Evaluation of the versatile character of a nanoemulsion formulation

Gué, E.; Since, Marc; Ropars, S.; Herbinet, Romuald; Pluart, Loïc Le; Malzert‐Fréon, Aurélie

doi:10.1016/j.ijpharm.2015.12.010

Cited by 49 publications

(30 citation statements)

References 65 publications

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“…Pseudo-ternary diagram with a mixture of surfactant-cosurfactant (S mix ) in the weight ratio of 1:1 displayed the greatest NE region and therefore was used for the incorporation of DPZ (Figure 2). DPZ-NE (6.25 mg/mL) was prepared by phase titration method, where spontaneous emulsification is produced by a low energy process [34]. In order to overcome rapid mucociliary clearance of the drug from the nose and increase the mucopenetrative ability of the drug, a non-ionic triblock copolymer of poly(ethylene glycol)-poly(propylene oxide)-poly(ethylene glycol) (PEG-PPO-PEG) was incorporated in the aqueous phase of the formulation to obtain DPZ-PNE.…”

Section: Discussionmentioning

confidence: 99%

Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil

et al. 2019

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Donepezil (DPZ) is widely used in the treatment of Alzheimer’s disease in tablet form for oral administration. The pharmacological efficacy of this drug can be enhanced by the use of intranasal administration because this route makes bypassing the blood–brain barrier (BBB) possible. The aim of this study was to develop a nanoemulsion (NE) as well as a nanoemulsion with a combination of bioadhesion and penetration enhancing properties (PNE) in order to facilitate the transport of DPZ from nose-to-brain. Composition of NE was established using three pseudo-ternary diagrams and PNE was developed by incorporating Pluronic F-127 to the aqueous phase. Parameters such as physical properties, stability, in vitro release profile, and ex vivo permeation were determined for both formulations. The tolerability was evaluated by in vitro and in vivo models. DPZ-NE and DPZ-PNE were transparent, monophasic, homogeneous, and physically stable with droplets of nanometric size and spherical shape. DPZ-NE showed Newtonian behavior whereas a shear thinning (pseudoplastic) behavior was observed for DPZ-PNE. The release profile of both formulations followed a hyperbolic kinetic. The permeation and prediction parameters were significantly higher for DPZ-PNE, suggesting the use of polymers to be an effective strategy to improve the bioadhesion and penetration of the drug through nasal mucosa, which consequently increase its bioavailability.

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Section: Discussionmentioning

confidence: 99%

Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil

et al. 2019

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“…Osmolarity of both F6H8-cEM was determined using the freezing-point method via a micro-osmometer autocal type 13 (Roebling, Berlin, Germany). For this, 100 μL of each native nanoemulsion were filled into a microtube and measurements were performed, as described previously 21…”

Section: Methodsmentioning

confidence: 99%

<p>Impact of different emulsifiers on biocompatibility and inflammatory potential of Perfluorohexyloctane (F6H8) emulsions for new intravenous drug delivery systems</p>

