Formulation, development, and characterisation of cilnidipine loaded solid lipid nanoparticles

Abstract

Objective: The aim of the present investigation is to develop solid lipid nanoparticles (SLNs) of cilnidipine using hot homogenization followed by ultrasonication technique and to improve the dissolution characteristics of the drug. Methods: The cilnidipine-loaded SLNs were formulated using stearic acid (SA), glyceryl monostearate (GMS), and palmitic acid (PA) as lipid matrix and tween-20, tween-80, and tween-40 as an emulsifier by hot homogenization and ultrasonication method. The physicochemical characteristics of SLN were analyzed for Fourier transform infrared studies, entrapment efficiency (EE), zeta potential, in vitro drug release, particle size analysis, scanning electron microscopy, and stability. Results: The SLNs with PA showed a sustained release of drug 82%–88%, respectively, after 10 h. The SLNs of PA using tween-80 as emulsifier resulted with high EE% than SLNs of SA and GMS. The compatibility studies are done by Fourier transformed infrared for formulations which contain PA as lipid matrix and tween-80 as an emulsifier, and it showed no drug excipient incompatibility. The formulation containing PA and tween-80 shown particles of average size 152 nm having polydispersity index of. 217 with 68.7 % EE were produced. The zeta potential of the formulation was found to be – 27 mV and the order of percentage drug release was from PA>GMS>SA, and steric stabilizers retard the drug release more than ionic stabilizers. Conclusion: SLN formulations showed the best results in EE as well as in in vitro drug release and therefore confirmed that the novel drug delivery system provides an improved strategy for the treatment of hypertension.