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Curcumin
CARBOHYDRATE POLYMERS · 2023 · IF 11.2

Dialdehyde xanthan gum and curcumin synergistically crosslinked bioprosthetic valve leaflets with anti-thrombotic, anti-inflammatory and anti-calcification properties

Mengyue Hu,Xu Peng,Shubin Shi,Chang Wan,Can Cheng,Xixun Yu

Currently commercial glutaraldehyde (GA)-crosslinked bioprosthetic valve leaflets (BVLs) suffer from thromboembolic complications, calcification, and limited durability, which are the major stumbling block to wider clinical application of BVLs. Thus, developing new-style BVLs will be an urgent need to enhance the durability of BVLs and alleviate thromboembolic complications. In this study, a quick and effective collaborative strategy of the double crosslinking agents (oxidized polysaccharide and natural active crosslinking agent) was reported to realize enhanced mechanical, and structural stability, excellent hemocompatibility and anti-calcification properties of BVLs. Dialdehyde xanthan gum (AXG) exhibiting excellent stability to heat, acid-base, salt, and enzymatic hydrolysis was first introduced to crosslink decellularized porcine pericardium (D-PP) and then curcumin with good properties of anti-inflammatory, anti-coagulation, anti-liver fibrosis, and anti-atherosclerosis was used to synergistically crosslink and multi-functionalize D-PP to obtain AXG + Cur-PP. A comprehensive evaluation of structural characterization, hemocompatibility, endothelialization potential, mechanical properties and component stability showed that AXG + Cur-PP exhibited better anti-thrombotic properties and endothelialization potential, milder immune responses, excellent anti-calcification properties and enhanced mechanical properties compared with GA-crosslinked PP . Overall, this cooperative crosslinking strategy provides a novel solution to achieve BVLs with enhanced mechanical properties and excellent anti-coagulation, anti-inflammatory, anti-calcification, and the ability to promote endothelial cell proliferation .

CAS / MDL: 133232-56-1
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2022 · IF 8.025

Improving the physicochemical stability of Pickering emulsion stabilized by glycosylated whey protein isolate/cyanidin-3-glucoside to deliver curcumin

Xiaoya Tao,Cheng Chen,Yaochang Li,Xinguang Qin,Haizhi Zhang,Yuanyuan Hu,Zhengqi Liu,Xiaoming Guo,Gang Liu

Protein-polysaccharide-polyphenol delivery systems function as a promising tool to deliver bioactive ingredients aiming to improve their solubility and bioavailability. In this study, whey protein isolate (WPI), short-chain inulin (SCI), and cyanidin-3-glucoside (C3G) were first used to stabilize Pickering emulsions. The physicochemical properties and stability of curcumin encapsulated or not in Pickering emulsions were explored. Results showed that glycosylation and C3G reduced surface and interfacial tension on protein surfaces and inhibited the aggregation of emulsion droplets, thereby reducing the emulsion's particle size. WPI-SCI/C3G stabilized Pickering emulsion had the best stability. The CLSM results showed that the WPI-SCI and WPI-SCI/C3G stabilized emulsions were uniformly dispersed, suggesting that glycosylation and the interaction between protein and C3G enhanced the adsorption capacity of the interfacial protein and improved the stability of the Pickering emulsion. The retention rates of curcumin-loaded WPI-SCI- (67.34 %) and WPI-SCI/C3G- (77.07 %) stabilized Pickering emulsions on day 8 of storage were higher than those in WPI- (33.97 %) and WPI/C3G- (37.02 %) stabilized emulsions, and the degradation half-life was also extended from 7 days to >15 days. These findings provide a theoretical basis for the application of WPI Pickering emulsion and indicate a useful means for the delivery of bioactive components.

CAS / MDL: 3326-32-7 7385-67-3
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Polymers · 2022 ·Vol. 15 ·期 1 ·116 · IF 4.967

The Dual Modification of PNIPAM and β-Cyclodextrin Grafted on Hyaluronic Acid as Self-Assembled Nanogel for Curcumin Delivery

Tisana Kaewruethai,Yuan Lin,Qian Wang,Jittima Amie Luckanagul

Curcumin is an extract of turmeric (Curcuma longa) which possesses anti-inflammatory, anti-cancer and wound-healing effects and has been used as an active compound in biomedical research for many years. However, its poor solubility presents challenges for its use in drug delivery systems. A modified nanogel delivery system, with PNIPAM and β-cyclodextrin grafted onto hyaluronic acid (PNCDHA), was utilized to enhance the solubility. The polymer was characterized by NMR, and the inclusion complex between curcumin and β-cyclodextrin was confirmed by FTIR. The potential of this PNCDHA polymer complex as a drug delivery vehicle was supported by a curcumin encapsulation efficiency of 93.14 ± 5.6% and the release of encapsulated curcumin at 37 °C. At a concentration of 0.5%w/vin water, PNCDHA nanogels were biocompatible with fibroblast cell line (L929) up to a curcumin concentration of 50 µM. There was a direct concentration between curcumin loading and cellular internalization. A more detailed study of the cellular internalization of PNCDHA nanogel should be considered in order to clarify cellular delivery mechanisms and to assess how its viability as a carrier may be optimized.Keywords:hyaluronic acid;β-cyclodextrin;PNIPAM;thermoresponsive;nanogel;self-assembly;curcumin

