Innovative Epicardial Bigels Containing Amiodarone Hydrochloride: Pharmacotechnical and Analytical Characterization

Abstract

Background/Objectives: The search for novel ways of providing treatment also targets the development of formulations used in drug delivery. Among the important characteristics of pharmaceutical gels are their ability to penetrate membranes, their capability to offer rapid response, and their capacity to avoid the hepatic metabolization route followed by many drugs. Bigels combine the advantages of both hydrogels and oleogels, creating a biphasic system that might improve the solubility of amiodarone in water, which is otherwise poorly soluble. This study aimed to succeed in formulating stable amiodarone hydrochloride bigels (coded from ABG1-ABG6) destined for atrial application and evaluating them from a pharmacotechnical perspective. Methods: Three of the six initial formulations presented stability and underwent studies of spreadability, rheology, drug content, textural properties, and microbiological activity. A statistical analysis was performed on penetrometry and drug assay data. Results: The spreadability varied from 1734.07 mm2 (ABG1) to 2163.85 mm2 (ABG6), while the drug concentration ranged between 1.35 and 1.49% (w/w). The textural profile analysis highlighted superior hardness, cohesiveness, and resilience for ABG6 and higher adhesion for ABG2. Both presented pseudoplastic thixotropic behavior, while a plastic thixotropic flow was registered in the case of ABG1. Conclusions: All three bigels are suitable for amiodarone incorporation; however, the influence of the type of ingredients chosen on the texture and properties of the formulations was reflected in the data gathered upon evaluation.

Keywords

• amiodarone hydrochloride
• bigels
• texture analysis
• rheological evaluation
• content assay
• microbiological evaluation