FOOD CHEMISTRY
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2024
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IF 8.5
Bao Zhang,Shen Long,Ran Feng,Meng-Jie Yu,Bao-Cai Xu,Han Tao
To achieve the effective loading and delivery of curcumin, novel disulfide-crosslinked nanoparticles based on modified dextrin were developed for the encapsulation of curcumin. Thiolated dextrin (Dt-SH) was obtained via sodium periodate oxidation and cysteamine grafting. The Dt-SH exhibited a rough, flake-like morphology, was classified as an amorphous material and demonstrated enhanced enzyme resistance. Subsequently, spherical nanoparticles with sizes ranging from 92.52 to 157.12 nm and zeta potentials between +23.59 and + 29.90 mV were self-assembled in an aqueous solution. Thiol modification promoted interconnection and aggregation of the nanoparticles. These nanoparticles exhibited pH-dependent size variations. Taking curcumin as a hydrophobic model, nanoparticles showed intestinal targeted release in vitro . Fluorescence spectroscopy and thermodynamic analysis indicated that curcumin bound to Dt-SH nanoparticles primarily through hydrogen bonding and van der Waals forces, with hydrophobic interactions contributing. These findings supported the potential of thiolated dextrin nanoparticles in the effective delivery of hydrophobic compounds.
研究领域:
药剂学
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生物材料科学
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药物化学
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DOI
PubMed
高影响因子
Applied Materials Today
·
2026
·
IF 7
Ruichen Wang,Xinbo Wei,Li Wang,Jiarui Tang,Xi He,Shuang Wang,Haojie Wei,Jiajia Jing,Haifeng Liu
A thrombin-responsive curcumin liposome-modified PCL/PLGA vascular graft (uPA-Cur-PDA@PCL/PLGA) was developed. • uPA-Cur-PDA@PCL/PLGA enabled on-demand uPA release for thrombolysis upon thrombin stimulation. • uPA-Cur-PDA@PCL/PLGA scavenged ROS and promoted M2 macrophage polarization via curcumin liposomes. • In vivo, uPA-Cur-PDA@PCL/PLGA maintained 3-month patency, promoted endothelialization, and reduced inflammation. • This strategy offers a promising approach for antithrombosis and vascular regeneration in small-diameter vascular grafts. The failure of small-diameter vascular grafts (SDVGs) is primarily attributed to thrombosis and pathological inflammation, leading to incomplete endothelialization and ultimately poor long-term patency. Current antithrombotic strategies are limited by insufficient durability and the risk of systemic coagulation disturbances associated with continuous anticoagulation. Herein, we developed a thrombin-responsive vascular graft enabling on-demand thrombolysis and modulation of the pathological microenvironment. Curcumin was encapsulated into liposomes to overcome its poor bioavailability, endowing the graft with reactive oxygen species (ROS) scavenging and immunomodulatory effects. Thrombin-responsive curcumin-loaded liposomes (uPA-Cur-Lip) were then constructed by sequentially conjugating a thrombin-cleavable peptide and urokinase-type plasminogen activator (uPA) to the liposomes. Subsequently, uPA-Cur-Lip was immobilized onto electrospun PCL/PLGA vascular grafts via polydopamine (PDA) coating, yielding uPA-Cur-PDA@PCL/PLGA. In vitro studies confirmed sustained curcumin release from the liposomes and thrombin-responsive "on-demand" thrombolytic activity. Furthermore, uPA-Cur-PDA@PCL/PLGA enhanced endothelial cell migration, alleviated oxidative stress, and promoted M2 macrophage polarization. The results of in vivo rat abdominal aorta implantation showed that uPA-Cur-PDA@PCL/PLGA exhibited sustained patency for 3 months without thrombosis, along with improved endothelialization and reduced inflammation. Overall, we developed a thrombin-responsive curcumin liposome-modified SDVG that enables on-demand thrombolysis and modulates the local microenvironment, thereby promoting vascular regeneration and improving long-term graft performance. Download: Download high-res image (194KB) Download: Download full-size image
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高影响因子
International Journal of Nanomedicine
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2026
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IF 8.7
Qin Yu,Xue-Ying Tan,Xian Liu,Hai-Bo Mao,Zhao-Gui Chen
