Polyelectrolyte Microcapsules-A Promising Target Delivery System of Amiodarone with the Possibility of Prolonged Release

聚电解质微胶囊——一种有前景的胺碘酮靶向递送系统,具有延长释放的潜力

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Abstract

Atrial fibrillation is one of the most common cardiac arrhythmias. Pharmacological preparations are used for treatment to control heart rate and rhythm. Amiodarone is one of these highly effective preparations, but, at the same time, it has significant toxicity and nonspecific accumulation in tissues. The drug delivery system based on polyelectrolyte microcapsules is one of the solutions. For this purpose, we compared different encapsulation methods of amiodaron: monoammonium salt of glycyrrhizic acid (Am:MASGA) complex (molar ratio 1:8). The concentration of amiodarone was determined by spectrophotometric methods at 251 nm. It has been shown that the co-precipitation method allows capturing 8% of Am:MASGA by CaCO(3) microspherulites, which is not sufficient for the long-acting drug. The adsorption method allows encapsulating more than 30% of Am:MASGA into CaCO(3) microspherulites and polyelectrolyte microcapsules CaCO(3)(PAH/PSS)(3), but, at the same time, an insignificant amount of substance is released into the incubation medium. The development of delivery and long-acting drug system based on such methods are not inexpedient. The most appropriate encapsulation method of Am:MASGA is the adsorption method into polyelectrolyte microcapsules with complex interpolyelectrolyte structure (PAH/PSS)(3). Such a type of PMC adsorbed about 50% of the initial amount of the substance and 25-30% of Am:MASGA was released into the medium after 115 h of incubation. The adsorption of Am:MASGA by polyelectrolyte microcapsules has electrostatic nature as evidenced by the acceleration of the release by 1.8 times as ionic strength increases.

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