Sipos Emese, Csatári Tamás, Kazsoki Adrienn, Gergely Attila, Bitay Enikő, Szabó Zoltán-István, Zelkó Romána
Department of Drugs Industry and Pharmaceutical Management, University of Medicine, Pharmacy, Sciences and Technology of Targu Mures, Gh. Marinescu 38, 540139 Targu Mures, Romania.
University Pharmacy Department of Pharmacy Administration, Semmelweis University, H-1092 Hőgyes Endre utca 7-9, 1085 Budapest, Hungary.
Pharmaceutics. 2020 Jun 30;12(7):612. doi: 10.3390/pharmaceutics12070612.
Fenofibrate-loaded electrospun microfibrous sheets were prepared in an attempt to enhance the dissolution of the poorly soluble antihyperlipidemic agent and to improve its bioavailability. Physicochemical changes that appeared during the electrospinning process were monitored using a wide array of solid-state characterization techniques, including attenuated total reflectance Fourier-transformed infrared spectroscopy and positron annihilation lifetime spectroscopy, while fiber morphology was monitored via scanning electron microscopy. Dissolution studies carried out both in 0.025 M sodium dodecyl sulfate and in water revealed an immediate release of the active agent, with an approximately 40-fold release rate enhancement in water when compared to the micronized active agent. The dramatic increase in dissolution was attributed partially to the amorphous form of the originally crystalline active agent and the rapid disintegration of the electrospun microfibrous sheet due to its high surface area and porosity. The obtained results could pave the way for a formulation of the frequently used antihyperlipidemic agent with increased bioavailability.
制备了载有非诺贝特的电纺微纤维片，旨在提高难溶性抗高血脂药物的溶出度并改善其生物利用度。使用包括衰减全反射傅里叶变换红外光谱和正电子湮没寿命光谱在内的一系列固态表征技术监测电纺过程中出现的物理化学变化，同时通过扫描电子显微镜监测纤维形态。在0.025 M十二烷基硫酸钠和水中进行的溶出度研究表明，活性剂能立即释放，与微粉化活性剂相比，在水中的释放速率提高了约40倍。溶出度的显著增加部分归因于原本结晶的活性剂的无定形形式以及电纺微纤维片因其高表面积和孔隙率而迅速崩解。所得结果可为制备具有更高生物利用度的常用抗高血脂药物制剂铺平道路。