Tsagogiorgas

Anger

Beck

et al. 2019

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Background Emulsions on the basis of Perfluorohexyloctane (F6H8), a semifluorinated alkane (SFA), have shown to dissolve and transport highly lipophilic compounds. It is unknown how F6H8-containing emulsions (F6H8-cEM) interact with compartment blood, the reticuloendothelial system (RES), or influence injured organs in vivo. The current study was conducted to investigate the in vitro biocompatibility of F6H8-cEM and their drug delivery properties. Afterward, an in vivo study was performed as a proof-of-concept study in a rat model of acute kidney injury (AKI), which focused on the potential influence of F6H8-cEM on inflammation in an injured organ. Methods Two different F6H8-cEM were stabilized by the emulsifying agents Poloxamer 188 (Pluronic ® F68) or lecithin (S75). The two resulting emulsions F6H8-Pluronic or F6H8-lecithin were tested in vitro for the potential modulation of acute inflammation via whole blood assay, FACS, and ELISA. Antioxidant capacity and drug delivery properties were measured with an oxidation assay. Secondly, AKI was induced in the rats, which were treated with the F6H8-lecithin emulsion. Renal function and inflammation were assessed. Results Both F6H8-cEM were phagocytized by monocytes and both dose-dependently affected apoptosis (Annexin V binding) in monocytes. TNF-α expression increased dose-dependency for F6H8-Pluronic emulsion but not for F6H8-lecithin in a whole blood assay. Both F6H8-cEM were able to carry α-tocopherol as a model drug. Animals with AKI treated with the F6H8-lecithin emulsion showed a significantly better renal function and less infiltration of inflammatory cells in renal tissue compared to the control, while inflammatory markers in renal tissue, except HO-1, were not affected by F6H8-lecithin. Conclusions Pluronic ® F68 does not seem suitable as a biocompatible surfactant for F6H8-cEM. The injured kidney was not negatively influenced by the F6H8-lecithin emulsion. Lecithin-stabilized F6H8-cEM could be tested for preclinical studies as a carrier system for lipophilic agents.

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“…4 The type of oil, surfactant and co-surfactant used in SNES formulation depend on the solubility of the drug in different media, surfactant/co-surfactant emulsifying capacity, zone of self-emulsification and the extent of droplet size distribution in the nanoemulsion. 16 Based on these considerations, the aim of our study is to develop, optimize, characterize and evaluate TZloaded SNES in order to enhance solubilization capacity of this poorly water-soluble drug for proper treatment of ocular fungal infections. Phase solubility of TZ was evaluated in various oils, surfactants, and co-surfactants.…”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Self-nanoemulsifying System Optimization for Higher Terconazole Solubilization and Non-Irritant Ocular Administration

et al. 2020

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Purpose: Eye drops’ formulations of poorly water-soluble drugs, offer the advantage of crossing the lipophilic cornea, but their limited aqueous solubility may lead to low ocular bioavailability limiting their therapeutic uses. Terconazole (TZ) is an antifungal drug with low aqueous solubility, restricting its application in ocular fungal infection. Thus, the aim of the work in this study is to enhance TZ solubilization, permitting better ocular permeation and higher bioavailability. To achieve this goal, different self-nanoemulsifying systems (SNESs) were prepared using different oils, surfactants and co-surfactants. Methods: Ternary phase diagrams were constructed to identify self nano-emulsification regions for each oil system examined; either Labrafil® M2125CS or Capryol™ 90. TZ saturated solubility in the different formulated systems were measured and systems showing highest potential for TZ solubilization were selected. The optimized systems were chosen based on their globule size, polydispersity index, self-emulsification characteristics. Finally, TZ release as well as the irritation effect via Hen’s Egg test-chorioallantoic membrane (HET-CAM test) of the optimized system was observed in vitro. Results: The optimized system was formulated using 20% w/w Labrafil® M2125 CS, 50% w/w Tween® 80 and 30% w/w Transcutol® HP. Oil globules showed size range of 15.13 nm and self-emulsification time of 12.80 seconds. The system released 100% of the drug within half an hour compared to 2 hours in case of TZ-suspension. Finally, HET-CAM test showed non-irritating response and normal vascularization of the chorioallantoic membrane. Conclusion: The formulated SNES could be a promising approach to enhance ocular efficacy of TZ.

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Evaluation of the versatile character of a nanoemulsion formulation

Cited by 49 publications

References 65 publications

Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil

Formulation Strategies to Improve Nose-to-Brain Delivery of Donepezil

<p>Impact of different emulsifiers on biocompatibility and inflammatory potential of Perfluorohexyloctane (F6H8) emulsions for new intravenous drug delivery systems</p>

Self-nanoemulsifying System Optimization for Higher Terconazole Solubilization and Non-Irritant Ocular Administration

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