Background Acute kidney injury (AKI) is a critical clinical syndrome with high morbidity and mortality, primarily driven by mitochondrial oxidative stress and tubular epithelial cell apoptosis. Current antioxidant therapies are limited by poor bioavailability and lack of renal specificity. To address this, we developed a dual-targeting nanomedicine based on ultrasmall chitosan oligosaccharide-functionalized ruthenium-curcumin nanodots (LMWC/Ru-Cur).Methods Ru-Cur coordination polymer nanodots were synthesized and subsequently coated with low-molecular-weight chitosan (LMWC). The nanoparticles were characterized for size, surface charge, stability, and antioxidant capacity. In vitro studies using HK-2 cells assessed cytocompatibility, cellular uptake, and protection against H2O2- or cisplatin-induced injury via measurements of viability, mitochondrial ROS, membrane potential, and apoptosis. In vivo efficacy and biodistribution were evaluated in murine models of ischemia-reperfusion- and cisplatin-induced AKI.Results The resulting LMWC/Ru-Cur nanodots exhibited uniform size (~7.6 nm), good aqueous stability, and potent broad-spectrum radical scavenging ability. They were efficiently internalized by renal tubular cells via megalin receptor-mediated endocytosis, leading to significantly enhanced renal accumulation. Treatment with LMWC/Ru-Cur attenuated oxidative stress, restored mitochondrial function, reduced apoptosis in injured HK-2 cells, and improved renal function (serum creatinine and blood urea nitrogen), histopathology, and inflammatory cytokine levels in both AKI models, outperforming free curcumin or unmodified Ru-Cur. The nanodots also demonstrated favorable short-term biocompatibility and in vivo biosafety.Conclusion LMWC/Ru-Cur nanodots represent a promising targeted nanotherapeutic strategy for AKI, integrating passive glomerular filtration with active receptor-mediated tubular delivery to effectively mitigate oxidative stress and mitochondrial damage, thereby preserving renal function. This work provides a rational design for metal-polyphenol based nanomedicines in the treatment of acute organ injury.
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PubMed
高影响因子
International Journal of Polymeric Materials and Polymeric Biomaterials
·
2026
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IF 3.2
Xi Su,Wei Xu,Lulu Liu,Qingxiang You,Wenchang Yi,Siyu Chen,Zhenying Wan,Shuya Huang
A novel ethyl cellulose-sodium alginate/chitosan/curcumin (EC-SA/CS/Cur) composite microgel system was developed through a one-step emulsion method. Optimized homogenization at 1,300 rpm for 2 min enabled consistent fabrication of EC-SA/CS/Cur microgels with a mean particle size of 2.85 μm. The microstructural morphology, particle size distribution, and chemical composition of the optimized EC-SA/CS/Cur microgels were characterized by microscopy, laser particle size analysis, and Fourier-transform infrared spectroscopy. The microgels exhibited a curcumin encapsulation efficiency of 54.4 ± 6.8% and a drug loading capacity of 0.032 ± 0.004%. The microgels exhibited excellent stability under enzymatic and physiological pH environments while displaying a unique sustained-release profile in ethanol-containing media; under agitated conditions, a cumulative release of 3.2 μg/mL was achieved within 6 h, representing a 28.0% increase in cumulative release compared to static conditions. The minimum inhibitory concentration of EC-SA/CS/Cur microgels was determined as 675 μg/mL; after 3 h of exposure, their antimicrobial efficacy significantly outperformed free curcumin. These results confirm that the EC-SA/CS microgel system acts as an effective delivery vehicle, markedly enhancing curcumin’s antimicrobial performance. This study provides a promising strategy for developing stable, high-efficiency curcumin delivery systems with improved therapeutic potential, particularly for oral/throat protection against alcohol-induced irritation via on-site curcumin release to alleviate local inflammatory damage.
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高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2025
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IF 5.4
Pengrui Wu,Chunling Nie,Zhihong Song,Xindi Wei,Yefan Niu,Mehdi Tabarsa,Li Wang,Jianguo Wang
The hydrophobicity and poor oral bioavailability of curcumin limit its application in the food industry. In this study, LP-CNCs/PNFs complexes were prepared by electrostatic interaction and used as stabilizers to prepare curcumin-loaded Pickering emulsions. The interaction between LP-CNCs and PNFs formed stable interface structures, which improved the emulsifying properties of LP-CNCs and enhanced the storage stability and rheological properties of emulsions. LP-CNCs/PNFs-based Pickering emulsions exhibited excellent protective capability for encapsulating curcumin. The stable and thick interface layer was formed on the surface of oil droplets, which provided a physical barrier against UV radiation and thermal resistance and slowed down the degradation of curcumin induced by the external environment. Moreover, during in vitro digestion, Pickering emulsions demonstrated excellent stability, leading to an improvement in curcumin's bioaccessibility from 37.29 % (C4P0) to 73.99 % (C4P4) after digestion. Consequently, double fibrils-based Pickering emulsions provide the theoretical foundation for improving the bioaccessibility of hydrophobic active substances and the development of healthy foods.
