Development and Optimization of PEGylated Nanoliposomes Loaded with Amiodarone Using Microfluidic Technique for Enhanced Cardiovascular Drug Delivery

Abstract

Amiodarone is an effective class III antiarrhythmic drug, but its clinical application is limited due to low solubility, irregular bioavailability, and severe side effects such as pulmonary toxicity. In this study, PEGylated nanoliposomes loaded with amiodarone were prepared and optimized using the microfluidic method to overcome these limitations. Six formulations with varying molar ratios of HEPC:Cholesterol: DSPE-PEG2000 were evaluated. The optimal formulation (55:40:5) exhibited the highest encapsulation efficiency (94.8 ± 1.6%), excellent colloidal stability (minimal change in size from 92 to 95 nm over 3 months), appropriate zeta potential (-8.2 ± 1.3 mV) due to PEG shielding, and uniform spherical morphology with sizes of 70–159 nm (mean ≈105 nm). SEM images confirmed the absence of aggregation and smooth particle surfaces. These characteristics highlight the system's potential for prolonged blood circulation, passive targeting to damaged cardiac tissue, and reduction of amiodarone side effects. The results indicate that the optimized formulation offers a promising advanced drug delivery platform for safer and more effective treatment of cardiac arrhythmias.