Investigations into the formation and characterization of phospholipid microemulsions. I. Pseudo-ternary phase diagrams of systems containing water-lecithin-alcohol-isopropyl myristate

Aboofazeli, Reza; Lawrence, M. Jayne

doi:10.1016/0378-5173(93)90174-e

Cited by 90 publications

(40 citation statements)

References 21 publications

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“…At predetermined intervals (15,30,45, and 60 minutes), 0.5 mL samples were taken from the internal medium, and 0.5 mL of fresh Tyrode's buffer (37°C) was then added to the sacs. The samples were diluted by methanol followed by centrifugation, and 50 µL of supernatant was then injected into a high-pressure liquid chromatography (HPLC) column to determine the concentration of HSYA.…”

Section: Microemulsion Lipolysis In Vitromentioning

confidence: 99%

“…15 Cremophor RH40 (surfactant) and ethanol (cosurfactant) were mixed in a vial at room temperature followed by the addition of PG (oil phase), and then the mixture was blended for 5 minutes until they had completely mixed. The HSYA solution was then added to the mixture and stirred for 3 minutes until a clear and transparent w/o microemulsion was obtained.…”

Section: Preparation Of Hsya W/o Microemulsionmentioning

confidence: 99%

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Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Zhuang²,

Wu³

et al. 2011

IJN

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Background: A microemulsion is an effective formulation for improving the oral bioavailability of poorly soluble drugs. In this paper, a water-in-oil (w/o) microemulsion was investigated as a system for enhancing the oral bioavailability of Biopharmaceutic Classification System (BCS) III drugs. Methods: The microemulsion formulation was optimized using a pseudoternary phase diagram, comprising propylene glycol dicaprylocaprate (PG), Cremophor ® RH40, and water (30/46/24 w/w). Results: The microemulsion increased the oral bioavailability of hydroxysafflor yellow A which was highly water-soluble but very poorly permeable. The relative bioavailability of hydroxysafflor yellow A microemulsion was about 1937% compared with a control solution in bile duct-nonligated rats. However, the microemulsion showed lower enhanced absorption ability in bile duct-ligated rats, and the relative bioavailability was only 181%. In vitro experiments were further employed to study the mechanism of the enhanced effect of the microemulsion. In vitro lipolysis showed that the microemulsion was digested very quickly by pancreatic lipase. About 60% of the microemulsion was digested within 1 hour. Furthermore, the particle size of the microemulsion after digestion was very small (53.3 nm) and the digested microemulsion had high physical stability. An everted gut sac model demonstrated that cumulative transport of the digested microemulsion was significantly higher than that of the diluted microemulsion. Conclusion: These results suggested that digestion of the microemulsion by pancreatic lipase plays an important role in enhancing oral bioavailability of water-soluble drugs.

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Section: Microemulsion Lipolysis In Vitromentioning

confidence: 99%

Section: Preparation Of Hsya W/o Microemulsionmentioning

confidence: 99%

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Zhuang²,

Wu³

et al. 2011

IJN

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“…This indicates that FVS could play an important role in the studies of many different human cancer cells in the near future. The optimum o/w microemulsion formulation consisted of 3.0% MCT (oil), 21 ). In addition, the pharmacokinetic study in rats revealed an improved oral bioavailability of FVSMs.…”

Section: Resultsmentioning

confidence: 99%

“…21,22 The phase diagram was used to assess the influence of different factors on the formation of the microemulsion and to determine the predominant microemulsion domains. Software Origin 7.0 (OriginLab Corp, Northampton, MA) was used to draw the ternary phase diagrams.…”

Section: Optimized Preparation Of Fvsms Phase Diagram Preparationmentioning

confidence: 99%

Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Yi¹,

Zhong²,

Tong³

et al. 2012

IJN

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Purpose:To investigate the growth inhibition activity of Flammulina velutipes sterol (FVS) against certain human cancer cell lines (gastric SGC and colon LoVo) and to evaluate the optimum microemulsion prescription, as well as the pharmacokinetics of encapsulated FVS. Methods: Molecules present in the FVS isolate were identified by gas chromatography/mass spectrometry analysis. The cell viability of FVS was assessed with methyl thiazolyl tetrazolium (MTT) bioassay. Based on the solubility study, phase diagram and stability tests, the optimum prescription of F. velutipes sterol microemulsions (FVSMs) were determined, followed by FVSMs characterization, and its in vivo pharmacokinetic study in rats. ). The optimal FVSMs prescription consisted of 3.0% medium chain triglycerides, 5.0% ethanol, 21.0% Cremophor EL and 71.0% water (w/w) with associated solubility of FVS being 0.680 mg ⋅ mL −1 as compared to free FVS (0.67 µg ⋅ mL −1 ). The relative oral bioavailability (area-under-the-curve values of ergosterol and 22,23-dihydroergosterol showed a 2.56-fold and 4.50-fold increase, respectively) of FVSMs (mean diameter ∼ 22.9 nm) as against free FVS were greatly enhanced. Our laboratory has been able to screen out lipid soluble sterols with an antitumor effect from F. velutipes by lipidraft chromatography, which was found to be linked to the tyrosine kinase receptor (data not published). In this study, our laboratory was interested in performing a preliminary investigation of the anticancer potential and bioavailability of F. velutipes sterol (FVS) as an in-depth contribution to the research of F. velutipes. FVS is a white powder, which can easily dissolve in ether, chloroform, hot ethanol, and other organic solvents, but barely dissolves in water. As a result, it is necessary to find a method to improve the solubility and oral bioavailability of this sterol. Dovepress 5067 O R I G I N A L R E S E A R C HMicroemulsions are thermodynamically stable nanometer systems with characteristics of easy preparation, small droplet size, low viscosity, and strong solubilization effect. 12It is formed spontaneously by water, oil, surfactant and cosurfactant. 13,14 According to the structure of a microemulsion, it can be divided into water-in-oil (w/o), oil-in-water (o/w) and bicontinuous microemulsion. 15 As a drug carrier, a microemulsion can increase the solubility and oral bioavailability of poorly soluble drugs, ameliorate the localization, improve systemic delivery of the drug, and possess the ability of targeting drug release. [16][17][18] The absolute bioavailability of a poorly soluble drug cyclosporin A which was loaded into a microemulsion system was increased to about 3.3-and 1.25-fold compared with free Sandimmun and Sandimmun Neoral (Novartis, Basel, Switzerland), which were used as commercial cyclosporin A. 19 In addition, it has been confirmed that the microemulsion system containing the poorly soluble drug docetaxel could improve the solubilization property and oral bioavailability of the drug. 20 Presently, there a...

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“…Today, it is known that microemulsions have four components; water, oil and a surfactant; in combination with a cosurfactant, typically a short or medium chain alcohol (18,19,22,24).…”

Section: Introductionmentioning

confidence: 99%

Microemulsions : Mi̇kroemülsi̇yonlar

ÇOMOĞLU¹,

GÖNÜL²

1997

Ankara Universitesi Eczacilik Fakultesi Dergisi

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Investigations into the formation and characterization of phospholipid microemulsions. I. Pseudo-ternary phase diagrams of systems containing water-lecithin-alcohol-isopropyl myristate

Cited by 90 publications

References 21 publications

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Enhanced effect and mechanism of water-in-oil microemulsion as an oral delivery system of hydroxysafflor yellow A

Enhanced oral bioavailability of a sterol-loaded microemulsion formulation of Flammulina velutipes, a potential antitumor drug

Microemulsions : Mi̇kroemülsi̇yonlar

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