JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2020
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IF 4.192
Shuangshuang Huang,Junbo He,Lei Cao,Hong Lin,Weinong Zhang,Qixin Zhong
To improve the water solubility, antioxidant activity, and chemical stability of curcumin, solid lipid nanoparticles (SLNs) were fabricated using equal masses of propylene glycol monopalmitate and glyceryl monostearate as the lipid matrix and sodium caseinate-lactose (NaCas-Lac) Maillard conjugate as the emulsifier. The entrapment efficiency was more than 90% when curcumin was 2.5% and 5.0% of lipid mass, and the SLNs were stable during 30-day storage. SLNs stabilized by NaCas-Lac showed better physicochemical properties than those prepared with NaCas, including higher sphericity and homogeneity; higher entrapment efficiency; better stability against pH, ionic strength, and simulated gastrointestinal digestions; and more controlled release. SLNs also greatly enhanced the antioxidant activity of encapsulated curcumin and the retention of curcumin during storage. Therefore, the present SLNs may find applications to deliver lipophilic compounds in functional foods and beverages.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2021
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IF 6.953
Aiping Zhang,Yucheng Zou,Yuhang Xi,Peng Wang,Yue Zhang,Liangru Wu,Hui Zhang
The feasibility of using unmodified bamboo shoot cellulose (BSC) to produce composite aerogels with sodium alginate (SA) in a fast and green way for sustained release of curcumin was explored for the first time, in which calcium ion-induced SA cross-linking could effectively retain the structural stability of aerogel skeleton. The aerogels were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry . The encapsulation and release of curcumin from aerogels were studied while the antioxidant activity of encapsulated curcumin was investigated. Curcumin was evenly encapsulated in the composite aerogels and showed a sustained release behavior, followed the first-order rate expression. Interpenetrating network structures were built between BSC and SA mainly through hydrogen bonding, which could be further reinforced by the cross-linking of CaCO 3 on the SA matrix. The original characteristics of BSC in the composite aerogels were well retained. The thermal stability and mechanical properties of the composite aerogels were improved by Ca 2+ -induced cross-linking, while the uncross-linked composite aerogels exhibited better encapsulation efficiency and in vitro antioxidant activity. Overall, this study was the first to use cellulose from bamboo shoot to develop aerogels for drug delivery purposes. The cellulose/alginate composite aerogels were promising to be used as biocompatible carriers for drug and nutraceutical delivery.
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RSC Advances
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2019
·Vol. 9
·期 70
·40873-40882
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IF 3.049
Lu Diao,Ao Shen,Yunxu Yang,Jin Tao,Ying Hu
Chemotherapeutic drug resistance poses a great challenge in cancer therapy. Drug efflux and anti-apoptotic processes are the two most common mechanisms leading to chemotherapy resistance. In this study, we focused on the applicability of curcumin (CUR) as a sensitizer for chemotherapeutics (doxorubicin [DOX] as the model drug) modified with hyaluronic acid (HA) as an effective therapeutic strategy against multidrug resistance (MDR) in cancer cells. We constructed an HA–CUR/DOX delivery system measuring approximately 180 nm with superior encapsulation efficacy and serum stabilities. In vitro, we found that HA modification could facilitate the efficient delivery of chemotherapeutics through CD44 receptor-mediated targeted delivery. MTT assay results confirmed that the combination of CUR and DOX/paclitaxel (PTX) had a significant synergistic effect and significantly reversed MDR. Further experiments including real-time polymerase chain reaction and western blotting proved that the main mechanisms by which CUR reversed MDR in tumor cells were inhibiting the expression and activity of P-glycoprotein (P-gp) and inducing apoptosis through mitochondrial pathway. Taken together, our new engineered tumor-targeting nanoparticle delivery system may have the potential for overcoming MDR in cancer.
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International Journal of Nanomedicine
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2019
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IF 4.471
Hong Jiang,Zhi-Peng Li,Gui-Xiang Tian,Rui-Yan Pan,Chong-Mei Xu,Bo Zhang,Jing-liang Wu
Background Recent efforts have been focused on combining two or more therapeutic approaches with different mechanisms to enhance antitumor therapy. Moreover, nanosize drug-delivery systems for codelivering two drugs with proapoptotic and antiangiogenic activities have exhibited great potential in efficient treatment of cancers. Methods Glycyrrhetinic acid (GA)–modified liposomes (GA LPs) for liver-targeted codelivery of curcumin (Cur) and combretastatin A4 phosphate (CA4P) were prepared and characterized. In vitro cellular uptake, cytotoxicity, cell migration, in vivo biodistribution, antitumor activity, and histopathological studies were performed. Results Compared with unmodified LPs (Cur-CA4P LPs), Cur-CA4P/GA LPs were taken up effectively by human hepatocellular carcinoma cells (BEL-7402) and showed higher cytotoxicity than free drugs. In vivo real-time near-infrared fluorescence–imaging results indicated that GA-targeted LPs increased accumulation in the tumor region. Moreover, Cur-CA4P/GA LPs showed stronger inhibition of tumor proliferation than Cur, Cur + CA4P, and Cur-CA4P LPs in vivo antitumor studies, which was also verified by H&E staining. Conclusion GA-modified LPs can serve as a promising nanocarrier for liver-targeted co-delivery of antitumor drugs against hepatocellular carcinoma.
