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含舒马曲坦的原位热敏性黏附鼻腔凝胶:制备与评价

In Situ Thermosensitive Mucoadhesive Nasal Gel Containing Sumatriptan: and Evaluations.

作者信息

Alshraim Aseel, Alshora Doaa, Ashri Lubna, Alhusaini Ahlam, Alanazi Nawal, Safwan Nisreen M

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

出版信息

Polymers (Basel). 2024 Dec 5;16(23):3422. doi: 10.3390/polym16233422.

Abstract

The aim of this study was to develop a thermosensitive mucoadhesive (MA) in situ nasal gel for sumatriptan. A 3D response surface methodology (Design of Expert version 11) was employed to formulate nine different formulations. The Pluronic F-127 concentration (X1) and chitosan concentration (X2) were selected as independent factors. The formulas were studied in terms of pH, clarity, drug content, gelation temperature, gelation time, gel strength, MA strength, viscosity, % release after 5 h, and release kinetics. The optimized formulas were studied for % permeated after 5 h and stability in addition to previous tests. The study of the stability of the optimized formula was performed under accelerated conditions (40 ± 2 °C, 75 ± 5% RH) for 3 months. The outcomes of the optimized formula were a clear gel with a gelation temperature of 33 °C and a reasonable gelation time of less than one minute, and the release and permeation during 5 h were 40% and 50%, respectively. The formulated gel decreased the mucociliary clearance (MCC) and thus increased the retention time in the nasal cavity, resulting in enhancing SMT absorption, which could improve the drug efficacy.

摘要

本研究的目的是开发一种用于舒马曲坦的热敏性黏膜黏附原位鼻腔凝胶。采用三维响应面法(Design of Expert版本11)制备了9种不同的制剂。选择泊洛沙姆F-127浓度(X1)和壳聚糖浓度(X2)作为独立因素。从pH值、澄清度、药物含量、胶凝温度、胶凝时间、凝胶强度、黏膜黏附强度、粘度、5小时后释放率和释放动力学等方面对配方进行了研究。除了之前的测试外,还对优化后的配方进行了5小时后渗透百分比和稳定性的研究。优化配方的稳定性研究在加速条件(40±2°C,75±5%相对湿度)下进行3个月。优化配方的结果是形成一种澄清凝胶,胶凝温度为33°C,胶凝时间合理,小于1分钟,5小时内的释放率和渗透率分别为40%和50%。所制备的凝胶降低了黏液纤毛清除率(MCC),从而增加了在鼻腔中的滞留时间,导致舒马曲坦吸收增强,进而提高药物疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1b6/11644292/91df9968b856/polymers-16-03422-g001.jpg

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