Aceclofenac is a new generational Non-Steroidal Anti-Inflammatory Drug (NSAID), and is considered a better alternative to the popular painkiller diclofenac, as it overcomes some of the adverse gastrointestinal and cardiac side effects associated with the latter. However, the bioavailability of the drug remains limited due to low aqueous solubility (0.058 µg/mL) and poor dissolution characteristics. Hence, improving its dissolution characteristics is of prime significance in order to establish its optimal therapeutic efficacy. In an effort to tackle this issue, we report the use of novel Soluplus ®-based nanocomposites, prepared from emulsion templates, as effective drug loading agent for aceclofenac. Nanoemulsion templates were prepared by high-shear homogenization using a probe sonicator. The emulsions were subsequently lyophilized to obtain free flowing powders. The amorphization of the drug with increasing polymer content was clearly observed from powder X-ray diffractogram, while the drug-polymer interaction was explored by FTIR spectroscopy. The phase purity and homogeneity of the formulation was characterized using Differential Scanning Calorimetry. The dissolution profiles of the formulations were established by an USP paddle apparatus. Phase solubility study was conducted to evaluate the effect of polymer concentration on aqueous solubility of aceclofenac. The values of Gibbs-free energy (ΔG˚tr) associated with the aqueous solubility of aceclofenac in the presence of Soluplus was used to optimize the polymer content. The in vitro dissolution rates of aceclofenac from the nanoparticles were significantly higher compared to the pure drug. Thus, Soluplus nanoparticles provide promising formulations for the improvement of the dissolution profiles and thus, the bioavailability, of aceclofenac.
In the present study, we have prepared nanosuspensions of piroxicam using Soluplus® as the matrix using aqueous-based conventional ball milling. The comparative physico-chemical characteristics were assessed using PXRD (powder X-ray diffraction), DSC (differential scanning calorimetry), FESEM (field emission scanning electron microscopy) and FTIR (Fourier transform infrared spectroscopy) analysis, indicating the nanoformulations displayed lower crystallinity with no chemical interactions between the drug and polymer molecules. The cytotoxicity of the formulations was established from MTT assay performed on Caco-2 cell lines. The release rate of piroxicam from various ratios of drug/polymer nanoparticles was investigated using a USP paddle apparatus. The nanoformulations exhibited higher release of the drug in comparison with the pure drug. The enhanced dissolution characteristics of the drug in the nanoformulations could possibly increase the anti-inflammatory effects of the drug owing to superior bioavailability characteristics.
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