Fast Dissolving Oral Drug Delivery System Based on Electrospun Nanofibrous Webs of Cyclodextrin/Ibuprofen Inclusion Complex Nanofibers.

Abstract

In this study, the polymer-free electrospinning was performed in order to produce cyclodextrin/ibuprofen inclusion complex nanofibers, which could have potential as the fast dissolving oral drug delivery system. Ibuprofen is a poorly water-soluble nonsteroidal anti-inflammatory drug; however, the water solubility of ibuprofen can be significantly enhanced by inclusion complexation with cyclodextrins. Here, hydroxypropyl-beta-cyclodextrin (HPβCyD) was chosen both as a nanofiber matrix and host molecule for inclusion complexation in order to enhance water solubility and fast dissolution of ibuprofen. Ibuprofen was inclusion-complexed with HPβCyD in highly concentrated aqueous solutions of HPβCyD (200%, w/v) having two different molar ratios: 1:1 and 2:1 (HPβCyD/ibuprofen). The HPβCyD/ibuprofen-IC (1:1) aqueous solution was turbid having some undissolved/uncomplexed ibuprofen, whereas HPβCyD/ibuprofen-IC (2:1) aqueous solution was homogeneous and clear, indicating that ibuprofen was totally complexed with HPβCyD and becomes water soluble. Then, both HPβCyD/ibuprofen-IC solutions (1:1 and 2:1) were electrospun into bead-free and uniform nanofibers having ∼200 nm fiber diameter. The electrospun HPβCyD/ibuprofen-IC nanofibers were obtained as nanofibrous webs having self-standing and flexible character, which is appropriate for fast dissolving oral drug delivery systems. Ibuprofen was completely preserved during the electrospinning process, and the resulting electrospun HPβCyD/ibuprofen-IC nanofibers were produced without any loss of ibuprofen by preserving the initial molar ratio of 1:1 and 2:1 (HPβCyD/ibuprofen). X-ray diffraction and differential scanning calorimetry measurements indicated the presence of some crystalline ibuprofen in HPβCyD/ibuprofen-IC (1:1) nanofibers, whereas ibuprofen was totally in the amorphous state in HPβCyD/ibuprofen-IC (2:1) nanofibers. Nonetheless, both HPβCyD/ibuprofen-IC (1:1 and 2:1) nanofibrous webs have shown very fast dissolving character when contacted with water or when wetted with artificial saliva. In brief, our results revealed that electrospun HPβCyD/ibuprofen-IC nanofibrous webs have potential as fast dissolving oral drug delivery systems.