Lercanidipine

The present study aimed at improvement of solubility and bioavailability of Lercanidipine HCl using self-nanoemulsifying drug delivery systems (SNEDDS). The extent of self-emulsification was checked with various oils with suitable surfactants and co-surfactants. The final optimized formulation contained Caproyl 90, Tween 80 and Labrosol as oil, surfactant and co-surfactant respectively. Based on Lercanidipine solubility analysis, ternary phase diagrams were constructed for optimizing the system. The formulations were evaluated for solubility, droplet size determination, zeta potential and stability studies. The droplet size was found to be 5.1 nm & Z-Average of 14.6 nm. The zeta potential of the optimized formulation (F16) was found to be -19.7 mV. In vitro drug release from SNEDDS was significantly higher than pure drug. From in vivo bioavailability studies the optimized formulation was exhibited a significantly greater Cmax (56.2±0.04ng/ml) than the pure drug suspension (35.1±0.03ng/ml). AUC0-∞ for SNEDDS formulation was higher (190.5±2.04 ng.h/ml) than the pure drug suspension 145.7±2.02ng.h/ml. Statistically, AUC0-t of the SNEDDS formulation was significantly higher (p<0.05) as compared to pure drug suspension formulation. The study demonstrated that SNEDDS was a promising strategy to enhance the solubility and oral bioavailability of Lercanidipine.

A rapid and sensitive High Performance liquid chromatography (HPLC) method has been developed and validated. The analyte was extracted from human plasma by simple precipitation technique. Nifedipine was used as the internal standard. A Princeton C18 column provided chromatographic separation of the analyte. A simple, selective, rapid, precise and economical reverse phase High Pressure Liquid Chromatographic method has been developed for the estimation of Lercanidipine in human Plasma. The method was carried out on a Princeton C18 (250 mm x 4.6 mm i.d., 5µ) column with a mobile phase consisting of acetonitrile: Water (adjusted to pH 3.5 using orthophosphoric acid) (55:45 v/v) at a flow rate of 1.0 ml/min. Detection was carried out at 235 nm. The retention time of Lercanidipine Nifedipine, was 5.31, 10.00 min, respectively. The proposed method has been validated with linear range of 5.0-250.0 ng/ml for Lercanidipine. The precision and accuracy values are within 10%. The overall recovery of Lercanidipine was 96.4 %. The developed and validated method was applicable for the pharmacokinetics studies.