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Curcumin
International Journal of Nanomedicine · 2022 · IF 7.033

Novel Curcumin Derivative-Decorated Ultralong-Circulating Paclitaxel Nanoparticles: A Novel Delivery System with Superior Anticancer Efficacy and Safety

Yumeng Wei,Mingtang Zeng,Chao Pi,Hongping Shen,Jiyuan Yuan,Ying Zuo,Jie Wen,Pu Guo,Wenmei Zhao,Ke Li,Zhilian Su,Xinjie Song,Shaozhi Fu,Robert J Lee,Ling Zhao

Purpose Paclitaxel (PTX) has been widely utilized for the treatment of breast cancer. However, drawbacks, such as poor aqueous solubility, rapid blood clearance and severe toxicity, greatly reduce its efficacy and safety. Herein, a novel self-developed curcumin derivative (CUD) was chosen as the carrier to develop a long-acting PTX nano-delivery system (PTX-Sln@CUD) in order to improve its pharmacokinetic behavior, anti-breast cancer efficacy and safety. Methods PTX-Sln@CUD was prepared using solid dispersion and ultrasonic technology. Relevant physical and chemical properties, including stability and release behavior, were characterized. The clearance of PTX-Sln@CUD in vivo was studied by pharmacokinetic experiments. The anti-tumor activity of PTX-Sln@CUD was investigated in vitro and in vivo. Hemolysis experiments, acute toxicity and cumulative toxicity studies were performed in mice to determine the safety of PTX-Sln@CUD. Results The average particle size, PDI, Zeta potential, encapsulation efficiency and loading efficiency of the PTX-Sln@CUD were 238.5 ± 4.79 nm, 0.225 ± 0.011, −33.8 ± 1.26 mV, 94.20 ± 0.49% and 10.98 ± 0.31%, respectively. PTX-Sln@CUD was found to be stable at room temperature for half a year. The cumulative release rates of PTX-Sln@CUD at 24, 96 and 168 h were 17.98 ± 2.60, 57.09 ± 2.32 and 72.66 ± 4.16%, respectively, which were adherent to zero-order kinetics. T 1/2 , MRT (0-t) and AUC (0-t) of the PTX-Sln@CUD group were 4.03-fold (44.293 h), 7.78-fold (38.444 h) and 6.18-fold (14.716 mg/L*h) of the PTX group, respectively. PTX-Sln@CUD group demonstrated stronger anti-breast cancer activity than the PTX group. Importantly, the PTX-Sln@CUD group was safer compared to the PTX group both in vitro and in vivo. Conclusion PTX-Sln@CUD was verified as promising therapeutic nanoparticles for breast cancer and provided a novel strategy to solve the problem of low efficacy and poor safety of clinical chemotherapy drugs.

研究领域: 药理学 · 肿瘤学 · 纳米医学
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EUROPEAN POLYMER JOURNAL · 2023 · IF 6

Sodium Alginate/carboxymethyl chitosan-CuO hydrogel beads as a pH-sensitive carrier for the controlled release of curcumin

Lu Wang,Xin Gang,Yu Xiao,Yi Ren,Jianhong Wang,Baolong Niu,Wenfeng Li

In this study, CMCS-CuO nanoparticles were added to the SA matrix by blending method to prepare SA/CMCS-CuO composite microspheres. The chemical structure and morphology of the composite beads were characterized. The results showed that there was a certain molecular interaction between CMCS-CuO NPs and SA matrix. The swelling experiment showed that with the increase of the mass of CMCS-CuO NPs, the maximum swelling ratio of gel microspheres decreased from 49.83% to 38.2%, and the time to reach the maximum swelling ratio also increased from 8 h to 11 h. Cytotoxicity test, hemolysis test, and cell migration test showed that the composite microspheres had good biocompatibility. Curcumin was added to the composite bead matrix by the blending method, and curcumin-loaded SA/CMCS-CuO composite beads were prepared by the crosslinking method. In vitro release experiments showed that SA/CMCS-CuO composite microspheres had good pH sensitivity, and the addition of CMCS-CuO NPs prolonged the in vitro release time of cur. It has certain application potential in the field of drug release.

