Lecithin-based oil-in-water microemulsions for parenteral use: Pseudoternary phase diagrams, characterization and toxicity studies

Moreno, Marco; Ballesteros, M.; Frutos, P.

doi:10.1002/jps.10412

Cited by 93 publications

(58 citation statements)

References 17 publications

(17 reference statements)

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“…However, on further increase of oil content up to 20% w/w, significant increase in mean size was observed ( p 5 0.05) ( Table 4). The results presented are in agreement with the previous report that reveals a directly proportional relationship between oil concentration and mean globules size [12,42]. Similar findings were reported by Yuan and associates [23], that the increase in IPM as oil from 5% to 15% w/w, globules size of meloxicam-loaded microemulsion was correspondingly increased.…”

Section: Characterisation Of Nanoemulsionssupporting

confidence: 93%

Enhanced transdermal delivery of carvedilol using nanoemulsion as a vehicle

Rizwan¹,

Aqil²,

Azeem³

et al. 2010

Journal of Experimental Nanoscience

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The aim of the present study was to develop nanoemulsion as a possible vehicle for enhanced transdermal penetration of carvedilol (CVD). For screening of nanoemulsion components, solubility of CVD in oils, surfactants and co-surfactants was determined. Various surfactants and co-surfactants were screened for their ability to nanoemulsify the selected oily phases. The obtained results indicated that Acconon CC6Õ had shown good nanoemulsification efficiency (minimum surfactant required S min ¼ 46.52% w/w) among the selected surfactants and further improved in presence of Õ (S min ¼ 37.11% w/w). The ranges of nanoemulsion existence were delineated through the construction of the pseudo-ternary phase diagram at different ratio of surfactant mixture (S/ CoS), and various nanoemulsions were selected from phase diagram of S/CoS ratio 1 : 1. The effect of content of oil and S/CoS (1 : 1) on the skin permeation of CVD was evaluated through an excised wistar rat skin using Franz diffusion cell. All the nanoemulsions showed a high skin permeation rate (92.251-161.53 mg/ cm 2 /h), good enhancement ratio (3.5-6.2) and high permeability coefficient in comparison to control groups. The optimised nanoemulsion formulation with the highest skin permeation rate (161.53 mg/cm 2 /h) consisted of 0.25% w/w CVD, 12.5% w/w Miglyol 810 Õ , 50% w/w Acconon CC6 Õ /CO-20 Õ (1 : 1) and water. The above formulation had the smallest mean globules size (9.28 nm). The superior transdermal flux of CVD may be due to nanorange size of oil globules that lead to intimate contact with the skin layer. These studies suggest that the nanoemulsion system is a promising vehicle for the transdermal delivery of CVD.

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Section: Characterisation Of Nanoemulsionssupporting

confidence: 93%

Enhanced transdermal delivery of carvedilol using nanoemulsion as a vehicle

Rizwan¹,

Aqil²,

Azeem³

et al. 2010

Journal of Experimental Nanoscience

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“…This result is of extreme importance in the development of a nanostructured cosmetic or pharmaceutical product with low cytotoxicity, and our results corroborate the studies that demonstrate that nanoemulsions present a reduction in toxicity. Moreno et al [41] reported that lecithin-based microemulsions used for parenteral use showed reduced toxicity. Wang et al [42] developed aclacinomycin A (E-ACM) emulsion and evaluated its toxicity in M5076 tumorbearing C57BL/6 mice.…”

Section: Discussionmentioning

confidence: 99%

Andiroba Oil (Carapa guianensis Aublet) Nanoemulsions: Development and Assessment of Cytotoxicity, Genotoxicity, and Hematotoxicity

Milhomem-Paixão

Fascineli

Muehlmann

et al. 2017

Journal of Nanomaterials

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Andiroba oil (AO) is obtained from an Amazonian plant and is used in traditional medicine. We carried out a comparative study to test the cytotoxicity, genotoxicity, and hematotoxicity of the oil and its nanoemulsion (AN) in vitro (fibroblasts, lineage NIH/3T3) and in vivo (Swiss mice). The AN was characterized by DLS/Zeta, and its stability was investigated for 120 days. The biological activity of AN was assessed in vitro by MTT test and cell morphology analyses and in vivo by micronucleus, comet, and hematotoxicity tests. The AN presented a hydrodynamic diameter (Hd) of 142.5 ± 3.0 and PDI of 0.272 ± 0.007 and good stability at room temperature. The MTT test evidenced the cytotoxicity of AO and of AN only at their highest concentrations, but AN showed lower cytotoxicity than AO. A lower cytotoxicity of AN, when compared to AO, is in fact an interesting data suggesting that during therapeutic application there will be a lower impact in the cell viability of healthy cells. Cytotoxicity, genotoxicity, and hematotoxicity were not observed in vivo. These tests on the biological and toxicological effects of andiroba oil and nanostructured oil are still initial ones but will give a direction to future application in cosmetics and/or the development of new phytotherapics.

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“…The thermodynamic stability of the prepared nanoemulsion formulae was assessed by centrifugation at 3500 rpm for 30 min (Moreno et al, 2003). Heating/cooling cycles between 4 C and 25 C, as well as freeze-thaw cycles between À21 C and 25 C were also carried out (Shafiq et al, 2007).…”

Section: Thermodynamic Stability Studiesmentioning

confidence: 99%

In vitroandin vivoevaluation of indomethacin nanoemulsion as a transdermal delivery system

2013

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Nanoemulsions were investigated as transdermal delivery systems for indomethacin. Six formulae were prepared using Triacetin, capryol 90 and labrafil as oils; Tween 80 and pluronic F127 as surfactants and transcutol and propylene glycol as co-surfactants. The continuous phase was that one with the larger volume fraction regardless of the hydrophile-lipophile balance of the surfactant/co-surfactant mixture. Surfactant type had significant effects on particle size and rheological properties of the nanoemulsions. Pluronicbased formulae recorded the lowest particle sizes and the highest viscosities. The prepared nanoemulsions increased drug solubility up to 610-fold compared with water. Refractive index measurements proved the compatibility between indomethacin and the used nanoemulsion components. Indomethacin was almost completely ionized at the pH values of the prepared nanoemulsions, suggesting drug absorption via the hydrophilic pathway of the skin upon topical application. Nanoemulsions controlled indomethacin release through semipermeable membrane and enhanced its permeation through excised newly born albino rat skin. The formulae were stable for six months at ambient conditions. Transdermal single application of selected formulae resulted in effective plasma levels up to 32 h in rats. Nanoemulsions were significantly superior to other investigated transdermal approaches at solubilizing indomethacin and achieving higher plasma levels.

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Lecithin-based oil-in-water microemulsions for parenteral use: Pseudoternary phase diagrams, characterization and toxicity studies

Cited by 93 publications

References 17 publications

Enhanced transdermal delivery of carvedilol using nanoemulsion as a vehicle

Enhanced transdermal delivery of carvedilol using nanoemulsion as a vehicle

Andiroba Oil (Carapa guianensis Aublet) Nanoemulsions: Development and Assessment of Cytotoxicity, Genotoxicity, and Hematotoxicity

In vitroandin vivoevaluation of indomethacin nanoemulsion as a transdermal delivery system

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