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Lysozyme Functionalized Alginate-Chitosan Beads and Films for Different Release Applications. 溶菌酶功能化海藻酸盐-壳聚糖微球和膜的不同释放应用。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-11 DOI: 10.3390/gels12010066
Beatriz Moutinho, Natalia Pyra, Zuzanna Styrna, Maria Emilia Rosa, Maria H L Ribeiro

The main goal of this work was to develop nanoparticles of lysozyme (Lys) for biological and biomedical applications. The developed biosystems were based on Lys-loaded calcium alginate 2% and chitosan 1% beads and films with different concentrations of each polymer. Encapsulation efficiency was 100%. The ratio of adsorbed Lys on the films, Lys activity, and the release profile of Lys were measured using water and buffer solution at pH similar to the environment of cancer cells, at a controlled temperature of 37 °C and a constant speed, to assess the efficacy of the encapsulation process. Lys antimicrobial activity was assessed using Micrococcus lysodeikticus. Moreover, the anti-inflammatory and antioxidant properties of the developed biosystems were also evaluated. The anti-inflammatory activity of Lys released from calcium alginate 2%-chitosan 1% beads loaded with Lys was about 99%. These findings highlight the potential of the developed beads and films for biomedical applications, particularly in antimicrobial and anti-inflammatory therapies.

这项工作的主要目标是开发用于生物和生物医学应用的溶菌酶纳米颗粒。所开发的生物系统是基于lys负载2%海藻酸钙和壳聚糖1%,每种聚合物具有不同浓度的微球和膜。包封率100%。采用pH与癌细胞环境相似的水和缓冲液,在37℃的控制温度和恒定速度下,测定膜上吸附的赖氨酸的比例、赖氨酸的活性和赖氨酸的释放曲线,以评价包封工艺的效果。采用溶血微球菌法测定其抑菌活性。此外,还对开发的生物系统的抗炎和抗氧化性能进行了评价。负载赖氨酸的2%海藻酸钙- 1%壳聚糖微球所释放的赖氨酸抗炎活性约为99%。这些发现突出了开发的微球和薄膜在生物医学应用方面的潜力,特别是在抗菌和抗炎治疗方面。
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引用次数: 0
Eutectogels as Delivery Media for Therapeutic Metal Complexes: What Are the Benefits? 共析凝胶作为治疗性金属配合物的递送介质:有什么好处?
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-11 DOI: 10.3390/gels12010065
Varvara O Veselova, Svetlana V Revtovich, Vitalia V Kulikova, Arina D Filippova, Kseniya A Koshenskova, Nikolay N Efimov, Irina A Lutsenko, Marina A Uvarova

Drugs and drug candidate compounds commonly suffer from poor solubility and permeability. One promising strategy to mediate these drawbacks is use of novel solvents, such as deep eutectic compositions. The present research aims to determine the applicability of this approach for therapeutic metal complexes on the example of [Cu(Fur)2(Phen)] (Fur = furoate-anion, Phen = 1,10-phenantroline) and [Cu(Fur)2(Neoc)(H2O)] (Fur = furoate-anion, Neoc = 2,9-dimetyl-1,10-phenanthroline) with molar weight of appx. 500 Da. Interaction of the metal complexes with the deep eutectic solvent (DES) reline was studied using electron paramagnetic resonance (EPR). Minimal inhibitory concentrations of the complexes dissolved in DES and dimethyl sulfoxide (DMSO) were determined and found to be equivalent in both solvents. That is, use of reline as a solvent did not alter the functional properties of the metal complexes. Changes in the transdermal permeation of the complexes in DMSO and DES were assessed using a Franz diffusion cell. It was discovered that depending on the structure of the complex, the permeability might either increase (from 15 to 30%) or decrease (from 13 to 8%) with changes in the solvent, and this can be used to develop dosing strategies. Therapeutic eutectogels were successfully produced by impregnating SiO2 nanoparticles with the metal complex solution in DES, facilitating convenient topical application.

