Title : Preparation and characterization of sulfasalazine loaded polymeric nanoparticles by solvent evaporation and salting out techniques
Abstract:
Sulfasalazine is used in the treatment for inflammatory bowel disease, Rheumatoid arthritis and Ankylosing spondylitis. It is chemically 2-hydroxy-5-[(E)-2-{4-[(pyridin-2yl) sulfamoyl]phenyl}diazen-1-yl] benzoic acid. The anti inflammatory activity of Sulfasalazine may rely on inhibition of the transcription factor NFkB. But the poor physico chemical parameters, low aqueous solubility, less oral bioavailability (15%) are responsible for its decreased biological activity. It is available as tablets, film coated and enteric coated tablets.
Nanoparticles have shown significant advancements in delivery of drugs and biomolecules. The primary objective of the study was to develop and characterize sulfasalazine polymeric nanoparticles (SZNPs). SZNPs were prepared by solvent evaporation method and salting out techniques by changing the drug : polymer ratio and stabilizers.
In Solvent evaporation technique, ethyl cellulose (EC) and eudragit S100 (ED) were used as polymers due to its less size and sustained release properties. Tween 20 was used as stabilizer. For each polymer five formulations were prepared by varying the concentration of drug and polymer. The obtained particles were characterised for Particle Size, Zeta potential, Scanning electron microscopy and FTIR. Out of five formulations of Ethylcellulose(EC),F2 formulation was showing promising results with a mean particle diameter of 188. 1nm and zeta potential value of 62. 7mV. Among all formulations of eudragit S100 (ED), F3 formulation was showing lower particle size of 207nm and greater stability with a zeta potential value of -59. 5mV. Comparative study was performed between F2 formulation of EC and F3 formulation of ED to determine the best formulation. Ethyl cellulose was found to be the best polymer for the preparation SZNPs for solvent evaporation technique.
In Salting out technique EC and ED were used as polymers, sodium carboxy methyl cellulose as a colloidal stabilizer and zinc sulfate as a salting out agent. For each polymer five formulations were prepared by varying the concentration of drug and polymer. The obtained particles were characterized for particle size, zeta potential, scanning electron microscopy and FTIR. Out of five formulations of EC, F3 formulation was showing promising results with a mean particle diameter of 211nm and zeta potential value of - 45. 7mV. Among all formulations of ED,F3 formulation was showing lower particle size of 245nm and greater stability with a zeta potential value of -43. 2mV.
Comparative study was performed between F3 formulation of EC and F3 formulation of ED to determine the best formulation. Ethyl cellulose was found to be the best polymer for the preparation SZNPs by salting out technique. Comparative study was performed among the best formulations of solvent evaporation and salting out techniques. The results were found to be best for solvent evaporation technique with lesser particle size, greater stability and controlled drug release properties.
Keywords: Sulfasalazine, Entrapment Efficiency, Loading Capacity, Particle Size
