AAPS PHARMSCITECH
·
2025
·Vol. 27
·期 1
·52
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IF 4
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.
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EUROPEAN POLYMER JOURNAL
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2026
·
IF 6.8
Xuewen Wu,Lingfeng Xia,Haican Liu,Xiaoqin Hu,Hongyan Zeng,Haitao Wang,Yan Xiong
The controlled synthesis of anisotropic polymer particles with precisely tunable morphologies remains a significant challenge in polymer science. Here, we report a straightforward and scalable strategy for the synthesis of Janus-like polymer particles via oxygen-tolerant photo-mediated reversible addition-fragmentation chain transfer (RAFT) Pickering emulsion polymerization. This method eliminates the need for prior deoxygenation, inert gas protection, or additives, offering a green and operationally simple approach to functional polymer particles. Key particle properties—including wettability, size, rigidity, and flexibility—can be precisely tuned by modulating the monomer-to-crosslinker ratio, introducing a third monomer, and varying the size of the calcium carbonate nanoparticle Pickering stabilizer. Notably, using 50-nm calcium carbonate nanoparticles enables the systematic evolution of particle morphology from spherical to fragmented, compositionally anisotropic Janus-like architectures. The resulting Janus-like polymer particles exhibit superior performance as solid emulsifiers for oil-in-water cinnamaldehyde (CA) emulsions, achieving exceptional stability and a sustained release profile (85% over 20 days, following the Weibull model). These emulsions demonstrate enhanced and sustained antibacterial activity against both E. coli and S. aureus , outperforming free CA. In a practical food preservation application, the Pickering emulsion reduces banana weight loss from 12.24% (blank control) to 8.97% and significantly delays peel browning over seven days. This work establishes a novel and green synthetic methodology for the controlled preparation of functional Janus-like polymer particles, with promising implications for polymer-based delivery systems in pharmaceutical and agricultural applications.
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Advanced Healthcare Materials
·
2026
·
IF 11
Jingwen Bai,Chi Wei,Yujia Guo,Ziyu Wang,Yang Yun,Bin Yu,Yanhui Wei,Yu Yang
Bacterial colitis remains a global health challenge. Clove essential oil (CEO), a natural plant extract, exerts potent activity against enteropathogenic Escherichia coli ( E. coli ). But its poor water solubility and insufficient stability limit its translation into a therapeutic agent for E. coli -induced colitis. Herein, we first synthesized β -cyclodextrin-grafted chitosan nanoparticles (CS-g-CD NPs) by electrostatic interactions based on a pH response and enzymatic degradation synergy. Subsequently, with the assistance of ultrasound waves, CEO was loaded into the nanoparticles through van der Waals forces, ultimately constructing a colon-targeted delivery system (CEO/CS-g-CD NPs). This system not only enhanced the water solubility and stability of CEO, but also improved its bioavailability (enhanced by 120.10%) through protecting it from gastric acid degradation and prolonging intestinal retention. In vitro and in vivo studies demonstrated that CEO/CS-g-CD NPs effectively inhibited E. coli proliferation and suppressed its virulence gene expression. Consequently, these nanoparticles alleviated the inflammatory response triggered by bacterial infection, regulated gut microbiota homeostasis, and further promoted the repair of the damaged colonic barrier. This study developed an intelligent on-demand release strategy for poorly water-soluble natural products, markedly boosting their ameliorative effect on bacterial colitis and facilitating the application of these products in pharmaceutical sectors.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Lele Chen,Shaofei Zhang,Tingyu Liang,Xu Ding,Ling Ding,Jipeng Shi,Ji Zhang,Jianping Wu
The therapeutic potential of essential oils in feed and medicine is limited by their volatility, degradation, and poor bioavailability. To overcome these challenges, a novel colon-targeted microsphere was engineered for the controlled delivery of tea tree essential oil (TEO), as illustrated in Scheme 1 . A critical component of this system is a pH-responsive coating composed of pectin and starch, which acts as a colon-specific polymeric barrier. This coating demonstrated precise pH-responsive release, with minimal leakage in simulated gastric fluid (SGF) (only 10.87 % release over 4 h) and sustained, colon-specific release in simulated intestinal fluid (SIF) (79.77 % over 14 h). The core of the system, designated TEOCMT, was fabricated through the modification of montmorillonite (MMT) with cetyltrimethylammonium bromide (CTAB), resulting in organo-montmorillonite (CMT). Tea tree essential oil was then encapsulated within the interlayer spaces of CMT, forming an effective sustained-release system (TEOCMT). Compared to raw MMT (5.63 %), the TEO loading capacity of CMT increased 8.3-fold, reaching 46.79 %. Furthermore, the antibacterial activity of PS/TEOCMT microspheres was triggered in alkaline media, where they dissolved and released the TEOCMT core. This resulted in enhanced efficacy, particularly against S. aureus (MIC = 1.25 mg mL −1 ), which was superior to that of pure TEO (MIC = 2.5 mg mL −1 ). The PS/TEOCMT microspheres also exhibited excellent biocompatibility. This work presents a robust and effective strategy for unlocking the full potential of essential oils in colon-specific applications.
