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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

Fabrication of targeted and pH responsive lysozyme-hyaluronan nanoparticles for 5-fluorouracil and curcumin co-delivery in colorectal cancer therapy

Maolin Li,Yin Liu,Yanbo Liu,Jiawei Lin,Lei Ding,Songgu Wu,Junbo Gong

Green nanotechnology is considered a promising method to construct functional materials with significant anticancer activity , while overcoming the shortcomings of traditional synthesis process complexity and high organic solvents consumption. Thus, in this study, we report for the first time the rational design and green synthesis of functionalized 5-fluorouracil and curcumin co-loaded lysozyme-hyaluronan composite colloidal nanoparticles (5-Fu/Cur@LHNPs) for better targeted colorectal cancer therapy with minimized side effects. The functionalized 5-Fu/Cur@LHNPs exhibit stabilized particle size (126.1 nm) with excellent homogeneity (PDI = 0.1), favorable colloidal stabilities, and excellent re-dispersibility. In vitro cell experiments illustrate that the cellular uptake of 5-Fu/Cur@LHNPs was significantly improved and further promoted a higher apoptosis ratio of HCT-116 cells. Compared with the control group, the 5-Fu/Cur@LHNPs formulation group achieved effective inhibition (60.1 %) of colorectal tumor growth. The alcohol-free self-assembly method to construct 5-Fu/Cur@LHNPs is simple and safe for a translational chemotherapy drug, also to promote more robust delivery systems for treating colorectal cancer.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2023 · IF 8.2

A co-carrier for plasmid DNA and curcumin delivery to treat pancreatic cancer via dendritic poly(l-lysine) modified amylose

Jiadong Pang,Baoxiong Zhuang,Li-Ming Zhang

Pancreatic cancer is one of the most lethal malignancies in the world and remains one of the leading causes of cancer related death. For its treatment, a lot of investigations have dealt not only with individual chemotherapy by using polymeric carriers to deliver anticancer drugs, but also with individual gene therapy by using polymeric carriers to deliver nucleic acids such as small interfering RNA (siRNA) and plasmid DNA . However, relatively few studies have been focused on the co -delivery of gene and anticancer drug by multifunctional polymeric carriers for its synergistic therapy. In this work, a DPLL-functionalized amylose (ADP) was prepared by the click reaction between azidized amylose and propargyl focal point poly( l -lysine) dendrons, and then used to co-deliver plasmid pIRES2-EGFP-TNFα and curcumin for pancreatic cancer treatment. Due to the internal hydrophobic cavity of amylose component, ADP could load efficiently curcumin with anticancer activity and showed a sustained release behavior. Moreover, the curcumin-loaded ADP could form colloidally stable nanocomplexes with plasmid DNA in aqueous system due to the existence of cationic poly( l -lysine) dendrons and exhibited high gene transfection efficiency. The in vitro and in vivo tests confirmed the effectiveness of using ADP to co-deliver plasmid pIRES2-EGFP-TNFα and curcumin for synergistic therapy of pancreatic cancer.

✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY · 2023 · IF 3.3

Synergistic effect of egg white protein particle and rhamnolipid on improving bioavailability of curcumin carried in high internal phase emulsions

