Journal of Biomedical Nanotechnology
·
2014
·Vol. 10
·期 2
·324-335
·
IF 7.578
Lv Li,Shen Yuanyuan,Li Min,Xu Xiaofen,Li Mingna,Guo Shengrong,Huang Shengtang
Novel poly(anhydride-ester)-b-poly(ethylene glycol) copolymers (PAE-b-PEGs) were synthesized by esterization of methyl poly(ethylene glycol) and poly(anhydride-ester), which were obtained by the melt polycondensation of α, ω- acetic anhydride-terminated poly(L-lactic
acid), and characterized by 1H-NMR and gel permeation chromatography. The two poly(anhydride-ester)-b-poly(ethylene glycols) (denoted as PAE-b-PEG2k and PAE-b-PEG5k) thus obtained can selfassemble in water to form micelles with hydrodynamic
diameters of 92.5 and 97.5 nm above their critical micelle concentrations of 3.78 and 2.36 μg/mL, respectively. The curcumin-loaded PAE-b-PEG2k and PAE-b-PEG5k micelles were prepared by the solid dispersion method, and they could encapsulate approximately
7% (w/w) curcumin. The diameters of the micelles were stable for 5 days. Curcumin is released faster from the micelles at pH 5.0 than at pH 7.4. Curcumin is released from the micelles at a fast rate during the initial 12 h, followed by a zero-order release during the subsequent 200 h, both
at pH 5.0 and 7.4. The IC50 values of the curcumin-loaded PAE-b-PEG2k and PAE-b-PEG5k micelles against HeLa cells are 12.41 and 15.31 μg/mL, respectively, which is lower than that of free curcumin (25.90 μg/mL). The PAE-bPEG2k
micelles are taken up faster than the PAE-b-PEG5k micelles by HeLa cells. Curcumin-loaded micelles can induce G2/M phase cell cycle arrest and apoptosis of HeLa cells.
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Nanoscale Research Letters
·
2015
·Vol. 10
·期 1
·1-10
·
IF 2.779
Wang Chuan,Ma Chao,Wu Zhenkai,Liang He,Yan Peng,Song Jia,Ma Nan,Zhao Qinghua
Nanofibers have attracted increasing attention in drug delivery and other biomedical applications due to their some special properties. The present study aims to prepare a fiber-based nanosolid dispersion system to enhance the bioavailability of curcumin (CUR). CUR-loaded polyvinyl pyrrolidone (CUR@PVP) nanofibers were successfully prepared via electrospinning. Scanning electron microscopy (SEM) was employed to observe the morphology of the nanofibers, and the SEM image showed that the drug-loaded nanofibers were smooth, and no CUR clusters were found on the surface of the nanofibers. The results of X-ray diffraction (XRD) demonstrated that the CUR was evenly distributed in the nanofibers in an amorphous state. Fourier transform infrared (FTIR) spectroscopy analysis indicated that intermolecular hydrogen bonding occurred between the CUR and the polymer matrix. In vitro dissolution profiles showed that CUR@PVP nanofiber could be quickly dissolved in phosphate-buffered saline (PBS) solution, while negligible dissolution was observed in pure CUR sample. Importantly, in vitro cell viability assays and in vivo animal tests revealed that the nanosolid dispersion system dramatically enhanced the bioavailability and showed effective anticancer effect of the CUR.