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CHEMICAL ENGINEERING JOURNAL
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2019
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IF 8.355
Yang Xiang,Xiaohui Duan,Longbao Feng,Shuqi Jiang,Li Deng,Jun Shen,Yijun Yang,Rui Guo
The successful treatment of gliomas relies on two important factors, namely therapeutic genes/drugs and efficient delivery vehicles to cross the blood-brain barrier. In this work, a new gene vector was constructed based on polycaprolactone (PCL), glutathione (reduced; GSH)-sensitive polyethylenimine (PEI-SS) and polyethylene glycol (PEG), and modified with a cell-penetrating peptide (tLyp-1); this yielded tLyp-1-conjugated GSH-sensitive biodegradable micelles (PPPt) that mediated enhanced tumour necrosis factor (TNF)-related apoptosis-inducing ligand (pUNO1-hTRAILa) and curcumin (CUR) co-delivery to gliomas. The sensitisation function of CUR was used to explore whether CUR and genes have a synergistic antitumour effect. The results showed that the drug loading efficiency of PPPt was about 8.6%. The PPPt possessed good cytocompatibility and blood compatibility when the concentration was less than 0.06 mg/mL. PPPt strongly condensed pUNO1-hTRAILa to form a nanocomplex and efficiently transfected C6 cells. The drug-release behaviour of PPPt/CUR/pUNO1-hTRAILa was reduction-sensitive and the cellular uptake results indicate that modification of tLyp-1 promoted the internalisation of micelles. The PPPt/CUR/pUNO1-hTRAILa complexes exhibited much better in vitro and in vivo antitumour effects than micelles loaded with CUR or pUNO1-hTRAILa alone. We also used magnetic resonance imaging for in vivo monitoring of the transcranial drug delivery and therapeutic effect of the tumour on rats bearing in situ glioma.
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MOLECULAR PHARMACEUTICS
·
2018
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IF 4.556
Feiyang Jin,Di Liu,Hui Yu,Jing Qi,Yuchan You,Xiaoling Xu,Xuqi Kang,Xiaojuan Wang,Kongjun Lu,Xiaoying Ying,Jian You,Yongzhong Du,Jiansong Ji
Acute lung injury (ALI) is a serious illness without resultful therapeutic methods commonly. Recent studies indicate the importance of oxidative stress in the occurrence and development of ALI, and mitochondria targeted antioxidant has become a difficult and hot topic in the research of ALI. Therefore, a sialic acid (SA)-modified lung-targeted microsphere (MS) for ALI therapy are developed, with triphenylphosphonium cation (TPP)-modified curcumin (Cur-TPP) loaded, which could specifically target the mitochondria, increasing the effect of antioxidant. The results manifest that with the increase of microsphere, lung distribution of microsphere is also increased in murine mice, and after SA modification, the microsphere exhibits the ideal lung-targeted characteristic in ALI model mice, due to SA efficiently targeting to E-selectin expressed on inflammatory tissues. Further investigations indicate that SA/Cur-TPP/MS has better antioxidative capacity, decreases intracellular ROS generation, and increases mitochondrial membrane potential, contributing to a lower apoptosis rate in human umbilical vein endothelial cells (HUVECs) compared to H2O2 group. In vivo efficacy of SA/Cur-TPP/MS demonstrates that the inflammation has been alleviated markedly and the oxidative stress is ameliorated efficiently. Significant histological improvements by SA/Cur-TPP/MS are further proved via HE stains. In conclusion, SA/Cur-TPP/MS might act as a promising drug formulation for ALI therapy.