研究领域:
食品科学
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生物化学
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高影响因子
LWT-FOOD SCIENCE AND TECHNOLOGY
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2024
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IF 6
Xinyu Zhang,Yingxue Cheng,Hong Lin,Hailong Zhang,Weinong Zhang,Junbo He
To overcome the instability of sodium caseinate (NaCas) and zein binary nanoparticles in gastric digestion, and to improve the encapsulation of curcumin (Cur), hexaglycerol monooleate (HGMO) was employed as an anti-pepsin component to form ternary nanoparticles. The NaCas-Zein-HGMO nanoparticles were prepared using a self-assembly method that only required mixing at room temperature, and the optimal mass ratio for the components was determined to be 2:2:1. At a mass ratio of 1:20 between curcumin and zein, the NaCas-Zein-HGMO nanoparticles showed high encapsulation efficiency (91.18%) and provided effective chemical protection for curcumin. The Cur-NaCas-Zein-HGMO nanoparticles exhibited nanoscale dispersion, with a particle size about 236 nm, and demonstrated remarkable stability. In addition, the Cur-NaCas-Zein-HGMO nanoparticles exhibited improved resistance to simulated gastric fluid (SGF) digestion, increased antioxidant activity, sustained release profile, and exceptional rehydration capability. The results clearly showed that HGMO plays a crucial role in improving the physicochemical properties and encapsulation of curcumin of NaCas-Zein-HGMO nanoparticle. Hence, the novel ternary nanoparticles, NaCas-Zein-HGMO, have the potential to serve as an excellent delivery carrier for hydrophobic bioactive compounds, thereby mitigating their susceptibility to degradation by gastric digestion.
研究领域:
食品科学
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材料科学
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生物化学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2018
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IF 3.862
Hui-Yun Zhang,Cong-yong Sun,Michael Adu-Frimpong,Jiang-nan Yu,Xi-ming Xu
The anti-tumor efficacy of curcumin can be markedly improved by nano-drug self-delivery systems with high drug loading capacity and smart stimulus-triggered drug release in tumor cells. Herein, a type of novel, glutathione (GSH)-responsive, PEGylated prodrug nano-micelles (PPNMs) was prepared by self-assembly of curcumin-s-s-vitamin E/mPEG2k-DSPE mixture. The PPNMs (entrapment efficiency: 96.7%) was acceptably stable in water with a mean particle size of 29.84 nm. Compared with curcumin-loaded mPEG2k-DSPE nano-micelles (CUR-NMs), PPNMs showed a higher drug loading (1.68% vs 27.3%) and remarkably improved the chemical stability of curcumin in phosphate buffer saline (PBS) (pH = 7.4), 10% FBS culture medium, and rat plasma. In vitro release study showed that PPNMs could redox responsively control the release of curcumin from the prodrug. Moreover, PPNMs showed a cytotoxicity in HepG2 cells similar to that of the free curcumin; however, when the HepG2 cells were pretreated with 1 mM GSH, PPNMs displayed a markedly enhanced cytotoxicity and cellular uptake than the free curcumin. After intravenous injection, PPNMs showed an increased half-life in blood circulation (10.6-fold) and bioavailability (107-fold) compared with the free curcumin injection. Altogether, the prodrug nano-micelles represent a promising preparation for sustained and controlled delivery of curcumin with enhanced antitumor activity.
研究领域:
药学
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肿瘤学
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纳米医学
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DOI
PubMed
高影响因子
MOLECULES
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2025
·Vol. 30
·期 12
·2536
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IF 4.6
Qiuxu An,Yuanyuan Liu,Guodong Liang,Yuewu Wang,Fengying Liang,Yunyang Bai,Chaolu Eerdun,Riqing Cheng,Haifeng Zhang,Xiaojie Lv
Curcumin exhibits compromised bioavailability upon oral administration due to its inherent limitations, including low aqueous solubility, poor membrane permeability, and chemical instability. Inspired by the efficient mechanism by which viruses penetrate mucus and cells, we constructed an electrically neutral and hydrophilic nanocarrier (C60-CPP5/Pser@CUR) using fullerene C60 as the matrix modified with cell-penetrating peptides and phosphoserine. CPP5 facilitates efficient cellular internalization of therapeutic agents, while the incorporation of phosphoserine serves as a charge reversal strategy. This design enables dynamic surface charge modulation to enhance curcumin’s trans-barrier delivery efficiency. Systematic in vitro and in vivo evaluations demonstrated that the synthesized carrier significantly improved the synergistic effects of mucus penetration and cellular uptake. The Caco-2 cellular uptake of curcumin-loaded carriers was 2.26 times higher than that of free drugs. In a single-pass intestinal perfusion study in rat models, this nanocarrier significantly enhanced the absorption of curcumin in the duodenal and colonic regions. In the in vivo experiments, compared with free curcumin, its Cmaxand AUC0–tachieved improvements of 2.60 times and 14.70 times, respectively. This virus-mimetic platform dynamically adapts to micro-environmental demands through charge reversal mechanisms, effectively overcoming sequential biological barriers and providing a robust strategy for oral delivery of hydrophobic therapeutics.
