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AAPS PHARMSCITECH · 2025 ·Vol. 27 ·期 1 ·52 · IF 4

Sustained-release Drug Delivery System of Trazodone Hydrochloride Based on Electrospray Technology: Preparation, Characterization, In vitro and In vivo Evaluation

Wang Chengwei,Wang Haiqiao,Adu-Frimpong Michael,Zou Zhihui,Jin Zhou,Lu Peiqi,Liu Zhenrong,Tian Haojie,Xu Ying,Yang Kailun,Yu Jiangnan,Xu Ximing,Zhu Yuan

Electrospray technology is a process capable of forming monodisperse drug nano/microparticles with enhanced solubility or sustained-release effects. This study aimed to fabricate a sustained-release drug delivery system containing trazodone hydrochloride (TZN-SRDDS) by combining electrospray technology with functional carriers (Soluplus®, Carbopol 940, HPMC K4M, and Lecithin) for solubility improving, drug release prolonging and bioavailability enhancing. The optimized TZN-SRDDS exhibited a spherical morphology, with a particle size of (3.456 ± 0.448) μm, a polydispersity index (PDI) of (0.456 ± 0.024), and a zeta potential of (-17.291 ± 2.351) mV. This system showed a high encapsulation efficiency (97.12 ± 1.82%) and maintained good stability for up to 30 days. In vitro release studies indicated that TZN-SRDDS followed first-order kinetics in pH 1.2 hydrochloric acid solution and the Higuchi model in pH 6.8 phosphate-buffered saline (PBS), with the cumulative release rate increased to (80.81 ± 4.26%); both release profiles exhibited a certain sustained-release effect. Cytotoxicity assays confirmed that TZN-SRDDS was non-toxic at concentrations below 2.6 mg/mL, and the formulation showed a relatively sustained cellular uptake effect. Pharmacokinetic studies in rats showed that the time to reach peak concentration (T max ) of TZN-SRDDS was extended from 0.25 h to 1 h, its half-life (t 1/2 ) was increased from (1.15 ± 0.17) h to (6.71 ± 0.39) h, resulting in a relative bioavailability of 374.64%. This study achieved the synergistic goals of drug solubilization, sustained-release delivery, and enhanced bioavailability. It provides new technical references for the development of pH-sensitive drug formulations using electrospray technology and also expands the research on the development of sustained-release formulations of trazodone hydrochloride.

研究领域: 药剂学 · 药物递送系统 · 纳米技术 · 生物药剂学 · 药代动力学 · 材料科学 · 控释制剂
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Polymer Chemistry · 2016 ·Vol. 7 ·期 44 ·6779-6788 · IF 5.687

Preparation of glucose responsive polyelectrolyte capsules with shell crosslinking via the layer-by-layer technique and sustained release of insulin

Dongjian Shi,Maoshuang Ran,He Huang,Li Zhang,Xiaojie Li,Mingqing Chen,Mitsuru Akashi

Phenylboronic acid based polymer capsules were confirmed to have glucose sensitivity. In order to investigate the effect of the capsule structural stability on the glucose sensitivity and sustained release of insulin, bio-based capsules with a glucose-responsive property were fabricated based on alginate (Alg) and chitosan oligosaccharide (CS) polyelectrolytes. Chitosan oligosaccharide-g-3-carboxyphenylboronic acid (CS-g-CPBA) that has glucose-responsive properties was firstly synthesized by grafting CPBA to CS. (Alg/CS-g-CPBAm)n capsules were then prepared by layer-by-layer (LBL) processes of Alg and CS-g-CPBAmvia electrostatic interaction on silica nanoparticles (SiO2) and subsequently removing the SiO2 templates. Capsules could be further crosslinked and kept more stable by chelating calcium ions (Ca2+). The sizes and morphologies of bio-polymer capsules were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The results showed that the (Alg/CS-g-CPBAm)n capsules had a good stability by increasing the multilayers and cross-linking with Ca2+. The size of the capsules increased rapidly with increasing the glucose concentration, due to the formation of a hydrophilic phenylboronic acid-glucose complex and swelling of the capsules. Insulin was encapsulated in the capsules, and the encapsulation efficiency was more than 65%. A cumulative release of insulin was observed from the capsules after being exposed in glucose solutions with various levels. The release speed of insulin reduced after it was cross-linked with Ca2+, which was induced by increasing the tightness of the inner layer. The (Alg/CS-g-CPBAm)n capsules have biocompatibility which was confirmed by cell viability on treatment with mouse embryonic fibroblast through the method of MTT.

