Similarity between the in vitro activity and toxicity of two different fungizone™ / lipofundin™ admixtures

Araújo, Ivonete Batista de; Brito, Cab; Urbano, Isabel A.; Dominici, Victor A.; Filho, Miguel A. Silva; Silveira, Walteçá Louis Lima da; Damasceno, Bolívar Ponciano Goulart de Lima; Medeiros, Aldo Cunha; Egito, Eryvaldo Sócrates Tabosa do

doi:10.1590/s0102-86502005000700022

Cited by 4 publications

(3 citation statements)

References 14 publications

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“…The phenomenon of K + release from model cells has been referred to as a chronic toxicity by some authors. 6,17 On the other hand, a strong toxicity level, which induces hemoglobin leakage, for RBCs, or cell death for Cp, has been classified as acute toxicity. 6,17 Four milliliter samples of RBCs (5 × 10 7 cells .…”

Section: Preparation Of Candida Parapsilosis Suspensionmentioning

confidence: 99%

“…6,17 On the other hand, a strong toxicity level, which induces hemoglobin leakage, for RBCs, or cell death for Cp, has been classified as acute toxicity. 6,17 Four milliliter samples of RBCs (5 × 10 7 cells . mL −1 ) were incubated for 1 hour at 37°C with the vehicle control or with different concentrations (50, 5, 0.5, and 0.05 mg .…”

Section: Preparation Of Candida Parapsilosis Suspensionmentioning

confidence: 99%

“…13 In an attempt to reduce the AmB-DOC toxicity, some lipid formulations such as liposomes and other AmB lipidassociated forms were developed. [14][15][16][17][18] These systems are able to immobilize the AmB monomers, preventing selfaggregation. They slowly release monomers to the media, and, therefore, are active only against fungal cells.…”

Section: Introductionmentioning

confidence: 99%

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How can micelle systems be rebuilt by a heating process?

Silva-Filho

Siqueira²,

Freire³

et al. 2012

IJN

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The aim of this work was to evaluate how an aqueous micellar system containing Amphotericin B (AmB) and sodium deoxycholate (DOC) can be rebuilt after heating treatment. Also, a review of the literature on the physicochemical and biological properties of this new system was conducted. Heated (AmB-DOC-H) and unheated (AmB-DOC) micelles were then diluted at four different concentrations (50 mg · L −1 , 5 mg · L −1 , 0.5 mg · L −1 , and 0.05 mg · L −1 ) to perform physicochemical studies and a pharmacotoxicity assay, in which two cell models were used for the in vitro experiments: red blood cells (RBC) from human donors and Candida parapsilosis ( Cp ). While potassium (K + ) and hemoglobin leakage from RBC were the parameters used to evaluate acute and chronic toxicity, respectively, the efficacy of AmB-DOC and AmB-DOC-H were assessed by K + leakage and cell survival rate from Cp . The spectral study revealed a slight change in the AmB-DOC aggregate peak from 327 nm to 323 nm, which is the peak for AmB-DOC-H. Although AmB-DOC and AmB-DOC-H exhibited different behavior for hemoglobin leakage, AmB-DOC produced higher leakage than AmB-DOC-H at high concentrations (from 5 mg · L −1 ). For K + leakage, both AmB-DOC and AmB-DOC-H showed a similar profile for both cell models, RBC and Cp ( P < 0.05). AmB-DOC-H and AmB-DOC also revealed a similar profile of activity against Cp with an equivalent survival rate. In short, AmB-DOC-H showed much less toxicity than AmB-DOC, but remained as active as AmB-DOC against fungal cells. The results highlight the importance of this new procedure as a simple, inexpensive, and safe way to produce a new kind of micelle system for the treatment of systemic fungal infections.

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Section: Preparation Of Candida Parapsilosis Suspensionmentioning

confidence: 99%

Section: Preparation Of Candida Parapsilosis Suspensionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

How can micelle systems be rebuilt by a heating process?

