Aspirin loaded xerogels for buccal and oral GIT delivery for patients with dysphagia to target deep vein thrombosis

Smirna Farias
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引用次数: 2

Abstract

This study aimed to develop xerogels for delivery of aspirin via the oral (buccal mucosa and GIT) route in geriatric patients with dysphagia. Xerogels were prepared using low molecular weight chitosan (CS), carrageenan (CAR) and metolose (MET) in different ratios, loaded with aspirin (75 mg). Gels (2.5% w/v and 4.0% w/v) were prepared (60 °C) using 40% v/v ethanol and freeze dried for 48 hours. Xerogels (2.5% w/v MET: CAR 3:1 and 1:1, 4.0% CAR: CS 1:3 and 1:1 and 4.0% MET: CS 1:3 gels) were characterised with texture analysis (TA) for hardness and mucoadhesion, swelling index (%) and porosity (%) to identify an optimised formulation for controlled release (buccal) and fast release (GIT) delivery. Scanning electron microscopy (SEM) was used to assess surface morphology and X-ray diffraction (XRD) to assess the physical form of the formulations (amorphous or crystalline). Xerogels from 2.5 % w/v MET: CAR 3:1 and 1:1 gels showed higher swelling capacity (%) (more than 2 hours to disintegrate) and can be applied to the buccal mucosa for controlled delivery of the API while 4.0 % w/v CAR: CS 1:3 and 1:1 can be used as rapid release xerogel (disintegrated within 2 minutes) for oral GIT delivery.
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含阿司匹林的干凝胶用于吞咽困难患者的口腔和口服GIT以治疗深静脉血栓
本研究旨在开发经口腔(颊粘膜和胃肠道)途径给药阿司匹林的干凝胶,用于老年吞咽困难患者。以低分子量壳聚糖(CS)、卡拉胶(CAR)和代谢糖(MET)为原料,分别以不同比例载阿司匹林(75 mg)制备干凝胶。用40% v/v的乙醇(60℃)制备2.5% w/v和4.0% w/v的凝胶,冷冻干燥48小时。采用质地分析(TA)对干燥凝胶(2.5% w/v MET: CAR 3:1和1:1,4.0% CAR: CS 1:3和1:1和4.0% MET: CS 1:3凝胶)的硬度和黏附性、膨胀指数(%)和孔隙率(%)进行表征,以确定控释(口腔)和快速释放(GIT)给药的优化配方。用扫描电子显微镜(SEM)评估表面形貌,用x射线衍射仪(XRD)评估配方的物理形态(无定形或结晶)。2.5% w/v MET: CAR 3:1和1:1凝胶的干燥凝胶具有较高的肿胀能力(%)(超过2小时崩解),可以应用于口腔黏膜进行API的控制递送,而4.0% w/v CAR: CS 1:3和1:1凝胶可以作为快速释放的干燥凝胶(在2分钟内崩解)用于口服GIT。
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