药物和候选药物通常具有较差的溶解度和渗透性。一种有前途的策略来调解这些缺点是使用新的溶剂,如深共晶组合物。以摩尔质量为appx的[Cu(Fur)2(Phen)] (Fur =糠酸-阴离子,Phen = 1,10-菲罗啉)和[Cu(Fur)2(Neoc)(H2O)] (Fur =糠酸-阴离子,Neoc = 2,9-二甲基-1,10-菲罗啉)为例,确定该方法在治疗性金属配合物中的适用性。500哒。利用电子顺磁共振(EPR)研究了金属配合物与深共晶溶剂(DES)线的相互作用。测定了溶解在DES和二甲基亚砜(DMSO)中的配合物的最小抑制浓度,发现在两种溶剂中是相等的。也就是说,使用线作为溶剂不会改变金属配合物的功能特性。使用Franz扩散池评估DMSO和DES中复合物的透皮渗透变化。研究发现,根据配合物的结构,渗透率可能随着溶剂的变化而增加(从15%到30%)或减少(从13%到8%),这可以用于制定剂量策略。将二氧化硅纳米颗粒与金属配合物溶液浸渍在DES中,成功制备出治疗性共凝胶,方便外用。
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引用次数: 0
Biomedical Interpenetrated Hydrogels Fabricated via Quaternary Ammonium Chitosan and Dopamine-Conjugated Gelatin Integrated with Genipin and Epigallocatechin Gallate. 以季铵壳聚糖和多巴胺偶联明胶结合Genipin和表没食子儿茶素没食子酸酯制备的生物医学互渗透水凝胶。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-11 DOI: 10.3390/gels12010067
Ling Wang, Shuxin Hu, Zheng Wei, Peng Ding, Yaling Deng, Yanting Han, Yanfang Sun, Guohua Jiang, Lei Nie

Multifunctional hydrogels with an interpenetrated network structure have shown great potential for biomedical and tissue-regeneration applications. In this work, the biomedical hydrogel was fabricated with an interpenetrated network based on dopamine grafted gelatin (DA-Gel), and genipin crosslinked quaternary ammonium chitosan (QCS), incorporating epigallocatechin gallate (EGCG). The EDC/NHS and Schiff-base bond connections occurred in the hydrogels, as confirmed by Fourier-transform infrared (FT-IR) analysis. The properties of the fabricated hydrogels, including microstructure, degradation rate, adhesive strength, mechanical strength, and rheological behavior, can be regulated by adjusting the DA-Gel/QCS ratio or by using different crosslinking approaches. In addition, the fabricated hydrogels exhibited self-healing properties and strong adhesion to various materials and organs. Furthermore, the hydrogels performed good antibacterial activity against the typical bacteria, Escherichia coli and Staphylococcus aureus. EGCG encapsulated hydrogels displayed excellent antioxidant activities and good hemocompatibility. The hydrogels also demonstrated excellent cytocompatibility and good cell migration ability. The above results provide a facile approach to fabricate the biomedical hydrogels with a regulated network structure and multifunctional characteristics with potential in biomedical applications.

具有互渗透网状结构的多功能水凝胶在生物医学和组织再生方面具有巨大的应用潜力。本研究以多巴胺接枝明胶(DA-Gel)和吉尼平交联季铵盐壳聚糖(QCS)为基础,结合表没食子儿茶素没食子酸酯(EGCG)制备了生物医用水凝胶。傅里叶变换红外(FT-IR)分析证实,EDC/NHS和席夫碱键连接发生在水凝胶中。制备的水凝胶的微观结构、降解速率、粘接强度、机械强度和流变性能可以通过调节DA-Gel/QCS的比例或使用不同的交联方法来调节。此外,制备的水凝胶具有自愈性能,对各种材料和器官具有较强的粘附性。此外,水凝胶对典型细菌大肠杆菌和金黄色葡萄球菌具有良好的抗菌活性。EGCG包封水凝胶具有良好的抗氧化活性和血液相容性。水凝胶还表现出良好的细胞相容性和细胞迁移能力。上述结果为制备具有调控网络结构和多功能特性的生物医用水凝胶提供了一种简便的方法,具有潜在的生物医学应用前景。
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引用次数: 0
Preparation Strategy of Hydrogel Loaded with Natural Products and Its Research Progress in Skin Repair. 天然产物负载水凝胶制备策略及其在皮肤修复中的研究进展。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-09 DOI: 10.3390/gels12010062
Lingchen Zhang, Qifan Li, Yuhan Zhou, Junran Yang, Xiaohang Sun, Xiaoyu Bi, Qiteng Ding, Xinglong Liu, Bo Yang

Hydrogels are three-dimensional hydrophilic network structures with one or more polymers cross-linked, with excellent biocompatibility, drug-carrying function, and biodegradability. Meanwhile, skin wound repair includes hemostasis and coagulation, an inflammation stage, a proliferation stage, and a remodeling stage. Therefore, hydrogels loaded with natural products are widely used in repairing skin wounds through various mechanisms such as hemostasis, antibacterial activity, anti-inflammatory activity, angiogenesis promotion, skin regeneration, and skin repair monitoring. In addition, this study provides the cross-linking mechanism (physical cross-linking and chemical cross-linking) and construction mode (self-assembly and physical parcels) of the loaded natural product hydrogel. In general, the purpose of this paper is to comprehensively understand the mechanism and preparation strategy of hydrogels loaded with natural products for skin repair and provide theoretical reference for future skin repair research.