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FOOD CHEMISTRY
·
2025
·
IF 9.8
Shasha Huang,Kuiyou Wang,Yi Ma,Zuzhe Wang,Mingqian Tan
Sea cucumber peptide (SCP) reacted with procyanidins and vanillin to form a food-grade nanoparticles (SPNs) via the Mannich reaction. After encapsulation astaxanthin (AXT), the SPNs was attached to a SCP-modified hyaluronic acid (HA) hydrogel to construct AXT@SPNs/HS. The AXT@SPNs/HS exhibited an average size of approximately 1281 nm, while the AXT@SPNs had an average size of 510 nm. The loading capacity of AXT in AXT@SPNs and AXT@SPNs/HS were 6.81 ± 0.10 and 6.56 ± 0.19 μg/mg, respectively. Sustained release of AXT was found during AXT@SPNs/HS digestion and HA-SCP hydrogel provided a significant advantage in protecting AXT in acidic conditions. AXT@SPNs/HS could effectively target RAW264.7 macrophages and mitigated oxidative stress inflammatory response caused by alcohol. AXT@SPNs/HS alleviated acute alcoholic liver damage in mice model. The results illustrated AXT@SPNs/HS might become a candidate with intestinal sustained release to enhance its bioavailability.
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POLYMERS FOR ADVANCED TECHNOLOGIES
·
2020
·Vol. 32
·期 3
·1262-1271
·
IF 2.578
Qingzhen Zhu,Baogang Zhang,Yuandou Wang,Xinghua Liu,Weiwei Li,Feng Su,Suming Li
Poly( D , L -lactide-co-glycolide)-poly(ethylene glycol) (PLGA-PEG) diblock copolymers with different compositions were synthesized by ring-opening polymerization of D , L -lactide and glycolide, using monomethoxy PEG as macro-initiator. The resulting copolymers were characterized by nuclear magnetic resonance, gel permeation chromatography, and critical micelle concentration analyses. Self-assembly of the copolymers yielded aggregates of different architectures, including spherical micelles and a mixture of spherical and worm-like micelles with Y-junctions. The self-assembled architecture depends on both the hydrophilic/hydrophobic balance and the molar mass of copolymers. Valsartan, a widely used drug in the treatment of hypertension, was loaded in micelles using a co-solvent evaporation method. High drug-loading content was obtained for worm-like micelles. in vitro drug release was performed at 37°C in pH 7.4 phosphate-buffered saline. An initial burst release is detected in all cases, followed by slower release up to 9 days. The overall release rate is strongly dependent on the degradation of micelles. Copolymers with short PLGA blocks exhibit faster drug release due to faster degradation of micelles, and worm-like micelles present slower drug release as compared to spherical ones. Therefore, PLGA-PEG copolymer micelles with high drug-loading capacity, different architectures, and variable drug release rates could be most attractive for sustained delivery of valsartan.
研究领域:
药剂学
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生物材料
·
高分子化学
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PROCESS BIOCHEMISTRY
·
2023
·
IF 4.4
Xiaoxuan Cai,Miaoen Huang,Xixiang Huang,Huan Liu,Tianji Wang,Li Li,Weiguang Yang,Hui Luo,Yingnian Lu
The organism Sipunculus nudus L is a good resource for marine peptides because of its rich protein. However, the disadvantage of biological peptides is their short metabolic half-life, therefore, structural modification of peptides is necessary. In this research, the enzymatic hydrolysis of Sipunculus nudus L was performed using trypsin and then peptides were isolated and purified from the hydrolysates, four novel tripeptides were identified by LC-MS-MS as Ser-Arg-Pro (SRP, m/z = 358.39), Pro-Arg-Pro (PRP, m/z = 368.43), Arg-Pro-Ala (RPA, m/z = 342.39), and Lue-Pro-Lys (LPK, m/z = 356.46), their ACE inhibitory activity was investigated with IC 50 value as following 0.046, 0.42, 0.97, and 6.54 mM, respectively. Because of its highest ACE inhibitory activity, SRP was further selected to modify the chemical structure for a sustained release agent DSPE-PEG-SRP. Compared with 7 h of free SRP, the release of DSPE-PEG-SRP in vitro was approximately 120 h. The ACE inhibition rate of SRP released from the synthetic product and the raw material SRP was almost the same, molecular docking demonstrated that ACE inhibitory activity was attributed to the formation of hydrogen bonds between SRP and ACE active sites . In conclusion, DSPE-PEG-SRP, a novel sustained release agent, has great potential and is expected to be further applied to treat hypertension.
