Abstract
Objective: This study aimed to enhance the oral solubility and dissolution of poorly soluble lornoxicam by anti-solvent precipitation, and the manufacture of oral tablets by the phase transition method. 
 Methods: The solvent was mixture of polyethylene glycol 400 and absolute ethanol. Three stabilizers Inutec SP1, Pluronic F127, Sucrose ester S1670 at two concentrations and two matrix formers Mannitol, and Avicel PH102 were used to obtain 12 formulae. The formulae were characterized regarding their infrared spectroscopy (IR), differential scanning calorimetry (DSC), particle size (PS) measurement, drug content and dissolution. Further characterizations were done for the optimum formula by scanning electron microscopy (SEM) and X-ray diffraction (XRD). Four tablet formulae were manufactured by phase transition method. The optimum tablets (T3) were evaluated through hardness, drug content, disintegration, dissolution, IR, and stability studies. Finally, (T3) was compared to conventional tablets in New Zealand rabbits using crossover design.
 Results: The dissolution rate for the prepared formulae was enhanced, from 3.44 to 5.96 folds. Statistical significance was obtained using one and two way ANOVA among formulae. The optimum tablet formula (T3) had hardness 5.637±1.57 kg, drug content 90.424±1.19%, disintegration time 341.5±9.62 s and the drug dissolved 72.107±0.0025%. Stability, after one month storage of the selected tablets at (25 °c/60% relative humidity), was satisfactory. The absorption extent of lornoxicam from (T3) compared to the conventional tablets was higher.
 Conclusion: Taken together, the obtained results confirmed successfully the potential of the promising formula (T3), over the conventional tablets of lornoxicam.
Highlights
Significant attention focused on nanomaterial based drug delivery has been propelled to the forefront by researchers
The aim of the work is to speed up the dissolution of lornoxicam in the gastric pH 1.2 by its formulation as nanoparticles utilizing anti-solvent precipitation technique, with the aid of different stabilizers, Inutec SP1, Pluronic F127 or Sucrose ester S1670 at different concentrations followed by lyophilization of the processed nanoparticles using either Mannitol or Avicel pH 102 as matrix formers
After several trials and errors, the parameters of the method were, three stabilizers Inutec SP1, Pluronic F127, Sucrose ester S1670, each in two different ratios above and below their critical micelle concentrations of 0.009% w/v, 0.1% w/v, and 0.0014% w/v respectively [11,12,13], the temperature of anti-solvent below 3 °C, the stirring rate was 1500, the ratio between the solvent and antisolvent was 1:5, the composition of the different formulae has complied in table 1
Summary
Significant attention focused on nanomaterial based drug delivery has been propelled to the forefront by researchers. Lornoxicam is slightly acidic with a pKa (acid dissociation constant) of 4.7 and has limited dissolution in an acidic environment [4] It is slightly lipophilic with an apparent partition coefficient of 1.8 (n-octanol/buffer pH 7.4) [5]. It exhibits low solubility and high permeability (class II) [6]. The tablet hardness was increased by the crystal change from an amorphous to a crystal state by the conditioning process This method provides sufficient hardness and low disintegration time for tablets. Stability study was evaluated for a month, and in vivo study was performed in rabbits to estimate the pharmacokinetic parameters for the optimized tablet formulation (T3) and to calculate the relative bioavailability in comparison to oral conventional tablets which was 2.04 folds higher
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