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PubMed
高影响因子
DRUG DELIVERY
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2017
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IF 6.402
Jiajiang Xie,Yanxiu Li,Liang Song,Zhou Pan,Shefang Ye,Zhenqing Hou
Recently, the global trend in the field of nanomedicine has been toward the design of combination of nature active constituents and phospholipid (PC) to form a therapeutic drug-phospholipid complex. As a particular amphiphilic molecular complex, it can be a unique bridge of traditional dosage-form and novel drug delivery system. In thisarticle, on the basis of drug-phospholipid complex technique and self-assembly technique, we chose a pharmacologically safe and low toxic drug curcumin (CUR) to increase drug-loading ability, achieve controlled/sustained drug release and improve anticancer activity. A novel CUR-soybean phosphatidylcholine (SPC) complex and CUR-SPC complex self-assembled nanoparticles (CUR-SPC NPs) were prepared by a co-solvent method and a nanoprecipitation method. DSPE-PEG-FA was further functionalized on the surface of PEG-CUR-SPC NPs (designed as FA-PEG-CUR-SPC NPs) to specifically increase cellular uptake and targetability. The FA-PEG-CUR-SPC NPs showed a spherical shape, a mean diameter of about 180 nm, an excellent physiological stability and pH-triggered drug release. The drug entrapment efficiency and drug-loading content was up to 92.5 and 16.3%, respectively. In vitro cellular uptake and cytotoxicity studies demonstrated that FA-PEG-CUR-SPC NPs and CUR-SPC NPs presented significantly stronger cellular uptake efficacy and anticancer activity against HeLa cells and Caco-2 cells compared to free CUR, CUR-SPC NPs and PEG-CUR-SPC NPs. More importantly, FA-PEG-CUR-SPC NPs showed the prolonged systemic circulation lifetime and enhanced tumor accumulation compared with free CUR and PEG-CUR-SPC NPs. These results suggest that the FA targeted PEGylated CUR-SPC complex self-assembled NPs might be a promising candidate in cancer therapy.
研究领域:
药学
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纳米医学
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肿瘤学
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DOI
高影响因子
Drug Design Development and Therapy
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2025
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IF 5.1
Hualu Wu,Qian Liu,Yuxin Shen,He Qi,Jiade Zhao,Qiaoying Li,Hailun Xia,Ren-Ai Xu,Lu Shi
Purpose The purpose of this study was to establish an in vitro incubation system and an in vivo model to investigate the potential kinetic interactions of macitentan with imperatorin and curcumin, and to validate the potential inhibitory mechanisms using molecular docking.Methods In vitro, the enzyme kinetic profile of macitentan was explored in rat liver microsomes (RLM) and human liver microsomes (HLM). Furthermore, molecular docking technique was used to study the sites of action of macitentan, imperatorin, and curcumin with CYP 3A4. In vivo, the pharmacokinetic parameters of macitentan were investigated in Sprague-Dawley (SD) rats administered the drug orally, both as a single agent and in combination with imperatorin and curcumin.Results In vitro, the results indicated that imperatorin and curcumin could inhibit the metabolism of macitentan, with IC50 values of 6.58 μM and 10.86 μM in RLM and 6.97 μM and 5.71 μM in HLM, respectively. And in the study of inhibition type, in RLM, the inhibition types of imperatorin and curcumin on macitentan were mixed and non-competitive, respectively; in HLM, the inhibition types of imperatorin and curcumin on macitentan were both mixed. Furthermore, additional molecular docking studies demonstrated that both imperatorin and curcumin occupied the CYP3A4 site. In vivo, the result showed significant increases in AUC(0-t), AUC(0-∞), Tmax, t1/2, and Cmax for macitentan while a decrease in CLz/F when combined with imperatorin. The metabolite ACT-132577 exhibited substantial increases in t1/2, Tmax, and Cmax. Combined with curcumin, the AUC(0-∞) and Tmax of macitentan were significantly increased, while CLz/F was significantly decreased. Conversely, the metabolite ACT-132577 exhibited a substantial decrease in CLz/F, accompanied by notable increases in AUC(0-∞) and Tmax.Conclusion In vitro and in vivo studies revealed that imperatorin and curcumin exhibited inhibitory effects on the metabolism of macitentan. Furthermore, molecular docking revealed that the metabolic inhibition of macitentan by imperatorin and curcumin occurred through binding to the site on CYP3A4. However, further investigation is necessary to ascertain whether this phenomenon will occur in humans.
