Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone

In this study, we aimed to design a highly swellable and mechanically robust matrix tablet
(SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution
behavior of β-lapachone with low aqueous solubility.

For the preparation of SMTs, the cogrinding technique and freeze–thaw method were used to disperse β-lapachone in SMTs in an amorphous state and to enhance the swelling and mechanical properties of SMTs, respectively. As a result, the crystallinity of coground β-lapachone incorporated in the SMTs was found to be considerably decreased; thereby, the dissolution rates of the drug in a simulated gastric fluid could be substantially increased.

The SMTs of β-lapachone also demonstrated significantly enhanced swelling and mechanical properties compared to those of a marketed product. The reason for this might be because the physically crosslinked polymeric networks with a porous structure that were formed in SMTs through the freeze–thaw method. In addition, β-lapachone was gradually released from the SMTs in 6 h. Therefore, SMTs of β-lapachone developed in this study could be used as GRDDS with appropriate swelling and mechanical properties for improving the dissolution behavior of hydrophobic drugs such as β-lapachone.

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Article Information: Hyeongmin Kim, Chung-Lyol Lee, Seohyun Lee, Tae Jin Lee, Iqra Haleem, Younghong Lee, Na Jung Hwang, Kyusun Shim, Dohyun Kim and Jaehwi Lee; Pharmaceutics 2019