A Nanoemulsion Formulation of Tamoxifen Increases Its Efficacy in a Breast Cancer Cell Line

Tagne, Jean-Bosco; Kakumanu, Srikanth; Ortiz, Daniela; Shea, Thomas M.; Nicolosi, Robert J.

doi:10.1021/mp700091j

Cited by 88 publications

(57 citation statements)

References 46 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: 62%

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: 62%

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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“…It is important to note, that at higher doses, both the NFP and PSD showed similar cytotoxic effects on both cell lines. These results are similar to previous work by our laboratory (25,26) with the chemotherapeutic drugs dacarbazine and tamoxifen, which also showed greater efficacy when utilized as a nanoemulsion formulation as compared to their suspension formulations in both a MCF-7 cancer cell line and a xenograft mouse model of melanoma.…”

Section: Discussionsupporting

confidence: 90%

“…Nanoemulsions are a class of stable emulsions formed by monolayers of phospholipids composed of a surfactant and oil suspended in water. The nanoemulsions are often referred to as "Approaching Thermodynamic Stability" [25,26]. Compared to typical suspension preparations which can be thousands of nanometers in size, nanoemulsion delivery systems utilized and reported from our lab, as well as those of others, with particle sizes approximately 100 nm or less have been shown to increase bioavailability and efficacy in vivo of delta and gamma tocopherol, aspirin, an antioxidant synergy formulation (ASF), and dacarbazine [22, 24, 26,].…”

Section: Introductionmentioning

confidence: 99%

In Vitro Efficacy Studies for Evaluating the Activity of a Self-assembled Nanoemulsion Formulation of Paclitaxel on Breast and Ovarian Cancer Cells

Bagul¹,

Kakumanu²,

Wilson

2014

Nano BioMed ENG

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The drug of choice for treating breast and ovarian cancers is usually paclitaxel. This study was designed to evaluate the efficacy of a self-assembled nanoemulsion (SANE) of paclitaxel (NFP) on human breast (MCF-7) and ovarian (OVCAR-3) cancer cell lines. Cells were treated with various doses (1.2 nM-1200 nM of paclitaxel) as the NFP or suspended in DMSO (PSD). While both significantly inhibited cell proliferation of MCF-7 at doses >40 nM, at 12 nM the NFP significantly inhibited cell proliferation (-57%; p < 0.05) greater than the PSD (-5%). With OVCAR-3 cells, doses >12 nM for both significantly inhibited cell proliferation, but at 4 nM, the NFP significantly inhibited cell proliferation (-60%; p < 0.05) greater than the PSD (-23%). These results demonstrate that the effect of NFP on the cell proliferation of MCF-7 and OVCAR-3 cells are significantly greater at a lower dose than the PSD and that the NFP exhibited similar mode of action by induction of apoptosis and cell cycle arrest as the PSD. Therefore a SANE formulation of Paclitaxel has the potential to be a promising delivery system for anti-cancer drugs.

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“…This may be explained by, the increased number of dextran particles in our nanocarrier, increasing attachment with the CHO cell membrane more effectively, and at reduced volume of medium. The increased attachment of the cells to the dextran polymer is also likely enhanced because of the dramatic reduction in the zeta potential as a result of the formation of nanoemulsion, as we have reported previously (23,24) From these studies, we conclude that dextran based nanocarriers produced by the SANE method, can improve media utilization. Accordingly, as nanocarriers enhance medium volume requirements for maximum cell growth, these formulation techniques can be used by the biopharmaceutical application for optimizing the cell growth with reduced volume of media.…”

Section: Figuresupporting

confidence: 71%

Dextran-based Nanocarriers as Efficient Media Delivery Vehicles to Cell Production Bioreactors

Anton¹,

Kambalapally²,

Thomas³

et al. 2010

Nano BioMed ENG

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Decreasing the volume of media required to maintain cell viability not only reduces contamination of bioreactors from the upstream process, but may contribute to cost-containment measures in the biopharmaceutical industry. Based on our recent finding that dextran-containing nanocarriers increased CHO cell density up to 20 fold compared to its cellulose-containing microcarrier counterpart (manuscript submitted), we then investigated the possibility of reducing media volume to maintain cell viability, by utilizing the same dextran-based nanocarrier prepared from a self assembling nanoemulsion (SANE) method, and an adherent Chinese hamster ovary (CHO) cell culture line to evaluate media volume requirements. At the same 60 mL volume of media, cell viability after day 3 was 6 fold greater in CHO cells exposed to dextran-containing nanocarriers compared to cellulose-based microcarriers. When CHO cells were exposed to 60 mL of media containing dextran-based nanocarriers compared to 100 mL of media for cellulose-microcarriers, at day 6, cell density was up to 7 fold greater. Similarly, cell lysate protein concentrations at day 6 was nearly 3 fold greater for CHO cells exposed to dextran-containing nanocarriers compared to the cellulose-based microcarriers. Furthermore, nanocarriers had 59% greater glucose concentration, used as a measure of the polymer dextran and cellulose content levels in the nanocarriers and microcarriers, respectively. In conclusion, nanocarriers with increased numbers of dextran molecules, developed in these studies may be useful to further optimize media volume requirements for maximum culture growth.

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A Nanoemulsion Formulation of Tamoxifen Increases Its Efficacy in a Breast Cancer Cell Line

Cited by 88 publications

References 46 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

In Vitro Efficacy Studies for Evaluating the Activity of a Self-assembled Nanoemulsion Formulation of Paclitaxel on Breast and Ovarian Cancer Cells

Dextran-based Nanocarriers as Efficient Media Delivery Vehicles to Cell Production Bioreactors

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