Nanoelectronics Laboratory, Electrical Engineering and Computer Science, University of Cincinnati, Cincinnati 45221-0030, USA; Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Ankara 06330, Turkey.
Nanoelectronics Laboratory, Electrical Engineering and Computer Science, University of Cincinnati, Cincinnati 45221-0030, USA.
Int J Pharm. 2020 Apr 15;579:119164. doi: 10.1016/j.ijpharm.2020.119164. Epub 2020 Feb 17.
Floating gastro-retentive delivery systems can prolong the gastric residence providing sustained drug release. In this study, we report on self-inflating effervescence-based electrospun nanofiber membranes embedding polyethylene oxide/sodium bicarbonate cast films. In this system, sodium bicarbonate results in an effervescence effect by creating carbon dioxide gas upon contacting an acidic gastric fluid, with the resulting gas bubbles being entrapped within the swollen network of nanofibers. Eudragit RL and RS polymers are utilized as a host material to manipulate release kinetics of incorporated drugs. Pramipexole, a common medication for chronic Parkinson's disease (PD), is used as a model drug. Uniform and bead-free nanofibers with diameters of ~300 nm were obtained. Although floating nanofibers initially exhibited high water contact angles (WCA), water droplets were quickly absorbed into the surface and the WCA decreased to ~0° within 60 s. Floating lag time, total floating time, swelling properties and drug release profiles were investigated both in a simulated gastric fluid (pH 1.2 buffer solution) and in a simulated intestinal fluid (pH 6.8 buffer solution) at 37 °C. All floating nanofiber formulations began to float instantly with nearly zero floating lag time and did not sink into the solution even after 24 h. By comparison, the same formulations without sodium bicarbonate cast films could not maintain continuous floating beyond 15 min. The floating nanofiber pouches presented lower initial release of between 20 and 57 %, compared to that of non-floating nanofiber pouches (40-82% within 2 h). Clearly, floating nanofibers reduced the initial burst release and provided sustained drug release. This demonstrates the potential to result in 'once-a-day' oral introduction of drugs that normally must be taken frequently. Effervescence-based floating nanofibers present a novel and promising prototype delivery system for the drug delivery in the upper gastro-intestinal (GI) tract.
漂浮型胃滞留给药系统可以延长胃内停留时间，实现药物的持续释放。在本研究中，我们报告了基于自膨胀泡腾的静电纺纳米纤维膜，其中嵌入了聚乙烯氧化物/碳酸氢钠铸膜。在该系统中，碳酸氢钠与酸性胃液接触时会产生泡腾效应，生成二氧化碳气体，所产生的气泡被包裹在溶胀的纳米纤维网络中。Eudragit RL 和 RS 聚合物被用作一种宿主材料，以控制所包含药物的释放动力学。盐酸普拉克索是一种治疗慢性帕金森病（PD）的常用药物，被用作模型药物。获得了直径约为 300nm 的均匀、无珠的纳米纤维。尽管漂浮纳米纤维最初表现出高的水接触角（WCA），但水滴滴迅速被吸收到表面，WCA 在 60s 内降低到约 0°。在 37°C 下，在模拟胃液（pH1.2 缓冲溶液）和模拟肠液（pH6.8 缓冲溶液）中，研究了漂浮滞后时间、总漂浮时间、溶胀性能和药物释放曲线。所有漂浮纳米纤维制剂都立即开始漂浮，几乎没有漂浮滞后时间，即使在 24 小时后也不会沉入溶液中。相比之下，没有碳酸氢钠铸膜的相同制剂在 15 分钟以上无法保持连续漂浮。漂浮纳米纤维囊泡的初始释放率较低，介于 20-57%之间，而无漂浮纳米纤维囊泡的初始释放率较高，介于 40-82%之间（2 小时内）。显然，漂浮纳米纤维减少了初始突释，并提供了持续的药物释放。这表明有可能将通常需要频繁服用的药物改为“每日一次”口服给药。基于泡腾的漂浮纳米纤维为上胃肠道（GI）的药物输送提供了一种新颖而有前途的原型给药系统。
