Design and Development of Valsartan-Loaded Solid Lipid Nanoparticles for the Enhanced Protection from Diabetic Neuropathy

Abstract

Valsartan has shown to be effective against diabetic neuropathy. In this study we designed, developed and characterized valsartan loaded solid lipid nanoparticles to enhance the protection against diabetic neuropathy. Nerve function parameters and behavioural studies were performed in male mice. Valsartan-loaded solid lipid nanoparticles (VSLNs) were formulated using palmitic acid as lipid and poloxamer188 as surfactant by solvent diffusion method. VSLNs were characterized for particle size and zeta potential analysis, morphology, drug entrapment efficiency and drug loading. In vitro drug release studies were performed in phosphate buffer of pH 7.4 by using dialysis bag method. In vivo studies such as motor nerve conduction velocity, thermal nociception and mechanical nociception studies were performed with both VSLNs and pure drug. The optimized batch was the one with 1:2 ratio of drug and lipid, and 1% surfactant was found to have the particle size of 457 nm, zeta potential of –16 mV, entrapment efficiency of 78.9±0.05%, drug loading of 26.22±0.05% and in vitro drug release of 84.84±0.07% over a period of 24 h. Based on these results, we concluded that VSLNs showed better protection from diabetic neuropathy.

Keywords

• valsartan
• palmitic acid
• poloxamer188
• solvent diffusion method
• diabetic neuropathy