by 1200-fold, comparing with free IVM (0.004 mg/mL). After subcutaneous administration, the pharmacokinetic study showed that IVM-SPC-SDC-MMs and commercially available IVM injection were bioequivalent. Also, the local irritation study confirmed that IVM-SPC-SDC-MMs reduced side reactions of the commercially available IVM injection. These results indicated that IVM-SPC-SDC-MMs represented a promising new drug formulation suitable for subcutaneous delivery of IVM.

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Development and in vitro antiviral activity of ivermectin liposomes as a potential drug carrier system

Kocas,

Comoglu,

Ozkul

2024

Archiv der Pharmazie

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This study aimed to assess and compare diverse formulations of ivermectin‐loaded liposomes, employing lipid film hydration and ethanol injection methods. Three lipids (DOPC, SPC, and DSPC) were used in predetermined molar ratios. A total of 18 formulations were created, and a factorial design determined the optimal formulation based on particle size, polydispersity index (PDI), zeta potential, and encapsulation efficiency. The average mean particle size, PDI and zeta potential of the selected formulations (F1, F2, F7, F9, and F11) was, respectively, 196.40 ± 44.60 nm, 0.39 ± 0.09, and −40.24 ± 9.17. The encapsulation efficiency exceeded 80%, with a mean loading capacity of 4.00 ± 1.70%. In vitro studies included transmission electron microscopy, Fourier transform infrared spectroscopy, drug release, and antiviral activity assessments against SARS‐CoV‐2. The liposomal formulations demonstrated superior antiviral activity compared to free ivermectin, as indicated by lower IC50 values. The results of this study emphasize the effectiveness of ivermectin‐loaded liposomes in inhibiting viral activity, highlighting their potential as promising candidates for antiviral therapy. The findings suggest that the strategic use of liposomes as drug carriers can significantly modulate and improve the antiviral properties of ivermectin, offering a novel approach to harnessing its full therapeutic potential. Collectively, these results provide a robust foundation for further exploration of ivermectin as a viral protection tool and optimization of its delivery mechanisms.

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Assessment of a liposomal formulation of ivermectin in rabbit after a single subcutaneous administration

Cited by 19 publications

References 35 publications

Plasma dispositions of ivermectin, doramectin and moxidectin following subcutaneous administration in rabbits

Plasma dispositions of ivermectin, doramectin and moxidectin following subcutaneous administration in rabbits

Subcutaneously injected ivermectin-loaded mixed micelles: formulation, pharmacokinetics and local irritation study

Development and in vitro antiviral activity of ivermectin liposomes as a potential drug carrier system

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