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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2025 · IF 4.9

Formulation of pH-sensitive ZIF-8 (MOF) impregnated amino-chitosan biocomposite beads for sustained release of 5-fluorouracil

Ahmed M. Omer,Eman M. Abd El-Monaem,Heba S. Hassan,Mahmoud A. Elmeligy,Angela Kleinová,Abdelazeem S. Eltaweil,Abolfazl Heydari

pH-sensitive carriers have emerged as an optimal choice for the oral administration of anticancer drugs, exhibiting the desired release performance. This study aims to develop biocomposite beads for the sustained release of the anticancer drug 5-fluorouracil (5-FU). Here, 5-FU was encapsulated within a ZIF-8 metal-organic framework (MOF), which was subsequently impregnated into amino-chitosan beads. The resulting Am-CS@ZIF-8 biocomposite beads were characterized for their chemical structure, surface morphology, elemental composition, crystallinity, surface charges, and mechanical properties utilizing Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD), zeta potential analysis, and a texture analyzer, respectively. The developed beads exhibited a textured surface, denser composition, and a positively charged surface with a maximum zeta potential of +12.4 at pH 7.4. In comparison to Am-CS beads, the Am-CS@ZIF-8 biocomposite beads demonstrated superior mechanical properties, achieving a maximum stress value of 5.668 MPa compared to the 1.874 MPa recorded for pure Am-CS beads. pH sensitivity was assessed through the investigation of water uptake behavior at pH 1.2 and pH 7.4. The Am-CS@ZIF-8 biocomposite beads demonstrated a high encapsulation efficiency of approximately 81.6 % for 5-FU. They exhibited pH-responsive release behavior, with only 17 % of the drug released at pH 1.2 after 2 h and a sustained release of 52 % at pH 7.4 over 24 h. The release mechanism was predominantly governed by Fickian diffusion, as closely fitted by the Peppas-Sahlin kinetic model. The formulated carrier confirmed its biodegradability under enzymatic physiological conditions, suggesting its potential applicability as an effective system for the oral delivery of anticancer drugs.

CAS / MDL: 10196-18-6 693-98-1
研究领域: 药剂学 · 生物材料学
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2026 · IF 4.9

Berberine hydrochloride sustained-release solid dispersion alleviates acetic acid-induced ulcerative colitis in rats by modulating intestinal flora

Dan Liu,Yaxian Yang,Jiacheng Meng,Honglei Guo,Xinchao Shi,Xin He,Xinghua Zhao

Berberine hydrochloride (BH) is a natural alkaloid compound known for its effectiveness in treating ulcerative colitis (UC). However, the clinical application of BH was limited due to the short half-life and rapid metabolism in body. Therefore, a sustained-release solid dispersion (SD) of BH was prepared using different proportions of ethyl cellulose as carrier. PXRD, DSC, and FT-IR analyses confirmed the transition of BH from a crystalline to amorphous state. This transformation significantly improved the drug release rate of BH and the pharmacokinetic characteristics in rats. The in vitro dissolution results showed that the cumulative dissolution rates of SD (1:4) were 29.47 % and 93.88 % at 10 min and 24 h respectively, and the in vivo study demonstrated that the t 1/2 (0−24) and the AUC 0−24 of SD (1:4) were 5.52 times and 6.30 times greater than those of BH, respectively, indicating SD (1:4) superior sustained-release effect compared to BH. In the acetic acid (AA)-induced UC rat model, SD treatment alleviates UC by increasing colon length, improving pathological damage, and reducing both the DAI score and levels of inflammatory factors. The 16S rRNA sequencing results indicated that SD treatment reshaped gut microbiota in rats with UC, particularly increasing the abundance of probiotic Romboutsia and decreasing the abundance of pathogenic bacteria Erysipelotrichaceae , Clostridia_UCG_014 and Dubosiella . In conclusion, we successfully prepared a sustained-release SD of BH and demonstrated that its therapeutic effect on UC is achieved by regulating intestinal microbiota.