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MOLECULES
·
2023
·Vol. 28
·期 18
·6626
·
IF 4.6
Lin Shan,Xuewei Li,Xiuli Zheng,Jiasheng Wu,Haohui Ren,Weimin Liu,Pengfei Wang
As a class of highly dynamic organelles, lipid droplets (LDs) are involved in numerous physiological functions, and the changes in polarity of LDs are closely related to a variety of diseases. In this work, we developed two polarity-sensitive fluorescent probes (CC-CH and CC-Cl) based on curcumin analogs. CC-CH and CC-Cl with a donor–acceptor–donor (D–A–D) structure exhibited the property of intramolecular charge transfer (ICT); thus, their fluorescence emissions were significantly attenuated with increasing ambient polarity. Cell experiments indicated that CC-CH and CC-Cl showed excellent photostability, a low cytotoxicity, and a superior targeting ability regarding LDs. After treatment with oleic acid (OA) and methyl-β-cyclodextrin (M-β-CD), the polarity changes of LDs in living cells could be visualized by using CC-CH and CC-Cl. In addition, CC-CH and CC-Cl could monitor polarity changes of LDs in different pathological processes, including inflammatory responses, nutrient deprivation, and H2O2-induced oxidative stress. Therefore, CC-CH and CC-Cl are promising potential fluorescent probes for tracking intracellular LD polarity changes.Keywords:polarity-sensitive;lipid droplet targeted;fluorescent probes;cell imaging
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MOLECULES
·
2020
·Vol. 25
·期 21
·4958
·
IF 3.267
Eirini Chainoglou,Argyris Siskos,Eleni Pontiki,Dimitra Hadjipavlou-Litina
The synthesis of the new hybrids followed a hybridization with the aid of hydroxy-benzotriazole (HOBT) and 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDCI.HCL) in dry DMF or thionyl chloride between curcumin analogues and cinnamic acid derivatives. IR,1H-NMR,13C-NMR, LC/MS ESI+, and elemental analysis were used for the confirmation of the structures of the novel hybrids. The lipophilicity values of compounds were calculated theoretically and experimentally via the reversed chromatography method as RMvalues. The novel derivatives were studied through in vitro experiments for their activity as antioxidant agents and as inhibitors of lipoxygenase, cyclooxygenase-2, and acetyl-cholinesterase. All the compounds showed satisfying anti-lipid peroxidation activity of linoleic acid induced by 2,2′-azobis(2-amidinopropane) hydrochloride (AAPH). Hybrid3ewas the most significant pleiotropic derivative, followed by3a. According to the predicted results, all hybrids could be easily transported, diffused, and absorbed through the blood–brain barrier (BBB). They presented good oral bioavailability and very high absorption with the exception of3h. No inhibition for CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 was noticed. According to the Ames test, all the hybrids induced mutagenicity with the exception of3d. Efforts were conducted a) to correlate the in vitro results with the most important physicochemical properties of the structural components of the molecules and b) to clarify the correlation of actions among them to propose a possible mechanism of action. Docking studies were performed on soybean lipoxygenase (LOX) and showed hydrophobic interactions with amino acids. Docking studies on acetylcholinesterase (AChE) exhibited: (a) hydrophobic interactions with TRP281, LEU282, TYR332, PHE333, and TYR336 and (b) π-stacking interactions with TYR336.Keywords:curcumin analogues;cinnamic acids;Hybrids;Alzheimer’s disease;therapy
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FOOD HYDROCOLLOIDS
·
2022
·
IF 11.504
Laiming Zhang,Jiaqi Zheng,Yi Wang,Xingqian Ye,Shiguo Chen,Haibo Pan,Jianle Chen
Rhamnogalacturonan-I (RG-I) was considered to be incompatible with gel formation. Due to its important health benefits, our previous study reported synergistic gelation of RG-I enriched pectin from citrus membranes with sequential acidic and alkaline treatment. In the present study, we further fabricated RG-I enriched pectin-based emulsion gels with the synergistic gelation for hydrophobic bioactive encapsulation. The effect of oil fraction and interfacial compositions including pectin itself and Tween 20 on the physical properties and delivery characteristics of emulsion gels was investigated. As to interfacial compositions, pectin reduced syneresis and swelling ratio and increased water holding capacity . Oil fraction had no marked influence on syneresis and swelling ratio, but significantly increased water holding capacity. Particularly, all the emulsion gels showed an elastic behavior and a full structure recovery after shearing. Increase in pectin instead of Tween 20 onto the surface of oil droplets and oil fraction markedly improved their gel strength. Curcumin was encapsulated within the oil phase of emulsion gels. Improvement in gel strength provided enhanced protection of curcumin against heat-induced degradation. In vitro digestion revealed that interfacial compositions decelerated curcumin release by increasing the proportion of pectin onto the surface, but didn't change its bioaccessibility eventually. Increase in oil fraction accelerated curcumin release, but reduced its bioaccessibility. Overall, fabrication of RG-I enriched pectin-based emulsion gel with pectin itself as interfacial composition and low oil fraction would contribute to improving curcumin bioavailability for its sustained release, which should be further validated in vivo .