CAS / MDL: 25952-53-8 6066-82-6
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2018 · IF 1.883

A W/O emulsion mediated film dispersion method for curcumin encapsulated pH-sensitive liposomes in the colon tumor treatment

Yi Chen,Qianming Du,Qianqian Guo,Jing Huang,Lina Liu,Xiangchun Shen,Jianqing Peng

The CaCO3 encapsulated liposome with pH sensitivity is an efficient carrier for the delivery of chemotherapeutic drugs. Herein, we provided an innovative method that take advantage of a W/O emulsion to prepare CaCO3 encapsulated liposomes for the delivery of curcumin. The liposomes with both CaCO3 and curcumin encapsulated (LCC) showed high sensitivity to reduced pH (the environment of lysosomes). Due to the inherent pH sensitivity of CaCO3, LCC swelled and released the encapsulated curcumin rapidly in acidic medium. The lysosome escape capability and promoted accumulation of curcumin in the cytosol from LCC was verified with respect to that of curcumin loaded liposomes (CLIPO). Despite the similar cytotoxicity within curcumin preparations in vitro at high concentration, LCC exhibited optimal antitumor effect in an azoxymethane (AOM)/dextran sodium sulfate (DSS)-induced colorectal cancer model, which was attributed to the long circulation time and efficient intracellular delivery of curcumin from LCC. It is suggested that the solubility and cytosolic delivery of curcumin are greatly improved by LCC, which accounts for the increased pharmacodynamic effect of curcumin. Thus, the CaCO3 encapsulated liposomes developed in this study is an ideal carrier for the hydrophobic drugs in potential clinical application.

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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2018 · IF 1.883

Preparation of curcumin-hydroxypropyl-β-cyclodextrin inclusion complex by cosolvency-lyophilization procedure to enhance oral bioavailability of the drug

Ning Li,Ning Wang,Tingni Wu,Changlu Qiu,Xueting Wang,Shaohong Jiang,Zina Zhang,Ting Liu,Chunliu Wei,Ting Wang

The curcumin (CUR)-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex (CUR-HP-β-CD) was prepared to erase its therapeutic restrictions of poor aqueous solubility and low oral bioavailability. CUR-HP-β-CD was prepared by a simple procedure of water-ethanol cosolvent incubation-lyophilization which may be suitable for scale up production, and characterized by Fourier transform-infrared spectroscopy (FT-IR), powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), phase solubility method and dissolution study; the in vitro cytotoxicity was assayed by MTT, whereas the in vivo pharmacokinetics was tested by HPLC in rats receiving formulations via intravenous and oral administration, respectively. CUR was successfully encapsulated in HP-β-CD with a loading capacity of about 1:7 of CUR to HP-β-CD mole ratio, which remarkably enhanced drug water solubility and maintained well the antitumour activity of CUR. The CUR-HP-β-CD and free CUR have a similar pharmacokinetic behaviour in rats after intravenous administration; however, the oral bioavailability of CUR was enhanced to 2.77-fold by the HP-β-CD. The CUR-HP-β-CD can be successfully prepared by a simple method, which may be feasible for industrial scaling up, to remarkably increase drug water solubility and oral bioavailability while maintaining its bioactivity and may be a promising therapeutic preparation.

CAS / MDL: 518-82-1 298-93-1
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Biomaterials Science · 2018 ·Vol. 6 ·期 12 ·3397-3409 · IF 5.831

An E-selectin targeting and MMP-2-responsive dextran–curcumin polymeric prodrug for targeted therapy of acute kidney injury

Jing-Bo Hu,Di Liu,Jing Qi,Kong-jun Lu,Fei-yang Jin,Xiao-Ying Ying,Jian You,Yong-Zhong Du

