Development and evaluation of decorated aceclofenac nanocrystals

• 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 24 h. Cell viability was evaluated for 24 h 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 725 nm 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 1 h followed by slow release for up to 4 h. Decorated ACF-NC exhibited viability approximately 63.9% of HCT-116 cells and also showed viability in 58.3% of MCF-7 cells at 15 μg/mL of drug concentration. In conclusion, decorated ACF-NC proved to be a promising approach for enhancing drug solubility and cytotoxicity.

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