QbD-based Formulation Optimization and Characterization of Polymeric Nanoparticles of Cinacalcet Hydrochloride with Improved Biopharmaceutical Attributes

Turkish Journal of Pharmaceutical Sciences

article

Debashish GHOSE¹  Chinam Niranjan PATRA¹  Bera Varaha Venkata RAVI KUMAR¹  Suryakanta SWAIN²  Bikash Ranjan JENA³  Punam CHOUDHURY¹  Dipthi SHREE¹ 

[1] Roland Institute of Pharmaceutical Sciences, Berhampur ,(Affiliated to Biju Patnaik University of Technology;Department of Pharmacy, School of Health Sciences, The Assam Kaziranga University;School of Pharmacy and Life Sciences, Centurion University of Technology and Management

关键词: PLGA;    polymeric nanoparticles;    Taguchi;    P-XRD;    optimization;    bioavailability potential;   

DOI  :  10.4274/tjps.galenos.2020.08522

来源: Galenos Yayinevi

【 摘 要 】

Objectives: The aim of the present work was to prepare QbD enabled optimization, and to improve the oral bioavailability of freeze–dried polymeric nanoparticles of cinacalcet hydrochloride manufactured by nanoprecipitation and ultrasonication methods using polymers PLGA, and poloxamer-188. Materials and Methods: The initial screening and optimization were carried out for the formulations by employing Taguchi and Box-Behnken Designs. The FT-IR and DSC revealed no interactions and had no incompatibility among the selected drug and polymers. The nanoparticles were characterized for % drug release, particle size analysis, zeta potential, PDI, SEM, TEM, P-XRD, TGA, DTA, in vitro, and in vivo drug release study. Results: In vitro drug release study showed sustained release of the drug from the optimized batch by diffusion mechanism. The optimized nanoparticle formulation was recognized by numerical and graphical methods using validation of the experimental model. The optimized batch was stable as per the ICH stability guidelines for 6 months with no considerable alternation noticed in particle size, entrapment efficiency, and in vitro drug release. The pharmacokinetic parameters of AUC and Cmax data for the optimized formulation increased 3- and 2.9-folds compared to the pure-drug suspension. Conclusion: The prepared polymeric nanoparticles formulation is an alternative delivery system for enhanced therapeutic efficacy and bioavailability potential of a model drug to manage long-term normocalcemia in patients with preliminary hyperparathyroidism.

【 授权许可】

Unknown