研究领域: 生物材料学 · 药物递送系统 · 高分子化学
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APPLIED SURFACE SCIENCE · 2026 · IF 6.6

Synthesis and characterization of spherical C/ZnO/polydopamine composites as carriers for 5-fluorouracil: a focus on sustained release performance

Mingli Yue,Zhikuan Feng,Long Gao,Ying Fu,Fei Ye

Drug delivery systems utilize micro-nanomaterials as drug carriers, encapsulating drugs within micro-nanoparticles and releasing them to target tissues or cells via specific pathways. This technology enhances drug stability, prolongs drug retention time in the body, and reduces damage to healthy tissues. This study successfully synthesized novel carbon-doped zinc oxide (C/ZnO) micro-nanomaterials and employed polydopamine (PDA) for surface modification, resulting in the construction of C/ZnO/PDA carriers. Experimental results demonstrate that PDA modification significantly enhances the drug delivery performance of the material. This composite material exhibits a 5-Fu loading efficiency of 37.8%, representing a 1.15-fold increase compared to unmodified C/ZnO. In vitro release tests demonstrate sustained drug release characteristics, showing a 1.62-fold increase over the unmodified system. In addition, these medicine particles significantly enhanced the indicators of antibacterial and bactericidal efficacy. In vitro cell experiments also confirmed that the drug carrier can enhance the lethality of the drug against HepG2 cells. Research on the binding energy between the carrier and the drug revealed that PDA modification promotes drug-carrier binding, resulting in more stable overall adsorption. These findings demonstrate the potential application value of micro-nanoparticle-based targeted drug delivery systems in disease prevention and treatment.

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MICROPOROUS AND MESOPOROUS MATERIALS · 2026 · IF 4.5

A study on a novel MIL-100(Fe)@UREA Nano-Fertilizer with high loading capacity and superior sustained-release performance

Yujing Zhou,Yizhe Yang,Yinqi Sun,Zihao Wang,Hengbo Ding,Kai Liu,Weiguo Zhang,Songke Feng

To overcome the low nitrogen use efficiency (<40%) of conventional urea, this study utilizes the metal–organic framework MIL-100(Fe)—characterized by ultrahigh surface area and tunable mesoporosity—as a promising carrier for nano slow-release fertilizers with enhanced nutrient stability. Fourier transform infrared spectroscopy, thermogravimetric analysis, and Brunauer–Emmett–Teller measurements confirmed that urea was uniformly accommodated within the MOF channels in an amorphous, physically adsorbed state without chemical bonding. High-performance liquid chromatography revealed that loading capacity was primarily determined by the urea-to-MOF mass ratio, whereas loading temperature and duration had negligible effects, enabling precise synthesis control. Orthogonal optimization identified the optimal parameters (mass ratio 1:1, 110°C, 7 h), yielding a urea loading of 59.2% and encapsulation efficiency of 51.8%. Release experiments demonstrated a 22.5-fold extension in release duration compared to pure urea, with 87.6% cumulative release over 180 h governed by Fickian diffusion. Furthermore, physical characterization and bench-scale metering tests verified the granules' mechanical adaptability, achieving stable, continuous discharge comparable to urea. This work validates MIL-100(Fe)@UREA as a high-capacity, mechanically viable platform for sustainable and precision nutrient delivery. These results not only highlight the potential of MIL-100(Fe) in advanced slow-release fertilizer systems but also provide valuable insights for designing efficient and environmentally sustainable nutrient delivery platforms.

CAS / MDL: 64-17-5 7758-02-3
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2020 · IF 5.162

Fabrication of emulsion gel based on polymer sanxan and its potential as a sustained-release delivery system for β-carotene