CAS / MDL: 9005-38-3
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Photodiagnosis and Photodynamic Therapy · 2023 · IF 3.3

Utilizing the Photodynamic Properties of Curcumin to Disrupt Biofilms in Cutibacterium acnes: A Promising Approach for Treating Acne

Nana Zheng,Yuanyuan Xie,Meng zhou,Yuzhen Liu,Haoxiang Xu,Rong Zeng,Chunping Wan,Min Li

Background : The treatment of acne vulgaris is often challenging due to the antibiotic resistance frequently observed in Cutibacterium acnes ( C.acnes ), a prevalent bacterium linked to this condition. Objective : The objective of this research was to examine the impact of curcumin photodynamic therapy (PDT) on the survival of C.acnes and activity of biofilms produced by this microorganism. Methods : Following the Clinical and Laboratory Standards Institute (CLSI) guidelines, we assessed the drug sensitivity of 25 clinical C.acnes strains to five antibiotics (erythromycin, clindamycin, tetracycline, doxycycline, minocycline) and curcumin by implementing the broth microdilution technique. In addition, we established C.acnes biofilms in a laboratory setting and subjected them to curcumin-PDT(curcumin combined with blue light of 180 J/cm 2 ). Afterwards, we evaluated their viability using the XTT assay and observed them using confocal laser scanning microscopy. Results : The result revealed varying resistance rates among the tested antibiotics and curcumin, with erythromycin, clindamycin, tetracycline, doxycycline, minocycline, and curcumin exhibiting resistance rates of 72%, 44%, 36%, 28%, 0%, and 100%, respectively. In the curcumin-PDT inhibition tests against four representative antibiotic-resistant strains, it was found that the survival rate of all strains of planktonic C. acnes was reduced, and the higher the concentration of curcumin, the lower the survival rate. Furthermore, in the biofilm inhibition tests, the vitality and three-dimensional structure of the biofilms were disrupted, and the inhibitory effect became more significant with higher concentrations of curcumin. Conclusion : The results emphasize the possibility of using curcumin PDT as an alternative approach for the treatment of C.acnes , especially in instances of antibiotic-resistant variations and infections related to biofilms.

CAS / MDL: 64-75-5
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2023 · IF 5.8

Curcumin-Containing polyphosphazene nanodrug for Anti-Inflammation and nerve regeneration to improve functional recovery after spinal cord injury

Xiaochen Su,Xunan Jing,Wanting Jiang,Meng Li,Kai Liu,Menghao Teng,Daquan Wang,Lingjie Meng,Yingang Zhang,Wenchen Ji

The microenvironment of excessive inflammation and the activation of apoptotic signals are primary barriers to neurological recovery following spinal cord injury (SCI). Thus, long-lasting anti-inflammation has become an effective strategy to navigate SCI. Herein, a curcumin (CUR)-containing nanosystem (FCTHPC) with high drug loading efficiency was reported via assembling hydrophobic CUR into cross-linked polyphosphazene (PPZ), and simultaneous loading and coordinating with porous bimetallic polymers for greatly enhanced the water-solubility and biocompatibility of CUR. The nanosystem is noncytotoxic when directing its biological activities. By inhibiting the expression of pro-inflammatory factors (IL-1β, TNF-α and IL-6) and apoptotic proteins (C-caspase-3 and Bax/Bcl-2), which may be accomplished by activating the Wnt/β-catenin pathway, the versatile FCTHPC can significantly alleviate the damage to tissues and cells caused by inflammation and apoptosis in the early stage of SCI. In addition, the long-term in vivo studies had demonstrated that FCTHPC could effectively inhibit the formation of glial scars, and simultaneously promote nerve regeneration and myelination, leading to significant recovery of spinal cord function. This study emphasises the promise of the biocompatible CUR-based nanosystem and provides a fresh approach to effectively treat SCI.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2023 · IF 5.8

Preparation of nano-sized multi-vesicular vesicles (MVVs) and its application in co-delivery of doxorubicin and curcumin