水凝胶是由一种或多种聚合物交联而成的三维亲水网络结构,具有良好的生物相容性、载药功能和生物降解性。同时,皮肤创面修复包括止血凝血、炎症期、增殖期和重塑期。因此,载有天然产物的水凝胶通过止血、抗菌、抗炎、促进血管生成、皮肤再生、监测皮肤修复等多种机制,广泛应用于皮肤创面修复。此外,本研究还提供了负载天然产物水凝胶的交联机理(物理交联和化学交联)和构建模式(自组装和物理包裹)。总的来说,本文的目的是全面了解负载天然产物的皮肤修复水凝胶的机理和制备策略,为未来的皮肤修复研究提供理论参考。
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引用次数: 0
Development of Human Serum Albumin-Based Hydrogels for Potential Use as Wound Dressings. 用于伤口敷料的人血清白蛋白基水凝胶的研制。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-09 DOI: 10.3390/gels12010064
Inna Zharkova, Irina Bauer, Oksana Gulyaeva, Evgenia Kozyreva, Zhanna Nazarkina, Elena Dmitrienko

Protein-based materials such as human serum albumin (HSA) have demonstrated significant potential for the development of novel wound management materials. For the first time, the formation of HSA-based hydrogels was proposed using a combination of thermal- and ethanol-induced approaches. The combination of phosphate-buffered saline (PBS) and limited (up to 20% v/v) ethanol content offers a promising strategy for fabricating human serum albumin-based hydrogels with tunable properties. The hydrogel formation was studied using in situ dynamic light scattering (DLS) for qualitative and semi-quantitative analysis of the patterns of protein hydrogel formation through thermally induced gelation. The rheological properties of human serum albumin-based hydrogels were investigated. Hydrogels synthesized via thermally induced gelation using a denaturing agent exhibit a dynamic viscosity ranging from 100 to 10,000 mPa·s. The biocompatibility, biodegradability, and structural stability of human serum albumin-based hydrogels were comprehensively evaluated in physiologically relevant media. These human serum albumin-based hydrogels represent a promising platform for developing topical therapeutic agents for wound management and tissue engineering applications. This study investigated the kinetics of tetracycline release from human serum albumin-based hydrogels in PBS and fetal bovine serum (FBS). All tested formulations of HSA-based hydrogels loaded with tetracycline (1 mg/mL) demonstrated antibacterial activity against Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, and Corynebacterium striatum strains.

以蛋白质为基础的材料,如人血清白蛋白(HSA)已经显示出开发新型伤口管理材料的巨大潜力。首次提出了热诱导和乙醇诱导相结合的方法来形成hsa基水凝胶。磷酸盐缓冲盐水(PBS)和有限(高达20% v/v)乙醇含量的组合为制造具有可调性质的人血清白蛋白基水凝胶提供了一种有前途的策略。采用原位动态光散射(DLS)技术,对热诱导凝胶形成蛋白质水凝胶的模式进行了定性和半定量分析。研究了人血清白蛋白基水凝胶的流变学特性。用变性剂热诱导凝胶合成的水凝胶的动态粘度范围为100 ~ 10,000 mPa·s。在生理相关介质中对人血清白蛋白水凝胶的生物相容性、生物降解性和结构稳定性进行了综合评价。这些基于人血清白蛋白的水凝胶为伤口管理和组织工程应用的局部治疗剂的开发提供了一个有前途的平台。本研究研究了人血清白蛋白水凝胶在PBS和胎牛血清(FBS)中的四环素释放动力学。所有被测试的含有四环素(1 mg/mL)的hssa基水凝胶均显示出对金黄色葡萄球菌、表皮葡萄球菌、溶血葡萄球菌和纹状杆杆菌菌株的抗菌活性。
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引用次数: 0
Preparation of Sustainable Alginate/Chitosan Blend Films by Thermo-Compression for Diverse Applications. 热压缩法制备海藻酸盐/壳聚糖复合膜的研究。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-09 DOI: 10.3390/gels12010063
Yodthong Baimark, Prasong Srihanam, Theeraphol Phromsopha, Nuanchai Khotsaeng