CAS / MDL: 9004-57-3
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2018 · IF 5.091

Synthesis, characterization and working mechanism of a novel sustained-release-type fluid loss additive for seawater cement slurry

Lei Cao,Jintang Guo,Jianhua Tian,Yang Xu,Miaomiao Hu,Chun Guo,Meiyu Wang,Jinjie Fan

Synthetic polymer fluid loss additive (FLA), an important type of admixture, was broadly applied in modern well cementation. However, the filter loss volume and fluidity of cement pastes containing polymer-FLA would deteriorate remarkably when sea water was used in mixing slurries instead of fresh water. In this study, a novel sustained-release-type fluid loss additive(S-FLA) was synthesized by means of anion-exchange intercalation reaction between an anionic type-copolymer and a calcium/aluminum type-Layered Double Hydroxide (Ca/Al-LDH). Based on the fluidity and compressive strength of experiments, it was found that in seawater mixing conditions, this composite material not only utilized its sustained release effect to significantly improve retention fluidity performance, but also the seed crystal effect of the Ca/Al-LDH effectively alleviated the declining in compressive strength of the slurries caused by the carboxyl group in the polymer. More interestingly, the realization of the slow release function increased actual adsorption capacity of the anionic polymer on the surface of cement hydrated particles, which made its controlling water loss effect was also better than that of the conventional FLA. The above advantages of this hybrid materials created the possibility to surmount the negative effect of electrolytes present in seawater, so as to provide some useful references for its practical application in the offshore well cement.

研究领域: 石油工程 · 材料科学 · 水泥化学 · 聚合物纳米复合材料 · 油气井固井
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Biomaterials Advances · 2026 · IF 6.7

A composite sustained-release system with immunomodulatory and synergistic osteogenic differentiation effects for repairing inflammatory alveolar bone defects

Tianyang Lv,Yuzhu Chen,Ning Li,Yumin Heng,Xiaoning Su,Yuping Zhang,Yang Jiang,Yayuan Guo,Kaijin Hu

Inflammation-associated alveolar bone defects, such as periodontitis, remain a major clinical challenge, as persistent inflammatory microenvironments severely impair bone regeneration and tissue repair. The cathepsin family plays a significant role in inflammatory responses and the clinicopathological process of periodontitis. Studies have shown that the cathepsin K inhibitor, odanacatib (ODN), can repair inflammatory bone defects. However, its administration via oral or local delivery fails to maintain sustained drug concentrations within the periodontal pocket. Here, we report a gel sustained-release system that coordinates immunomodulation with osteogenic induction to overcome inflammation-impaired bone regeneration. We utilized the emulsification-solvent evaporation method to prepare ODN-loaded poly(lactic- co -glycolic acid) (PLGA) microspheres (ODN-MS). These microspheres were thoroughly mixed with gelatin methacryloyl (GelMA) to form a gel composite sustained-release system (ODN-MS-Gel). The ODN-MS-Gel prepared has excellent photopolymerization properties and can achieve sustained release of ODN for a long time, thus enabling local and targeted drug delivery within the periodontal pocket. In vitro, ODN-MS-Gel not only promoted the proliferation, adhesion, and migration of BMSCs but also induced macrophage polarization toward the M2 phenotype, demonstrating a significant ability to promote osteogenic differentiation under inflammatory conditions. Furthermore, this study also distinguished the differences between the two situations of continuous release and non-continuous release and revealed the potential role of macrophage immune regulation in conjunction with stem cell osteogenic differentiation. In vivo, ODN-MS-Gel gradually degraded over time, exhibiting excellent long-term biocompatibility. By using a rat periodontitis model, it was demonstrated that ODN-MS-Gel could reduce inflammatory expression in periodontal tissues under inflammatory conditions and repair the alveolar bone defect to 77% of its normal height. In conclusion, ODN-MS-Gel achieves anti-inflammatory and bone repair effects with a single drug, representing a promising biomaterial for treating inflammatory alveolar bone defects.

CAS / MDL: 75-09-2 9003-20-7
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PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY · 2026 · IF 2.9

Development of an enteric-coated sustained-release powder for oral suspension of paroxetine Based on cation exchange resin

Hongfei Liu,Zhiguo Sun,Xiaoya Xie,Yujing Huang,Caleb Kesse Firempong,Yingshu Feng,Haibing He,Guoqing Zhang,Xin Lv,Zhigang Xing