Cuihua Chang,Xinyang Shen,Yujie Su,Luping Gu,Yanjun Yang,Junhua Li

Summary High internal phase emulsions (HIPEs) are potential carrier of fat-soluble nutrients due to their high loading capacity. This study, egg white protein particle (EWPP) and rhamnolipid (Rha) were used to co-emulsify oil/water HIPEs to carry curcumin (Cur). The results showed that, the Cur loading efficiency, microstructure, protein composition, molecular distribution of protein hydrolysates, protein interfacial adsorption rate and Cur bioavailability were measured. The results showed that, incorporation with Rha was unhelpful for improving loading efficiency of Cur, which decreased from 80.8% to 73.7% at pH 3.8 after incorporation with Rha, due to the decreased viscosity and destroyed continuous interface membrane, while beneficial for restricting coalescence of oil droplets. As studied, Rha could effectively reduce droplet size to slow down the speed of coalescence and form EWPP-Rha complex to inhibit proteolysis. Finally, Cur bioavailability in EWPP-Rha co-emulsified HIPE was the highest (40.3%), indicating the synergistic effect of EWPP and Rha promoting the effective adsorption of Cur, related to the increased coalescence stability during digestion and participation of Rha in the micellization reaction. In comparison, fibrous (pH 3.8) and granular (pH 7.0) EWPP stabilized HIPEs, showed no obvious difference in Cur bioavailability, due to the balance between interfacial adsorption ability and digestion resistance of EWPP with various morphology. This study has important significance for the construction of lipid soluble nutrient “carriers” with high load and high bioavailability.

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Food & Function · 2023 · IF 6.1

Konjac glucomannan assisted curcumin alleviated Dextran sulfate sodium-induced mice colitis via regulating immune response and maintaining intestinal barrier integrity

Pengkui Xia,Mengge Zhao,Hong Jin,Tao Hou,Zhichang Deng,Mengting Zhang,Qiaoyun Zhou,Fuchao Zhan,Bin Li,Jing Li

Curcumin has been proved to be an effective strategy to reduce inflammatory responses. However, low bioavailability and instability at physiological pH have limited its anti-inflammation in ulcerative colitis patients. In the present study, the complex of curcumin and konjac glucomannan (KGM) could inhibit intestinal inflammation more effectively and this effect was associated with KGM degradation degrees. Results demonstrated that treatment with complex markedly mitigated colitis symptoms and decreased the inflammatory cytokines levels, especially in the complex treatment groups with K110 (KGM treated in 110 ℃) and konjac oligosaccharides (KOS). Furthermore, increasing KOS content in KOC (complex of curcumin and KOS) promoted the gene expressions of intestinal barrier and inhibited the gene expressions of inflammatory cytokines as well as improved gut microbiota dysregulation. Overall, our researches suggest that the complex of curcumin and KGM exerts more effective anti-inflammatory effects via regulating the intestinal immune response and modulating microbiota diversity and composition.

CAS / MDL: 64-19-7 107-92-6 79-09-4
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FOOD CHEMISTRY · 2021 · IF 7.514

Preparation of Pickering emulsion gels based on κ-carrageenan and covalent crosslinking with EDC: Gelation mechanism and bioaccessibility of curcumin

Bao Zhang,Ran Meng,Xiao-Long Li,Wen-Jie Liu,Jie-Shun Cheng,Wu Wang

Pickering emulsions stabilized by zein/carboxymethyl dextrin nanoparticles were added to the κ-carrageenan-based gel matrix to prepare emulsion gels via EDC - induced covalent crosslinking. Texture, WHC and freeze–thaw stability of the emulsion gels increased after crosslinking. The Confocal laser scanning microscope and SEM suggested that droplet clusters could be observed in gel with higher concentration of emulsion. The rheological measurements indicated that the viscosity and gel-like structure were relied on crosslinking agent and emulsion concentration. The photothermal stability of curcumin was significantly enhanced after crosslinking. In addition, in vitro digestion study suggested that the bioaccessibility of curcumin in emulsion gel crosslinked was lower compared to emulsion gel without crosslinking agent. These studies might facilitate the preparation of emulsion gels with excellent stability for bioactive compounds delivery in food and pharmaceutical applications.

CAS / MDL: 25952-53-8 6066-82-6
✓ 已验证 产品关联 DOI PubMed 高影响因子
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NANOTECHNOLOGY · 2021 ·Vol. 32 ·期 37 ·375712 · IF 3.874

Preparation and characterization of sodium alginate/phosphate-stabilized amorphous calcium carbonate nanocarriers and their application in the release of curcumin

Bin Nie,Hong Wang,Chaohui Rao,Yanwei Zhang,Huifang Wang,Xiaojie Lian,Xianghua Gao,Baolong Niu,Wenfeng Li

