Development and evaluation of alginate-based gastroretentive raft-forming systems enabling sustained release of propolis in gastric ulcer treatment.

IF 8 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Drug Delivery Pub Date : 2026-12-31 Epub Date: 2026-01-21 DOI:10.1080/10717544.2026.2616887
Haniye Takbirgou, Maryam Salami, Gholamreza Askari, Zahra Emam-Djomeh, Raimar Löbenberg, Michael J Serpe, Neal M Davies, Wing-Fu Lai
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Abstract

This study aimed to develop alginate-based raft-forming systems incorporating propolis-whey protein isolate (5%) nanocomplexes to alleviate reflux symptoms and enable the sustained, gastric-specific delivery of propolis for ulcer management. Propolis-protein complexes were prepared at four ratios (2.5:100, 5:100, 7.5:100, and 10:100 w/v) by heating at 85 °C for 5 h at pH 2, producing nanofibrils characterized by thioflavin T fluorescence, intrinsic fluorescence, encapsulation efficiency (up to 78%), and antioxidant activity. The optimal complex was incorporated into alginate rafts at 5%, 10%, and 15% (w/v). Rafts exhibited prolonged floatability (>8 h), increased thickness (from 3.2 ± 0.4 mm to 4.7 ± 0.3 mm with higher propolis loading), enhanced mechanical strength (up to 1.6-fold improvement), and improved reflux resistance. SEM imaging revealed a more compact and uniform porous structure, while FT-IR confirmed molecular interactions between alginate and the propolis-protein complex. In vitro release studies in simulated gastric fluid showed suppression of initial burst release, with sustained propolis release over 6-8 h. Overall, alginate rafts containing propolis-protein nanocomplexes demonstrated enhanced structural performance, controlled release behavior, and promising potential for targeted gastric delivery in the management of gastric ulcers.

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以海藻酸盐为基础的胃保留筏形成系统的开发和评价,使蜂胶在胃溃疡治疗中持续释放。
本研究旨在开发以海藻酸盐为基础的筏状形成系统,其中包含蜂胶-乳清分离蛋白(5%)纳米复合物,以减轻反流症状,并使蜂胶的持续、胃特异性输送用于溃疡管理。以2.5:100、5:100、7.5:100和10:100 w/v的四种比例制备蜂胶-蛋白复合物,在85℃、pH 2下加热5 h,制备的纳米原纤维具有硫黄素T荧光、固有荧光、包封效率(高达78%)和抗氧化活性。将最佳配合物以5%、10%和15% (w/v)的比例掺入海藻酸筏子中。竹筏的可浮性延长(8小时),厚度增加(从3.2±0.4 mm增加到4.7±0.3 mm,蜂胶含量增加),机械强度增强(提高1.6倍),抗回流性提高。扫描电镜(SEM)成像显示其多孔结构更加致密和均匀,而红外光谱(FT-IR)证实了海藻酸盐与蜂胶蛋白复合物之间的分子相互作用。在模拟胃液中的体外释放研究显示,初始爆发释放受到抑制,蜂胶持续释放超过6-8小时。总的来说,含有蜂胶-蛋白质纳米复合物的藻酸盐筏显示出增强的结构性能,控制释放行为,以及在胃溃疡治疗中靶向胃递送的潜力。
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
Drug Delivery
Drug Delivery 医学-药学
CiteScore
11.80
自引率
5.00%
发文量
250
审稿时长
3.3 months
期刊介绍: Drug Delivery is an open access journal serving the academic and industrial communities with peer reviewed coverage of basic research, development, and application principles of drug delivery and targeting at molecular, cellular, and higher levels. Topics covered include all delivery systems including oral, pulmonary, nasal, parenteral and transdermal, and modes of entry such as controlled release systems; microcapsules, liposomes, vesicles, and macromolecular conjugates; antibody targeting; protein/peptide delivery; DNA, oligonucleotide and siRNA delivery. Papers on drug dosage forms and their optimization will not be considered unless they directly relate to the original drug delivery issues. Published articles present original research and critical reviews.
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