In this work, sodium alginate/chitosan (SA/CS) blend films were prepared by thermo-compression for the first time. Glycerol and lactic acid were used as de-structuring agents for SA and CS, respectively. The chemical structures, thermal stability, phase morphology, mechanical properties, water resistance, film opacity, film color, and soil burial test of thermo-compressed SA/CS films were investigated. The results indicate that intermolecular interactions in polyelectrolyte complexes in SA/CS blends were detected. Blending with CS improved the thermal stability of SA-based films. The SA/CS films showed excellent phase compatibility between SA and CS. The addition of CS improved the tensile properties of the SA-based films. The incorporation of CS in SA films resulted in enhanced water resistance and opacity and a decrease in biodegradability under soil burial. Thermo-compressed SA/CS films show promise for development and increased production capacity. These films can be tailored by varying the SA/CS ratios to display different properties. This versatility makes them suitable for a range of sustainable and diverse applications, including wound dressing, drug delivery, biosorbents, and packaging.

本文首次采用热压法制备了海藻酸钠/壳聚糖(SA/CS)共混膜。甘油和乳酸分别作为SA和CS的去结构剂。研究了热压SA/CS薄膜的化学结构、热稳定性、相形态、力学性能、耐水性、成膜不透明度、成膜颜色和土埋试验。结果表明,在SA/CS共混物中检测到多电解质配合物的分子间相互作用。与CS共混提高了sa基薄膜的热稳定性。SA/CS薄膜具有良好的相相容性。CS的加入提高了sa基薄膜的拉伸性能。CS在SA膜中的掺入增加了膜的耐水性和不透明度,降低了膜在土壤掩埋下的生物降解性。热压SA/CS薄膜显示出发展和提高生产能力的希望。这些薄膜可以通过改变SA/CS比率来定制,以显示不同的性能。这种多功能性使它们适用于一系列可持续和多样化的应用,包括伤口敷料,药物输送,生物吸附剂和包装。
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引用次数: 0
Correction: Yu, C.; Song, Y.S. Characterization of Phase Change Materials Fabricated with Cross-Linked Graphene Aerogels. Gels 2022, 8, 572. 更正:Yu, C.;宋玉生。用交联石墨烯气凝胶制备相变材料的表征。盖尔斯2022,8,572。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-08 DOI: 10.3390/gels12010059
Chengbin Yu, Young Seok Song

In the original publication [...].

在原出版物中[…]。
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引用次数: 0
A Novel Polyvinyl Alcohol/Salecan Composite Hydrogel Dressing with Tough, Biocompatible, and Antibacterial Properties for Infected Wound Healing. 一种新型聚乙烯醇/Salecan复合水凝胶敷料,具有韧性、生物相容性和抗菌性能,用于感染伤口愈合。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-08 DOI: 10.3390/gels12010060
Jiayu Li, Can Li, Qi Zhang, Zhenhao Rao, Qinghuan Meng, Miao Li, Juan Dai, Ke Deng, Pengfei Chen

Polysaccharide-based wound dressings face challenges in mechanical properties and effective wound repair for infected wound surfaces. This study presents a novel polyvinyl alcohol (PVA)/Salecan (Sal) composite hydrogel dressing with high toughness, biocompatibility, and wound healing capabilities, developed using an interpenetrating polymer network strategy. The primary network was formed through electrostatic interactions between polydopamine (PDA) and biocompatible polysaccharide Salecan, followed by incorporation of AgNO3, which was in situ reduced to silver nanoparticles within the hydrogel. PVA was introduced as a secondary matrix, further reinforcing the hydrogel network through cyclic freeze-thawing. The resulting hydrogel exhibited a tensile strength of 0.31 MPa, an elongation at break of 158.9%, and a toughness of 31.16 J·m-2, demonstrating enhanced mechanical performance compared to both Salecan/PDA and previously reported Salecan/Fe3+ hydrogel. Co-culture experiments showed the hydrogel's strong antibacterial effects, inhibiting 80.1% of Escherichia coli (E. coli) and 99.5% of Staphylococcus aureus (S. aureus). Fibroblast culture tests confirmed its excellent cytocompatibility. In vivo studies on infected wounds showed nearly complete healing in the S. aureus + hydrogel group within 12 days. Quantitative immunohistochemical analysis of CD31 revealed that hydrogel treatment significantly upregulated CD31 expression, indicating enhanced neovascularization. Complementary Western blot analysis further demonstrated that hydrogel-treated groups exhibited a marked downregulation of pro-inflammatory factors alongside CD31 upregulation. In summary, the PVA/Sal-based hydrogel represents a valuable strategy for reducing inflammation and promoting regeneration in the management of infected wounds.

