CARBOHYDRATE POLYMERS
·
2012
·
IF 3.628
Jinsong Liu,Lihua Xu,Chuantong Liu,Dafeng Zhang,Siqian Wang,Zhennan Deng,Weiwei Lou,Haihong Xu,Qing Bai,Jianfeng Ma
In the present paper, cationic nanoparticles of curcumin, chitosan and poly(ɛ-caprolactone) were developed by a simple nano-precipitation method. The developed curcumin loaded chitosan/poly(ɛ-caprolactone) (chitosan/PCL) nanoparticle showed almost spherical shape and its diameter was varied between 220 nm and 360 nm and zeta potential was varied between +30 mV and 0 mV as a function with pH value. The encapsulation of curcumin into nanoparticles was confirmed by fluorescence spectral analysis. In vitro release study showed the sustained release behavior of curcumin from nanoparticles during the period of 5 days study. In vitro cytotoxicity test revealed the drug concentration dependent on the cell viability against Hela cells and OCM-1 cells after 48 h co-incubation. Furthermore, in vitro cell uptake study revealed that the cell uptake of curcumin was greatly enhanced by encapsulated curcumin into cationic chitosan/PCL nanoparticles. Therefore, the developed cationic chitosan/PCL nanoparticles might be a promising candidate for curcumin delivery to cancer cells.
研究领域:
药剂学
·
生物医学工程
·
肿瘤学
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产品关联
DOI
PubMed
高影响因子
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
·
2018
·Vol. 34
·期 2
·203-211
·
IF 1.248
Song Shengmei,Li Minglu,Gong Xiaojuan,Han Hui,Zhou Yehong,Wang Li,Shuang Shaomin,Dong Chuan
In the paper, folic acid(FA)-mediated and β -cyclodextrin( β -CD) derivatives functionalized magnetic Fe 3 O 4 nanoparticles(MNPs) were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticancer drug. FA-sulfobutyl ether- β -CD-MNPs(FA-SBE- β -CD-MNPs), FA-hydroxypropyl- β -CD-MNPs(FA-HP- β -CD-MNPs) and FA-carboxymethyl- β -CD-MNPs(FA-CM- β -CD-MNPs) were fabricated, and the loading efficiency and relative entrapment rate of curcumin are 12.04 mg/g, 95.56% for FA-SBE- β -CD-MNPs, 9.6 mg/g, 81.63% for FA-HP- β -CD-MNPs and 7.88 mg/g, 85.28% for FA-CM- β -CD-MNPs, respectively. Meanwhile, at pH=5.0, the optimal release rate of curcumin is about 46.07% for FA-SBE- β -CD-MNPs in 5 h. Cellular uptake indicates that curcumin can be selectively transported to targeting site and released from the internalized carriers. The in vitro cytotoxicity reveals that non-toxic FA-SBE- β -CD-MNPs have excellent biocompatibility on HepG2 cells in the tested concentrations. Therefore, FA-SBE- β -CD-MNPs could provide a promising platform for the targeting delivery of water insoluble anti-cancer drugs for different treatment needs of cancer therapy.
研究领域:
药剂学
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生物医学工程
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
·
2020
·
IF 2.365
Xinrui Li,Jing Su,Zul Kamal,Pengcheng Guo,Xinyi Wu,Lina Lu,Hongbing Wu,Mingfeng Qiu
Curcumin (Cur) is a promising drug for neurological diseases. Nevertheless, the application of Cur has been limited due to its difficulty in penetrating blood-brain barrier (BBB). Intranasal drug delivery, a noninvasive alternative delivery of Cur, can effectively help Cur cross BBB and inert into central nervous system directly. Odorranalectin (OL) which is the smallest lectin can prolong the residence time of Cur in the nasal mucosa and promote cellular uptake. In this work, a nasal delivery system incorporating OL modified Cur-loaded nanoparticles (Cur–OL–NPs) was developed and expected to bypass BBB and promote the absorption of Cur. We conjugated OL to polyethylene glycol-poly (lactic-co-glycolic acid) (PEG–PLGA), and combined polyethylene glycol-poly (γ-benzyl-L-glutamate) (PEG–PBLG) and OL–PEG–PLGA to prepare nanoparticles to improve the stability, bioavailability and targeting of Cur. Compared with unmodified NPs, increased efficiency of Cur–OL–NPs cellular uptake by Calu-3 cells had been obtained with no severe toxicity. Furthermore, in vivo pharmacokinetic studies also showed that Cur–OL–NPs had higher relative bioavailability. Thus, it is concluded that the results indicated that OL–NPs as carriers of Cur had a promising future in nasal drug delivery system.
