European Journal of Biomedical and Pharmaceutical Sciences

FORMULATION DEVELOPMENT FOR SOLUBILITY ENHANCEMENT AND IN VITRO EVALUATION OF TERIFLUNOMIDE NANOSUSPENSIONS

P. Mounika*, T. Malyadri, P. Sreenivasa Prasanna and K. Thejomoorthy

ABSTRACT

Teriflunomide is used to treat multiple sclerosis-MS. It is not a cure for MS but is thought to work by decreasing certain immune system cells (lymphocytes) which can attack the nerves in your brain and spinal cord. This helps decrease the number of flare-ups (relapses) and may help slow down physical problems caused by MS. Teriflunomide is a BCS class II drug having low solubility and high permeability, so to increase its solubility Teriflunomide is formulated as a Nanosuspension. Nanosuspension is a novel technique used to increase the solubility of the drug prepared by Solvent evaporation method. The present trend of pharmaceutical research lies in the usage of biodegradable polymer because of its availability and low toxicity. Nanosuspension containing drug was prepared by solvent evaporation method by using SLS, Polaxomer, PVP K30, PVA and acetone as organic solvent. The Nanosuspension were evaluated for parameters such as Entrapment efficiency, scanning electron microscopy, particle size analysis, zeta potential, in-vitro release, drug excipient interactions (FTIR). The entrapment efficacy of the formulated Nanosuspension was found to be in the range of 79.52%- 92.16% respectively. Zeta potential value for the optimized formulation (F3) was found to be within the acceptable limits. Average particle size of nanosuspension of optimized formulations (F3) was found to be 489.7nm. From the invitro studies we can say that formulation F3 shows best drug release of 99 % within 45 minutes where as all the other formulations takes about 60-180 minutes to release the drug. Based on the regression values it was concluded that the optimized formulation F3 follows Zero order kinetics.

Keywords: Teriflunomide, Nanosuspension, SLS, Polaxomer, PVP K30, PVA.