Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, 34116, Beyazit, Istanbul, Turkey.
AAPS PharmSciTech. 2017 Oct;18(7):2673-2682. doi: 10.1208/s12249-017-0747-8. Epub 2017 Mar 9.
The purpose of the present work was to develop a mucoadhesive thermoreversible nasal gel with a tailored gelling temperature to provide the prolonged contact between mometasone furoate and the nasal mucosa and in order to prevent drainage of the formulation. For this purpose, in situ gel containing a thermogelling polymer poloxamer 407 (Pluronic® F-127) and a mucoadhesive polymer Carbopol® 974P NF was prepared. In this content, formulations were designed to have gelation temperature below 34°C to obtain gelation at intranasal cavity. Evaluation of the prepared in situ gels was carried out by the determination of sol-gel transition temperature, rheological and mechanical characteristics, mucoadhesion strength, drug content, physicochemical stability, in vitro release profiles, and ex vivo permeation across sheep nasal mucosa of formulations. Consequently, the in situ gel (CP5) which had favorable gelation temperature (30.1 ± 0.24°C), rheological and mechanical characteristics, in vitro release profile (T%100 180 min), and mucoadhesion strength (0.289 ± 0.0069 mJ) was developed. Consequently, the in situ gel system has been concluded as a promising approach in order to improve the therapeutic effects of intranasal mometasone furoate administration.
本工作旨在开发一种具有靶向胶凝温度的鼻用黏附型热可逆原位凝胶，以延长糠酸莫米松与鼻黏膜的接触时间，并防止制剂的排出。为此，制备了含有温敏聚合物泊洛沙姆 407（Pluronic® F-127）和黏附聚合物 Carbopol® 974P NF 的原位凝胶。在本内容中，设计了制剂的胶凝温度低于 34°C，以在鼻腔内获得凝胶化。通过测定溶胶-凝胶转变温度、流变和力学特性、黏附强度、药物含量、物理化学稳定性、体外释放曲线以及制剂在绵羊鼻黏膜上的体外渗透，对制备的原位凝胶进行了评价。结果，开发了一种具有良好胶凝温度（30.1 ± 0.24°C）、流变和力学特性、体外释放曲线（T%100 180 min）和黏附强度（0.289 ± 0.0069 mJ）的原位凝胶（CP5）。因此，原位凝胶系统被认为是一种有前途的方法，可提高鼻内给予糠酸莫米松的治疗效果。