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JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
·
2016
·Vol. 16
·期 6
·6258-6264
·
IF 1.338
Lian Ting,Peng Mingli,Vermorken Alphons J. M,Jin Yanyan,Luo Zhiyi,Van de Ven Wim J. M,Wan Yinsheng,Hou Peng,Cui Yali
Curcumin, a polyphenol extracted from turmeric (Curcuma longa), has emerged as a potent multimodal cancer-preventing agent. It may attenuate the spread of cancer and render chemotherapy more effective. However, curcumin is neither well absorbed nor well retained in the blood,
resulting in low efficacy. In an attempt to enhance the potency and to improve the bioavailability of curcumin, new delivery agents, hydroxypropyl-beta-cyclodextrin (HP-β-CD)-modified GoldMag nanoparticles (CD-GMNs) were designed and synthesized to incorporate curcumin. The CD-GMNs
were characterized by Fourier Transform Infrared Spectroscopy (FT-IR), Thermo-gravimetric Analysis (TGA), X-ray Diffraction (XRD), Dynamic Light Scattering measurements (DLS), Transmission Electron Microscopy (TEM) and Vibrating Sample Magnetometer (VSM) analyses. For the magnetic carrier
of CD-GMNs, the content of HP-β-CD was 26.9 wt%. CD-GMNs have a saturation magnetization of 22.7 emu/g with an average hydrodynamic diameter of 80 nm. The curcumin loading, encapsulation efficiency and releasing properties in vitro were also investigated. The results showed
that the drug encapsulation ratio was 88% and the maximum curcumin loading capacity of CD-GMNs was 660 μg/5 mg. in vitro drug release studies showed a controlled and pH-sensitive curcumin release over a period of one week. Collectively, our data suggest that HP-β-CD-modified
GoldMag nanoparticles can be considered to form a promising delivery system for curcumin to tumor sites. Targeting can be achieved by the combined effects of the application of an external magnetic field and the effect on drug release of lower pH values often found in the tumor microenvironment.
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TROPICAL JOURNAL OF PHARMACEUTICAL RESEARCH
·
2021
·Vol. 18
·期 12
·2531-2538
·
IF 0.533
Jun Tang,Jingfang Yang
Purpose: To investigate the potential role of curcumin in osteosarcoma (OS) cell migration and invasion, and also to explore the underlying mechanism of action.
Methods: OS cell lines, Saos-2 and U2OS, were treated with various concentrations of curcumin (0, 10, 20, 50 μM) for 48 h. Transwell assay was used to determine the migratory and invasive activities of human OS cells while miR-33b-5p expression levels were measured using quantitative real time polymerase chain reaction (qRT-PCR). Expressions of metastasis-related genes, such as matrix metalloproteinases (MMPs), were quantified by qRT-PCR or western blot. The interaction between miR33b-5p and Sirtuin 6 (SIRT6) was evaluated by luciferase assay.
Results: Curcumin inhibited the migratory and invasive activities of huamn OS cells, and downregulated MMP2 and MMP9 (p < 0.05). Moreover, in curcumin-treated OS cells, miR-33b-5p expression was upregulated while SIRT6 expression was significantly downregulated (p < 0.05). Overexpression of miR-33b-5p downregulated SIRT6 mRNA and protein expression, whereas transfection with miR-33b-5p inhibitor upregulated SIRT6 expression in OS cells (p < 0.05). Furthermore, curcumin suppressed SIRT6 expression by upregulating miR-33b-5p expression in OS cells. Finally, overexpression of SIRT6 or miR-33b-5p inhibitor reversed the suppression of OS cell metastasis induced by curcumin (p < 0.05).