Silva-Filho

Siqueira²,

Freire³

et al. 2012

IJN

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Influence of the Freeze-Drying Process on the Physicochemical and Biological Properties of Pre-heated Amphotericin B Micellar Systems

et al. 2014

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The moderate heat treatment of amphotericin B (AmB) in its micellar form (M-AmB) results in superaggregates (H-AmB) that present a substantially lower toxicity and similar activity. The aim of this work was to evaluate the H-AmB behavior after a freeze-drying process. H-AmB and M-AmB micelles were evaluated before and after freeze-drying concerning their physicochemical and biological properties by spectrophotometry and activity/toxicity assay, respectively. Four concentrations of M-AmB and H-AmB were studied aiming to correlate their aggregation state and the respective biological behavior: 50 mg L(-1), 5 mg L(-1), 0.5 mg L(-1), and 0.05 mg L(-1). Then, potassium leakage and hemoglobin leakage from red blood cells were used to evaluate the acute and chronic toxicity, respectively. The efficacy of M-AmB and H-AmB formulations was assessed by potassium leakage from Candida albicans and by the broth microdilution method. After heating, in addition to an evident turbidity, a slight blueshift from 327 to 323 nm was also observed at the concentrations of 50 and 5 mg L(-1) for H-AmB. Additionally, an increase in the absorbance at 323 nm at the concentration of 0.5 mg L(-1) was detected. Concerning the toxicity, H-AmB caused significantly lower hemoglobin leakage than M-AmB. These results were observed for H-AmB before and after freeze-drying. However, there was no difference between H-AmB and M-AmB concerning their activity. Accordingly, the freeze-drying cycle did not show any influence on the behavior of heated formulations, highlighting the suitability of such a method to produce a new AmB product with a long shelf life and with both greater efficiency and less toxicity.

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Getting the Jump on the Development of Bullfrog Oil Microemulsions: a Nanocarrier for Amphotericin B Intended for Antifungal Treatment

et al. 2018

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Amphotericin B (AmB), a potent antifungal drug, presents physicochemical characteristics that impair the development of suitable dosage forms. In order to overcome the AmB insolubility, several lipid carriers such as microemulsions have been developed. In this context, the bullfrog oil stands out as an eligible oily phase component, since its cholesterol composition may favor the AmB incorporation. Thus, the aim of this study was to develop a microemulsion based on bullfrog oil containing AmB. Moreover, its thermal stability, antifungal activity, and cytotoxicity in vitro were evaluated. The microemulsion formulation was produced using the pseudo-ternary phase diagram (PTPD) approach and the AmB was incorporated based on the pH variation technique. The antifungal activity was evaluated by determination of minimal inhibitory concentration (MIC) against different species of Candida spp. and Trichosporon asahii. The bullfrog oil microemulsion, stabilized with 16.8% of a surfactant blend, presented an average droplet size of 26.50 ± 0.14 nm and a polydispersity index of 0.167 ± 0.006. This system was able to entrap AmB up to 2 mg mL. The use of bullfrog oil as oily phase allowed an improvement of the thermal stability of the system. The MIC assay results revealed a growth inhibition for different strains of Candida spp. and were able to enhance the activity of AmB against T. asahii. The microemulsion was also able to reduce the AmB toxicity. Finally, the developed microemulsion showed to be a suitable system to incorporate AmB, improving the system's thermal stability, increasing the antifungal activity, and reducing the toxicity of this drug.

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Similarity between the in vitro activity and toxicity of two different fungizone™ / lipofundin™ admixtures

Cited by 4 publications

References 14 publications

How can micelle systems be rebuilt by a heating process?

How can micelle systems be rebuilt by a heating process?

Influence of the Freeze-Drying Process on the Physicochemical and Biological Properties of Pre-heated Amphotericin B Micellar Systems

Getting the Jump on the Development of Bullfrog Oil Microemulsions: a Nanocarrier for Amphotericin B Intended for Antifungal Treatment

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