研究领域:
药剂学
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神经科学
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生物材料学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
KOREAN JOURNAL OF CHEMICAL ENGINEERING
·
2019
·Vol. 36
·期 5
·822-827
·
IF 2.476
Pan Jie,Cao Duanlin,Ma Xuemei,Yang Jing
Curcumin is a kind of natural polyphenol whose functions are anti-tumor, anti-oxidant, anti-inflammatory and anti-microbial with low side effects. Solubility of Cur in water is poor, which results in low bioavailability, rapid metabolism, instability and poor absorption in vivo. Based on the crosslinking mechanism of pectin-calcium, the curcumin-pectin film (PT-Curf) was prepared by casting method, where chitosan and sodium alginate were added to the film, forming a system for blending modification to improve the performance of PT-Curf. Furthermore, the release of the curcumin films in vitro was studied and the effects of natural polysaccharides on the drug delivery system were discussed. According to our results, the natural polysaccharides involving pectin, chitosan and sodium alginate were excellent carriers of the fat-soluble drug Cur, and Cur was uniformly dispersed in the composite films in different crystal forms. Out of different drug delivery media, the three films exhibited different release rate and sustained release effect in vitro. However, the pectin-sodium alginate curcumin film (PT-SA-Curf) exhibited the most sustained release effect, the pectin-chitosan curcumin film (PT-CS-Curf) was second.
研究领域:
药学
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材料科学
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生物技术
✓ 已验证
产品关联
DOI
高影响因子
LWT-FOOD SCIENCE AND TECHNOLOGY
·
2019
·
IF 3.714
Shenghua He,Cheng Gu,Deguo Wang,Weili Xu,Rongchun Wang,Ying Ma
Konjac glucomannan (KGM) was used to characterize the structure of the curcumin emulsions stabilized with whey protein isolate (WPI). With an increasing concentration of KGM from 0.1% to 0.3%, the fat droplet size decreased significantly (p < 0.05) with increasing KGM content. The retention of curcumin in emulsions with KGM was significantly higher (p < 0.05) than the emulsions without KGM, after heating at 85 °C for 90 min. These two emulsions showed good stability in the pH range of 2–8 in addition to pH 5. Both emulsions with/without KGM were stable at 0–80 mM salt concentration, however the curcumin emulsion with KGM was unstable at 100 mM NaCl concentration. The droplet size analysis and microscopic observations indicated that the aggregation of fat droplets in these two emulsions occurred under simulated gastric fluid (SGF) conditions with a digestion time of 10 min. There were more undigested fat droplets in the curcumin emulsion with KGM than the emulsion without KGM under simulated intestinal fluid conditions after 120 min of digestion. The addition of KGM in WPI-stabilized curcumin emulsions slowed down the release rate of free fatty acids and curcumin from the emulsion droplets. These findings indicated that KGM could be used to achieve a controlled and sustainable release of bioactive compounds from emulsions.
研究领域:
食品科学
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生物化学
✓ 已验证
DOI
高影响因子
RSC Advances
·
2014
·Vol. 4
·期 103
·59211-59217
·
IF 3.708
Qiyu Huang,Lili Zhang,Xiaoyi Sun,Ke Zeng,Juan Li,You-Nian Liu
In this work, carboxymethyl dextran (CMD), a polysaccharidic dextran derivative with well-known biocompatibility and biodegradability, was used to modify curcumin-loaded liposomes for improving the anticancer efficacy of curcumin. The CMDylated curcumin-loaded liposomes (CMD-Cur-Lip) were successfully prepared and characterized in comparison with unmodified and two PEGylated curcumin-loaded liposomes. The results showed that: (1) the encapsulation efficiency of curcumin in the liposomes was improved after being modified with CMD; (2) all the curcumin-loaded liposomes displayed controlled release characteristics; (3) the CMD-Cur-Lip demonstrated improved cell cytotoxicity against cancer cells, as compared to other liposomal formulations and free curcumin; (4) CMD-Cur-Lip exhibited the highest cellular uptake as compared to other liposomal formulations.
