Lamotrigine Ultrafine Particles Preparation by Antisolvent Precipitation Technique with Salting Out Effect

Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This strategy results in increased surface area, the potential to increase saturation solubility, and decreased diffusional distance, all of which lead to an increase in the extent and the rate of dissolution. The purpose of this research was to develop antisolvent precipitation system for the preparation of stable aqueous suspension from ultrafine particles of lamotrigine as a poorly water soluble drug. Use of high stream velocities enhances mixing of lamotrigine acetic acid solution with water, that water was containing of polymer or surfactant inhibitor, was prepared a solution with lamotrigine particles with size <250 nm. Several experimental parameters, such as the type of stabilizer, the concentration of stabilizer, the concentration of salt (NaCl) and the concentration of drug that affected on size of the particles were optimized by undertaking Taguchi experimental design methodology. Using different analytical tools, such as X-ray diffraction (XRD), dynamic light scattering (DLS) and differential scanning calorimetry (DSC), the effect of different parameters on the size of the produced particles was investigated. The results showed that the best stabilizer is PEG (poly ethylene glocal) 4 mg ml-1, concentration of lamotrigine 10 mg ml-1 and NaCl concentration: 2 mol L-1, that the produced submicrometer suspension had a mean particle size of 248.5 nm and size distribution 243.9 – 252.2 nm.