Enhanced Oral Bioavailability of Felodipine from Solid Lipid Nanoparticles Prepared Through Effervescent Dispersion Technique

AAPS PharmSciTech
Yingmeng HeYumeng Wei

Abstract

Felodipine (FLD), a dihydropyridine calcium channel blocker with excellent antihypertensive effect, is poorly soluble and undergoes extensive hepatic metabolism, which lead to poor oral bioavailability (about 15%) and limit its clinic application. The goal of this study was to develop solid lipid nanoparticles (SLNs) loading FLD to improve the oral bioavailability. The FLD loaded solid lipid nanoparticles (FLD-SLNs) were prepared by the effervescent dispersion technique developed by our laboratory, which might have some advantages over traditional methods. The FLD-SLNs showed desired particle characteristics with particle size (198.15 ± 1.82 nm), poly dispersity index (0.26 ± 0.02), zeta-potential (- 25.53 ± 0.60 mV), entrapment efficiency (95.65 ± 0.70%), drug loading (2.33 ± 0.10%), and a spherical appearance. Pharmacokinetic results showed that the FLD-SLNs presented 3.17-fold increase in area under the curve (AUC(0-t)) compared with free FLD after oral administration in beagle dogs, which indicated that SLNs prepared using the effervescent dispersion technique can improve the bioavailability of lipophilic drugs like felodipine by enhancement of absorption and reduction first-pass metabolism.

References

Apr 20, 2001·Advanced Drug Delivery Reviews·W Mehnert, K Mäder
Dec 13, 2006·International Journal of Pharmaceutics·Venishetty Vinay KumarPrakash Vamanrao Diwan
Mar 3, 2007·Nature Reviews. Drug Discovery·Christopher J H PorterWilliam N Charman
Dec 25, 2007·Advanced Drug Delivery Reviews·Natalie L TrevaskisChristopher J H Porter
May 3, 2008·International Journal of Pharmaceutics·Feng WanFu-Qiang Hu
Dec 16, 2010·The Journal of Pharmacy and Pharmacology·Ling ZhaoYu-meng Wei
Aug 13, 2011·Expert Opinion on Drug Delivery·Harshad HardeSanyog Jain
Sep 8, 2011·Journal of Young Pharmacists : JYP·P Ekambaram, Hasan Sathali A Abdul
May 23, 2012·Colloids and Surfaces. B, Biointerfaces·Shailesh S ChalikwarMrunal U Patil
Oct 15, 2013·International Journal of Nanomedicine·Ling ZhaoJunjiang Fu
Nov 8, 2013·European Journal of Drug Metabolism and Pharmacokinetics·Bhanu P Sahu, Malay K Das
May 15, 2015·Current Drug Safety·Kinjal Navadiya, Sanjay Tiwari
Oct 28, 2015·Advanced Pharmaceutical Bulletin·Neda NaseriParvin Zakeri-Milani
Jan 26, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Roberta B RigonMarlus Chorilli
Oct 30, 2016·Drug Discovery Today·Jianping QiWei Wu
Nov 5, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Narendar Dudhipala, Kishan Veerabrahma
Feb 10, 2018·Drug Delivery and Translational Research·Mahendra SinghShubhini A Saraf
Feb 13, 2018·International Journal of Biological Macromolecules·Chao PiYumeng Wei
Feb 16, 2019·Acta Pharmaceutica Sinica. B·Wei WuJianping Qi
Apr 6, 2019·Materials Science & Engineering. C, Materials for Biological Applications·Imran AhmadMohd Aqil
Jun 30, 2019·Advanced Drug Delivery Reviews·Yi LuTonglei Li
Nov 21, 2019·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Deepti ParasharRamakrishna Sistla

❮ Previous
Next ❯

Citations

Nov 17, 2020·Frontiers in Molecular Biosciences·Sebastián Scioli MontotoMaría Esperanza Ruiz

❮ Previous
Next ❯

Methods Mentioned

BETA
transmission electron microscopy
X-Ray

Software Mentioned

SPSS17
DAS

Related Concepts

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.