Preparation and Characterization of Solid Lipid Nanoparticles of Cinnacalcet HCl

Objective: The objective of the present research is to formulate solid lipid nanoparticles of cinnacalcet HCl to improve its oral bioavailability.

Methods: Cinnacalcet hydrochloride exhibits poor oral bioavailability of 20 to 25 % because of low aqueous solubility and first pass metabolism. The formulations were optimised using Box-Behnken Design. Solid lipid nanoparticles formulation was prepared using hot homogenization and ultra sonication method.

Results and Discussion: Precirol ATO 05, Soya lecithin and poloxamer 407 were selected as lipid, surfactant and co-surfactant respectively. For optimistaion the desirable goal was fixed for various responses entrapment efficiency, particle size and (time taken for diffusion of 85% drug) T85%. The optimized single dose of solid lipid nanoparticle obtained using box behnken design consisting of 30 mg of cinnacalcet HCl, 200 mg of precirol ATO 05, 250 mg of soya lecithin and 0.2% w/v of poloxamer. 407. The pharmacokinetic study revealed that optimized formulation was found to increase the oral bioavailability nearly 3 times compared to aqueous suspension of pure drug.

Conclusion: Thus optimized solid lipid nanoparticle explicated the potential of lipid-based nanoparticles as a potential carrier in improving the oral delivery.