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JOURNAL OF CONTROLLED RELEASE · 2024 · IF 10.5

Polyvinylpyrrolidone-curcumin nanoparticles with immune regulatory and metabolism regulatory effects for the treatment of experimental autoimmune uveitis

Fan Cao,Kun Liang,Wei-Wei Tang,Qin-Yu Ni,Zhi-Yu Ji,Chen-Kai Zha,Ya-Kun Wang,Zheng-Xuan Jiang,Shengping Hou,Li-Ming Tao,Xianwen Wang

Uveitis comprises a cluster of intraocular inflammatory disorders characterized by uncontrolled autoimmune responses and excessive oxidative stress leading to vision loss worldwide. In the present study, curcumin (CUR) was conjugated with polyvinylpyrrolidone (PVP) to form PVP-CUR nanoparticles with significantly elevated solubility and outstanding multiple radical scavenging abilities. In vitro studies revealed that PVP-CUR nanoparticles markedly mitigated oxidative stress and reduced apoptosis in a H 2 O 2 -induced human retinal pigment epithelial cell line (ARPE-19) and promoted phenotypic polarization from M1 to M2 in an LPS-induced human microglial cell line (HMC3). Further in vivo studies demonstrated the prominent therapeutic effects of PVP-CUR nanoparticles on experimental autoimmune uveitis (EAU), which relieved clinical and pathological progression, improved perfusion and tomographic manifestations of retinal vessels, and reduced blood–retinal barrier (BRB) leakage; these effects may be mediated by mitigating oxidative stress and attenuating macrophage/microglia-elicited inflammation. Notably, treatment with PVP-CUR nanoparticles was shown to regulate metabolite alterations in EAU rats, providing novel insights into the underlying mechanisms involved. Additionally, the PVP-CUR nanoparticles showed great biocompatibility in vivo . In summary, our study revealed that PVP-CUR nanoparticles may serve as effective and safe nanodrugs for treating uveitis and other oxidative stress- and inflammation-related diseases.

CAS / MDL: 67-68-5 121-44-8
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Phenylboronic acid functionalized dextran loading curcumin as nano-therapeutics for promoting the bacteria-infected diabetic wound healing

Sheng Ni,Kun Zhang,Xiong Zhao,Shuai Wu,Meng Yan,Da Sun,Li Zhu,Wei Wu

Chronic bacterial infections, excessive inflammation, and oxidative stress significantly hinder diabetic wound healing by prolonging the inflammatory phase and complicating the healing process. In this study, phenylboronic acid functionalized dextran (PODP) was developed to encapsulate curcumin , referred to as PODP@Cur. Experimental results indicate that PODP significantly improves the water solubility of curcumin and exhibits synergistic biological activity both in vitro and in vivo . PODP@Cur is capable of accelerating drug release under the pathological microenvironment with ROS accumulation. Furthermore, phenylboronic acid (PBA) has demonstrated potential for targeted bacterial drug delivery, enhancing antibacterial efficacy and trapping free LPS/PGN from dead bacteria to reduce undesirable inflammation. In a diabetic mouse model, PODP@Cur exhibits an excellent antibacterial, anti-inflammatory and antioxidant activities to ultimately promote the efficient and safe wound healing. Due to the specific interaction between PBA and LPS , PODP@Cur could enhance antibacterial activity against bacteria, reduce toxic side effects on normal cells, and alleviate the LPS-mediated pro-inflammatory pathological microenvironment. Therefore, PODP@Cur is capable of being exploited as an efficient and safe candidate for promoting the bacteria-infected diabetic wound healing.

