Enhanced oral bioavailability of nisoldipine-piperine-loaded poly-lactic-co-glycolic acid nanoparticles

Nanotechnology Reviews

article

Permender Rathee¹  Anjoo Kamboj²  Shabir Sidhu³ 

[1] Department of RIC, IKG Punjab Technical University;Chandigarh College of Pharmacy;Department of Food Engineering, IKG Punjab Technical University

关键词: bioenhancer;    CYP3A4;    nisoldipine;    optimization;    piperine;    PLGA;   

DOI  :  10.1515/ntrev-2017-0151

学科分类：社会科学、人文和艺术（综合）

来源: De Gruyter

【 摘 要 】

Background: Piperine helps in the improvement of bioavailability through pharmacokinetic interaction by modulating metabolism when administered with other drugs. Nisoldipine is a substrate for cytochrome P4503A4 enzymes. The study was undertaken to assess the influence of piperine on the pharmacokinetics and pharmacodynamics of nisoldipine nanoparticles in rats. Methods: Optimization studies of nanoparticles were performed using Taguchi L 9 orthogonal array, and the nanoparticles were formulated by the precipitation method. The influence of piperine and nanoparticles was evaluated by means of in vivo kinetic and dynamic studies by oral administration in rats. Results: The entrapment efficiency, drug loading, ζ potential, and average particle size of optimized nisoldipine-piperine nanoparticles was 89.77±1.06%, 13.6±0.56%, −26.5 mV, and 132±7.21 nm, respectively. The in vitro release in 0.1 n HCl and 6.8 pH phosphate buffer was 96.9±0.48% and 98.3±0.26%, respectively. Pharmacokinetic studies showed a 4.9-fold increase in oral bioavailability and a >28.376±1.32% reduction in systemic blood pressure by using nanoparticles as compared to control (nisoldipine suspension) in Wistar rats. Conclusion: The results revealed that piperine being an inhibitor of cytochrome P4503A4 enzymes enhanced the bioavailability of nisoldipine by 4.9-fold in nanoparticles.

【 授权许可】

CC BY