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LWT-FOOD SCIENCE AND TECHNOLOGY
·
2022
·
IF 6.056
Hui Wang,Jinming Liu,Xu Fan,Jing Ren,Qian Liu,Baohua Kong
In this study, natural crab-shell particles (CSP) and deacetylated crab-shell particles (dCSP) were used as crosslinking agents at the present of glucolactone to obtain high strength mono-crosslinked and bi-crosslinked sodium alginate (NaAlg) hydrogel films, respectively. The results indicated that the CSP in the system could occur Ca 2+ crosslinking, and the addition of dCSP could help to form both Ca 2+ crosslinking and polyelectrolytes interactions with NaAlg. The remaining unreacted CaCO 3 could enhance the thermal stability of the films due to the high thermally stable CaCO 3 . The surface hydrophobicity, gel properties, mechanical strength and thermal stabilities of those bi-crosslinked NaAlg hydrogel films were better than those of neat NaAlg film and mono-crosslinked NaAlg hydrogel films, which overcome the inferior thermo-mechanical properties for traditional hydrogel films. In addition, the releasing time of those prepared hydrogel films for diclofenac sodium was higher than 36 h, which illustrated sustained drug releasing activity. The CSP modified NaAlg hydrogel film with 0.5% GDL content exhibited the highest cumulative release amount. The proposed approach is a promising green crosslinking technique to develop high performance NaAlg hydrogel films that can realize active ingredients and drugs sustained release in food packaging and medical wound dressing areas.
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Polymers
·
2022
·Vol. 14
·期 4
·694
·
IF 4.967
Zhaowen Liu,Xiuqiong Chen,Zhiqin Huang,Hongcai Wang,Shirui Cao,Chunyang Liu,Huiqiong Yan,Qiang Lin
In this paper, we developed an organic solvent-free, eco-friendly, simple and efficient one-pot approach for the preparation of amphiphilic conjugates (Ugi-OSAOcT) by grafting octylamine (OCA) to oxidized sodium alginate (OSA). The optimum reaction parameters that were obtained based on the degree of substitution (DS) of Ugi-OSAOcT were a reaction time of 12 h, a reaction temperature of 25 °C and a molar ratio of 1:2.4:3:3.3 (OSA:OCA:HAc:TOSMIC), respectively. The chemical structure and composition were characterized by Fourier transform infrared spectroscopy (FTIR),1H nuclear magnetic resonance (1H NMR), X-ray diffraction (XRD), thermogravimetry analyser (TGA), gel permeation chromatography (GPC) and elemental analysis (EA). It was found that the Ugi-OSAOcT conjugates with a CMC value in the range of 0.30–0.085 mg/mL could self-assemble into stable and spherical micelles with a particle size of 135.7 ± 2.4–196.5 ± 3.8 nm and negative surface potentials of −32.8 ± 0.4–−38.2 ± 0.8 mV. Furthermore, ibuprofen (IBU), which served as a model poorly water-soluble drug, was successfully incorporated into the Ugi-OSAOcT micelles by dialysis method. The drug loading capacity (%DL) and encapsulation efficiency (%EE) of the IBU-loaded Ugi-OSAOcT micelles (IBU/Ugi-OSAOcT = 3:10) reached as much as 10.9 ± 0.4–14.6 ± 0.3% and 40.8 ± 1.6–57.2 ± 1.3%, respectively. The in vitro release study demonstrated that the IBU-loaded micelles had a sustained and pH-responsive drug release behavior. In addition, the DS of the hydrophobic segment on an OSA backbone was demonstrated to have an important effect on IBU loading and drug release behavior. Finally, the in vitro cytotoxicity assay demonstrated that the Ugi-OSAOcT conjugates exhibited no significant cytotoxicity against RAW 264.7 cells up to 1000 µg/mL. Therefore, the amphiphilic Ugi-OSAOcT conjugates synthesized by the green method exhibited great potential to load hydrophobic drugs, acting as a promising nanocarrier capable of responding to pH for sustained release of hydrophobic drugs.Keywords:amphiphilic conjugates;sodium alginate;nanocarrier;self-assembly;sustained release
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Zhaohui Liang,Ze Zhou,Liheng Chen,Xueqing Qiu
