Abstract
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.
Highlights
Cinnacalcet HCl is used for the treatment of hypercalcemia and secondary hyperparathyroidism in patients with parathyroid carcinoma and chronic kidney disease respectively [1]
The use of non polar solvent chloroform contributed in quick solubilization of solid lipid i.e. Precirol ATO 05 (PREC) and polar solvent methanol contributed in solubilization of cinacalcet hydrochloride
The value of EE ranges from 61 % to 85.96.The % EE increased with increase in the concentration of PREC which acts as solubiliser for lipophilic drug [9]
Summary
Cinnacalcet HCl is used for the treatment of hypercalcemia and secondary hyperparathyroidism in patients with parathyroid carcinoma and chronic kidney disease respectively [1]. It exhibits poor oral bioavailability of 20 to 25 % owing to its poor aqueous solubility and first pass metabolism. Solid lipid nanoparticles can be considered as a suitable drug delivery system to improve the poor oral bioavailability of BCS class IV drug Cinnacalcet HCl. Solid lipid nanoparticles (SLNs) has the advantage of good loading for both lipophilic and hydrophilic drugs [4-6]. In the present research, preparation and characterization of SLN of Cinnacalcet HCl were attempted to improve oral bioavailability
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