Zhong Shi,Zhuangzhuang Shi,Mengmeng Wu,Yaqi Shen,Guoqiang Li,Ting Ma

Food-grade emulsion gels have attracted increasing attention in food and drug manufacturing, owing to their potential as novel delivery systems for lipophilic bioactive ingredients. Emulsion gels are structurally either a polymeric gel matrix with incorporated emulsion droplets (emulsion-filled gels), or a network of aggregated emulsion droplets (emulsion particulate gels). In this study, a novel emulsion gel was prepared by formulating an oil-in-water (O/W) emulsion stabilized by sanxan alone, followed by heating and cooling treatment, resulting in a structured solid system. Stable O/W type sanxan emulsion gels (SEGs) were obtained at sanxan concentration >0.5% ( w /w). Fluorescence microscopy results confirmed the adsorption of sanxan on oil droplet surfaces. The effect of temperature and sanxan/oil concentrations on the rheological and textural properties of the SEGs was evaluated: the SEG containing 1% (w/w) sanxan and 20% (w/w) sunflower oil exhibited excellent rheological and textural properties. Further, the addition of 10 mM Na + or 5 mM Ca 2+ greatly enhanced the thermostability of the SEG. The potential of SEGs as sustained-release delivery systems for β-carotene was also explored. The findings are of great interest for the development of novel delivery systems based on emulsion gels stabilized by sanxan for the sustained release of lipophilic components.

研究领域: 食品科学 · 药物制剂
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ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH · 2020 ·Vol. 27 ·期 11 ·12624-12634 · IF 3.056

Cell membrane damage induced by continuous stress of artemisinin sustained-release microspheres (ASMs) on Microcystis aeruginosa at different physiological stages

Ni Lixiao,Yue Feifei,Zhang Jianhua,Rong Shiyi,Liu Xuanyu,Wang Yifei,Wang Peifang,Li Danye,Wang Na,Wu Hanqi,Li Shiyin

Artemisinin sustained-release microspheres (ASMs) with long-term inhibition effects (> 40 days) on harmful freshwater bloom-forming cyanobacteria have been found in previous studies, but the inhibition mechanism is not completely clear. In the present study, we examined the growth effect of ASMs on Microcystis aeruginosa ( M. aeruginosa ) cells at different physiological stages. Growth experiments indicated that M. aeruginosa of different initial densities could be inhibited immediately and chlorophyll-a content both showed significant decreases following exposure of cyanobacteria to optimal dosage of ASMs for 20 days. The algicidal mechanism of ASMs was tested through a suite of physiological parameters (membrane permeability, antioxidant enzymes activity, and lipid peroxidation). The rise of cell membrane permeability indices (intracellular protein, nucleic acid contents, and conductivity) showed that the cellular membrane structure of M. aeruginosa was attacked by ASMs directly causing the leakage of cytoplasm. Antioxidant enzyme activity was a sensitive indicator of the impacts of ASMs which showed a significant downtrend after a few days. ASMs caused a great increase in •O 2 − and malondialdehyde (MDA) level of the algal cells which indicated the increase in lipid peroxidation of M. aeruginosa. Irreversible membrane damage induced by ASMs via the oxidation of ROS may be an important factor responsible for the algicidal mechanism of ASMs on M. aeruginosa cells . The application of ASMs might provide a new direction to control M. aeruginosa , especially before the exponential phase according to the optimal economy and inhibition effect. Graphical abstract

研究领域: 环境生物学 · 藻类学
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2015 · IF 4.152

Galactosylated chitosan-grafted multiwall carbon nanotubes for pH-dependent sustained release and hepatic tumor-targeted delivery of doxorubicin in vivo

Xiaole Qi,Yao Rui,Yuchao Fan,Haiyan Chen,Ning Ma,Zhenghong Wu

Carbon nanotubes (CNTs) are well known for their distinctive drug-loading ability that is mainly due to their large surface area, which permits covalent attachment of various target ligands or drug molecules by π–π stacking, allowing them to act as potential tumor-targeting carriers. Herein, we describe the development of galactosylated chitosan-graftedoxidized CNTs (O-CNTs-LCH) for pH-dependent sustained release and hepatic tumor-targeted delivery of doxorubicin (DOX). The in vitro release behavior in aqueous release media of different pH values (5.5, 6.5 and 7.4) verified the pH-dependent sustained release of DOX from O-CNTs-LCH-DOX. Moreover, these nanocarriers exhibited significant in vitro tumor-targeting properties, with a higher cellular uptake efficiency than that of free DOX in HepG2 cells. In addition, the good biocompatibility and low toxicity of O-CNTs-LCH-DOX was demonstrated by evaluating HepG2 cytotoxicity, vascular irritation and the maximum tolerated dose. Moreover, after intravenous administration in mice bearing the H22 tumor, O-CNTs-LCH-DOX showed higher antitumor activity and stronger fluorescent intensity in tumor tissue compared to free DOX. These results indicated the selective hepatic tumor targeting and the therapeutic effect of those nanocarriers.