Qiankun Sun,Ju Liang,Yang Lin,Yunyun Zhang,Fuqing Yan,Wenlan Wu

Multi-vesicular vesicles (MVVs) offer structural advantages in terms of drug encapsulation and physiological stability. In this study, we address the challenge of preparing small-sized MVVs for drug delivery. The nano-sized MVVs (~120   nm) loaded with doxorubicin (DOX) and curcumin (CUR) (DOX/ [email protected] ) were successfully prepared using a glass bead combined with a thin film dispersion method. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) analysis confirmed the independent non-homocentric vesicle structures of DOX/ [email protected] with homogeneous particle sizes. The experimental results showed high encapsulation rates of DOX and CUR in DOX/ [email protected] , reaching 82.5±0.75% and 85.9±0.69%, respectively. Moreover, the MVVs exhibited good biosafety and sustained release properties. Notably, the bioavailability of DOX and CUR in DOX/ [email protected] was enhanced compared to free DOX and CUR, with increases of 4.2 and 2.1 times, respectively. And the half-life of DOX and CUR was extended by 10 times in DOX/ [email protected] In vivo antitumor experiments demonstrated that nano-sized DOX/ [email protected] significantly improved the antitumor activity while reducing the toxic side effects of DOX. Overall, the successful preparation of nano-sized DOX/ [email protected] and their potent and low-toxic antitumor effects provide a critical experimental reference for the combined antitumor therapy of MVVs and liposomes.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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Foods · 2023 ·Vol. 12 ·期 13 ·2533 · IF 5.2

Effects of Different Molecular Weight Oxidized Dextran as Crosslinkers on Stability and Antioxidant Capacity of Curcumin-Loaded Nanoparticles

Dongyan Shen,Hongzhou Chen,Mingwei Li,Ling Yu,Xiangfei Li,Huawei Liu,Qiaobin Hu,Yingjian Lu

Curcumin is a polyphenolic compound that has been widely investigated for its health benefits. However, the clinical relevance of curcumin is limited due to its low water solubility and inefficient absorption. Therefore, curcumin is often encapsulated in nanocarriers to improve its delivery and function. In this study, composite nanoparticles composed of stearic acid-modified chitosan (SA-CS) and sodium caseinate (NaCas) were formed using sodium periodate-oxidized dextran with different molecular weights as a crosslinking agent. The effects of oxidized dextran (Odex) with different molecular weights on the composite nanoparticles were compared. The optimal SA-CS/NaCas/Odex composite nanoparticle (NPO) was obtained using an Odex (150 kDa)-to-SA-CS mass ratio of 2:1. Its size, polydispersity index (PDI), and zeta potential (ZP) were 130.2 nm, 0.149, and 25.4 mV, respectively. The particles were highly stable in simulated gastric fluid (SGF) in vitro, and their size and PDI were 172.3 nm and 0.263, respectively. The encapsulation rate of NPO loaded with curcumin (Cur-NPO) was 93% under optimal ultrasonic conditions. Compared with free curcumin, the sustained release of Cur-NPO significantly reduced to 17.9%, and free-radical-scavenging ability improved to 78.7%. In general, the optimal prepared NPO exhibited good GI stability and has potential applications in the formulation of orally bioactive hydrophobic drugs.Keywords:curcumin;modified chitosan;oxidized dextran;nanoparticles;stability;antioxidant capacity

✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD HYDROCOLLOIDS · 2022 · IF 11.504

Hydrolyzed rice glutelin nanoparticles as particulate emulsifier for Pickering emulsion: Structure, interfacial properties, and application for encapsulating curcumin

Zhenyu Yang,Jiakai Yan,Yanhua Duan,Lei Dai,Yanfei Wang,Qingjie Sun,David Julian McClements,Xingfeng Xu