基于多糖的创面敷料在机械性能和有效修复感染创面方面面临挑战。本研究提出了一种新型聚乙烯醇(PVA)/Salecan (Sal)复合水凝胶敷料,具有高韧性、生物相容性和伤口愈合能力,采用互穿聚合物网络策略开发。初级网络是通过聚多巴胺(PDA)和生物相容性多糖Salecan之间的静电相互作用形成的,随后加入AgNO3, AgNO3在水凝胶中原位还原为银纳米颗粒。引入聚乙烯醇作为二次基质,通过循环冻融进一步强化水凝胶网络。所得水凝胶的抗拉强度为0.31 MPa,断裂伸长率为158.9%,韧性为31.16 J·m-2,与Salecan/PDA和之前报道的Salecan/Fe3+水凝胶相比,力学性能有所提高。共培养实验表明,水凝胶具有较强的抗菌作用,对大肠杆菌(E. coli)和金黄色葡萄球菌(S. aureus)的抑制率分别为80.1%和99.5%。成纤维细胞培养试验证实其具有良好的细胞相容性。对感染伤口的体内研究表明,金黄色葡萄球菌+水凝胶组在12天内几乎完全愈合。CD31的定量免疫组织化学分析显示,水凝胶处理显著上调CD31的表达,表明新生血管增强。补充Western blot分析进一步表明,水凝胶处理组显示出促炎因子的显著下调和CD31的上调。总之,PVA/ sal为基础的水凝胶代表了减少炎症和促进感染伤口再生的有价值的策略。
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引用次数: 0
Comparable Effectiveness of Novel and Commercial Saliva Substitute Gels in Dental Patients Experiencing Xerostomia: A Randomized, Double-Blind Crossover Trial. 一项随机、双盲交叉试验:新型和商业唾液替代凝胶在口腔干燥患者中的有效性比较。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-08 DOI: 10.3390/gels12010061
Supanee Thanakun, Wipaporn Kajornwongwattana, Boonruthai Wattanaurai, Chanchanan Kobutr, Chayapa Parnnium, Kankanit Konta, Pornpailin Vasusopon, Supitchaya Lomloy, Thanapat Songsak, Suchada Vuddhakanok

Saliva substitutes are the standard treatment for dry mouth. This study aimed to evaluate the clinical effectiveness of a novel artificial saliva gel (RSU gel) compared with a commercial product (GC Dry Mouth Gel®). A randomized, double-blind, two-phase crossover clinical trial was conducted with 37 participants with xerostomia. In the short-term phase, oral wetness, xerostomia scores, and clinical score of oral dryness (CSOD) were assessed up to 60 min after a single gel application. In the short-term repeated-use phase, each gel was applied 4 times daily for 14 days, separated by a 14-day washout period. The same parameters, including patient satisfaction and adverse events, were re-evaluated. Data were analyzed using generalized linear mixed models and generalized estimating equations. Both the RSU and GC Dry Mouth Gel® significantly improved oral wetness immediately after a single application. No significant difference was observed for the RSU gel relative to the GC Dry Mouth Gel® for oral wetness (OR = 1.01, 95% CI 0.98, 1.04, p = 0.248), xerostomia score (OR = 1.10, 95% CI 0.42, 2.88, p = 0.661), or CSOD (OR = 0.95, 95% CI 0.58, 1.55, p = 0.765) at 60 min. After 14 days of use, oral wetness increased significantly in both groups (2.94%, 95% CI 0.30%, 5.76%, p = 0.030) and did not differ significantly between the two products (p = 0.110). The xerostomia scores and CSOD also significantly improved, independent of product type (OR = 7.21, 95% CI 2.56, 20.34, p < 0.001, and OR = 2.82, 95% CI 1.50, 5.32, p = 0.001, respectively). The participants reported high satisfaction and acceptable taste, and no adverse effects were detected in those using the RSU gel throughout the study. Its lower cost and local availability make it a practical option for xerostomia management, particularly in populations with limited access to commercial saliva substitutes.