Phosphate-stabilized amorphous calcium carbonate (ACCP) has excellent biocompatibility, bioactivity, and biodegradability, and can be easily synthesized and stored. However, unmodified ACCP, as a controlled drug release carrier, decomposes rapidly in an acidic environment and highly depends on the system's pH value, which can not meet the need for long-term release of active substances, thus limiting its application scope. To realize the specific pH responsiveness of ACCP nanoparticles, we designed and synthesized monodisperse sodium alginate/ACCP (Alginate/ACCP) composite nanoparticles in this paper. After ultrasonic treatment, nanoparticles with an average particle size less than 200 nm could form stable water dispersion that could be dispersed for up to 10 d. Based on the specific pH sensitivity of sodium alginate, the drug-controlled release performance of composite nanoparticles and the therapeutic effect of drug-loaded nanoparticles on A549 cancer cells were studied. The results indicated that under the same pH condition, the curcumin (Cur) release rate of composite nanoparticles gradually decreased with sodium alginate addition. When the dosage of sodium alginate was 1.0 mg ml−1, the cumulative drug release rate of nanoparticles in 40 h was only about 35%. Besides, the drug-loaded nanoparticles showed the excellent killing ability of cancer cells, and the survival rate of cancer cells decreased in a concentration-dependent manner. Therefore, through reasonable optimization design, we can synthesize composite nanoparticles with excellent sustained-release properties to provide a new strategy for cancer cells' long-term treatment.

CAS / MDL: 458-37-7
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2021 · IF 6.953

Development and characterization of electrospun nanofibers based on pullulan/chitin nanofibers containing curcumin and anthocyanins for active-intelligent food packaging

Mengxia Duan,Shan Yu,Jishuai Sun,Haixin Jiang,Jianbo Zhao,Cailing Tong,Yaqin Hu,Jie Pang,Chunhua Wu

An electrospun nanofiber based on pullulan/chitin nanofibers (PCN) containing curcumin (CR) and anthocyanins (ATH) was developed using an electrospinning technique for active-intelligent food packaging. The results of scanning electron microscopy and attenuated total reflection Fourier transform infrared spectroscopy indicated that CR and ATH were successfully immobilized on the film-forming substrate based on PCN. The physical and chemical properties of nanofibers with no colorant, a single colorant, and double colorants were compared. The nanofiber containing ATH and CR (PCN/CR/ATH) had stronger antioxidant and antimicrobial activities than those of nanofibers containing CR (PCN/CR) or ATH (PCN/ATH). With respect to pH sensitivity, the color of the PCN/CR nanofibers did not change obviously, but the color of the PCN/ATH and PCN/CR/ATH nanofibers changed significantly with the change in pH. Furthermore, the PCN/CR/ATH nanofibers clearly changed color with the progressive spoilage of Plectorhynchus cinctus at room temperature. Therefore, the electrospun PCN/CR/ATH nanofiber have great application potential in active–intelligent food packaging.

CAS / MDL: 458-37-7
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International Journal of Nanomedicine · 2021 · IF 6.4

Development and Evaluation of Curcumin Encapsulated Self-assembled Nanoparticles as Potential Remedial Treatment for PCOS in a Female Rat Model