CAS / MDL: 9048-71-9 9004-54-0
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FOOD CHEMISTRY · 2021 · IF 7.514

Lactoferrin particles assembled via transglutaminase-induced crosslinking: Utilization in oleogel-based Pickering emulsions with improved curcumin bioaccessibility

Tianhang Xia,Yuxing Gao,Yu Liu,Zihao Wei,Changhu Xue

In this study, the optimal environmental condition for preparation of lactoferrin particles assembled via transglutaminase-induced crosslinking (TG-LF particles) was pH 8, 100 U/g of TG concentration, 50 °C and 2 h of crosslinking time. Contact angle of TG-LF particles was 79°. Then, corn oil-based oleogels were prepared with carnauba wax (CW), behenyl alcohol (BA) and CW-BA mixture at 1:4 ratio (MT). To investigate the effect of oleogels on oleogel-based Pickering emulsions, oleogel-based Pickering emulsions were prepared by a two-step method using different oleogels as the oil phase and the TG-LF particles as the emulsifier. In vitro digestion study revealed that CW oleogel-based Pickering emulsion had the highest lipolysis rate and curcumin bioaccessibility. This study demonstrated that TG-LF particle-stabilized oleogel-based Pickering emulsions had good performance in curcumin delivery, which provided a new idea for the preparation of Pickering emulsifier and enriched the knowledge in the field of oleogel-based Pickering emulsion.

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CNS & Neurological Disorders-Drug Targets · 2023 ·Vol. 22 ·期 7 ·1120-1132 · IF 3

Bis-iodine-labeled Curcumin as a Potential CT Imaging Agent for β-amyloid Plaques in the Brain

Dai Yaqian,Peng Liduo,Tian Xiaoyan,Wu Xingwang,Xu Yuanhong,Jiang Taoshan,Qiao Jinping

Background: Alzheimer's disease (AD) is one of the most common causes of dementia, affecting many old people. Objectives: By designing and synthesizing intracerebral imaging probes, we tried to provide a new solution for the early diagnosis of AD. Methods: We designed and synthesized bis-iodine-labeled curcumin, and verified its performance through in vivo and in vitro experiments. Results: In this study, bis-iodine-labeled curcumin (7, BICUR) was synthesized. In the in vitro mass spectrum binding assay, Kd values of BICUR with Aβ1-40 and Aβ1-42 aggregates were 46.29 nM and 64.29 nM, respectively. Aβ plaques in AD brain adjacent sections were positively stained by BICUR, which was similar to some other curcumin derivatives. The Log P value of BICUR was 1.45. In the biodistribution experiment, BICUR showed the highest initial brain uptake (5.87% compared to the blood concentration) two minutes after the tail vein injection and rapid clearance from the mouse brain. In the acute toxicity experiment, BICUR showed low toxicity, and the LD50 was >100 mg/kg. Moreover, BICUR showed a high stability in vitro (86.68% unchanged BICUR after incubation for 120min in mouse brain homogenate). Besides, BICUR produced an enhanced CT imaging effect that could be sensitively detected in vitro, but it also showed an obvious differentiation from surrounding tissues after intracerebral injection. Conclusion: All results suggested that BICUR could probably act as a targeted CT imaging agent for Aβ plaques in the brain.

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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2016 · IF 3.994

pH-sensitive micelles based on acid-labile pluronic F68–curcumin conjugates for improved tumor intracellular drug delivery

Xiao-Bin Fang,Jin-Ming Zhang,Xi Xie,Di Liu,Cheng-Wei He,Jian-Bo Wan,Mei-Wan Chen

Curcumin (Cur) is a highly pleiotropic anticancer agent that inhibits cell proliferation and induces apoptosis in cancer cells. A variety of nano-systems constituted by polymer–drug conjugates have been designed to overcome its shortages on water solubility, chemical instability, and poor bioavailability. However, most of them suffer from ineffective release of Cur in cancer cells in vivo . This work developed a novel flexible acid-responsive micelle formulation by covalently conjugating Cur on the hydrophilic terminals of pluronic F68 chains via cis -aconitic anhydride linkers. The synthesized F68-Cis–Cur conjugates can readily precipitate to form homogeneous micelles with average size about 100   nm in aqueous solution. In acid environments, F68-Cis–Cur conjugates would break down and subsequently release Cur rapidly, for the reason of pH-sensitive cleavage of cis -aconitic anhydride linkers. In vitro anticancer activity tests demonstrated that F68-Cis–Cur micelles induced higher cytotoxicity against both A2780 and SMMC 7721 cells than free Cur. It provided a larger decrease of mitochondrion membrane potential and induced cellular apoptosis. F68-Cis–Cur micelles remarkably increased cellular uptake of Cur than free Cur through caveolae-mediated endocytosis in an energy-dependent manner. This study demonstrates F68-Cis–Cur conjugation as a promising tool for improving intracellular drug delivery in cancer therapy.

