Evaluation of Lapatinib-Loaded Microfibers Prepared by Centrifugal Spinning

Author:

Bitay EnikőORCID,Gergely Attila LeventeORCID,Kántor József,Szabó Zoltán-IstvánORCID

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.

Funder

Hungarian Academy of Sciences

Publisher

MDPI AG

Subject

Polymers and Plastics,General Chemistry

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