Development and evaluation of decorated aceclofenac nanocrystals

[Display omitted] •Optimizing simple preparation method for aceclofenac nanocrystals.•Enhancing solubility with stabilizer and particle size reduction.•Enhancing cytotocitiy to human cancer lines (HCT-116 and MCF-7 cells). This study was aimed at achieving enhanced solubility of aceclofenac (ACF) in...

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Veröffentlicht in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2016-07, Vol.143, p.206-212
Hauptverfasser: Park, Jeong-Joo, Meghani, Nilesh, Choi, ​Jin-Seok, Lee, Beom-Jin
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Sprache:eng
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Zusammenfassung:[Display omitted] •Optimizing simple preparation method for aceclofenac nanocrystals.•Enhancing solubility with stabilizer and particle size reduction.•Enhancing cytotocitiy to human cancer lines (HCT-116 and MCF-7 cells). This study was aimed at achieving enhanced solubility of aceclofenac (ACF) in nanocrystaline forms (ACF-NC) and evaluating the effects of ACF-NC on cell viability. Decorated ACF-NC were prepared by nano-precipitation with stabilizers. Three kinds of stabilizers were investigated: Tween 80, Poloxamer 407, and PEG 6000. The crystal structure and morphology of ACF-NC were characterized by field emission scanning electron microscopy (FE-SEM) and differential scanning calorimetry (DSC). The solubility of ACF-NC and ACF (pure) was evaluated in different media (pH 1.2 and pH 6.8 buffers and distilled water [DW]). A drug release study was performed in PBS for 24h. Cell viability was evaluated for 24h using a human colon cancer cell-line (HCT-116) and a human breast cancer cell-line (MCF-7). Decorated ACF-NC with a mean size of 725nm were successfully prepared. The solubility of the decorated ACF-NC were 4–7 times higher than that of ACF in DW and pH 6.8 buffer. A peak shift from 153.1°C to 150.5–151.0°C was observed in the DSC thermogram of decorated ACF-NC versus ACF. In terms of drug release, there was an initial burst in decorated ACF-NC within 1h followed by slow release for up to 4h. Decorated ACF-NC exhibited viability approximately 63.9% of HCT-116 cells and also showed viability in 58.3% of MCF-7 cells at 15μg/mL of drug concentration. In conclusion, decorated ACF-NC proved to be a promising approach for enhancing drug solubility and cytotoxicity.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2016.03.022