✓ 已验证 DOI PubMed 高影响因子
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ACS Applied Polymer Materials · 2021 · IF 4.089

Amphiphilic Graft Copolymers of Quaternized Alginate-g-Polytetrahydrofuran for Anti-protein Surfaces, Curcumin Carriers, and Antibacterial Materials

Yu-Zhuang Gao,Jun-Cai Chen,Yi-Xian Wu

Amphiphilic quaternized alginate-g-polytetrahydrofuran (QA-g-PTHF) graft copolymers were successfully synthesized via nucleophilic substitution of living PTHF+ chains obtained via cationic ring-opening polymerization with the −OH side functional groups in QA. This unique graft copolymer exhibits low cytotoxicity and anti-protein adsorption. The QA-g-PTHF nanospheres (328 ± 21 nm) loaded with curcumin exhibit ninefold higher anticancer effect to HeLa cells than pure curcumin due to the synergistic roles from the graft copolymer. Both the interactions of cationic quaternary ammonium with the negatively charged HeLa cell surface and the hydrophobic PTHF branches with the hydrophobic cell membrane result in a great improvement in the entrance of nanospheres into HeLa cells and effective drug release therein. The QA-g-PTHF/Ag nanocomposites prepared in situ during the synthetic process demonstrate more than 98% killing efficiency for Escherichia coli and Staphylococcus aureus. To the best of our knowledge, this is the first example of an amphiphilic, anti-protein, and antibacterial QA-g-PTHF copolymer with low cytotoxicity for potential anticancer applications.

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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2019 · IF 2.606

(NaPO3)6-assisted formation of dispersive casein-amorphous calcium phosphate nanoparticles: An excellent platform for curcumin delivery

Baolong Niu,Jie Guo,Xia Guo,Xiaoqing Sun,Chaohui Rao,Chun Liu,Jin Zhang,Ce Zhang,Yan-Ying Fan,Wenfeng Li

Although much effort has been focused on the preparation of stable amorphous calcium phosphate (ACP) nanoparticles , the poor dispersity of ACP nanoparticles in aqueous solution remain an unresolved problem. In this work, hexametaphosphate ((NaPO 3 ) 6 ) was used as a green dispersant to disperse casein-stabilized ACP (casein-ACP) nanoparticles in aqueous solution. Characterization of casein-ACP nanoparticles by X-ray diffraction (XRD) proved that the casein-induced amorphous structures could maintained for at least 3 months at room temperature. Moreover, the effects of (NaPO 3 ) 6 solutions for dispersing casein-ACP nanoparticles in water was studied and their ability to stabilize aqueous casein-ACP dispersions was demonstrated by digital photos. A typical anticancer drug , curcumin (Cur), was employed to evaluate the drug loading abilities and drug release behaviors of prepared nanoparticles. The results showed that the resultants have high drug loading capacity and favorable pH-responsive drug release properties. Furthermore, this drug delivery system showed an excellent ability to damage A549 cells, indicated that the as-prepared casein-ACP-(NaPO 3 ) 6 nanoparticles are promising for the applications in drug delivery.