Paroxetine (PX) is a first-line selective serotonin reuptake inhibitor (SSRI) for major depressive disorder. Currently, the enteric-coated sustained-release tablet represents the dominant clinical standard due to its ability to mitigate gastric irritation and ensure sustained release in the intestine to reduce adverse effects. However, these tablets must be swallowed intact, making them unsuitable for patients with dysphagia; manipulation (e.g. crushing or chewing) destroys the functional coating, leading to dose dumping and unpredictable systemic exposure. To address these critical therapeutic gaps, this study developed a novel reconstitutable enteric-coated sustained-release powder using ion-exchange resin technology for oral suspension of PX. PX was loaded onto Amberlite® IRP88 and subsequently coated with cellulose acetate phthalate via fluidized-bed processing to inhibit gastric release while enabling prolonged release in the intestine. The optimized formulation (PX@CM) demonstrated high drug entrapment efficiency and a robust zero-order release profile in simulated intestinal fluid. In vivo pharmacokinetic studies in rats confirmed its potential clinical advantages: compared to commercial immediate-release (IR) oral tablets, the suspension significantly lowered Cmax (0.24 vs. 0.44 μg/mL) and prolonged Tmax (6.67 vs. 4.00 h). These pharmacokinetic improvements provide a ‘peak-blunting’ effect that suggests a potential to minimize concentration-dependent side effects. Consequently, this formulation emerges as a promising, patient-centric alternative for vulnerable populations requiring long-term antidepressant therapy.

CAS / MDL: 84-66-2
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SEPARATION AND PURIFICATION TECHNOLOGY · 2026 · IF 9.1

In situ long-acting ammonium removal from groundwater using a modified sustained-release candle-constructed SO4•-–Cl- system

Kaijie Pei,Hang Lyu,Ai-Bo Jia,Rong Zhong,Chuping Chang,Xiaosi Su

Ammonium in groundwater hampers sustainable water use, calling for efficient, stable in-situ remediation technologies. In this study, we design a novel coated sustained-release candle (CSRC) that contains peroxymonosulfate (PMS) and chloride ions (Cl − ). The aim is to construct an in situ long-acting SO 4 • − –Cl − oxidation system for groundwater ammonium removal. The outer coating effectively addressed the issue of “burst release” of paraffin-based sustained-release materials during the initial release stage. It also prolonged the effective release period and guaranteed the synchronous PMS and Cl − release. Systematic static release experiments revealed the critical roles of the CSRC diameter and reagent-to-paraffin mass ratio in regulating the release profiles. Column experiments demonstrated that CSRC deployment within an injection well significantly enhanced the reagent release compared to direct embedding. In addition, the groundwater flow rate exerted no influence on the CSRC release. The long-term operation confirmed the sustained generation of Cl•/ClO• and effective ammonium removal along the flow path. Moreover, three-dimensional tank experiments under varying hydraulic gradients and screen lengths showed that increases in the hydrodynamic conditions and well-screen length markedly improved the radial penetration and vertical dispersion of reagents in the aquifer and enabled the effective ammonium removal for up to 56 days. Collectively, this work presents a feasible and engineered strategy by adjusting the reagents ratio, diameter, and CSRC length that achieves the stable, long-term in-situ chemical oxidation of ammonium in groundwater. This work offers theoretical insights and practical guidance for applying sustained-release material-based remediation systems in the field.

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Polymers · 2026 ·Vol. 18 ·期 9 ·1087 · IF 5.8

pH-Responsive Sodium Alginate/Carboxymethyl Cellulose Hydrogels for Enhanced Stability and Gastrointestinal Sustained Release Delivery of Chlorogenic Acid

Lanxin Ke,Linqing Qian,Yincong Chen,Yanchen Ren,Meiqi Shi,Kun Wang,Ting Wang

Chlorogenic acid (CGA) is a natural polyphenol with various biological activities, but its poor stability and premature release in the gastrointestinal tract limit oral application. Herein, a pH-responsive bilayer hydrogel based on sodium alginate (SA) and carboxymethyl cellulose (CMC) was developed to enhance the gastrointestinal stability and controlled release of CGA. CGA-loaded SA hydrogels were prepared via Ca 2+ -induced ionotropic gelation, followed by CMC coating to form a bilayer structure. The SA/CMC hydrogels showed a drug loading capacity of 15.2–16.7% and pH-dependent swelling behavior. In vitro release studies revealed that the bilayer hydrogel suppressed CGA release in simulated gastric fluid (pH 1.2), with a cumulative release of approximately 30%, while enabling sustained release in simulated intestinal fluid (pH 6.8), reaching about 70% within 10 h. Release kinetics indicated that CGA release was controlled by Fickian diffusion under acidic conditions and by a diffusion-polymer relaxation mechanism under intestinal conditions. Moreover, encapsulation in the SA/CMC hydrogel improved the thermal, light, and pH stability of CGA while maintaining its antioxidant activity and biocompatibility. These results indicate that SA/CMC bilayer hydrogels provide a promising strategy for stabilized gastrointestinal delivery of chlorogenic acid.

