Microemulsions: A Potential Drug Delivery System

Ghosh, Pradip; Murthy, R. S. R.

doi:10.2174/156720106776359168

Cited by 176 publications

(94 citation statements)

References 93 publications

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“…However, it may cause no significant difference between solution and nanoemulsion in the in vitro anti-tumor activity because of the continuous contact of cells with drug that dissolved in either solution or nanoemulsion. Meanwhile, it was reported that an enhanced membrane permeability or increased efficacy of drug could be achieved by the utilization of nanoemulsion owing to its decreased particle size, or interference of components in nanoemulsion with cell membrane (29,30). Therefore, it may be employed in the nuclear gene delivery systems to achieve nuclear transport of drug (31), which was further demonstrated by the fact that Nile red incorporated in the nanoemulsion could be transported into cell nucleus as showed in the present study.…”

Section: Discussionsupporting

confidence: 63%

A Novel Camptothecin Derivative Incorporated in Nano-Carrier Induced Distinguished Improvement in Solubility, Stability and Anti-tumor Activity Both In Vitro and In Vivo

Han

Fang

et al. 2008

Pharm Res

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Purpose. An oil/water nanoemulsion was developed in the present study to enhance the solubility, stability and anti-tumor activity of a novel 10-methoxy-9-nitrocamptothecin (MONCPT). Materials and Methods. MONCPT nanoemulsion was prepared using Lipoid E80 and cremophor EL as main emulsifiers by microfluidization. The droplet size of the nanoemulsion was measured by dynamic light scattering. In vitro drug release was monitored by membrane dialysis. Kinetics of MONCPT transformed into carboxylic salt was performed in phosphate buffer at different pH. Hemolysis of MONCPT nanoemulsion was conducted in rabbit erythrocytes. Solubilization character of MONCPT in nanoemulsion was experimented using Nile red as a solvatochromic probe. In vitro cytotoxicity of the nanoemulsion was measured in A549 and S180 cells using Sulforhodamine B protein stain method, and suppression rate of tumor growth was investigated in S180-bearing mice. The cell cycle effects of MONCPT nanoemulsion on S180 cells were analyzed by flow cytometry. Distribution of the nanoemulsion in A549 cells and S180-bearing mice were also investigated by fluorescence image. Results. MONCPT is incorporated in the nanoemulsion in form of lactone with concentration of 489 µg/ml, more than 200 folds higher than that in water. Experiments using Nile red as a solvatochromic probe indicated that more MONCPT might be located in the interfacial surfactant layer of the nanoemulsion than that in discrete oil droplet or continuous aqueous phase. Nanoemulsion could release MONCPT in a sustained way, and it was further shown to notably postpone the hydrolysis of MONCPT with longer hydrolysis half-life time (11.38 h) in nanoemulsion at pH 7.4 than that of MONCPT solution (4.03 h). No obvious hemolysis was caused by MOCPT nanoemulsion in rabbit erythrocytes. MONCPT nanoemulsion showed a marked increase in cytotoxic activity, 23.6 folds and 28.6 folds in S180 cells and A549 cells respectively via arresting the cell at G2 phase, compared to that induced by MONCPT injection. It correlated well to the in vivo anti-tumor activity of MONCPT nanoemulsion with suppression rate of 93.6%, while that of MONCPT injection was only 24.2% at the same dosage. Moreover, nanoemulsion exhibited enhanced capability of delivering drug into malignant cell's nucleus in vitro and induced drug accumulation in tumor in S180-bearing mice using in vivo imaging. Conclusion. The nanoemulsion prepared exhibited an improved MONCPT solubility, stability and antitumor activity, providing a promising carrier for cancer chemotherapy using MONCPT.