研究领域:
药理学
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分子生物学
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DOI
PubMed
高影响因子
JOURNAL OF FOOD BIOCHEMISTRY
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2025
·Vol. 2025
·期 1
·6134296
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IF 4.2
Ruixi Luo,Jing Zhang,Peng Chen,La Wang,Wenjia Wang,Ping Wang,Xing Zhao,Weiyi Tian
The aim of this study was to construct curcumin-loaded mesenchymal stem cell-derived exosomes (Cur-exos) and explore their effects on nonalcoholic fatty liver disease (NAFLD) models both in vitro and in vivo. Cur-exos were prepared using three common drug-loading techniques—incubation, sonication, and freeze–thaw cycles. Among these, Cur-exos prepared via repeated freeze–thawing demonstrated higher encapsulation efficiency and drug-loading rates than those produced by other methods. In vitro, Cur-exos exhibited enhanced stability, were efficiently taken up by hepatocytes, and mitigated palmitic acid (PA)–induced lipotoxicity in HepG2 cells. Moreover, Cur-exos significantly ameliorated liver damage in NAFLD model mice, reduced inflammation, decreased reactive oxygen species (ROS) levels, and mitigated endoplasmic reticulum (ER) stress. Additionally, Cur-exos effectively regulated lipid metabolism disorders and improved impaired glucose tolerance. Overall, we demonstrate that, compared with free curcumin, Cur-exos significantly improve curcumin stability and offer superior therapeutic effects in NAFLD mouse models. This study provides a novel approach for developing treatments for NAFLD.
研究领域:
药理学
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肝病学
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干细胞研究
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药物递送系统
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代谢性疾病
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DOI
高影响因子
Pharmaceuticals
·
2025
·Vol. 18
·期 4
·448
·
IF 4.8
Xueli Guo,Zhongyan Liu,Lina Wu,Pan Guo
Background : Liver cancer, especially hepatocellular carcinoma, a prevalent malignant tumor of the digestive system, poses significant therapeutic challenges. While traditional chemotherapy can inhibit tumor progression, its clinical application is limited by insufficient efficacy. Hydrophobic therapeutic agents further encounter challenges including low tumor specificity, poor bioavailability, and severe systemic toxicity. This study aimed to develop a liver-targeted, glutathione (GSH)-responsive micellar system to synergistically enhance drug delivery and antitumor efficacy. Methods : A GSH-responsive disulfide bond was chemically synthesized to conjugate glycyrrhetinic acid (GA) with curcumin (Cur) at a molar ratio of 1:1, forming a prodrug Cur-GA (CGA). This prodrug was co-assembled with glycyrrhizic acid (GL) at a 300% w / w loading ratio into micelles. The system was characterized for physicochemical properties, in vitro drug release in PBS (7.4) without GSH and in PBS (5.0) with 0, 5, or 10 mM GSH, cellular uptake in HepG2 cells, and in vivo efficacy in H22 hepatoma-bearing BALB/c mice. Results : The optimized micelles exhibited a hydrodynamic diameter of 157.67 ± 2.14 nm (PDI: 0.20 ± 0.02) and spherical morphology under TEM. The concentration of CUR in micelles can reach 1.04 mg/mL. In vitro release profiles confirmed GSH-dependent drug release, with 67.5% vs. <40% cumulative Cur release observed at 24 h with/without 10 mM GSH. Flow cytometry and high-content imaging revealed 1.8-fold higher cellular uptake of CGA-GL micelles compared to free drug ( p < 0.001). In vivo, CGA-GL micelles achieving 3.6-fold higher tumor accumulation than non-targeted controls ( p < 0.001), leading to 58.7% tumor volume reduction ( p < 0.001). Conclusions : The GA/GL-based micellar system synergistically enhanced efficacy through active targeting and stimuli-responsive release, providing a promising approach to overcome current limitations in hydrophobic drug delivery for hepatocellular carcinoma therapy.
研究领域:
药剂学
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肿瘤学
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DOI
PubMed
高影响因子
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