Review of Clinical Pharmacology and Pharmacokinetics – International Edition Volume 38 (2024) – Supplementary Issue 2

Open Access Research

Preparation and characterization of azelnidipine-loaded D-α-tocopheryl polyethylene glycol succinate (TPGS) / solutol micelles
Ali Kathem Ala Allah¹, Shaimaa Nazar Abd Alhammid²,*
¹Babylon Health Directorate, Hillah, Iraq
²Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq

*Corresponding author: Shaimaa Nazar Abd Alhammid, Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq; Tel.: +964-(0)7703951999
E-mail: Shaimaa.Abd@copharm.uobaghdad.edu.iq

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Published: 5 May 2024; https://doi.org/10.61873/JYHN9753

Abstract
Azelnidipine is a calcium-channel antagonist classified as a “class 2” drug with high permeability and low aqueous solubility. It is used in the treatment of angina pectoris and hypertension without reflex tachycardia. Improvement of the solubility of azelnidipine and increasing drug’s bioavailability can be achieved through the drug encapsulation in solutol / D-α-tocopheryl polyethylene glycol succinate (TPGS) micelles. Six formulas were prepared by direct dissolution after using different amounts of solutol and TPGS. TPGS and solutol act as solubilizers, permeation enhancers, and P-glycoprotein inhibitors. The particle size, particle size distribution, zeta potential, and entrapment efficiency were determined. Depending on particle size and entrapment efficiency, formula #6 was selected and subjected to in vitrodilution stability and in vitro release studies. The results obtained showed that formula #6 was the best formula, with a high entrapment efficiency percentage equal to 86.5%±0.58% and a small particle size equal to 21.9±7.75 nm that did not change significantly after dilution up to 100-fold; a fact that reveals the high thermodynamic and kinetic stability of the optimum formula. The formula #6 release profile showed a controlled release of the drug from micelles when compared to plain drug release. Based on these results, polymeric nanomicelles are regarded as a promising delivery system for azelnidipine.

Keywords: Azelnidipine, TPGS, solutol HS15, micelles, drug delivery

Please cite as:
Ala Allah A. K., Abd Alhammid S. N. Preparation and characterization of azelnidipine-loaded D-α-tocopheryl polyethylene glycol succinate (TPGS) / solutol micelles. Rev. Clin. Pharmacol. Pharmacokinet. Int. Ed. 38 (Sup2): 51-54 (2024). https://doi.org/10.61873/JYHN9753