Based on the overproduction of matrix metalloproteinase-2 (MMP-2) in renal tissue during acute kidney injury (AKI) occurrence, we developed a MMP-2 enzyme-triggered polymeric prodrug with sialic acid (SA) as the targeting group to the inflamed vascular endothelial cells for enhanced therapeutic outcomes. An MMP-2-responsive peptide, PVGLIG, was used to endow the polymeric prodrug with the ability to rapidly release the anti-inflammatory drug, curcumin (CUR), after the targeted site is reached and to improve the drug concentration in the target tissue. The sialic acid–dextran–PVGLIG–curcumin (SA-DEX-PVGLIG-CUR) polymeric prodrug was successfully synthesized via multi-step chemical reactions and characterized by 1H NMR. The water solubility of CUR was significantly increased in the polymeric prodrug and was approximately 23-fold higher than that of free CUR. The in vitro drug release results showed that the release rate of SA-DEX-PVGLIG-CUR was significantly enhanced compared to that of SA-DEX-CUR in a dissolving medium containing the MMP-2 enzyme, suggesting that SA-DEX-PVGLIG-CUR had rapid drug release characteristics in an inflammatory environment. A cellular uptake test confirmed that SA-DEX-PVGLIG-CUR was effectively internalized by inflamed vascular endothelial cells in comparison with that by normal cells, and the mechanism was associated with the specific interaction between SA and E-selectin receptors specifically expressed on inflamed vascular endothelial cells. Bio-distribution results further demonstrated the rapid and increased renal accumulation of SA-DEX-PVGLIG-CUR in AKI mice. Benefiting from the rapid drug release in renal tissue, SA-DEX-PVGLIG-CUR effectively ameliorated the pathological progression of AKI compared with free CUR and SA-DEX-CUR, as reflected by the improved renal functions, histopathological changes, pro-inflammatory cytokine production, oxidative stress and expression of apoptosis related proteins. Altogether, this study provided a new therapeutic strategy for the treatment of AKI.

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Food Bioscience · 2024 · IF 4.8

Co-delivery of resveratrol and curcumin based on Mesona chinensis polysaccharides/zein nanoparticle for targeted alleviation of ulcerative colitis

Jun Yang,Xianxiang Chen,Jieqiong Lin,Mingyue Shen,Yuanxing Wang,Anwesha Sarkar,Huiliang Wen,Jianhua Xie

Herein, a novel oral nano-delivery system (CR-NPs) was designed for co-delivering curcumin and resveratrol to treat ulcerative colitis (UC) using Mesona chinensis polysaccharides and zein via antisolvent precipitation and continuous water evaporation crosslinking. It showed high encapsulation rates for both bioactives due to hydrogen bonding and hydrophobic forces. CR-NPs have favorable in vitro gastrointestinal stability and low pre-colonic release rates, resulting in increased accumulation in the colon. In vivo therapeutic effects of CR-NPs were confirmed through alleviation of UC symptoms and inflammation of UC mice. CR-NPs maintained the balance of intestinal flora and promoted the production of short-chain fatty acids in UC mice. Furthermore, CR-NPs intervention can alleviate the development of UC by modulating arachidonic acid, linoleic acid, and tryptophan metabolism. This study provides some theoretical basis using a novel dietary protocol option that co-delivering natural bioactives to the colon for alleviation of UC.

CAS / MDL: 501-36-0
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2016 · IF 3.902

Mucoadhesive microparticulates based on polysaccharide for target dual drug delivery of 5-aminosalicylic acid and curcumin to inflamed colon

Haogang Duan,Shaoyu Lü,Chunmei Gao,Xiao Bai,Hongyan Qin,Yuhui Wei,Xin’an Wu,Mingzhu Liu

In this work, thiolated chitosan/alginate composite microparticulates (CMPs) coated by Eudragit S-100 were developed for colon-specific delivery of 5-aminosalicylic acid (5-ASA) and curcumin (CUR), and the use of it as a multi drug delivery system for the treatment of colitis. The physicochemical properties of the CMPs were evaluated. In vitro release was performed in gradually pH-changing medium simulating the conditions of different parts of GIT, and the results showed that the Eudragit S-100 coating has a pH-sensitive release property, which can avoid drug being released at a pH lower than 7. An everted sac method was used to evaluate the mucoadhesion of CMPs. Ex vivo mucoadhesive tests showed CMPs have excellent mucosa adhesion for the colonic mucosa of rats. In vivo treatment effect of enteric microparticulates systems was evaluated in colitis rats. The results showed superior therapeutic efficiency of this drug delivery system for the colitis rats induced by TNBS. Therefore, the enteric microparticulates systems combined the properties of pH dependent delivery, mucoadhesive, and control release, and could be an available tool for the treatment of human inflammatory bowel disease.

