A micrometer sized porous β-cyclodextrin polymer for improving bioavailability of poorly soluble drug

Abstract

A novel micrometer-sized porous cyclodextrin polymer (PCDP) was synthesized through the cross-linking of carboxymethyl β-cyclodextrin with 1,6-diaminohexane. We hypothesized that PCDP could be utilized as a drug carrier to enhance the dissolution rate and oral bioavailability of poorly soluble drugs. Ibuprofen (IBU), selected as the model poorly soluble drug, was successfully loaded into PCDP, resulting in a significant improvement in IBU release within simulated gastric fluid. Compared to IBU alone, IBU-loaded PCDP markedly increased the oral bioavailability of IBU, with an approximately 4-fold increase in the area under the curve (AUC) and a 3-fold increase in C_max, thereby enhancing the anti-inflammatory effects in rat models. Additionally, PCDP demonstrated good biocompatibility with Caco-2 cells. These findings suggest that the micrometer sized PCDP may be a promising drug carrier for improving the dissolution and oral bioavailability of poorly soluble drugs.