唾液替代品是治疗口干的标准方法。本研究旨在评估一种新型人工唾液凝胶(RSU凝胶)与商业产品(GC口干凝胶®)的临床效果。一项随机、双盲、两期交叉临床试验对37名口干症患者进行了研究。在短期阶段,在单次凝胶应用后60分钟内评估口腔湿润度、口干评分和口腔干燥临床评分(CSOD)。在短期重复使用阶段,每种凝胶每天使用4次,持续14天,中间有14天的洗脱期。同样的参数,包括患者满意度和不良事件,重新评估。采用广义线性混合模型和广义估计方程对数据进行分析。RSU和GC口干凝胶®在单次使用后立即显着改善口腔湿润度。60分钟时,RSU凝胶与GC口干凝胶®在口腔湿润度(OR = 1.01, 95% CI 0.98, 1.04, p = 0.248)、口干评分(OR = 1.10, 95% CI 0.42, 2.88, p = 0.661)和CSOD (OR = 0.95, 95% CI 0.58, 1.55, p = 0.765)方面均无显著差异。使用14天后,两组口腔湿润度均显著增加(2.94%,95% CI 0.30%, 5.76%, p = 0.030),两组产品间无显著差异(p = 0.110)。与产品类型无关,口干评分和CSOD也有显著改善(OR = 7.21, 95% CI 2.56, 20.34, p < 0.001); OR = 2.82, 95% CI 1.50, 5.32, p = 0.001)。参与者报告了高满意度和可接受的味道,并且在整个研究中使用RSU凝胶的人没有发现任何不良反应。其较低的成本和当地可用性使其成为口干症治疗的实用选择,特别是在无法获得商业唾液替代品的人群中。
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引用次数: 0
Supramolecular Organogels Based on Cinnarizine as a Potential Gastroretentive System: In Vitro and In Silico Simulations. 基于肉桂碱的超分子有机凝胶作为潜在的胃保留系统:体外和计算机模拟。
IF 5.3 3区 化学 Q1 POLYMER SCIENCE Pub Date : 2026-01-08 DOI: 10.3390/gels12010058
Masar Basim Mohsin Mohamed, Ghaidaa Hameed, Mohanad Naji Sahib, Zainab Kadoori, Hasanain Shakir Mahmood, Aqeel Abdulridha Khudhair

(1) Background: Gastroretentive systems are an interesting option for enhancing the bioavailability of weak bases and poorly soluble drugs. The aim of this study was to formulate supramolecular organogels based on cinnarizine (CIN) as a potential gastroretentive system. (2) Methods: The organogels were prepared with different oils in different ratios. Thereafter, their pharmaceutical characteristics and in vitro gastric retention were evaluated through in vitro and in silico simulations. (3) Results: Organogels with different proportions of CIN to oils were successfully obtained. The DSC thermal analysis results demonstrated that all organogels showed gel-sol temperature transitions. The frequency sweep test verified that all organogels presented frequency-independent behavior. Optical imaging revealed longitudinal spherulites of the 1:4 CIN in organogels in all oils. The CIN organogels in all oils (1:4) were observed to float in gastric media during the entire release study. The pharmacokinetic parameters of CIN in peppermint oil (1:4) revealed a close Cmax value to that of the 25 mg immediate-release tablet, but a different AUC. (4) Conclusions: The organogels in all oils floated throughout the release study, establishing their potential as a gastroretentive system. Furthermore, these dosage forms were assessed as a gastric-controlled system through in silico simulations, which enabled prediction of their pharmacokinetic parameters.

(1)背景:胃保留系统是提高弱碱和难溶性药物生物利用度的一个有趣的选择。本研究的目的是制备基于肉桂碱(CIN)的超分子有机凝胶作为潜在的胃保留系统。(2)方法:以不同比例的油脂制备有机凝胶。然后,通过体外和计算机模拟评估它们的药物特性和体外胃潴留。(3)结果:成功获得了不同CIN与油脂比例的有机凝胶。DSC热分析结果表明,所有有机凝胶都表现出凝胶-溶胶的温度转变。频率扫描测试证实所有的有机凝胶都表现出与频率无关的行为。光学成像显示所有油的有机凝胶中存在1:4 CIN的纵向球粒。在整个释放研究过程中,观察到所有油中的CIN有机凝胶(1:4)漂浮在胃介质中。薄荷油(1:4)中CIN的药动学参数与25 mg速释片的Cmax值接近,但AUC不同。(4)结论:在整个释放过程中,所有油中的有机凝胶都在漂浮,这表明了它们作为胃保留系统的潜力。此外,这些剂型通过计算机模拟作为胃控制系统进行评估,从而能够预测其药代动力学参数。
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引用次数: 0
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Gels
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