研究领域: 纳米医学 · 药物递送 · 癌症治疗 · 生物材料 · 靶向治疗
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Journal of Orthopaedic Surgery and Research · 2026 ·Vol. 21 ·期 1 ·101 · IF 3.8

Preparation and in vitro sustained release performance of thermosensitive gel microsphere composite loaded with Anti-Tuberculosis drug PaMZ/BMP-2

Li Gui,Song Qianbo,Song Ye,Liao Wenxing,Zhao Dong,Hong Binqing,Cao Guangru

Background To meet the needs of local treatment for spinal tuberculosis, this study developed a thermosensitive gel microsphere composite with both anti-tuberculosis and osteogenesis-promoting functions for efficient drug sustained release. The composite consists of anti-tuberculosis drugs (Pretomanid, Pa-824; Moxifloxacin, M; Pyrazinamide, Z) and bone morphogenetic protein-2 (BMP-2) to optimize drug release kinetics and enhance local therapeutic effects. Methods PaMZ/BMP-2 microspheres were prepared using microfluidics and characterized by SEM, particle size analysis, and XRD. LC–MS and ELISA measured drug and BMP-2 release. The thermosensitive gel (P407/P188) ratio was optimized to ensure it remained liquid at room temperature and formed a gel at 37 °C for sustained release. Results Microspheres were spherical with an average size of 203.92 ± 27.76 μm. Encapsulation rates were 112.69%, 24.15%, and 15.18% for Pa, M, and Z, respectively. In vitro release showed Pa and M sustained release for over 17 days, with the gel prolonging drug release. Conclusion This study successfully prepared PaMZ/BMP-2 microspheres with good morphology and drug loading capacity, achieving controlled sustained release through thermosensitive gel. This offers a potential formulation approach for future localized therapy of spinal tuberculosis and lays the foundation for subsequent in vivo experiments and clinical translation.

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Advanced Healthcare Materials · 2026 · IF 11

A Hydrogel-Mediated Sustained-Release Platform Alters the Biodistribution of Umbilical Cord Mesenchymal Stem Cell-Derived Extracellular Vesicles in Mice

Zongbin Sun,Qiuxia Zheng,Chongyang Bai,Desheng Liu,Yue Zhang,Ping Yang,Fanghong Wang,Rui Li,Jia Yao,Xun Li

Mesenchymal stem cell-derived exosomes represent a promising therapeutic avenue for tissue regeneration, yet their clinical translation is hindered by rapid clearance following systemic administration and the lack of optimized, sustained-release delivery strategies. To address these challenges, we crafted a biomimetic hydrogel to carry and gently release MSC-derived exosomes. We engineered a biocompatible, dextran-based composite hydrogel (carboxymethyl chitosan-oxidized dextran/tannic acid-iron complex, CMC-OD/TA-Fe(III)) for the encapsulation and sustained release of human umbilical cord MSC-derived exosomes. We systematically compared the organ biodistribution of exosomes delivered via this hydrogel platform using three distinct local routes: intraperitoneal injection, oral (intragastric) administration, and rectal administration, employing in vivo imaging and tissue immunofluorescence analyses in C57BL/6J mice. Following a single intraperitoneal dose, released exosomes accumulated primarily in the liver and spleen, with minimal brain enrichment. Notably, both oral and rectal administration—non-invasive alternatives to injection—facilitated considerable exosome dissemination to multiple organs. The significant distribution observed via the oral route specifically challenges the prevailing assumption regarding the inefficacy of gastrointestinal delivery for exosome-based therapeutics. This study provides critical insights into administration-route-dependent biodistribution patterns and proposes novel, non-invasive delivery strategies to enhance the therapeutic efficacy and application scenarios of exosomes.

