Abstract

Bronchial asthma is a chronic disease which is currently treated using various inhalants. However, the medication adherence with the inhalants is poor due to complex procedure to use them along with frequent dosing. In this paper, we have developed tulobuterol loaded Pluronic® F127-reduced graphene oxide transdermal hydrogel to sustain the release of tulobuterol to manage asthma for days. The synthesis of Pluronic^® F127-reduced graphene oxide was confirmed by Fourier transform infrared spectroscopy, X-ray diffraction, and Raman spectroscopy. The transmission electron microscope showed wrinkled flat nano sheets. The hydrogel showed sufficient mechanical properties for topical application and was safe in the skin irritation study (rabbit model). The ex vivo release data demonstrated the ability of reduced graphene oxide to sustain the release of tulobuterol for 72 h, due to strong π-π interaction between drug and graphene oxide. The pharmacokinetic profile in Sprague-Dawley rat model confirmed the potential of tulobuterol-Pluronic^® F127-reduced graphene oxide hydrogel to sustain the release of tulobuterol for effective management of asthma.

摘要

支气管哮喘是一种慢性疾病，目前使用各种吸入剂进行治疗。然而，吸入剂的药物依从性很差，因为使用它们的程序复杂，而且给药频率高。在本文中，我们开发了负载妥洛特罗的 Pluronic® F127 还原氧化石墨烯透皮水凝胶，以维持妥洛特罗的释放以控制哮喘数天。通过傅里叶变换红外光谱、X 射线衍射和拉曼光谱证实了Pluronic ^® F127 还原氧化石墨烯的合成。透射电子显微镜显示起皱的扁平纳米片。该水凝胶显示出足够的局部应用机械性能，并且在皮肤刺激研究（兔模型）中是安全的。在体外释放数据表明，由于药物和氧化石墨烯之间的强 π-π 相互作用，还原的氧化石墨烯能够持续释放妥洛特罗 72 小时。Sprague-Dawley 大鼠模型的药代动力学特征证实了妥洛特罗-Pluronic ^® F127 还原氧化石墨烯水凝胶持续释放妥洛特罗以有效控制哮喘的潜力。