Preparation and Characterization of the Release Behavior of PVA: Na-Alg Microsphere Containing Fampridine

This study focuses on both the formulation of bio-based microspheres containing fampridine for the treatment of multiple sclerosis and provides an alternative to the commercially available product (Fampyra 10 mg, Biogen).

The encapsulation of fampridine was achieved using polyvinyl alcohol (PVA) and sodium alginate (Na-Alg) polymers. Glutaraldehyde (GA) and hydrochloric acid (HCI) were used as crosslinking agents. The polymer ratio (PVA: Na-Alg), drug: polymer (d:p) ratio, cross-linking agent ratio, and cross-linking time were evaluated for fampridine release. Release studies were analyzed using an ultraviolet spectrophotometer. The microspheres were characterized using scanning electron microscopy, differential scanning calorimetry, and Fourier transform-infrared transform infrared spectroscopy (FT-IR). The particle sizes of the fampridine-loaded microspheres were determined using a laser light scattering device.

The study revealed that the optimal conditions for achieving the highest fampridine release involved microspheres formulated with a polymer ratio of PVA:Na-Alg (w:w) at 1:1, a drug-to-polymer (d:p) ratio of 1:2 (w:w), cross-linking agent concentrations of 2.5% (w:w) GA and 3% (w:w) HCI, and a cross-linking time of 5 minutes. The particle size analysis showed that all microspheres were within the 300-800 μm range, and an increase in the d:p ratio correlated with larger particle sizes.

The findings demonstrate that bio-based microspheres containing fampridine can be successfully formulated using PVA and sodium alginate polymers, providing a promising alternative to the commercially available product.