Conclusion: Curcumin inhibits SIRT6 expression via upregulating miR-33b-5p expression, which leads to the inhibition of OS cell migration and invasion. Thus, curcumin is a potential therapeutic agent for the management of OS.
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Journal of Materials Chemistry B
·
2016
·Vol. 4
·期 13
·2253-2263
·
IF 4.872
Mingxian Liu,Yanzhou Chang,Jing Yang,Yuanyuan You,Rui He,Tianfeng Chen,Changren Zhou
Halloysite nanotubes (HNTs) have a unique tubular structure in nanoscale, and have shown potential as novel carriers for various drugs. Coating the nanotubes with a hydrophilic polymer shell can significantly decrease the toxicity and provide colloidal stability during blood circulation. Here, we synthesized chitosan grafted HNTs (HNTs-g-CS) and investigated their potential as a nano-formulation for the anticancer drug curcumin. The structure and properties of HNTs-g-CS were characterized using water contact angle, zeta-potential, Fourier transform infrared (FTIR) spectroscopy, thermogravimetric analysis (TGA), and transmission electron microscopy (TEM) techniques. HNTs-g-CS exhibit a maximum 90.8% entrapment efficiency and 3.4% loading capacity of curcumin, which are higher than those of raw HNTs. HNTs-g-CS also show no obvious hemolytic phenomenon and good stability in serum. The cumulative release ratio of curcumin from HNTs-g-CS/curcumin at cell lysate after 48 hours is 84.2%. The curcumin loaded HNTs-g-CS show specific toxicity to various cancer cell lines, including HepG2, MCF-7, SV-HUC-1, EJ, Caski and HeLa, and demonstrate an inhibition concentration of IC50 at 5.3–192 μM as assessed by cytotoxicity studies. The anticancer activity of this nanoformulation is extremely high in EJ cells compared with the other cancer cell lines. The cell uptake of HNTs-g-CS is confirmed by fluorescence microscopy. Flow cytometric analysis of curcumin loaded HNTs-g-CS shows that curcumin loaded HNTs-g-CS increase apoptosis on EJ cells. The content of ROS created by HNTs-g-CS/curcumin is more than that of free curcumin. All these results suggest that HNTs-g-CS are potential nanovehicles for anticancer drug delivery in cancer therapy.
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COLLOID AND POLYMER SCIENCE
·
2021
·Vol. 299
·期 10
·1557-1566
·
IF 1.931
Hua Chenghuan,Yu Wenjie,Yang Mingyue,Cai Qun,Gao Tian,Zhang Silong,Xu Huan,He Huan,Peng Na,Liu Yi
New nanocomplexes containing curcumin-loaded casein micelles and surface-coated pectin via electrostatic interaction were fabricated. Curcumin-loaded nanocomplexes prepared at pH 4 showed the most excellent performance than that at pH 3 and pH 2, which had an average size of 266.4 nm (polydispersity index = 0.193) and loading capacity of 93%. The morphology of nanocomplexes exhibited as monodisperse spherical nanoparticles observed by SEM and TEM. The experiment of anti-oxidant activity demonstrated that nanocomplexes tremendously kept the bioactivity of curcumin. Moreover, in vitro release behaviors of curcumin from casein-pectin nanocomplexes indicated that the surface coating layer of pectin obviously delayed the release of curcumin in simulated gastric fluid, and the controlled release ability in simulated intestinal fluid was greatly enhanced. The casein-pectin nanocomplexes exhibited as a promising oral delivery vehicle of bioactive ingredients in food and pharmacy. Graphical abstract
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2020
·
IF 5.162
Nan Liu,Yao Lu,Yanhui Zhang,Yanxiang Gao,Like Mao
The current study developed ethylcellulose (EC) based oleogels with the addition of a surface active ingredient (sorbitan monopalmitate, SP), in order to increase the active loading of curcumin by reducing lipid oxidation , improving curcumin solubility and chemical stability. With the increase in SP content, EC oleogels had more compact gel networks with evenly distributed smaller pores. Rheological analysis revealed that the gels had shear-thinning behavior, and higher concentration of SP contributed to the systems with higher viscosity. The inclusion of SP also worked to reinforce gel strength as determined by frequency sweep, creep recovery and textural analyses. EC oleogels with higher content of SP were capable to hold more liquid oil during centrifugation , and the T 2 relaxation time was much lower as determined by NMR. Peroxide value of the oleogels was significantly lower in the systems with SP, and a SP content of 4% or 6% was effective in inhibiting lipid oxidation during storage. When curcumin was incorporated within the gel networks, its effective concentration was more retained with the addition of SP, as no curcumin crystals were detected by DSC during a 9-day storage test, and curcumin had much higher retention when exposed to UV light for 8 h.