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International Journal of Nanomedicine
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2018
·
IF 4.37
Fei Tong,Rongkui Chai,Haiying Jiang,Bo Dong
Background The objective of this study was to survey the therapeutic function of curcumin-encapsulated poly(gamma-benzyl l-glutamate)-poly(ethylene glycol)-poly(gammabenzyl l-glutamate) (PBLG-PEG-PBLG) (P) on diabetic cardiomyopathy (DCM) via cross regulation effect of calcium-sensing receptor (CaSR) and endogenous cystathionine-γ-lyase (CSE)/hydrogen sulfide (H 2 S). Methods Diabetic rats were preconditioned with 20 mg/kg curcumin or curcumin/P complex continuously for 8 weeks. The blood and myocardiums were collected, the level of serum H 2 S was observed, and the [Ca 2+ ] i content was measured in myocardial cells, and hematoxylin-eosin, CaSR, CSE, and calmodulin (CaM) expression were detected. Results Both curcumin and curcumin/P pretreatment alleviated pathological morphological damage of myocardium, increased H 2 S and [Ca 2+ ] i levels, and upregulated the expression of CaSR, CSE, and CaM as compared to DCM group, while curcumin/P remarkably augmented this effect. Conclusion PBLG-PEG-PBLG could improve water-solubility and bioactivity of curcumin and curcumin/PBLG-PEG-PBLG significantly alleviated diabetic cardiomyopathy.
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PLoS One
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2013
·Vol. 8
·期 8
·e70565
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IF 3.73
Luyan Guo,Yanyan Xing,Rui Pan,Mingliang Jiang,Zheng Gong,Liqing Lin,Junbing Wang,Guoyin Xiong,Jun Dong
Curcumin is a molecule found in turmeric root that has anti-inflammatory, antioxidant, and anti-tumor properties and has been widely used as both an herbal drug and a food additive to treat or prevent neurodegenerative diseases. To explore whether curcumin is able to ameliorate HIV-1-associated neurotoxicity, we treated a murine microglial cell line (N9) and primary rat cortical neurons with curcumin in the presence or absence of neurotoxic HIV-1 gp120 (V3 loop) protein. We found that HIV-1 gp120 profoundly induced N9 cells to produce reactive oxygen species (ROS), tumor necrosis factor-α (TNF-α) and monocyte chemoattractant protein-1 (MCP-1). HIV-1 gp120 also induced apoptosis of primary rat cortical neurons. Curcumin exerted a powerful inhibitory effect against HIV-1 gp120-induced neuronal damage, reducing the production of ROS, TNF-α and MCP-1 by N9 cells and inhibiting apoptosis of primary rat cortical neurons. Curcumin may exert its biological activities through inhibition of the delayed rectification and transient outward potassium (K + ) current, as curcumin effectively reduced HIV-1 gp120-mediated elevation of the delayed rectification and transient outward K + channel current in neurons. We conclude that HIV-1 gp120 increases ROS, TNF-α and MCP-1 production in microglia, and induces cortical neuron apoptosis by affecting the delayed rectification and transient outward K + channel current. Curcumin reduces production of ROS and inflammatory mediators in HIV-1-gp120-stimulated microglia, and protects cortical neurons against HIV-1-mediated apoptosis, most likely through inhibition of HIV-1 gp120-induced elevation of the delayed rectification and transient outward K + current.
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International Journal of Nanomedicine
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2015
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IF 4.383
Jingjing Li,Tong Chen,Feng Deng,Jingyuan Wan,Yalan Tang,Pei Yuan,Liangke Zhang
We have designed and developed curcumin (Ccn)-loaded albumin nanoparticles (BNPs) surface-functionalized with glycyrrhetinic acid (Ccn-BNP-GA) for GA receptor-mediated targeting. Ccn-BNP-GA was prepared by conjugating GA as a hepatoma cell-specific binding molecule onto the surface of BNPs. Ccn-BNP-GA showed a narrow distribution with an average size of 258.8±6.4 nm, a regularly spherical shape, an entrapment efficiency of 88.55%±5.54%, and drug loading of 25.30%±1.58%. The density of GA as the ligand conjugated to BNPs was 140.48±2.784 μg/g bovine serum albumin. Cytotoxicity assay results indicated that Ccn-BNP-GA was significantly more cytotoxic to HepG2 cells and in a concentration-dependent manner. Ccn-BNP-GA also appeared to be taken up to a greater extent by HepG2 cells than undecorated groups, which might be due to the high affinity of GA for GA receptors on the HepG2 cell surface. These cytotoxicity assay results were corroborated by analysis of cell apoptosis and the cell cycle. Further, Ccn-BNP-GA showed an approximately twofold higher rate of cell apoptosis than the other groups. Moreover, proliferation of HepG2 cells was arrested in G 2 /M phase based on cell cycle analysis. These results, which were supported by the GA receptor-mediated endocytosis mechanism, indicate that BNPs surface-functionalized with GA could be used in targeted cancer treatment with high efficacy, sufficient targeting, and reduced toxicity.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2016
