WITHDRAWN: Gastroretentive fibrous dosage forms for prolonged delivery of sparingly soluble tyrosine kinase inhibitors. Part 2: Experimental validation of the models of expansion, mechanical strength, and in vitro drug release

Abstract

In Part 1, we have introduced gastroretentive fibrous dosage forms with expandable, strengthened excipient fibers, and drug-loaded inter-fiber space for prolonged delivery of sparingly soluble tyrosine kinase inhibitors. The in vitro expansion rate, post-expansion mechanical strength, and drug release rate were modeled for a dosage form containing 200 mg of nilotinib. In the present part, the dosage form was prepared and tested in vitro to validate the models. Upon immersing in a dissolution fluid, the fibrous dosage form expanded at a constant rate to a normalized radial expansion of 0.5 by 4 h, and then formed an expanded viscoelastic mass of high strength. The drug was released at a constant rate over a day. For comparison, a particle-filled gelatin capsule with the same amount of nilotinib disintegrated almost immediately, and released eighty percent of the drug content in just 10 min. The data validate the models of Part 1.