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Journal of Materials Chemistry A · 2015 ·Vol. 3 ·期 8 ·4604-4611 · IF 7.443

Highly cross-linked fluorescent poly(cyclotriphosphazene-co-curcumin) microspheres for the selective detection of picric acid in solution phase

Wei Wei,Rongjie Lu,Shuyuan Tang,Xiaoya Liu

Highly cross-linked and organic–inorganic hybrid poly(cyclotriphosphazene-co-curcumin) microspheres (PCPC-MS) were facilely prepared by a one-step precipitation copolymerization method, and served as a fluorescent chemical sensor for the detection of picric acid (PA) in solution phase. The photochemically inert cyclotriphosphazene moieties intentionally introduced into the structure of the sensor could play a role not only in connecting curcumin fluorophores to construct a highly cross-linked fluorescent architecture with excellent thermal stability and photobleaching stability, but also in effectively enriching PA from bulk solution to the surface of the sensor by the acid–base interaction between the acidic phenolic hydroxyl groups of PA molecules and the electron-rich nitrogen atoms of the cyclotriphosphazene units, which might facilitate the formation of a ground-state non-fluorescent complex of the microspheres and PA as well as the excited-state energy transfer from the microspheres to PA. Therefore, PCPC-MS exhibited a fluorescence quenching response towards PA with high sensitivity, efficiency, and selectivity over a number of other analytes such as 2,4,6-trinitrotoluene, 2,4-dinitrotoluene, 1,3-dinitrobenzene, 4-nitrotoluene, nitrobenzene, 4-benzoquinone, chlorobenzene, and nitromethane in methanol. In addition, PCPC-MS could also effectively detect PA in the presence of the other analytes, indicating their remarkable ability for resisting interferences and specific recognition of PA. This study provides new insights into the design and preparation of a polymer-based fluorescence chemical sensor for PA with low toxicity, a simple preparation process, and high selectivity.

CAS / MDL: 118-96-7
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TOXICOLOGY AND APPLIED PHARMACOLOGY · 2014 · IF 3.63

Tetrachloro-p-benzoquinone induces hepatic oxidative damage and inflammatory response, but not apoptosis in mouse: The prevention of curcumin

Demei Xu,Lihua Hu,Chuanyang Su,Xiaomin Xia,Pu Zhang,Juanli Fu,Wenchao Wang,Duo Xu,Hong Du,Qiuling Hu,Erqun Song,Yang Song

This study investigated the protective effects of curcumin on tetrachloro- p -benzoquinone (TCBQ)-induced hepatotoxicity in mice. TCBQ-treatment causes significant liver injury (the elevation of serum AST and ALT activities, histopathological changes in liver section including centrilobular necrosis and inflammatory cells), oxidative stress (the elevation of TBAR level and the inhibition of SOD and catalase activities) and inflammation (up-regulation of iNOS , COX-2, IL-1β, IL-6, TNF-α and NF-κB). However, these changes were alleviated upon pretreatment with curcumin. Interestingly, TCBQ has no effect on caspase family genes or B-cell lymphoma 2 (Bcl-2)/Bcl-2 associated X (Bax) protein expressions, which implied that TCBQ-induced hepatotoxicity is independent of apoptosis. Moreover, curcumin was shown to induce phase II detoxifying/antioxidant enzymes HO-1 and NQO1 through the activation of nuclear factor erythroid-derived 2-like 2 (Nrf2). In summary, the protective mechanisms of curcumin against TCBQ-induced hepatoxicity may be related to the attenuation of oxidative stress, along with the inhibition of inflammatory response via the activation of Nrf2 signaling.

CAS / MDL: 458-37-7 118-75-2
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2024 · IF 6

Effects of gelatin-transglutaminase crosslinking, vitamin addition, and storage temperature on the properties of curcumin/fish oil-loaded emulsions

Jiamin Xu,Guangyi Kan,Kefeng Yang,Juan Wang,Xichang Wang,Jian Zhong

The effects of gelatin-transglutaminase (TG) crosslinking and anti-oxidant types on the stabilization of curcumin in emulsions have not been studied. This work aimed to analyze the effects of bovine bone gelatin (BBG)-TG crosslinking and vitamin (vitamin C, VC; vitamin E, VE) addition on the properties of curcumin/fish oil-loaded gelatin-stabilized emulsions. The BBG-TG was prepared via a crosslinking method and the emulsions were prepared using a homogenization method. The gelatin-TG crosslinking and low-temperature (4 ± 1 °C) storage increased, VC decreased, and VE had no obvious effect on the emulsion creaming stability. The synergetic use of gelatin-TG crosslinking with VC + VE decreased the peroxidation values at day 7 to 2.1 ± 0.2 mmol/kg oil (room temperature) and 1.6 ± 0.1 mmol/kg oil (4 ± 1 °C). The low-temperature storage induced better curcumin retention than both vitamin addition and gelatin-TG crosslinking. In the in vitro digestion process, the gelatin-TG crosslinking increased the transformation, bio-accessibility, and bio-accessibility index of curcumin, whereas it decreased accumulative released free fatty acid percentages. Vitamin addition increased the bio-accessibility and the bio-accessibility index of curcumin in the emulsions after the in vitro digestion process. This work benefited the encapsulation of curcumin and anti-oxidants (VC and VE) in oil-in-water emulsions and its application in dairy functional food development.

CAS / MDL: 6104-58-1
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