Industrial alkali lignin is an abundant aromatic biological macromolecule with intrinsic UV shielding ability, but its structural heterogeneity and aqueous self-aggregation limit its use as a stable carrier matrix. Herein, industrial alkali lignin was valorized through zein regulated co-assembly to construct surfactant free hybrid biological macromolecular nanocapsules (LZNP@Abm) for abamectin (Abm) delivery. The composite macromolecular matrix afforded excellent colloidal stability and a loading capacity of 79.22%, and LZNP@Abm retained 74.94% Abm after 72 h of UV irradiation, effectively mitigating photolytic degradation. By integrating lignin derived UV shielding with zein mediated interfacial stabilization and pH and temperature responsive gating, LZNP@Abm suppressed release, with only 34.18% release after 180 h under weakly acidic leaf surface and soil conditions, while accelerating release at pH 9 and 35 °C, conditions relevant to alkaline and warm lepidopteran larval midguts. Molecular dynamics and density functional theory analyses identified key zein residues, including asparagine, serine, and proline, that enhanced Abm binding through cooperative hydrogen bonding and van der Waals interactions. Improved foliar wettability and liquid retention further promoted leaf deposition and reduced potential non-target pesticide loss. LZNP@Abm achieved 5.7–23.5-fold reductions in LC 50 against Spodoptera frugiperda and complete mortality of S. litura , restored seed germination to 85.56%, and maintained earthworm survival at 83.33 to 96.67%. This work demonstrates a mechanism informed biopolymer carrier strategy for converting industrial lignin into a functional pesticide delivery platform with photoprotection, controlled release, and improved biosafety. Download: Download high-res image (119KB) Download: Download full-size image
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NANOTECHNOLOGY
·
2021
·Vol. 32
·期 27
·275707
·
IF 3.874
Songfa Qiu,Fan Gao,Zhijun Liang,Ximing Zhong,Li Hao,Huayao Chen,Xinhua Zhou,Hongjun Zhou
Tea tree oil, a natural antibacterial compound, cannot be used effectively because of its volatile nature. In this work, a biocompatible carrier was prepared and loaded with tea tree essential oil. The carrier was prepared via the electrostatic or chemical action of aminated mesoporous silica and sodium rosin for achieving a low volatilization rate of tea tree essential oil. A synergistic antibacterial effect was observed between sodium rosin and tea tree essential oil. This method utilized the positive charge of the amino group and the condensation reaction with the carboxyl group to achieve physical and chemical interactions with sodium rosin. Fourier Transform Infrared, Brunauer–Emmet–Teller, Zeta potential, SEM, TEM, and TG were performed to characterize the structure and properties of the samples. Compared to the electrostatic effect, the chemically modified system exhibited a longer sustained release, and the sustained release curve followed the Korsmeyer–Peppas release model. Also, the antibacterial properties of the chemically modified system exhibited better minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) respectively, the MIC and MBC for E. coli were 0.3 mg ml−1 and 0.6 mg ml−1 respectively, for S. aureus were 0.15 mg ml−1 and 0.3 mg ml−1 respectively. More strikingly, the sample also demonstrated long-term antibacterial performance. Therefore, this work provides a new way for the delivery of volatile antibacterial drugs to achieve sustained-release and long-lasting antibacterial effects.
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CERAMICS INTERNATIONAL
·
2021
·
IF 4.527
Cong Wu,Xinghui Wei,Kang Zhao,Junyi Jiang,Mengzhen Jiao,Junhua Cheng,Zhen Tang,Zheng Guo,Yufei Tang
Nanotube coatings on titanium surfaces have favorable biocompatibility and structures and are widely used in local drug delivery. However, when a drug freely diffuses out of a nanotube, it leads to an explosive release, making the duration of action extremely short. In this study, a high concentration of vancomycin hydrochloride region similar to a dam was formed on a nanotube coating surface by exploiting the attraction of the electric charge generated by the energy conversion of the piezoelectric effect to vancomycin hydrochloride. The “dam” not only reduces the diffusion rate of vancomycin hydrochloride inside the nanotube into the dam and the diffusion rate of the dam to the outside but also forms a high concentration of vancomycin hydrochloride action region. The free diffusion rate of vancomycin hydrochloride loaded on the TiO 2 @ BaTiO 3 coaxial nanotubes was reduced by the piezoelectric effect, and the cumulative release of vancomycin hydrochloride for 7 days is reduced by 54.8%. The polarized vancomycin-containing coaxial nanotube coating has a long-lasting antibacterial effect on Staphylococcus aureus . The TiO 2 @ BaTiO 3 coaxial nanotubes loaded with vancomycin hydrochloride coating with piezoelectric properties has potential application value in controlled drug delivery.
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