Poznan University of Technology, Department of Chemical Technology, Berdychowo 4, 60-965 Poznan, Poland.
Poznan University of Medical Sciences, Department of Pharmaceutical Technology, Grunwaldzka 6, 60-780 Poznan, Poland.
Colloids Surf B Biointerfaces. 2018 Dec 1;172:586-593. doi: 10.1016/j.colsurfb.2018.09.014. Epub 2018 Sep 6.
The aim of this study is to characterize the matrices for the controlled release of fluconazole and to expand the knowledge of their physicochemical properties that influence the process of mucoadhesion. Polymeric carriers of fluconazole were prepared using the following mucoadhesive polymers: Carbopol 974 P NF, Noveon AA-1, HPMC, HEC, chitosan and film-forming polymer Kollidon VA 64. The potential mucoadhesive properties of the polymers and their blends were evaluated by measuring the wettability and then calculating the surface free energy defined by OWRK and vOCG models, determining the polar and dispersion forces, spreading coefficients and work of adhesion of polymers and their blends with fluconazole in the form of tablets. Prepared tablets were characterized by swelling capacity and in vitro drug release to estimate the amount of fluconazole release from selected polymer blends. The study of drug release from selected blends both in simulated saliva fluid (pH = 6.8) and in simulated vaginal fluid (pH = 4.2) containing mucin confirmed the ability of polymeric carriers to continuously deliver drug over a period of about 8 h.
本研究的目的是对氟康唑的控释基质进行表征，并扩展对影响粘膜黏附过程的其物理化学性质的了解。使用以下几种粘膜黏附聚合物制备氟康唑的聚合物载体：Carbopol 974P NF、Noveon AA-1、HPMC、HEC、壳聚糖和成膜聚合物 Kollidon VA 64。通过测量润湿性，然后通过 OWRK 和 vOCG 模型计算表面自由能来评估聚合物及其混合物的潜在粘膜黏附特性，确定极性和色散力、聚合物及其与氟康唑混合物的铺展系数和粘附功，这些聚合物及其混合物均以片剂的形式存在。通过溶胀能力和体外药物释放对制备的片剂进行表征，以估计从选定的聚合物混合物中释放的氟康唑的量。在含有粘蛋白的模拟唾液液（pH = 6.8）和模拟阴道液（pH = 4.2）中对选定混合物的药物释放研究证实了聚合物载体在大约 8 小时的时间内持续输送药物的能力。
