Formulation of Polymeric Nanoparticles of Lercanidipine by Two Bottom Down Techniques Optimized by Design of Experiment

Abstract

Lercanidipine has found to be effective in lowering blood pressure among the potent calcium channel blockers, through its action on L- type calcium channels. However, the major disadvantage associated with Lercanidipine is, it is a BCS class II drug having low solubility bioavailability is around 10% through oral route due of extensive first pass metabolism. The present study is aimed to prepare and evaluate polymeric nanoparticles of Lercanidipine using a combination of two bottom down techniques, High speed homogenizer and Probe sonication. Preformulation studies like, DSC, FTIR using surfactants such as Tween 80, Sodium Lauryl sulphate, Polyvinyl Alcohol, singely and in combination were used. A full factorial method was utilized to study the effect of various factors such as surfactant concentration, homogenization speed, sonication amplitude and sonication time on Lercanidipine nanoparticles in two levels. Optimized nanoparticles (with PVA as surfactant) showed an average particle size of 141 nm, PDI 0.248 and zeta potential +6.46. Formulation was further optimized using Design Expert 10 software. Optimized formulation was found to be stable during 3 months stability studies as per ICH guidelines.