Mazhar Ali Raja,Martin Maldonado,Jianying Chen,Ying Zhong,Jiang Gu

Purpose Polycystic ovary syndrome (PCOS) is one of the most common endocrinopathies affecting women of reproductive age and leads to metabolic disorders and infertility. The present study was conducted to investigate the therapeutic effects of curcumin (Cur) encapsulated arginine (Arg) and N-acetyl histidine (NAcHis) modified chitosan (Arg-CS-NAcHis/Cur) nanoparticles (NPs). Methods In this study, amphiphilic chitosan (CS) conjugate was developed by modification with hydrophilic arginine (Arg) and hydrophobic N-acetyl histidine (NAcHis) group (Arg-CS-NAcHis). The synthesized conjugate was well characterized by FTIR and NMR studies. Self-assembled nanoparticles based on the synthesized conjugate were developed by simple sonication method and characterized for the physicochemical properties of zeta potential, particle size and drug encapsulation. Next, in vitro drug release, cytotoxicity, and cellular uptake studies of the NPs were evaluated. Finally, the developed nanoparticles were examined for their therapeutic potential against estradiol valerate (EV) induced PCOS rats by evaluating hormone level changes and ovarian morphology. Results The results showed that zeta potential of the nanoparticles was 39.8±2.52 mV and the average size was 200 nm. The in vitro drug release profile showed sustained release pattern. Cytotoxicity and cellular uptake studies also showed preferential effectiveness than free curcumin. Both the biochemical and histopathological studies showed positive effects in reverting the symptoms of PCOS rats to normalcy. Conclusion Curcumin encapsulated arginine and N-acetyl histidine modified chitosan (Arg-CS-NAcHis/Cur) nanoparticles have been successfully developed. The present study suggested that treatment of the nanoparticles might reverse many of the PCOS symptoms. Therefore, these nanoparticles might be used as promising new candidate for delivery of curcumin to treat PCOS.

CAS / MDL: 458-37-7
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EUROPEAN JOURNAL OF PHARMACOLOGY · 2021 · IF 4.432

LncRNA H19 abrogates the protective effects of curcumin on rat carotid balloon injury via activating Wnt/β-catenin signaling pathway

Feiran Zhou,Xinyi Hu,Weijing Feng,Minghui Li,Bin Yu,Chenxing Fu,Caiwen Ou

Intimal hyperplasia-induced restenosis is a common response to vascular endothelial damage caused by mechanical force or other stimulation, and is closely linked to vascular remodeling . Curcumin , a traditional Chinese medicine , exhibits potent protective effects in cardiovascular diseases; for example, it attenuates vascular remodeling. Although the suppressive effects of curcumin on diseases caused by vascular narrowing have been investigated, the underlying mechanisms remain unknown. Long non-coding RNAs (lncRNAs) regulate various pathological processes and affect the action of drugs. In the present study, we found that the curcumin remarkably downregulated the expression of lncRNA H19 and thereby inhibited intimal hyperplasia-induced vascular restenosis. Furthermore, the inhibition of the expression of H19 by curcumin resulted in the inactivation of the Wnt/β-catenin signaling. Overall, we show that curcumin suppresses intimal hyperplasia via the H19/Wnt/β-catenin pathway, implying that H19 is a critical molecule in the suppression of intimal hyperplasia after balloon injury by curcumin. These insights should be useful for potential application of curcumin as a therapeutic intervention in vascular stenosis.

CAS / MDL: 7447-41-8
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Food & Function · 2021 ·Vol. 12 ·期 21 ·10512-10523 · IF 5.396

A self-assembled amphiphilic polysaccharide-based co-delivery system for egg white derived peptides and curcumin with oral bioavailability enhancement

Meng Yang,Jingbo Liu,Yajuan Li,Qi Yang,Xuanting Liu,Chunmei Liu,Sitong Ma,Boqun Liu,Ting Zhang,Hang Xiao,Zhiyang Du

Egg white derived peptides (EWDP) and curcumin are well known for diverse biological activities, but the combinational usage of the two natural nutraceuticals is extremely limited by their low oral bioavailability and distinctly different polarities. Therefore, this study aimed to exploit a facile self-assembled amphiphilic system for oral co-delivery of hydrophilic egg white derived peptides (EWDP) and hydrophobic curcumin. The hydrophobic curcumin was first loaded into the hydrophobic cavity of β-cyclodextrin (β-CD) as a core. Then, the hydrophilic EWDP was absorbed into the region between the core and the N-[(2-hydroxy-3-trimethyl ammonium) propyl] chitosan (HTCC) shell to form the amphiphilic nanoparticles (NPs) via layer-by-layer self-assembly. The resulting NPs showed ideal oral applicability with excellent colloidal properties and encapsulation capacity for EWDP and curcumin at pH 2.0–7.0. X-ray Photoelectron Spectroscopy (XPS), Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (1H NMR), X-ray diffraction (XRD) and differential scanning calorimetry (DSC) results indicated that hydrogen bonding and hydrophobic interaction were the main driving force for the formation of amphiphilic NPs. Upon combination with HTCC, EWDP (both shell material and core nutraceuticals) could facilitate curcumin loading into the deeper β-CD cavity site with admirable solubility improvement. Moreover, EWDP and curcumin after co-delivery exhibited superior bioavailability (especially for bioactivity and cellular absorption) than the simple mixture and conventional curcumin inclusion complex. Overall, these findings are enlightening for the rational peptide based oral co-delivery system formulations for a broader range of hydrophilic and hydrophobic nutraceuticals (initially synergistic or not) in the food and related health-promoting fields.

