Title:Nanostructured Lipid Carrier of Cinacalcet HCl: Formulation, BBD Enabled Optimization, Pharmacokinetic and In-Vitro Cytotoxicity Study
Volume: 13
Issue: 3
Author(s): Sabita Nayak*, Jammula Sruti, Chinam Niranjan Patra, Goutam Kumar Jena, Kanhu Charan Panigrahi and Nandika Khirod Kumar
Affiliation:
- Department of Pharmaceutics, Roland Institute of Pharmaceutical Sciences, Berhampur, Odisha, Affiliated to Biju Patnaik University of Technology, Rourkela, India
Keywords:
GMS, Labraaol, tween 20, solubility, stability, bioavailability.
Abstract:
Background: Cinacalcet hydrochloride (CINH) is a BCS class IV drug. It is mainly used
for the treatment of chronic renal disease and parathyroid cancer. It exhibits poor oral bioavailability
of less than 25%.
Objectives: The main objective is to improve the bioavailability of CINH by formulating the
nanostructure lipid carrier (NLC).
Methods: In this research, glyceryl monostearate (GMS), labrasol, and tween 20 were the main excipients
selected for the formulation of NLC. Hot high-speed homogenization and ultra-sonication
method was used for the NLC formulation of CINH. The characterization of the NLCs was done as
per standard procedures. Optimization of the formulated NLC was carried out by applying Box-
Behnken Design (BBD) with the help of the Design Expert software. The pharmacokinetic study
was conducted to determine the improvement in the bioavailability of the CINH. The cytotoxicity
study was performed by using the MTT assay method to know the cell viability.
Results: The optimized NLC formulation exhibited high drug content with a particle size of less
than 200nm. A pharmacokinetic study showed 4 fold increase in oral bioavailability for the optimized
NLC in comparison to the aqueous suspension of CINH. Minimum viability was determined
as 94%, which indicates the safety of the incubated formulations.
Conclusion: NLC formulation has the potential to improve oral bioavailability with high drug loading
and cell viability for CINH.
