Optimization of Olive Oil-Based Nanoemulsion Preparation for Intravenous Drug Delivery

Karami, Zahra; Khoshkam, Maryam; Hamidi, Mehrdad

doi:10.1055/a-0654-4867

Cited by 19 publications

(20 citation statements)

References 24 publications

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“…However, as olive oil could solubilize more RPG than the two others, olive oil was selected as internal phase of NE preparation. The RPG‐NEs was prepared from olive oil, polysorbate 80 (tween 80), sorbitan monooleate (span 80), based on our previous report (Karami et al, ). Then, five formulations were prepared in triplicate in view to optimize P188 and chitosan content.…”

Section: Resultsmentioning

confidence: 99%

“…RPG‐NEs were prepared under high‐speed homogenization as described in our previous study with some modifications (Karami, Khoshkam, & Hamidi, ). In brief, RPG (0.1% wt/vol), oleic acid (0.3% wt/vol), α‐tocopherol (0.25% wt/vol), and S80 (3.2% wt/vol) were added to olive oil (7.45% wt/vol) and stirred well until reaching to a transparent solution.…”

Section: Methodsmentioning

confidence: 99%

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Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan‐coated nanoemulsion

et al. 2019

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The aim of the present study was to develop modified nanoemulsions to improve the oral bioavailability and pharmacokinetics of a poor water‐soluble drug, repaglinide (RPG). The repaglinide‐loaded nanoemulsions (RPG‐NEs) were prepared from olive oil as internal phase, span 80, tween 80, and poloxamer 188 as emulsifiers, using homogenization technique. The mean droplet size, zeta potential, and entrapment efficiency of RPG‐NEs were 86.5 ± 3.4 nm, −33.8 ± 2.1 mV, and 96.3 ± 2.3%, respectively. The chitosan‐coated RPG‐NEs (Cs‐RPG‐NEs) showed an average droplet size of 149.3 ± 3.9 nm and a positive zeta‐potential of +31.5 ± 2.8 mV. Drug release profile of RPG‐NEs was significantly higher than free drug in the simulated gastrointestinal fluids (p < .005). The in vivo study revealed 3.51‐ and 1.78‐fold increase in the AUC0‐12h and Cmax of the drug, respectively, in RPG‐NEs‐receiving animals in comparison to the free drug. The pharmacokinetic analysis confirmed that Cs‐RPG‐NEs were more efficient than uncoated ones for the oral delivery of RPG. Cs‐RPG‐NEs showed a longer t1/2 and higher AUC0‐∞ compared to control group. The relative bioavailability of Cs‐RPG‐NEs was higher than that of uncoated RPG‐NEs and free drug. Collectively, these findings suggest that chitosan‐coated nanoemulsions are promising carrier for improving the oral bioavailability of RPG.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan‐coated nanoemulsion

et al. 2019

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“…A high negative or positive value of zeta potential indicates a high electric charge on the surface of the NEs, which can cause strong electrostatic repulsion forces between droplets to prevent coalescence in order to maintain long-term physical stability. Both blank NEs exhibited negative zeta potentials in the range of −15.5 to −18.7 mV, which can be attributed to the presence of oleic acid in olive oil [15]. All formulations have high PDI value except F5.…”

Section: Effect Of Oil Phase/aqueous Phase Volume Ratiomentioning

confidence: 97%

Development and characterization of camphor-loaded ozonated olive oil nanoemulsions

Yalcin¹,

Takka²

2020

JRP

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The purpose of present study is to prepare and characterize camphor-loaded ozonated olive oil nanoemulsions (NEs). In this study, olive oils were ozonated with different times (up to 24 h) and their viscosities were examined. NEs were prepared by high-energy ultrasonication technique and characterized according to droplet size distribution, zeta potential, microscopic evaluation, and storage stability. The effect of oil phase/aqueous phase volume ratio, sonication time, and co-solvent (glycerol) on formulations were evaluated. 6 h ozonated olive oil was chosen for developing NEs due to its liquid form and viscosity (189 mPas). The obtained camphor-loaded NEs (with or without glycerol) had nearly 300 nm droplet size with negative zeta potential. Microscopic analysis revealed the spherical shape of droplets. The long-term stability tests showed that camphor-loaded NEs with glycerol were more stable than NEs without glycerol at 4 °C and 25 °C. According to the results, ozonated olive oil based NEs with glycerol might be promising nanosystems for topical delivery of camphor.

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“…The surface charge of nanoparticles may impact their biodistribution. Although negative zeta potential values ensure good electrochemical stability of nanoemulsions [63,64], neutral nanoparticles (±10 mV) show lower mononuclear phagocytic system uptake and the longest circulation compared to positive-or negative-charged particles [65], which is favourable to achieve efficient drug delivery after IV administration.…”

Section: Droplet Size and Zeta Potentialmentioning

confidence: 99%

Design of Non-Haemolytic Nanoemulsions for Intravenous Administration of Hydrophobic APIs

et al. 2020

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Among advanced formulation strategies, nanoemulsions are considered useful drug-delivery systems allowing to improve the solubility and the bioavailability of lipophilic drugs. To select safe excipients for nanoemulsion formulation and to discard any haemolytic potential, an in vitro miniaturized test was performed on human whole blood. From haemolysis results obtained on eighteen of the most commonly used excipients, a medium chain triglyceride, a surfactant, and a solubilizer were selected for formulation assays. Based on a design of experiments and a ternary diagram, the feasibility of nanoemulsions was determined. The composition was defined to produce monodisperse nanodroplets with a diameter of either 50 or 120 nm, and their physicochemical properties were optimized to be suitable for intravenous administration. These nanoemulsions, stable over 21 days in storage conditions, were shown to be able to encapsulate with high encapsulation efficiency and high drug loading, up to 16% (w/w), two water practically insoluble drug models: ibuprofen and fenofibrate. Both drugs may be released according to a modulable profile in sink conditions. Such nanoemulsions appear as a very promising and attractive strategy for the efficient early preclinical development of hydrophobic drugs.

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Optimization of Olive Oil-Based Nanoemulsion Preparation for Intravenous Drug Delivery

Cited by 19 publications

References 24 publications

Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan‐coated nanoemulsion

Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan‐coated nanoemulsion

Development and characterization of camphor-loaded ozonated olive oil nanoemulsions

Design of Non-Haemolytic Nanoemulsions for Intravenous Administration of Hydrophobic APIs

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