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基于芦荟水凝胶的左氧氟沙星胃滞留漂浮药物递送系统:体外和体内试验

Gastro retentive floating drug delivery system of levofloxacin based on Aloe vera hydrogel: In vitro and in vivo assays.

作者信息

Feroze Fouzia, Sher Muhammad, Hussain Muhammad A, Abbas Azhar, Haseeb Muhammad T, Fatima Arooj, Naeem-Ul-Hassan Muhammad, Amin Hatem M A

机构信息

Institute of Chemistry, University of Sargodha, Sargodha 40100, Pakistan.

Institute of Chemistry, University of Sargodha, Sargodha 40100, Pakistan.

出版信息

Int J Biol Macromol. 2025 Jan;284(Pt 1):138156. doi: 10.1016/j.ijbiomac.2024.138156. Epub 2024 Nov 28.

DOI:10.1016/j.ijbiomac.2024.138156
PMID:39613082
Abstract

Gastro retentive drug delivery systems (GRDDS) have gained immense popularity as they reduce dosing frequency, improve bioavailability, and enhance patient compliance. Herein, a plant-based, controlled swelling, and pH-sensitive GRDDS based on Aloe vera hydrogel and cellulose was developed for the sustained release of levofloxacin (LEVO). The properties of five various floating tablet formulations including dynamic swelling, pH-responsiveness, hardness, friability, drug release, and buoyant time were evaluated. The optimized formulation (FF) was characterized using FTIR and SEM, and the surface morphology exhibited a porous texture with microchannels that facilitated tablet swelling and prolonged release of LEVO. The formulation FF remained buoyant (> 12 h) in the simulated gastric fluid with a buoyancy time of 303 s. A pH-dependent swelling behavior of the formulation FF was revealed with the highest swelling (7.1 g/g) in water, followed by buffers of pH 6.8 (5.4 g/g), 4.5 (3.8 g/g), and 1.2 (2 g/g). The controlled release of LEVO was demonstrated for >12 h following the Hixson-Crowell model and non-Fickian diffusion. Pharmacokinetic parameters of LEVO were determined using in vivo studies. The non-toxic nature of the formulation under study was demonstrated. The results render this approach promising in reducing the dosing frequency, suggesting its potential for clinical applications.

摘要

胃滞留型药物递送系统(GRDDS)因其减少给药频率、提高生物利用度和增强患者顺应性而广受欢迎。在此,开发了一种基于芦荟水凝胶和纤维素的植物基、可控溶胀和pH敏感的GRDDS,用于左氧氟沙星(LEVO)的缓释。评估了五种不同漂浮片制剂的性能,包括动态溶胀、pH响应性、硬度、脆碎度、药物释放和漂浮时间。使用傅里叶变换红外光谱(FTIR)和扫描电子显微镜(SEM)对优化后的制剂(FF)进行了表征,其表面形态呈现出具有微通道的多孔质地,有助于片剂溶胀和LEVO的长效释放。制剂FF在模拟胃液中保持漂浮状态(>12小时),漂浮时间为303秒。制剂FF呈现出pH依赖性溶胀行为,在水中溶胀度最高(7.1 g/g),其次是pH 6.8的缓冲液(5.4 g/g)、pH 4.5的缓冲液(3.8 g/g)和pH 1.2的缓冲液(2 g/g)。根据希克森-克劳威尔模型和非菲克扩散,LEVO实现了>12小时的控释。通过体内研究确定了LEVO的药代动力学参数。证明了所研究制剂的无毒性质。结果表明这种方法在减少给药频率方面具有前景,表明其在临床应用中的潜力。

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