研究领域:
药学
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肿瘤学
·
纳米技术
✓ 已验证
产品关联
DOI
高影响因子
Journal of Functional Foods
·
2016
·
IF 3.973
Jin Feng,Shanshan Wu,Hua Wang,Songbai Liu
In this work, ovalbumin-dextran nanogels were fabricated via the Maillard reaction followed by a heat-gelation process and their potential to improve curcumin bioavailability was investigated using an in vitro gastrointestinal tract. The result of electrophoresis, conjugation efficiency and yield, and far-UV circular dichroism verified the covalent attachment of dextran to ovalbumin by the Maillard reaction. The conjugates were then heated at the isoelectric point of ovalbumin to give stable nanogels. The transmission electron microscopy observation suggested that nanogels displayed a spherical structure. Curcumin was loaded into nanogels by a pH-driven method and the incorporation of curcumin affected the morphology of nanogels marginally. The transformation of curcumin in nanogels was significantly higher than that in ovalbumin nanoparticle. On the other hand, the bioaccessibility was similar for curcumin in nanogels and nanoparticle. The ovalbumin-dextran nanogels hold the potential as delivery systems for curcumin to fortify functional foods and beverages.
研究领域:
食品科学
·
生物化学
✓ 已验证
产品关联
DOI
高影响因子
Artificial Cells Nanomedicine and Biotechnology
·
2018
·
IF 3.026
Nana Li,Zhi Wang,Yongtai Zhang,Kai Zhang,Jianxu Xie,Ying Liu,Wansi Li,Nianping Feng
Hypothesis: The antitumor applications of curcumin (CUR) are limited because of its low water solubility, poor stability, and low bioavailability. We developed novel nanocarrier systems for tumour targeting and controlled CUR release and evaluated their therapeutic efficacy.Experiments: The surface of mesoporous silica nanoparticles (MSN) was modified with hyaluronan (HA) or polyethyleneimine-folic acid (PEI-FA) via disulfide bonds. The capacity of the resultant nanocarriers (MSN-HA and MSN-PEI-FA, respectively) for CUR delivery was evaluated in a breast cancer cell line and a mouse xenograft model.Findings: MSN/CUR-PEI-FA and MSN/CUR-HA were cytotoxic to MDA-MB-231 breast cancer cells. Both formulations showed an enhanced cellular uptake compared with that of a non-targeted nanocarrier, with a greater cellular uptake of FA-modified nanoparticles than that of HA-modified nanoparticles. Accordingly, MSN-PEI-FA showed more precise targeting and higher accumulation in tumours than did MSN-HA, as visualized by live imaging. Both types of nanoparticles had good biocompatibility and low toxicity, and MSN/CUR-PEI-FA inhibited the tumour growth to a greater degree than did free CUR. Thus, MSN/CUR-PEI-FA are a promising drug delivery system for the treatment of breast cancer.
研究领域:
药学
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纳米技术
·
癌症研究
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2015
·
IF 2.858
Ming Ying,Fengwen Huang,Haidong Ye,Hong Xu,Liangliang Shen,Tianwen Huan,Shitong Huang,Jiangfeng Xie,Shengli Tian,Zhangli Hu,Zhendan He,Jun Lu,Kai Zhou
The interaction between curcumin and pepsin was investigated by fluorescence, synchronous fluorescence, UV–vis absorption, circular dichroism (CD), and molecular docking. Under physiological pH value in stomach, the fluorescence of pepsin can be quenched effectively by curcumin via a combined quenching process. Binding constant ( K a ) and binding site number ( n ) of curcumin to pepsin were obtained. According to the theory of Förster's non-radiation energy transfer, the distance r between pepsin and curcumin was found to be 2.45 nm within the curcumin–pepsin complex, which implies that the energy transfer occurs between curcumin and pepsin, leading to the quenching of pepsin fluorescence. Fluorescence experiments also suggest that curcumin is located more closely to tryptophan residues than tyrosine residues. CD spectra together with UV–vis absorbance studies show that binding of curcumin to pepsin results in the extension of peptide strands of pepsin with loss of some β-sheet structures. Thermodynamic parameters calculated from the binding constants at different temperatures reveal that hydrophobic force plays a major role in stabilizing the curcumin–pepsin complex. In addition, docking results support the above experimental findings and suggest the possible hydrogen bonds of curcumin with Thr-77, Thr-218, and Glu-287 of pepsin, which help further stabilize the curcumin–pepsin complex.