CAS / MDL: 50-81-7
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MICROCHIMICA ACTA · 2019 ·Vol. 186 ·期 10 ·1-12 · IF 5.479

One-step synthesis of N-doped carbon dots, and their applications in curcumin sensing, fluorescent inks, and super-resolution nanoscopy

Bu Lingli,Luo Tao,Peng Huanjun,Li Ling,Long Dengying,Peng Jingdong,Huang Jing

Nitrogen-doped carbon dots (N-CDs) with fluorescence excitation/emission maxima at 365/450 nm were prepared by a one-step hydrothermal approach. The dots possess remarkable photostability, fluorescence blinking and good biocompatibility, and this favors utilization in stochastic optical reconstruction microscopy (STORM). A spatial resolution down to ~60 nm was achieved when imaging HeLa cells using 647-nm laser excitation. This opens new possibilities for various super-resolution techniques based on stochastic optical switching. The remarkable optical properties of the N-CDs also enable them to be applied as invisible security ink for use in patterning, information storage and anti-counterfeiting. Further, it is found that the fluorescence of the N-CDs can be quenched by curcumin with high efficiency due to a combination of inner filter effect and static quenching. Based on this, a fluorometric assay with a detection limit of 21 ng mL −1 was developed for the determination of curcumin. Schematic representation of the applications of N-doped carbon dots (N-CDs). Curcumin quenches the fluorescence of N-CDs with high efficiency. The remarkable optical properties of the N-CDs enable them to be applied in fluorescent ink, cell imaging and stochastic optical reconstruction microscopy (STORM).

CAS / MDL: 458-37-7 107-15-3
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2019 · IF 4.213

Involvement of metabolism-permeability in enhancing the oral bioavailability of curcumin in excipient-free solid dispersions co-formed with piperine

Ruoning Wang,Jiawei Han,Ai Jiang,Rong Huang,Tingming Fu,Lingchong Wang,Qin Zheng,Wen Li,Junsong Li

Curcumin (CUR) has gained increasing interest worldwide due to multiple biological activities . However, the therapeutic application remains limited because of its low aqueous solubility, intestinal metabolism and poor membrane permeability. In present study, an excipient-free CUR solid dispersion co-formed with piperine (PIP), the absorption enhancer involving metabolism-permeability, was successfully prepared by melting and quench cooling (co-amorphous CUR-PIP). The co-amorphous CUR-PIP exhibited superior performance in non-sink dissolution compared with crystalline and amorphous CUR, and showed physically stable at least 3 months, attributing to the strong molecular interactions between CUR and PIP as evaluated by FTIR spectra. Furthermore, the combination of PIP with CUR in the co-amorphous formulation could inhibit the glucuronidation of CUR, as exhibited in the in vitro assay of rat intestinal microsomes. The co-amorphous CUR-PIP would also exhibit higher gastrointestinal membrane permeability of CUR, as confirmed by P app of CUR in Caco-2 model. After administration of co-amorphous CUR-PIP, the AUC of CUR significantly increased by 2.16- and 1.92-fold those in crystalline and amorphous CUR, respectively. This study demonstrates that the developed co-amorphous CUR-PIP can enhance the bioavailability of CUR by increasing its dissolution, inhibiting metabolic processes, and facilitating membrane permeability.

CAS / MDL: 27061-78-5
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