Formulation Considerations and in vitro Characterization of Polymeric Micelles Loaded with Asenapine Maleate

Objectives: An effort has been utilized to incorporate ASPM into polymeric micelles using single and mixed copolymers. Materials and Methods: A thin-film hydration approach was used to create the ASPM polymeric micelles, which comprised TPGS, Solutol®HS-15, and Pluronics. Micelles characterization was performed by particle size distribution, zeta potential, while Encapsulation Efficiency (EE%), Drug Loading (DL%) content and in vitro drug release were determined also by HPLC analysis. Results: The ASPM loaded micelles, specifically F1, F4, and F8, exhibited a mean particle size of less than 200 nm, characterized by a narrow size distribution. The encapsulation rate reached up to 72±1.571%, with a drug loading of 14.12±0.3%, and a zeta potential indicating a negative charge of approximately -2 mV. ASPM was continuously released from polymeric micelles in PBS medium (pH 7.4) for 6 hr at 37°C, F8 was selected as the optimized mixed polymeric micelle. Conclusion: Polymeric micelles composed of TPGS, Tetronic® and TPGS:Solutol®HS 15 at concentration (2% w/v) can effectively incorporate ASPM and prolong drug release.