Abstract <p><b>Objective:</b> The study aimed to develop and characterize albumin-based nanoparticles loaded with the antiarrhythmic drug amiodarone to afford enhancement of therapeutic efficacy and reduction of systemic toxicity of the drug. <b>Methods:</b> Bovine serum albumin nanoparticles were synthesized by sequentially using the methods of desolvation, surface modification with cationic block copolymer PEG<sub>5k</sub>-b-PLL<sub>50</sub>, and crosslinking with 3,3′-dithiobis(sulfosuccinimidyl propionate) (DTSSP). The obtained nanoparticles were characterized by dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA). The encapsulation efficiency (EE) and loading capacity (LC) were determined spectrophotometrically. Drug release kinetics were studied in <i>vitro</i> under physiological conditions. <b>Results and Discussion:</b> It was shown that the particles had a hydrodynamic size ranging from ~180 to ~250 nm. The ζ-potential values demonstrated high colloidal stability of the obtained systems. The loading capacity and encapsulation efficiency for amiodarone were 23.4 and 36.8%, respectively. <i>In vitro</i> release studies revealed a sustained release profile, with 55.8% of the drug released within 120 h. The release kinetics followed a first-order model, suggesting concentration-dependent drug desorption from the albumin matrix. <b>Conclusions:</b> The developed amiodarone-loaded albumin nanoparticles exhibit favorable physicochemical properties and prolonged release behavior, indicating their potential as a nanocarrier system for targeted delivery of amiodarone in antiarrhythmic therapy.</p>

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Albumin Nanoparticles as a Carrier System for the Delivery of the Antiarrhythmic Drug Amiodarone

  • A. V. Doroshchenko,
  • A. D. Lapanik,
  • P. D. Orlova,
  • A. V. Lopukhov,
  • I. M. Le-Deygen,
  • Yu. I. Oshchepkova,
  • Sh. I. Salikhov,
  • N. L. Klyachko

摘要

Abstract

Objective: The study aimed to develop and characterize albumin-based nanoparticles loaded with the antiarrhythmic drug amiodarone to afford enhancement of therapeutic efficacy and reduction of systemic toxicity of the drug. Methods: Bovine serum albumin nanoparticles were synthesized by sequentially using the methods of desolvation, surface modification with cationic block copolymer PEG5k-b-PLL50, and crosslinking with 3,3′-dithiobis(sulfosuccinimidyl propionate) (DTSSP). The obtained nanoparticles were characterized by dynamic light scattering (DLS) and nanoparticle tracking analysis (NTA). The encapsulation efficiency (EE) and loading capacity (LC) were determined spectrophotometrically. Drug release kinetics were studied in vitro under physiological conditions. Results and Discussion: It was shown that the particles had a hydrodynamic size ranging from ~180 to ~250 nm. The ζ-potential values demonstrated high colloidal stability of the obtained systems. The loading capacity and encapsulation efficiency for amiodarone were 23.4 and 36.8%, respectively. In vitro release studies revealed a sustained release profile, with 55.8% of the drug released within 120 h. The release kinetics followed a first-order model, suggesting concentration-dependent drug desorption from the albumin matrix. Conclusions: The developed amiodarone-loaded albumin nanoparticles exhibit favorable physicochemical properties and prolonged release behavior, indicating their potential as a nanocarrier system for targeted delivery of amiodarone in antiarrhythmic therapy.