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

IF 7.7 1区 化学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY
Fouzia Feroze, Muhammad Sher, Muhammad A Hussain, Azhar Abbas, Muhammad T Haseeb, Arooj Fatima, Muhammad Naeem-Ul-Hassan, Hatem M A Amin
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引用次数: 0

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.

以芦荟和纤维素水凝胶为基础的左氧氟沙星胃内保留漂浮给药系统:体外和体内试验。
胃保留给药系统(GRDDS)由于减少给药频率、提高生物利用度和增强患者依从性而获得了极大的普及。本研究以芦荟水凝胶和纤维素为基础,开发了一种以植物为基础、控制溶胀、ph敏感的左氧氟沙星(LEVO)缓释GRDDS。考察了5种不同浮片配方的动态溶胀、ph响应性、硬度、脆性、药物释放和浮力时间等性能。通过FTIR和SEM对优化后的FF进行表征,其表面形貌呈多孔结构,微通道有利于溶胀,延长LEVO的释放时间。配方FF在模拟胃液中保持浮力(> 12 h),浮力时间为303 s。FF在水中溶胀率最高(7.1 g/g),其次为 6.8(5.4 g/g)、4.5(3.8 g/g)和1.2(2 g/g)缓冲液。根据Hixson-Crowell模型和非菲克式扩散,证明了LEVO在bbb12 h的控释。LEVO的药动学参数通过体内研究确定。所研究的配方的无毒性被证明。结果表明,该方法有望减少给药频率,提示其临床应用潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
International Journal of Biological Macromolecules
International Journal of Biological Macromolecules 生物-生化与分子生物学
CiteScore
13.70
自引率
9.80%
发文量
2728
审稿时长
64 days
期刊介绍: The International Journal of Biological Macromolecules is a well-established international journal dedicated to research on the chemical and biological aspects of natural macromolecules. Focusing on proteins, macromolecular carbohydrates, glycoproteins, proteoglycans, lignins, biological poly-acids, and nucleic acids, the journal presents the latest findings in molecular structure, properties, biological activities, interactions, modifications, and functional properties. Papers must offer new and novel insights, encompassing related model systems, structural conformational studies, theoretical developments, and analytical techniques. Each paper is required to primarily focus on at least one named biological macromolecule, reflected in the title, abstract, and text.
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