Improvement of Drug Delivery Properties of Risperidone via Preparation of Fast Dissolution Tablet Containing Nanostructured Microparticles

Aimed to improve the dissolution profile of risperidone and increase the compliance of psychotic patients, we designed a fast dissolution tablet (FDT) containing nanoparticles. Risperidone nanoparticles were prepared by the acid-alkali neutralization method, and their size and stability were evaluated. Spray freeze-drying (SFD) process was then employed to fabricate the nanoaggregates using sugars. The physicochemical properties of the dried powders were assessed. Finally, nanoaggregates were compressed into tablets, and their properties were evaluated. The results show that the synergic effect of cremophore EL and hydroxypropyl methyl cellulose E(15) can give rise to the formation of risperidone nanosuspension with the particle size of 188 nm. Moreoevr, it is shown that the fabrication of risperidone nanoaggregate enhanced the drug dissolution and decreased that to 2 min, which is faster than coarse risperidone powder (with dissolution time of 60 min). The formulations of FDT containing 9.5% of sodium starch glycolate and 83.2% microcrystalline cellulose were selected with a disintegration time of less than 30 s and a dissolution time of 10 min. This investigation shows that the preparation of FDT containing nanoparticles using SFD is an easy and feasible method for improving the dissolution profile of many drugs with low solubility.