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Abstract <p>The development of new prolonged forms of antiarrhythmic drugs with improved biopharmaceutical properties is an urgent problem today. This study proposes a method for loading a poorly soluble antiarrhythmic drug, allapinin, into solid lipid nanoparticles of variable compositions to solve this problem. The parameters of the method for producing the solid lipid nanoparticles by temperature-induced phase inversion are optimized. The hydrodynamic characteristics of the particles and their stability to aggregation are assessed using dynamic light scattering. The systems based on stearic acid and a surfactant, Brij 56, have the best characteristics. The drug loading efficiency is almost 100%. FTIR spectroscopy data have revealed that the incorporation of allapinin into the particle cores leads to the formation of noncovalent bonds with the polar moiety of stearic acid. The prolonged release of allapinin from the particles in sodium phosphate buffer at the physiological temperature of 37°C has been shown. The data obtained may provide the foundation for the development of a novel allapinin formulation with enhanced biopharmaceutical characteristics.</p>

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Optimization of the Composition of Solid Lipid Nanoparticles for Delivery of an Antiarrhythmic Drug, Allapinin

  • 期刊论文

  • 发表日期：

    2026年3月18日

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  • A. A. Shalybkova,
  • Yu. I. Oshchepkova,
  • I. M. Le-Deigen,
  • N. A. Kozyrev,
  • N. L. Klyachko,
  • Sh. I. Salikhov

摘要

Abstract

The development of new prolonged forms of antiarrhythmic drugs with improved biopharmaceutical properties is an urgent problem today. This study proposes a method for loading a poorly soluble antiarrhythmic drug, allapinin, into solid lipid nanoparticles of variable compositions to solve this problem. The parameters of the method for producing the solid lipid nanoparticles by temperature-induced phase inversion are optimized. The hydrodynamic characteristics of the particles and their stability to aggregation are assessed using dynamic light scattering. The systems based on stearic acid and a surfactant, Brij 56, have the best characteristics. The drug loading efficiency is almost 100%. FTIR spectroscopy data have revealed that the incorporation of allapinin into the particle cores leads to the formation of noncovalent bonds with the polar moiety of stearic acid. The prolonged release of allapinin from the particles in sodium phosphate buffer at the physiological temperature of 37°C has been shown. The data obtained may provide the foundation for the development of a novel allapinin formulation with enhanced biopharmaceutical characteristics.