Formulation and Evaluation of Azelnidipine Solid Lipid Nanoparticles
Keywords:
Azelnidipine, solid lipid nanoparticles, ultrasonication, particle size, entrapment efficiency, in-vitro release.Abstract
Introduction: Azelnidipine is a third-generation, long-acting dihydropyridine calcium channel blocker used to treat high blood pressure. The aim of the study was to prepare Azelnidipine solid lipid nanoparticles (SLN) to improve the solubility and bioavailability.
Methods: Six SLN formulations F1-F6of Azelnidipine were developed using three different lipids - Trimyristin, Tripalmitin and Tristearin at varying concentrations by the hot homogenization followed by ultrasonication method. All the formulations were characterized for their particle size (Ps), zeta potential (ZP), entrapment efficiency (EE), assay and drug release. The stability study test was conducted on optimized formulation at room temperature and refrigerated conditions for 3 months.
Results: The particle sizes of the formulations ranged from 167 ± 2.1 to 325 ± 1.3 nm, with PDI values between 0.267 ± 0.03 and 0.384 ± 0.03. Zeta potential ranged from –18.17 ± 1.1 to –23.01 ± 1.3 mV, and entrapment efficiency was between 84.21 ± 0.1% and 94.16 ± 0.1%. In vitro drug release studies, conducted using the dialysis method in 0.1 N HCl and pH 6.8 phosphate buffer, demonstrated a slower release in acidic medium compared to the phosphate buffer. Among all formulations, F5 prepared with Tripalmitin exhibited the highest drug release of 79.21% over 24 hours in pH 6.8 phosphate buffer. Based on particle size, entrapment efficiency, and drug release profile, F5 was selected as the optimized formulation. Stability studies confirmed that F5 remained stable for at least three months.
Conclusion: The optimized formulation (F5) demonstrated the highest zeta potential, excellent entrapment efficiency, small particle size, and sustained drug release over 24 hours, indicating that SLN are a promising delivery system for enhancing the bioavailability of Azelnidipine.
Downloads
Metrics
References
Mukherjee S, Ray S, Thakur RS. Solid lipid nano particles: A modern formulation approach in drug delivery system. Indian J Pharm Sci. 2009; 71: 349–58.
Ekambaram P, Abdul HA, Priyanka K. Solid lipid nano particles: a review. Chem. Commun, 2012; 2(1): 80-102.
Carretero OA, Oparil S. Essential hypertension. Part I: Definition and etiology. Circulation. 2010; 101(3): 329-35.
Chen BL, Zhang YZ, Luo JQ, Zhang W. Clinical use of azelnidipine in the treatment of hypertension in Chinese patients. Therapeutics and clinical risk management. 2015; 24: 309-18.
Xiao Y, Hu G. The effects of azelnidipine and amlodipine in treatment of mild to moderate hypertension: a systematic review. Int J Clin Exp Med. 2017; 10(7): 11273-8.
Thatipamula RP, Palem CR, Gannu R.Formulation and in vitro characterization of domperidone loaded solid lipid nano particles and nano structured lipid carriers. Daru, 2011; 19: 23–32.
Imran B, ud Din F, Ali Z, Fatima A, Khan MW, Kim DW, Malik M, Sohail S, Batool S, Jawad M, and Shabbir K. Statistically designed dexibuprofen loaded solid lipid nanoparticles for enhanced oral bioavailability. J.Drug Deliv.Sci.Tech.2022; 77:103904.
Amira A Rashad, S.Nageeb El-Helaly, Randa T Abd El Rehim, Omaima N El-Gazayerly Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and Muco adhesive strength. Acta Pharma., 2019; 69: 1-18.
El-Assal MI, Samuel D. Optimization of rivastigmine chitosan nanoparticles for neuro degenerative alzheimer; in vitro and ex vivo characterizations. Int J Pharm Pharm Sci. 2022; 14(1):17-27.
Elbahwy IA, Ibrahim HM, Ismael HR, Kasem AA. Enhancing bioavailability and controlling the release of glibenclamide from optimized solid lipid nanoparticles. J Drug Deliv Sci Technol. 2017; 38:78-89.
Nagaraj B, Tirumalesh C, Dinesh S, Narendar D. Zotepine loaded lipid nanoparticles for oral delivery: development, characterization, and in vivo pharmacokinetic studies. Futur J Pharm Sci. 2020; 6(1):1.
Vaidya A, Jain S, Jain A, Jain A. Simvastatin-loaded pegylated solid lipid nanoparticles: lipid functionalization to improve blood circulation. Bio Nano Science. 2020; 10(3):773-82.
Kushwaha AK, Vuddanda PR, Karunanidhi P, Singh SK, Singh S. Development and evaluation of solid lipid nanoparticles of Raloxifene hydrochloride for enhanced bioavailability. Bio Med Res Int. 2013; 20: 539-549.
Shaveta S, Singh J, Afzal M, Kaur R, Imam SS, Alruwaili NK. Development of solid lipid nano particle as carrier of Pioglitazone for amplification of oral efficacy: formulation design optimization, in vitro characterization and in vivo biological evaluation. J Drug Deliv Sci Technol. 2020; 57: 126-132.
Downloads
Published
How to Cite
Issue
Section
License
This work is licensed under a Creative Commons Attribution 4.0 International License.
You are free to:
- Share — copy and redistribute the material in any medium or format
- Adapt — remix, transform, and build upon the material for any purpose, even commercially.
Terms:
- Attribution — You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use.
- No additional restrictions — You may not apply legal terms or technological measures that legally restrict others from doing anything the license permits.