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CARBOHYDRATE POLYMERS · 2016 · IF 4.219

Hybrid liposomes composed of amphiphilic chitosan and phospholipid: Preparation, stability and bioavailability as a carrier for curcumin

Shengfeng Peng,Liqiang Zou,Weilin Liu,Ziling Li,Wei Liu,Xiuting Hu,Xing Chen,Chengmei Liu

Hybrid liposomes, composed of amphiphilic chitosan and phospholipid , were prepared and used to evaluate the effect of amphiphilic polymers on the properties of liposomes. Successful preparation of the hybrid liposomes was confirmed using physicochemical characteristics, including morphology, particle size and zeta potential. Physical stability studies (exposure to solutions of increasing ionic strength and heat treatment) indicated that the hybrid liposomes had better ionic stability than amphiphilic chitosan-based polymeric liposomes and higher thermal stability than traditional phospholipid liposomes. Curcumin was then encapsulated in the hybrid liposomes. Compared with phospholipid liposomes, the hybrid liposomes displayed better storage stability and more sustained curcumin release. Cellular uptake experiments showed that the hybrid liposomes significantly increased the bioavailability of curcumin. The study highlights the potential of well-designed stable hybrid liposomes that increase the stability and bioavailability of lipophilic bioactive, such as curcumin.

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FOOD CHEMISTRY · 2025 · IF 9.8

Smartphone-assisted curcumin-based fluorescence sensing platform for alcohol content in Chinese liquor via hydrogen bond manipulation

Fang Xu,Longfei Su,Zhenxing Guo,Qiang Cheng,Jiachen Guan,Yuhang Guo,Liqiang Xu,Guoping Sheng

Alcohol content is one of the most important quality control metrics in Chinese liquor production, and its accurate determination is highly desired in safeguarding product quality, consumer health, and tax assessment. This study presents an innovative fluorescence sensing platform for alcohol content determination. Curcumin was used as a fluorescent indicator, which demonstrated distinct fluorescence responses to hydrogen bonding interaction with ethanol and water. Experimental results demonstrated an excellent linear correlation between fluorescence intensity changes and alcohol content (20–80 %, vol%) with a strong correlation coefficient (R 2  = 0.991), excellent precision (relative standard deviation <1.67 %) and accuracy (recovery rate 96.78–102.79 %, relative error ± 3.22 %). Further integrated with smartphone technology, a portable fluorescence sensing platform was developed, which enables accurate alcohol content determination through RGB analysis of fluorescent images. This novel method demonstrates promising potential in practical applications, offering a portable and user-friendly solution for alcohol content determination in food and beverage industries.

CAS / MDL: 458-37-7
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DRUG DELIVERY · 2025 · IF 8.1

Targeted strategy by curcumin and tideglusib biomimetic nano-systems alleviates oxidative stress and inflammation under ischemic stroke

Jiajia Li,Yiliang Yang,Meng Lin,Yitian Du,Yiwei Peng,Yu Zhou,Datong Gao,Yanxia Zhou,Xinru Li,Xianrong Qi

Ischemic stroke represents one of the leading causes of disability and death worldwide. Neuroprotection aimed at mitigating oxidative stress and inflammation is crucial for improving the prognosis of patients. However, the inadequate accumulation of drugs at the ischemic site significantly restricts their clinical efficacy. We found that platelet membrane (PLTM)-biomimetic nanosystems loaded with curcumin (Cur@PLTM) and tideglusib (Tid@PLTM) actively targeted the ischemic brain and facilitated transcytosis into the ischemic parenchyma via caveolin-dependent transcytosis, mimicking the recruitment of platelets in damaged cerebral vessels. This represented the first application of tideglusib nanoformulations in treating ischemic stroke, further demonstrating that the therapeutic effects were associated with M2 microglia regulation. Additionally, Cur@PLTM and Tid@PLTM synergistically scavenged reactive oxygen species (ROS) and promoted the secretion of neuroprotective cytokines via redox and cellular regulatory mechanisms to mitigate ischemia/reperfusion (I/R) injury. Overall, this platelet membrane-biomimetic nanosystem offers a prospective strategy for targeted brain delivery and combined treatment through antioxidative and anti-inflammatory approaches against ischemic stroke.