✓ 已验证 DOI PubMed 高影响因子
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ACS Applied Materials & Interfaces · 2026 · IF 7.8

Self-Sacrificial Sustained-Release Effects Synergistically Modulate Dual-Electrode Interfacial Chemistry in a Biphasic Electrolyte for Electrolytic Zn–MnO2 Batteries

Xiaoli He,Song Huang,Yueliang Chen,Jiaming Xiong,Huatai Liang,Zuyang Hu,Minghui Ye,Yufei Zhang,Zhipeng Wen,Yongchao Tang,Qi Liu,Jian Zhu,Cheng Chao Li

Electrolytic zinc–manganese batteries (ZMBs) featuring high energy density and low cost hold significant potential for large-scale energy storage. However, their development is hindered by severe zinc corrosion and poor reversibility of the Mn2+/MnO2 conversion, originating from drastic pH fluctuations and an acidic environment. Herein, we propose an organic/inorganic self-stratifying electrolyte, which synergizes with the self-sacrificial sustained-release Zn(BF4)2 to regulate the zinc interface and MnO2 conversion chemistry. The design innovatively utilizes the in situ hydrolysis of BF4– to create an HF/F– buffer and free F– ions. The former stabilizes cathode pH and promotes uniform deposition and deep conversion of MnO2. Additionally, the released F– fosters a robust ZnF2-rich SEI on the zinc anode in a water-lean environment (organic phase), effectively suppressing corrosion and side reactions. Therefore, the zinc-symmetric battery with an organic phase exhibited a lifespan of over 650 h, exceeding conventional aqueous electrolytes by 38-fold. The Zn–MnO2 batteries deliver exceptional stability for 1800 cycles at 2C with an average Coulombic efficiency of 98.7%. This biphasic buffering-interface regulation strategy provides a generalizable approach to decouple interfacial challenges, which is promising for extension to other corrosion cell systems.

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FOOD CHEMISTRY · 2026 · IF 10.4

Modified chitosan micelles improving physical stability, sustained release, and antibacterial activity of fir essential oil: performance optimization and mechanistic insights

Ying Lu,Qiang Yin,Xiangzhou Li,Jun Zhou,Yanhong Yang,Bowen Fu,Yuqing Wang

To meet consumer demand for the application of natural ingredients such as essential oils in food systems, this study developed a chitosan-g-poly(lactic acid) (CS-g-PLA) micellar system for fir essential oil (FEO) delivery. The research focused on investigating the regulatory effects of PLA side-chain parameters on micellar properties. Results demonstrated that increasing parameters enhanced hydrophobic interactions, forming compact micelles with a minimal particle size (229.7 nm) and critical micelle concentration (0.012 mg/mL). The hydrophobic core enabled efficient FEO loading (30.99%) with stable sustained release. FEO@CS-g-PLA micelles also showed broad-spectrum antimicrobial activity by disrupting cell membranes. Molecular dynamics simulations visualized the self-assembly of CS-g-PLA and the FEO loading process, providing theoretical support for experimental observations. In summary, this work offers microscopic insights into the micellization of modified CS-g-PLA and FEO loading mechanisms, providing a feasible strategy for applying essential oils in food preservation.

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FOOD CHEMISTRY · 2026 · IF 10.4

β-Cyclodextrin/tea saponin complex-stabilized eugenol emulsion functionalized composite films with antibacterial and sustained-release properties for fruit preservation

Longbin Li,Chi Feng,Fuhou Lei,Jiufang Duan,Kun Wang,Jianxin Jiang

β-Cyclodextrin/tea saponin (CT) complexes were prepared. • CT-stabilized eugenol emulsion shows superior storage and environmental stability. • CT complex retards the release rate of eugenol in the composite film. • Cationic guar gum maintained emulsion structural integrity during film formation. • The film integrates antibacterial, UV-shielding, and sustained-release properties. Addressing the severe postharvest losses of perishable fruits and environmental concerns caused by plastic packaging, this study developed a multifunctional composite film. Specifically, a composite of β-cyclodextrin and tea saponin—a byproduct of camellia oil processing—was synthesized and served as a stabilizer for the eugenol emulsion. This composite exhibited favorable surface activity, endowing the emulsion with excellent storage stability. Further, incorporating the emulsion into a κ-carrageenan/cationic guar gum film-forming matrix, the obtained film exhibited favorable mechanical properties (tensile strength: 22.62 MPa, elongation at break: 33.16%), outstanding antioxidant activity (scavenging rates of 60.77% for DPPH and 94.03% for ABTS radicals), and excellent sustained-release effect. Strawberry preservation experiment further confirmed that the composite film can inhibit microbial growth and reduce water loss, thereby extending the shelf life of fruits. This study provides valuable insights for advancing green packaging technologies and promoting the sustainable utilization of food processing byproducts. Download: Download high-res image (142KB) Download: Download full-size image

CAS / MDL: 7585-39-9 97-53-0
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