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FOOD CHEMISTRY
·
2020
·
IF 6.306
Guohuan Huang,Yuping Yan,Danxia Xu,Jia Wu,Chuanhui Xu,Lihua Fu,Baofeng Lin
Food spoilage is one of the biggest concerns for food safety worldwide. Here, we describe the construction of a carrier for biological agents by chemical combination of porous nanoMOFs and carboxymethylated filter paper (CMFP). When curcumin was encapsulated in nanoMOFs@CMFP, they showed the ability to act as super-long-acting food preserving agents with controllable release of curcumin. Although only 22.3% of curcumin was released into water in 600 h, 65.8% was released into PBS in the same time, and the release into PBS could be tuned by adding citric acid at the time of greatest requirement. Furthermore, the chemical stability of curcumin in nanoMOFs@CMFP was >4.9 times greater than for free curcumin. The outstanding antioxidant and antimicrobial activity of curcumin-loaded nanoMOFs@CMFP paste was demonstrated by prolonging the shelf life of pitayas, which illustrates its potential for development as long-acting and stable preserving paste for use in food preservation.
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PHYTOMEDICINE
·
2020
·
IF 4.268
Chunjing Guo,Xiaoya Hou,Yanhui Liu,Yanchun Zhang,Haiyu Xu,Feng Zhao,Daquan Chen
Background Using natural polysaccharides from Traditional Chinese Medicine as nanodrug delivery systems have considerable potential for tumor diagnostics and therapeutics. Purpose On the basis of targeted therapy and combining the advantages of natural polysaccharides (angelica polysaccharide, APS) and natural Chinese medicine (curcumin, Cur) to design functionalized nanoparticles to improve the therapeutic through cell membrane encapsulation and immunotherapy . Study Design and Methods Cur-loaded, glycyrrhetic acid (GA)-APS-disulfide bond (DTA)-Cur nanomicelle (GACS-Cur), which were prepared by the dialysis method. GACS-Cur was encapsulated with the membranes from red blood cells (RBCm) termed GACS-Cur@RBCm, which were prepared by the principle of extrusion using a miniature extruder. The developed formulations were subjected to various in vitro and in vivo evaluation tests. Results The resulting APS nanocarriers supported a favorable drug-loading capacity, biocompatibility , and enhanced synergistic anti-hepatoma effects both in vitro and in vivo . After administration in mice, in vivo imaging results showed that the GACS-Cur and RBCm-coated groups had an obvious stronger tumor tissue targeting ability than the control treatment groups. Additionally, the immunomodulatory effect increased IL-12, TNF-α and IFN-γ expression and CD8+ T cell infiltration (1.9-fold) than that of the saline group. Notably, in comparison with hyaluronic acid (HA) nanocarriers , APS nanocarriers possess higher anti-hepatoma efficiency and targeting capabilities and, thus, should be further studied for a wide range of anti-cancer applications. Conclusion Our data demonstrated that APS nanocarriers encapsulated with erythrocyte membrane mighty be a promising clinical method in the development of efficacy, safety and targeting of liver cancer therapy.
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