CAS / MDL: 371-90-4 9002-89-5
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

3-Carboxyphenylboronic acid functionalized polydopamine-coated cellulose nanocrystals as a pH-responsive nanocarrier for targeted curcumin delivery

Ziqi Li,Yuying Wang,Wengang Chen,Lili Zheng,Weimin Wan,Xi Wang

Targeted and stimuli-responsive drug delivery systems (DDS) hold significant potential for improving therapeutic efficacy and mitigating adverse effects in cancer treatment. Here, we developed a pH-responsive nanocarrier through a surface modification strategy, which enables active targeting of hepatocellular carcinoma (HCC) cells for the delivery of drug curcumin (Cur), a poorly water-soluble therapeutic agent. Briefly, a polydopamine (PDA) layer was first deposited onto the surface of cellulose nanocrystals (CNCs) via the self-polymerization of dopamine hydrochloride. Subsequently, 3-carboxyphenylboronic acid (CA) was grafted onto the PDA-coated surface to obtain CNCs@PDA-CA. After that, Cur was loaded onto CNCs@PDA-CA by forming a boronate ester linkage with the boronic acid groups of CA, resulting in the final nanocomposite CNCs@PDA-CA-Cur with a drug loading capacity of 10.58 ± 1.32 %. This nanocarrier not only exhibited active targeting ability toward HCC cells, but also achieved controlled Cur release in response to the acidic tumor microenvironment. Specifically, CNCs@PDA-CA-Cur showed high pH-responsive ability that released 3.18-folds of Cur in acidic environments (pH = 5.4) more than in neutral environments (pH = 7.2). Furthermore, the nanocarrier demonstrated efficient active targeting to HCC cells, leading to elevated intracellular Cur accumulation and enhanced cytotoxicity in both 2D and 3D HCC models in vitro. Collectively, these results highlight the potential of the targeted and pH-responsive nanocarrier to improve the therapeutic delivery of poorly soluble drugs for HCC treatment.

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Carbohydrate Polymer Technologies and Applications · 2025 · IF 6.5

pH and temperature dual-responsive Pickering emulsion stabilized by alginate-based microgel particles for encapsulation of curcumin

Yao Fu,Shuwen Tan,Xiaojia Xu,Wenlong Xing,Qi He,Yi Lu,Jia Tang,Xiaoyan Liu,Yu Fang

Natural polysaccharides are widely used in biomedical and pharmaceutical applications due to their biocompatibility and biodegradability. In this study, alginate-based Poly( N -vinylcaprolactam)- co -sodium alginate (P(VCL- co -SA)) microgel particles with different mass ratios of VCL/SA were synthesized and employed as stabilizers for curcumin-loaded Pickering emulsions. The obtained P(VCL- co -SA) microgels display a uniform, spherical morphology with low polydispersity. Moreover, the microgels demonstrated high interfacial activity at the dodecane/water interface, enabling the stabilization of dodecane-in-water emulsions across a broad pH range (3–9) at 25°C. At an elevated temperature (55°C), the emulsions remained stable at pH 6 and 9 (above the p K a of alginate, ∼3.5), while phase separation was observed at pH 3 below the p K a . The emulsion stability was further enhanced by optimizing Ca 2+ ion concentration. Furthermore, high internal phase soybean oil-in-water emulsions stabilized by P(VCL 83 - co -SA 17 ) microgels were successfully developed for curcumin encapsulation. The emulsions provided excellent protection for curcumin at room temperature. When incubated at 37°C, curcumin retention was significantly enhanced after the addition of Ca 2+ ions. Compared to previously reported systems that encapsulate curcumin in emulsions, the present approach exhibits superior performance, such as, encapsulation efficiency and retention rate. These findings provide insights into the development of high-performance Pickering emulsions that are stabilized by natural products and highlight their potential applications in food technology and the pharmaceutical industry.

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