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IF 3.994
Fanfei Meng,Sajid Asghar,Yurui Xu,Jianping Wang,Xin Jin,Zhilin Wang,Jing Wang,Qineng Ping,Jianping Zhou,Yanyu Xiao
Many nanoparticle matrixes have been demonstrated to be efficient in brain targeting, but there are still certain limitations for them. To overcome the shortcomings of the existing nanoparticulate systems for brain-targeted delivery, a lipoprotein resembling protein-free nanostructured lipid carrier (PS80-NLC) loaded with curcumin was constructed and assessed for in vitro and in vivo performance. Firstly, single factor at a time approach was employed to investigate the effects of various formulation factors. Mean particle sizes of ≤100 nm, high entrapment efficiency (EE, about 95%) and drug loading (DL, >3%) were obtained for the optimized formulations. In vitro release studies in the presence of plasma indicated stability of the formulation under physiological condition. Compared with NLC, PS80-NLC showed noticeably higher affinity for bEnd.3 cells (1.56 folds greater than NLC) but with lower uptake in macrophages. The brain coronal sections showed strong and widely distributed fluorescence intensity of PS80-NLC than that of NLC in the cortex. Ex vivo imaging studies further confirmed that PS80-NLC could effectively permeate BBB and preferentially accumulate in the brain (2.38 times greater than NLC). The considerable in vitro and in vivo performance of the safe and biocompatible PS80–NLC makes it a suitable option for further investigations in brain targeted drug delivery .
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CHINESE JOURNAL OF CHEMISTRY
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2016
·Vol. 34
·期 6
·599-608
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IF 1.872
Yehong Zhou,Congli Wang,Fei Wang,Chenzhong Li,Chuan Dong,Shaomin Shuang
β -Cyclodextrin ( β -CD) and its derivatives functionalized magnetic nanoparticles (MNPs) with high saturated magnetism were fabricated successfully by an effective grafting method. The resultant carboxymethyl/hydroxypropyl/sulfobutyl ether- β -CD-MNPs (CM/HP/SBE- β -CD-MNPs) nanocomposites were characterized by the TEM, FTIR, DLS, Zeta potential, XRD and VSM. In addition, the loading and release performance of the as-prepared nanocarriers for the hydrophobic anti-cancer drug curcumin was also investigated. The results revealed that the SBE- β -CD-MNPs possessed the highest loading and release capacity in comparison with other two nanosystems. Cellular uptake and imaging suggested that the SBE- β -CD-MNPs entered into the cell, and curcumin could be successfully delivered into the cell by SBE- β -CD-MNPs nanocarrier. Moreover, cell toxicity experiments demonstrated the SBE- β -CD-MNPs were non-toxic, while curcumin loaded SBE- β -CD-MNPs showed high potential to kill the HepG2 cells. The as-prepared magnetic composites were expected to expand their potential applications in biomedical field.
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MEDIATORS OF INFLAMMATION
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2017
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IF 3.232
Tao Cheng,Yaochao Zhao,Bin Li,Mengqi Cheng,Jiaxing Wang,Xianlong Zhang
Wear particle-induced chronic inflammation and osteoclastogenesis are two critical factors in the osteolytic process. Curcumin (CUR) is an active compound of the medicinal herb Curcuma longa and has anti-inflammatory and antiosteoclastogenic properties. Our study tested the hypothesis that CUR might attenuate polymethylmethacrylate- (PMMA-) induced inflammatory osteolysis using mouse calvaria osteolysis model in vivo and in vitro. The mice were divided into four groups: phosphate-buffered saline group, CUR, PMMA, and PMMA + CUR groups. Three days before PMMA particle implantation, the mice were intraperitoneally injected with CUR (25 mg/kg/day). Ten days after the operation, the mouse calvaria was harvested for microcomputed tomography, histomorphometry, and molecular biology analysis. As expected, CUR markedly reduced the secretion of tumor necrosis factor-α, interleukin- (IL-) 1β, and IL-6 in the calvarial organ culture. Moreover, CUR suppressed osteoclastogenesis and decreased bone resorption in vivo compared with PMMA-stimulated calvaria. Furthermore, CUR downregulated the osteoclast-specific gene expression and reversed the receptor activator of nuclear factor kappa-B ligand (RANKL)/osteoprotegerin messenger RNA and protein ratio in PMMA particle-stimulated mice. These results suggest that CUR attenuated PMMA particle-induced inflammatory osteolysis by suppressing the RANKL signaling pathway in the murine calvarium, which could be a candidate compound to prevent and treat AL.
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