Department of Fiber Science & Apparel Design, College of Human Ecology , Cornell University , Ithaca , New York 14853 , United States.
Mol Pharm. 2019 Oct 7;16(10):4387-4398. doi: 10.1021/acs.molpharmaceut.9b00798. Epub 2019 Sep 4.
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.
在这项研究中，进行了无聚合物静电纺丝，以生产环糊精/布洛芬包合物纳米纤维，作为快速溶解的口服药物递送系统具有潜力。布洛芬是一种水溶性较差的非甾体抗炎药；然而，通过与环糊精包合，布洛芬的水溶性可以显著提高。在这里，羟丙基-β-环糊精（HPβCyD）被选为纳米纤维基质和主体分子，以提高布洛芬的水溶性和快速溶解。布洛芬与 HPβCyD 在具有两种不同摩尔比的 HPβCyD（200%，w/v）的高浓度水溶液中进行包合：1:1 和 2:1（HPβCyD/布洛芬）。HPβCyD/布洛芬-IC（1:1）水溶液混浊，有一些未溶解/未包合的布洛芬，而 HPβCyD/布洛芬-IC（2:1）水溶液均相透明，表明布洛芬与 HPβCyD 完全包合并变得水溶性。然后，将两种 HPβCyD/布洛芬-IC 溶液（1:1 和 2:1）静电纺成无珠状且均匀的纳米纤维，纤维直径约为 200nm。静电纺丝得到的 HPβCyD/布洛芬-IC 纳米纤维呈纤维状网络状，具有自立和柔韧的特性，适用于快速溶解的口服药物递送系统。在静电纺丝过程中布洛芬完全保留，并且通过保留初始摩尔比 1:1 和 2:1（HPβCyD/布洛芬），没有任何布洛芬损失来制备所得的静电纺丝 HPβCyD/布洛芬-IC 纳米纤维。X 射线衍射和差示扫描量热法测量表明，HPβCyD/布洛芬-IC（1:1）纳米纤维中存在一些结晶布洛芬，而 HPβCyD/布洛芬-IC（2:1）纳米纤维中布洛芬完全处于无定形态。尽管如此，当与水接触或用人工唾液润湿时，两种 HPβCyD/布洛芬-IC（1:1 和 2:1）纳米纤维网都表现出非常快速的溶解特性。简而言之，我们的结果表明，静电纺丝 HPβCyD/布洛芬-IC 纳米纤维网具有作为快速溶解的口服药物递送系统的潜力。