Oil-in-water Pickering emulsions prepared by food-grade particles have gained increasing interest on account of their potential application in the delivery system for lipophilic active compounds. In this project, hydrolyzed rice glutelin (HRG) nanoparticles were successfully fabricated inducing by different concentrations of ethanol. The structure, interfacial properties of HRG nanoparticles, Pickering emulsion stability and in vitro gastrointestinal digestion characteristics were investigated. With ethanol concentration increasing from 25% to 100%, the Z-average diameter and surface activity of HRG nanoparticles increased firstly and then decreased, whereas the magnitudes of the ζ-potential and surface hydrophobicity increased. Quartz crystal microbalance with dissipation (QCM-D) indicated that HRG nanoparticles induced by ethanol with the concentration of 50% (HRG50) and 75% (HRG75) showed a more viscous interfacial film. HRG50- and HRG70-stabilized emulsions had better storage stability compared with other samples. Furthermore, the curcumin was loaded into Pickering emulsions using the pH-shift method. The light stability and gastrointestinal fate were assessed. Compared with curcumin-loaded HRG75-Pickering emulsion, HRG50-Pickering emulsion exhibited higher photochemical stability, whereas the lower FFAs release, bioaccessibility and transformation. This behavior was attributed to the thicker interfacial layer for HRG50 Pickering emulsion. This knowledge indicated that emulsion stabilized by HRG nanoparticles could be used as a delivery system to protect hydrophobic bioactive compounds . This research provided theoretical support to develop the utilization of HRG nanoparticles.

CAS / MDL: 2917-26-2
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Current Research in Food Science · 2022 · IF 6.269

Anti-fatigue and anti-oxidant effects of curcumin supplementation in exhaustive swimming mice via Nrf2/Keap1 signal pathway

Yong Chen,Jiajun Wang,Ziheng Jing,Jose M. Ordovas,Jing Wang,Lirong Shen

Demands for dietary supplements with anti-fatigue effects are growing fast due to increasing societal demands. Moreover, in highly physically active individuals, there are also significant needs for supplements to improve exercise performance. The present study evaluated the potential anti-fatigue and anti-oxidant effects of curcumin in mice using exhaustive swimming test. Male C57BL/6J mice were randomized into six groups: blank control (Rest), swimming control (Con), Vitamin C (Vc), low-dose curcumin (C 50 ), middle-dose curcumin (C 100 ), and high-dose curcumin (C 200 ). After a 4-week intervention, the mice in all groups except the Rest group were subject to an exhaustive swimming test. Then, mice were sacrificed to examine serum biochemical markers and fatigue-related enzymes. Moreover, the gene and protein expressions of signal transduction factors involved in the Nrf2/Keap1 signaling pathway were measured. The results indicated that curcumin significantly enhanced the exercise tolerance of mice in the exhaustive swimming test. Particularly, the swimming time of mice in the C 100 group was increased by 273.5% when compared to that of mice in the Con group. The levels of blood urea nitrogen, blood ammonia, lactic acid, creatine kinase and lactate dehydrogenase in the C 100 group were decreased by 13.3%, 21.0%, 18.6%, 16.7% and 21.9%, respectively, when compared to those of mice in the Con group. Curcumin alleviated exercise-induced oxidative stress and significantly enhanced the activities of superoxide dismutase, catalase and glutathione peroxidase by activating the Nrf2 signaling. These findings indicated that curcumin supplementation exerted remarkable anti-oxidant and anti-fatigue effects in mice, providing additional evidence supporting the use of curcumin as functional food, especially by those engaged in sports-related activities.

CAS / MDL: 9004-32-4
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Photodiagnosis and Photodynamic Therapy · 2022 · IF 3.577

Curcumin-loaded multifunctional chitosan gold nanoparticles: An enhanced PDT/PTT dual-modal phototherapeutic and pH-responsive antimicrobial agent

Ying Zhang,Peiyuan Li,Rixiang Su,Fangzhou Wen,Zhiruo Jia,Yingbin Lv,Jinyun Cai,Wei Su

