Evaluation of Thrombolytic and Antithrombin Activity of Rivaroxaban Loaded Liposomes

Abstract

The active drug loading approach, also called remote drug loading, involves loading the drug agent after empty liposomes are produced. The transmembrane gradient of pH or ion concentration is the driving force to promote the drug diffuse across the membrane into the inner core of liposomes. Based on the rank order performed for all conventional RIV liposomes formulae depending on their characterization and evaluation tests, one optimized liposome formulation was selected. From the in vitro drug release data, drug loading efficiency and particle size analysis formulae F4 were selected as optimized formulation. An in vitro study of the thrombolytic activity of liposomes was carried out using a similar procedure to that used for RIV. The results indicate that the formulation of RIV into liposomes doesn’t result in a significant loss of activity in vitro. This might be due to the effect of polymers used in the formulation and the properties of liposomes like porous surfaces.

Key words: Rivaroxaban; Chromogenic Assay; Antithrombin Activity; Prothrombin time; Anticoagulant