Innovative Epicardial Bigels Containing Amiodarone Hydrochloride: Pharmacotechnical and Analytical Characterization

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery Systems

Background:

• Pharmaceutical gels offer advantages like membrane penetration and avoiding hepatic metabolism.
• Bigels, combining hydrogels and oleogels, can potentially enhance the solubility of poorly soluble drugs like amiodarone hydrochloride.
• This research focuses on developing bigels for atrial application to improve amiodarone delivery.

Purpose of the Study:

• To formulate and characterize stable amiodarone hydrochloride bigels for atrial application.
• To evaluate the pharmacotechnical properties of the developed bigel formulations.
• To assess the potential of bigels as an improved drug delivery system for amiodarone.

Main Methods:

• Six amiodarone hydrochloride bigel formulations (ABG1-ABG6) were initially prepared.
• Three stable formulations underwent pharmacotechnical evaluations including spreadability, rheology, drug content, and textural analysis.
• Microbiological activity and statistical analysis of penetrometry and drug assay data were also performed.

Main Results:

• Spreadability ranged from 1734.07 mm² (ABG1) to 2163.85 mm² (ABG6).
• Drug concentration was consistently between 1.35% and 1.49% (w/w).
• Formulation ABG6 showed superior hardness, cohesiveness, and resilience, while ABG2 exhibited higher adhesion. Rheological studies indicated pseudoplastic thixotropic behavior for ABG2 and ABG6, and plastic thixotropic flow for ABG1.

Conclusions:

• The evaluated bigels are suitable for amiodarone hydrochloride incorporation.
• The choice of ingredients significantly influences the texture and overall properties of the bigel formulations.
• These findings support the potential of bigels as effective drug delivery systems for amiodarone.