Overuse of antibiotics has led to the emergence of multidrug resistant (MDR) bacteria.. Photothermal (PTT) and photodynamic therapy (PDT) have may be effective alternatives for antibiotics in the treatment of bacterial infections. In this study, based on chitosan (CS)-coated gold nanoparticles, a pH stimulus-responsive drug delivery system was developed, which can anchor to the cell membrane for photodynamic therapy and photothermal therapy, and enhance the therapeutic potential of curcumin (Cur). Release experiments showed that AuNPs/CS-Cur nanocomposites released curcumin in a pH-dependent manner, which may facilitate the drug to be delivered to the acidic bacterial infection environment. CS as the outer layer covered on gold nanoparticles could improve the dispersibility of Cur in aqueous solution, gold nanoparticles prevent rapid photobleaching of curcumin, thus ensuring the yield of singlet oxygen under irradiation, and enhance the electrostatic binding with bacteria cell membrane. Under light conditions, AuNPs/CS-Cur can produce a large amount of reactive oxygen species and heat to kill S. aureus and E. coli . Compared with free Cur-mediated PDT, the complex significantly improved the synergistic PTT/PDT photoinactivation ability against S. aureus and E. coli . In addition, AuNPs/CS-Cur had good biocompatibility. Therefore, AuNPs/CS-Cur possessed the characteristics of electrostatic targeting, photodynamic and photothermal antibacterial therapy, which would become an efficient and safe antibacterial nano-platform and provide new ideas for the treatment of bacterial infection.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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EUROPEAN POLYMER JOURNAL · 2022 · IF 5.546

Preparation of curcumin loaded hyaluronic acid-poly (lactic-co-glycolic acid) micelles with pH response and tumor targeting

Hong Wang,Yanwei Zhang,Yaru Liu,Yi Ren,Jianhong Wang,Baolong Niu,Wenfeng Li

Cancer, a cause of high mortality in the world today, is a serious threat to the public health security of various countries. Targeted drug delivery systems with good biocompatibility have become a hot research topic in the field of cancer therapy. In this paper, HA-SS-PLGA copolymer was prepared using cystine (SS) containing disulfide bond as the linker, hyaluronic acid (HA) as the hydrophilic end and poly (lactic- co -glycolic acid) (PLGA) as the hydrophobic end. It will self-assemble in aqueous solution to form amphiphilic micelles with the hydrophilic end outside and the hydrophobic end inside. Among them, SS can react with glutathione in cancer cells by reduction, making the polymer reduction-sensitive. Then, reduction-sensitive Cur-HA-SS-PLGA nanoparticles loaded with Cur were prepared and characterized using curcumin as a model drug. The results showed that HA-SS-PLGA with pH sensitivity and good hemocompatibility could actively target to tumor cell surface overexpression receptors (CD44 receptors) and enter MCF-7 cells through endocytosis, and inhibit the proliferation of cancer cells after drug release. Therefore, the prepared HA-SS-PLGA is expected to be a good drug carrier in the field of cancer therapy.

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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2022 · IF 6.51

Colon-targeted oral nanoparticles based on ROS-scavenging hydroxyethyl starch-curcumin conjugates for efficient inflammatory bowel disease therapy

Chenlan Xu,Shuting Chen,Cuiping Chen,Yangcan Ming,Jiahao Du,Jinyi Mu,Fang Luo,Da Huang,Na Wang,Zhenyu Lin,Zuquan Weng

Co-delivery of anti-inflammatory drugs and reactive oxygen species (ROS) scavengers by stimuli-responsive oral nanoparticles is deemed to be a favorable strategy for inflammatory bowel disease (IBD) therapy. In this study, using micelles formed by CUR conjugated hydroxyethyl starch (HES) as vehicles, dexamethasone (DEX)-loaded HES-CUR nanoparticles (DHC NPs) with desirable size, negative surface charge, good stability in the harsh gastric environment, and excellent ROS scavenging activity are developed as a colon-targeted oral formulation for treating IBD. Due to the degradation of HES in response to α-amylase overexpressed in the inflamed colon, the DHC NPs release drugs in an α-amylase-responsive manner. Meanwhile, the DHC NPs can be effectively internalized by macrophages and show excellent cytocompatibility with macrophages since they are composed of food-derived compounds. Importantly, in vivo studies reveal that the DHC NPs are capable of targeting the inflamed colon induced by dextran sulfate sodium (DSS), and the targeted and combination therapy enhances the efficacy of free DEX and significantly relieves the impairment caused by DSS-induced ulcerative colitis. Incorporating the merits of targeted drug delivery and combined therapy with an anti-inflammatory drug and ROS scavenger, the DHC NPs are promising for developing novel oral formulations for IBD therapy.

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