✓ 已验证 DOI PubMed 高影响因子
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Biomaterials Science · 2026 · IF 6.1

Photothermal self-adjuvant porous microneedles for self-healing encapsulation and sustained release of antigens to improve adaptive immunity

Xin Wang,Zhiming Li,Jiahui Fu,Xueyu Wen,Zhenni Chen,Shaohua Li,Tianqi Liu,Fei Jia,Hao Chang

Effective vaccination hinges on overcoming persistent challenges in delivery site optimization, sustained antigen release, maintaining antigen integrity, and providing safe adjuvanticity. Here, we report a photothermal self-adjuvant porous microneedle (PSAPMN) patch as an all-in-one platform that comprehensively addresses these issues. Fabricated from polylactic-co-glycolic acid (PLGA) and polydopamine nanoparticles (PDA-NPs), the microneedles possess a unique interconnected porous architecture, enabling exceptionally mild, diffusion-based antigen loading. Upon brief near-infrared (NIR) irradiation, the photothermal effect of PDA-NPs not only accelerates pore self-healing for complete antigen encapsulation within 20 minutes but also creates a biodegradable depot for sustained intradermal release over 15 days. Crucially, the localized NIR-generated heat simultaneously serves as a potent physical adjuvant, promoting dendritic cell activation. In vivo, this integrated strategy elicits significantly more potent and durable antigen-specific immunity and immunological memory than conventional methods. This work presents a versatile platform for developing next-generation vaccines by synergistically solving multiple critical delivery challenges in a single device.

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Foods · 2026 ·Vol. 15 ·期 16 ·2924 · IF 6

TEMPO-Oxidized Bacterial Cellulose-Stabilized Clove Essential Oil Pickering Emulsions for Sustained-Release Sodium Alginate Active Packaging Films

Fengge Yu,Jieying Fan,Xiangying Liu,Hongrui Sun,Jialin Zhang,Lining Kang

Developing biodegradable active packaging films that combine mechanical reinforcement, barrier improvement, antibacterial activity, and controlled release of natural antimicrobials remains challenging. Here, TEMPO-oxidized bacterial cellulose (TOBC) was used to stabilize clove essential oil (CEO) Pickering emulsions, which were incorporated into sodium alginate (SA) matrices. The effects of TOBC concentration on emulsion stability and emulsion loading on film-forming solutions, film structure, mechanical performance, barrier properties, antioxidant and antibacterial activities, and CEO release were evaluated. The emulsion stabilized with 0.7 wt% TOBC showed good visual stability after 30 days and was selected for film preparation. Moderate incorporation of the TOBC-stabilized CEO Pickering emulsion improved SA film performance, with SA-E10 showing the best overall balance. SA-E10 reached a tensile strength of 38.56 ± 1.66 MPa and an elongation at break of 10.27%, while the moisture content decreased from 36.48 ± 2.32% to 27.93 ± 0.46%. The films also showed enhanced UV-shielding capacity and lower water vapor permeability. Antioxidant activity increased with emulsion loading, reaching 71.43 ± 2.55% for DPPH and 83.66 ± 1.49% for ABTS. Film-coated paper disks showed visible inhibition zones againstEscherichia coliandStaphylococcus aureus. Compared with direct CEO incorporation, the Pickering emulsion system delayed CEO release, indicating potential for sustained-release active packaging.

