Sipos Emese, Szabó Zoltán István, Rédai Emőke, Szabó Péter, Sebe István, Zelkó Romána
Department of Pharmaceutical Industry and Management, University of Medicine and Pharmacy of Tîrgu Mureș, R-540139, Marinescu Street 38, Tirgu Mureș, Romania.
Department of Pharmaceutical Technology, University of Medicine and Pharmacy of Tîrgu Mureș, R-540139, Marinescu Street 38, Tirgu Mureș, Romania.
J Pharm Biomed Anal. 2016 Sep 10;129:224-228. doi: 10.1016/j.jpba.2016.07.004. Epub 2016 Jul 5.
Nebivolol-loaded electrospun nanofibrous sheets were prepared for the dissolution enhancement of the active with the aim of improving its oral bioavailability. Physicochemical characterization of nanofibers including differential scanning calorimetry, attenuated total reflectance Fourier transform infrared spectroscopy and positron annihilation lifetime spectroscopy were carried out in order to track the physicochemical changes related to the electrospinning process. The obtained results unanimously indicated the amorphous transition of nebivolol as a result of electrospinning, furthermore supramolecular ordering of chains of polyvinyl alcohol matrix could be revealed by positron annihilation lifetime spectroscopy. The crystalline-amorphous conversion of the active, along with the increased specific surface area of the nanofibers enabled rapid and complete dissolution. More than twice amount of active released from the fibrous sheets than from the commercial tablets. In contrast to the control tablets, the dissolution was complete and was not influenced by the pH of the applied media.
制备了载有奈必洛尔的电纺纳米纤维片，旨在提高活性成分的溶出度，以改善其口服生物利用度。对纳米纤维进行了包括差示扫描量热法、衰减全反射傅里叶变换红外光谱法和正电子湮没寿命谱法在内的物理化学表征，以追踪与电纺过程相关的物理化学变化。所得结果一致表明，电纺导致奈必洛尔发生非晶态转变，此外，正电子湮没寿命谱法可揭示聚乙烯醇基质链的超分子有序排列。活性成分的晶态-非晶态转变以及纳米纤维比表面积的增加使得溶解迅速且完全。从纤维片中释放的活性成分量是市售片剂的两倍多。与对照片剂相比，溶解是完全的，且不受所用介质pH值的影响。
