DOI: 10.21276/ajptr
Fri, 18 Jan 2019

In Vivo Evaluation of A Self Nanoemulsifying Drug Delivery System for Lercanidipine HCL

J. Venkateswara Rao*1, T Rama Mohan Reddy2

1.Research Scholar, Mewar University, Chittorgarh, Rajasthan, India.

2.Research Supervisor, Mewar University, Chittorgarh, Rajasthan, India


ABSTRACT

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.

Keywords: Lercanidipine, Hypertension, Labrosol, Bioavailability, Self-nano emulsifying drug delivery system


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