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Section: Discussionsupporting

confidence: 63%

A Novel Camptothecin Derivative Incorporated in Nano-Carrier Induced Distinguished Improvement in Solubility, Stability and Anti-tumor Activity Both In Vitro and In Vivo

Han

Fang

et al. 2008

Pharm Res

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“…[29][30][31] The presence of cosurfactants provides the interfacial film sufficient flexibility to assume the different curvatures required to form MEs over a wide range of compositions. [32][33][34] In our preliminary test, the best solubilization and microemulsifying effect and resistance to infinite dilution were found for the MCT/BJO/S75/HS 15/PEG 400 combination, the ratio of which was confirmed by aqueous phase titration.…”

Section: Me Formulationmentioning

confidence: 55%

Intravenous microemulsion of docetaxel containing an anti-tumor synergistic ingredient (Brucea javanica oil): formulation and pharmacokinetics

Shi-lin¹,

Chen²,

Ye³

et al. 2013

IJN

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“…One of the main reasons for the enhanced drug oral bioavailability by SEDDS is the excellent efficiency of SEDDS in improving the drug solubility and in increasing the dissolution rate. 25,26) Following self-emulsification in the GI tract after oral administration, SEDDS provides ultra low interfacial tensions and large o/w interfacial areas, resulting in the incorporation of poorly water-soluble pharmaceuticals inside the fine oil droplets. The large specific surface area of the fine oil droplets also enables a more efficient drug transport through the intestinal aqueous boundary layer, leading to an improvement in oral bioavailability.…”

Section: Resultsmentioning

confidence: 99%

Enhanced Oral Bioavailability of Curcumin via a Solid Lipid-Based Self-Emulsifying Drug Delivery System Using a Spray-Drying Technique

Yan

Kim

Kwak

et al. 2011

Biological & Pharmaceutical Bulletin

102

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In this study, a novel liquid self-emulsifying drug delivery system (SEDDS) containing curcumin was formulated and further developed into a solid form by a spray drying method using Aerosil 200 as the solid carrier. The optimum liquid SEDDS consisted of Lauroglycol Fcc, Labrasol and Transcutol HP as the oil phase, the surfactant and the co-surfactant at a weight ratio of 15.0 : 70.8 : 14.2 (w/w/w), respectively. There was no difference in droplet size between the emulsions obtained from the liquid and solid forms of SEDDS. Solid state characterization of the solid SEDDS was performed by scanning electron micrograph (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD). The drug formulated in the solid SEDDS was quickly and completely dissolved within 5 min, both in 0.1 N HCl and phosphate buffer pH 6.8 dissolution media, whereas crude curcumin powder was significantly less dissoluble. The solid SEDDS formulation was stable for at least 3 months at 40°C with 75% relative humidity. After oral administration to rats, curcumin in the solid SEDDS resulted in significant improvement in in vivo absorption compared with that of curcumin powder. As the dose of curcumin formulated in solid SEDDS increased from 25 to 100 mg/kg, the C max and area under the drug concentration time curve (AUC) of curcumin were increased by 4.6 and 7.6 times, respectively. However, the over-proportional increase in the AUC in the higher dose group might be due to underestimation of AUC in the lower dose group. In conclusion, this solid SEDDS is a promising solid dosage form for poorly water-soluble curcumin.

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Microemulsions: A Potential Drug Delivery System

Cited by 176 publications

References 93 publications

A Novel Camptothecin Derivative Incorporated in Nano-Carrier Induced Distinguished Improvement in Solubility, Stability and Anti-tumor Activity Both In Vitro and In Vivo

A Novel Camptothecin Derivative Incorporated in Nano-Carrier Induced Distinguished Improvement in Solubility, Stability and Anti-tumor Activity Both In Vitro and In Vivo

Intravenous microemulsion of docetaxel containing an anti-tumor synergistic ingredient (Brucea javanica oil): formulation and pharmacokinetics

Enhanced Oral Bioavailability of Curcumin via a Solid Lipid-Based Self-Emulsifying Drug Delivery System Using a Spray-Drying Technique

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