Evaluation of Lapatinib-Loaded Microfibers Prepared by Centrifugal Spinning

Abstract

Lapatinib (Lap) is a lypophilic drug frequently used in cancer treatment; however, due to its limited solubility and permeability, achieving therapeutic dose through oral administration proves to be a challenge. There are various methods for enhancing the solubility of Lap and other similar drugs, one being the preparation of amorphous solid dispersions (ASD). In this study, a Lap-loaded polyvinylpyrrolidone (PVP) fiber mat was created with centrifugal spinning from a PVP/Lap solution in dimethyl formamide and ethanol. The production rate was 12.2 g/h dry fibers, and the fibers had an average thickness of 2.55 ± 0.92 μm. In the differential scanning calorimetry (DSC) thermogram of the fiber mat, the melting peak of the crystalline Lap was not visible, suggesting that Lap was in an amorphous state. A dissolution study was carried out in 0.2 M phosphate buffer saline solution at 37 °C. UV spectrophotometry data indicated that in the sample containing the fiber mat, the Lap concentration was 332 μg/mL (66%) in 10 min, decreasing to 227 μg/mL by 45 min. Meanwhile the crystalline Lap formed a 30–40 μg/mL (6–8%) solution in 5 min, maintaining that concentration. We conclude that centrifugal spinning can be an effective and easy method to produce ASDs.

Keywords

• lapatinib
• centrifugal spinning
• fiber mat
• amorphous solid dispersion
• scale-up