Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, 34116, Istanbul, Türkiye.
Department of Analytical Chemistry, Faculty of Pharmacy, Istanbul University, 34116, Istanbul, Türkiye.
AAPS PharmSciTech. 2022 Dec 20;24(1):23. doi: 10.1208/s12249-022-02477-5.
Buccal film formulations, including antifungal nystatin, anti-inflammatory agent hydrocortisone acetate, and local anesthetic lidocaine hydrochloride for pain relief, were developed. Bioadhesive films were fabricated with hydrophilic polymers, hydroxyethyl cellulose (HEC), and xanthan gum (XG) and dried in the incubator. Textural, swelling, and bioadhesive properties, physicochemical and in vitro release characteristics, and antifungal activities of bioadhesive films were evaluated.Bioadhesive films significantly extended nystatin release by prolonging retention time of the target area formulation while rapidly releasing hydrocortisone acetate and lidocaine HCl, reducing drug administration. The polymer type affected bioadhesion strength and erosion ratio, and XG formulations had more polymer suitability. Consequently, XT-O2 formulation that was prepared with xanthan gum and tween 80, was best for its highest antifungal film activity (20.00 ± 0.07 mm), released nystatin (44.296% ± 1.695), and lowest erosion matrix (36.719% ± 0.249). The selected formulation can be used for compatibility, stability and in vivo studies targeted oral candidiasis infections.
开发了颊膜制剂，包括抗真菌制霉菌素、抗炎剂醋酸氢化可的松和局部麻醉剂盐酸利多卡因，以缓解疼痛。使用亲水性聚合物羟乙基纤维素（HEC）和黄原胶（XG）制备了生物粘附膜，并在培养箱中干燥。评估了生物粘附膜的质地、溶胀和生物粘附特性、物理化学和体外释放特性以及抗真菌活性。生物粘附膜通过延长目标区域制剂的保留时间显著延长了制霉菌素的释放，同时迅速释放了醋酸氢化可的松和盐酸利多卡因，减少了药物的使用。聚合物类型影响生物粘附强度和侵蚀率，XG 制剂具有更高的聚合物适用性。因此，制备了含有黄原胶和吐温 80 的 XT-O2 制剂，因其具有最高的抗真菌膜活性（20.00±0.07mm）、释放制霉菌素（44.296%±1.695%）和最低的侵蚀基质（36.719%±0.249%）而表现最佳。所选制剂可用于口腔念珠菌病感染的相容性、稳定性和体内研究。
