Match of Solubility Parameters Between Oil and Surfactants as a Rational Approach for the Formulation of Microemulsion with a High Dispersed Volume of Copaiba Oil and Low Surfactant Content

Background: Ceftriaxone is one of the most common types of antibiotics used to treat most deadly bacterial infections. One way to alleviate the side effects of medication is to reduce drug consumption by changing the ordinary drug forms into nanostructured forms. In this study, a nanostructured lipid carrier (NLC) containing hydrophilic ceftriaxone sodium drug is developed, and its effect on eliminating gram-negative bacteria Escherichia coli death is investigated.Methods: Double emulsion solvent evaporation method is applied to prepare NLC. Mathematical modeling based on the solubility study is performed to select the best materials for NLC preparation. Haftyzer-Van Krevelen and Hoy's models are employed for this purpose. Drug release from optimized NLC is examined under in vitro environment. Then, the efficacy of the optimized sample on eliminating gram-negative bacteria Escherichia coli is investigated. Results: Mathematical modeling reveals that both methods are capable of predicting drug encapsulation efficiency trends by chaining solid and liquid lipids. However, Haftyzer-Van Krevelen's method can precisely predict the particle size trend by changing the surfactant types in water and oily phases of emulsions. The optimal sample has a mean particle size of 86 nm and drug entrapment efficiency of 83%. Also, a controlled drug release in prepared nanostructures over time is observed under in-vitro media. The results regarding the effectiveness of optimized NLC in killing Escherichia coli bacteria suggests that by cutting drug dosage of the nanostructured form in half, an effect comparable to that of free drug can be observed at longer times. Conclusion: Results confirm that NLC structure is an appropriate alternative for the delivery of ceftriaxone drug with a controlled release behavior.

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“…In Eq. 12, W A, W B, and W C represent the weight fraction of components A, B, and C, respectively C [15].…”

Section: Materials Selection Based On Mathematical Methodsmentioning

confidence: 99%

Enhanced bactericidal effect of ceftriaxone drug encapsulated in nanostructured lipid carrier against gram-negative Escherichia coli bacteria: drug formulation, optimization, and cell culture study

Ebrahimi

Farhadian

Karimi

et al. 2020

Antimicrob Resist Infect Control

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“…The effects of seven complexes of mixed surfactants (Span 80 and glycerolmonooleate at ratios of 3:2 and 3:4; glycerolmonooleate and Tween-80 at ratios of 2:1, 3:1 and 4:1, and Span 80/Tween-80 at ratios of 3:1 and 4:1) were investigated on the NE-forming area of a pseudo-ternary phase diagram in the surfactant/anhydrous ethanol/soybean oil/water system [surfactant and co-surfactant ratio ( K m ) of 2:1] at room temperature ( 18 ).…”

Section: Methodsmentioning

confidence: 99%

Preparation and evaluation of spirulina polysaccharide nanoemulsions

Wang

Cai

Liu³

et al. 2018

Int J Mol Med

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The aim of the present study was to prepare spirulina polysaccharide (PSP) into an oral nanoemulsion (NE) with the aim of improving its oral bioavailability and prolonging its sustained release effect. The PSP-NE was prepared through a phase transformation method, and its formulation components were screened through the use of a pseudo-ternary phase diagram. The optimal formulation of PSP-NE was determined to be: 11.9% Span 80, 6.0% Tween-80, 9.0% ethanol, 62.8% soybean oil, and 10.3% PSP aqueous solution. The prepared PSP-NE was clear and transparent, had a uniform color and spherical morphology, exhibited stability and no adhesion. The average particle size was 79.93±19 nm, the polydispersity index was 0.185±0.04 (n=3), and the entrapment rate was 62%. Small-animal imaging results showed that the prepared PSP-NE exhibited a sustained release and tissue effect in contrast to the PSP aqueous solution. The present study showed that the prepared PSP-NE not only exhibited a sustained release and tissue effect in contrast to the PSP aqueous solution, but also had superior performance in terms of antitumor and antioxidant effects.

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“…The PDI was set as a criterion of the particle size distribution [ 28 , 29 ]. The value of PDI less than 0.25 demonstrated a narrow distribution [ 30 , 31 , 32 ]. The PDIs of MS1 and MS2 aqueous dispersions were measured to be 0.10 ± 0.02 and 0.07 ± 0.05, showing monodispersity via SPG emulsification.…”

Section: Resultsmentioning

confidence: 99%

Antagonistic Effect of Azoxystrobin Poly (Lactic Acid) Microspheres with Controllable Particle Size on Colletotrichum higginsianum Sacc

et al. 2018

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Size-controlled azoxystrobin-poly (lactic acid) microspheres (MS) were prepared by an oil/water emulsion solvent evaporation approach. The hydrated mean particle sizes of the MS1, MS2, and MS3 aqueous dispersions were 130.9 nm, 353.4 nm, and 3078.0 nm, respectively. The drug loading and encapsulation efficiency of the azoxystrobin microspheres had a positive relationship with particle size. However, the release rate and percentage of cumulative release were inversely related to particle size. The smaller-sized microspheres had a greater potential to access the target mitochondria. As a result, the more severe oxidative damage of Colletotrichum higginsianum Sacc and higher antagonistic activity were induced by the smaller particle size of azoxystrobin microspheres. The 50% lethal concentrations against Colletotrichum higginsianum Sacc of MS1, MS2, and MS3 were 2.0386 μg/mL, 12.7246 μg/mL, and 21.2905 μg/mL, respectively. These findings reveal that particle size is a critical factor in increasing the bioavailability of insoluble fungicide.

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Match of Solubility Parameters Between Oil and Surfactants as a Rational Approach for the Formulation of Microemulsion with a High Dispersed Volume of Copaiba Oil and Low Surfactant Content

Abstract: O/W microemulsions with a high volume fraction of complex natural oil and a reasonable surfactant concentration were formulated. These microemulsions can be proposed as delivery systems for the oral administration of poorly soluble drugs.

Cited by 15 publications

References 45 publications

Enhanced bactericidal effect of ceftriaxone drug encapsulated in nanostructured lipid carrier against gram-negative Escherichia coli bacteria: drug formulation, optimization, and cell culture study

Enhanced bactericidal effect of ceftriaxone drug encapsulated in nanostructured lipid carrier against gram-negative Escherichia coli bacteria: drug formulation, optimization, and cell culture study

Preparation and evaluation of spirulina polysaccharide nanoemulsions

Antagonistic Effect of Azoxystrobin Poly (Lactic Acid) Microspheres with Controllable Particle Size on Colletotrichum higginsianum Sacc

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