CAS / MDL: 56-81-5 7385-67-3
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Journal of Aquatic Food Product Technology · 2025 · IF 1.3

The Sustained-Release Oxygen Granule Preparation and Its Application in the Transportation of Live Sea Cucumber Apostichopus Japonicus

Yimeng Li,Jinghe Sun,Yan Zhou,Liming Sun,Jingfeng Yang

This study developed a sustained-release oxygen granule (SOG) to improve the transport of live sea cucumbers. During 8-day storage, SOG provided continuous oxygen while keeping seawater pH stable at 7.10 without affecting salinity. Compared to controls with added air, SOG significantly better preserved sea cucumber quality, delaying tissue autolysis and maintaining superior appearance and texture for up to 7 days. Furthermore, SOG prevented hypoxic stress, as evidenced by stable activities of key enzymes (AKP, ACP, SDH, LDH), supporting the organisms’ immune response throughout the storage period.

CAS / MDL: 110-17-8
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2022 · IF 5.062

Transdermal drug delivery system of domperidone sustained-release coated microsphere gels: In vitro characterization and in vivo evaluation

Wantong Zhao,Lin Ma,Song Guo,Jia Yan Liu,Jingshu Piao,Mingguan Piao

Domperidone (DMP) is an effective peripheral D2 dopamine receptor antagonist . It is commonly used in the treatment of nausea and vomiting caused by Parkinson's disease . An oral preparation, which is rapidly absorbed after administration, and reaches a peak plasma concentration within 15–30 min, is commonly used. However, owing to the “first-pass effect” of liver metabolism and intestinal wall metabolism, the oral bioavailability of domperidone is low, and the action period is long. Therefore, in the present study, spray drying and emulsion solvent evaporation were combined to prepare a coated microsphere preparation with sustained release effect, and a gel matrix was selected to prepare a sustained-release coated microsphere gel for transdermal drug delivery. The pharmacokinetic results showed that the transdermal sustained-release coated microsphere gel effectively increased the Tmax, Cmax, T 1/2 , and AUC compared with those of an oral DMP group ( P  < 0.05), and the relative bioavailability was 3.2 times that of the oral DMP group. This indicates that the preparation was able to ameliorate the problems associated with a traditional oral DMP formulation. Therefore, the present study may provide a theoretical basis for the transdermal delivery of DMP sustained-release microspheres.

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JOURNAL OF MOLECULAR LIQUIDS · 2022 · IF 6.633

Dual-targeting magnetic fluorescent mesoporous organosilicon hollow nanospheres for gambogic acid loading, sustained release and anti-tumor properties

Ziling Chang,Yuxiang Yang,Bo Zhao,Huafei Li,Yuxia Guan,Yi Zhao,Hongming Yuan,Chaoying Ni

Hydrophilic mesoporous organosilica nanoparticles (HMNPs) were synthesized by introducing Fe 3 O 4 on the basis of mesoporous organosilicon nanoparticle hollow spheres as a drug carrier. N- and S- doped graphene quantum dots (NS-GQDs) and polyethylenimine (PEI) were grafted onto the surface of HMNPs. Finally, two types of composite mesoporous particles, HMNPs-NS-GQDs-PEI-HA and HMNPs-NS-GQDs-PEI-FA which can enter VX2 cells for fluorescence confocal imaging, were further modified by targeting ligand hyaluronic acid (HA) and folic acid (FA). The heteroatoms of NS-GQDs have intelligent functional effects, which can not only improve the photoluminescence performance of GQDs, but also generate conjugated quantum dots with GA, so as to synergistically improve the drug effectiveness. Under illumination by near-infrared (NIR) radiation, gambogic acid (GA)-loaded HMNPs was promoted to the sustained release of gambogic acid. The loading and sustained release of the anticancer drug GA on the compound mesoporous particles were studied. The cytotoxicity and antitumor properties of the compound mesoporous particles were investigated by both in vitro cell experiments and in vivo experiments in mice. The results showed that HMNPs-NS-GQDs-PEI-HA and HMNPs-NS-GQDs-PEI-FA have desired fluorescence and magnetic properties for cell fluorescence imaging and magnetic targeting of cancer cells. Both of composite mesoporous particles have desired loading capacity on GA and pH-responsive drug release behavior as well as low cytotoxicity and good biocompatibility. The cell survival rate of HMNPs-NS-GQDs-PEI-HA and HMNPs-NS-GQDs-PEI-FA loaded with GA was only 7.69% and 8.71%, respectively, after 24 h, which can effectively induce the apoptosis of VX2 cells. Tumor experiments in mice demonstrated that HMNPs-NS-GQDs-PEI-HA inhibits tumor growth and exhibits magnetic targeting function.

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