Authors : Jahan Israt, Sharmin Sadia, Mirza Sabiruddin, Mohammad Shariare

Abstract : Purpose In drug formulation, poor aqueous solubility often acts as a hindrance to improve bioavailability and achieve targeted drug delivery. Therefore, the aim of this study was to develop carrier free nanosuspension by precipitation method using paracetamol as a model drug. Methods Three different batches of paracetamol nanosuspension, Batch1= Paracetamol+(Poloxamer188+TEA), Batch2= Paracetamol +Poloxamer188 and Batch3 = Paracetamol + PEG6000 have been formulated by precipitation method using ethanol as solvent and water as antisolvent containing stabilizer. For dissolution study USP apparatus II (paddle) was used at 25rpm and 0.1N HCl as medium. UV absorbance was obtained at 249nm. A microsuspension using raw paracetamol (particle size 300–600µm) was prepared for dissolution study. Results Microscopic data (Figure1) showed that particle size obtained for Batch1, Batch2 and Batch3 were in nanometer range. These results are also supported by particle size distribution data obtained using Malvern Zetasizer (Figure 2). The average particle size of Batch1, 2 and 3 found by this method are 182±5nm, 174±48nm and 429±23nm respectively. Both characterization methods showed smaller particle size for Batch1 and Batch2 compared to Batch3, which is probably related to the faster addition rates of drug solution into antisolvent for those batches compared to Batch3 (0.2ml/sec., 0.3ml/sec. and 0.13 ml/sec. respectively). This might be related to generation of high supersaturated solution for Batch1 and Batch2 resulting in production of large number of nuclei [1].Until now all nanosuspension batches are physically stable for 2 months at room temperature (~25°c), however particle size distribution data showed bi modal distribution. This is possibly due to aggregation of particles occurring at certain level.Dissolution data after 5 minutes show that the percentage of drug release for raw paracetamol suspension was 50%, while for nanosuspension Batches of 1, 2 and 3 it was 97%, 94% and 92% respectively. This is thought to be related to the average particle size observed for the batches used in dissolution study (Figure 2). Conclusion Experimental results demonstrate enhancement of dissolution rate for paracetamol nanosuspension compared to raw paracetamol suspension. However, further study is required to improve the stability of nanosuspension batches

Journal : Volume : Year : 2014 Issue :
Pages : City : Sandiego, USA Edition : Editors :
Publisher : AAPS annual meeting and exposition , 2014 ISBN : Book : Chapter :
Proceeding Title : American Association of Pharmaceutical scientists (AAPS) annual Meeting and Exposition, USA Institution : Issuer : Number :