研究领域:
生物化学
·
药物化学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
Regenerative Biomaterials
·
2015
·Vol. 2
·期 2
·97-105
·
IF 0
Li Xiaomeng,Qin Jinli,Ma Jun
A silk fibroin/poly (vinyl alcohol) porous scaffold with a water vapor transmission rate of 2125 ± 464 g/m2/day has been developed via thermally induced phase separation (gelation) and freeze-drying process. A hierarchical architecture of micropores and nanofibers was observed inside the scaffolds, and the related structures were analyzed. The viability and proliferation of 3T3 fibroblasts were examined, which indicated that the scaffolds exerted low cytotoxicity. After loading curcumin, the scaffolds can suppress the growth of 3T3 fibroblasts. The release behavior of curcumin from the scaffolds was investigated. At pH = 7.2, the release profiles showed no significant difference for the loading amounts of 0.5 mg and 0.25 mg per sample. Meanwhile, the cumulative amount of released drug at pH = 5.7 was significantly more than that in neutral solution due to more degradation of the scaffolds. It was suggested that the silk fibroin/poly (vinyl alcohol) blend scaffolds could be potentially used as wound dressing materials.
研究领域:
生物材料学
·
药剂学
✓ 已验证
产品关联
DOI
PubMed
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2018
·
IF 3.862
Lijun Hu,Min Li,Zhipeng Zhang,Yuanyuan Shen,Shengrong Guo
Paclitaxel (PTX), one of the most potent anticancer agents , has showed a remarkable activity against varieties of tumors. However, the bioavailability of PTX is quite low due to its poor aqueous solubility. Moreover, the emerging multidrug resistance (MDR) in cancer to PTX remains a major obstacle for successful chemotherapy. In order to address these problems, we developed self-assembly of biotinylated poly(ethylene glycol)-poly(curcumin) (Biotin-PEG-PCDA) for PTX delivery (termed as PTX-BPC NPs) with the application of mPEG 2K -P(CL-co-LLA) as an emulsifier . The loading content and encapsulation efficiency of PTX were 13.2% and 92.0%, respectively. In vitro drug release study showed that PTX-BPC NPs could degrade rapidly and then release the PTX payload in a 10 mM glutathione (GSH) environment. Compared with free PTX, PTX-BPC NPs exhibited enhanced anticancer efficacy (IC 50(MCF-7/ADR cells) , 17.28 µg/mL vs. 1.15 µg/mL). In addition, these biotin-modified nanoparticles could also significantly reverse PTX resistance by suppressing the over-expression of P-gp, thus resulting in increased intracellular drug accumulation and reduced drug efflux in MCF-7/ADR cells, which showed a great anticancer effect.
研究领域:
药学
·
纳米技术
·
癌症研究
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CELLULAR PHYSIOLOGY AND BIOCHEMISTRY
·
2017
·Vol. 44
·期 2
·618-633
·
IF 5.104
Qi Zhangyang,Wu Meihao,Fu Yun,Huang Tengfei,Wang Tingting,Sun Yanjie,Feng Zhibo,Li Changzheng
Background/Aims: The generation of reactive oxygen species (ROS) caused by amyloid-β (Aβ) is considered to be one of mechanisms underlying the development of Alzheimer’s disease. Curcumin can attenuate Aβ-induced neurotoxicity through ROS scavenging, but the protective effect of intracellular curcumin on neurocyte membranes against extracellular Aβ may be compromised. To address this issue, we synthesized a palmitic acid curcumin ester (P-curcumin) which can be cultivated on the cell membrane and investigated the neuroprotective effect of P-curcumin and its interaction with Aβ. Methods: P-curcumin was prepared through chemical synthesis. Its structure was determined via nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS). An MTT assay was used to assess Aβ cytotoxicity and the protective effect of P-curcumin on SH-SY5Y cells. The effect of P-curcumin on Aβ-induced ROS production in vitro and in vivo were assessed based on changes in dichlorofluorescein (DCF) fluorescence. A spectrophotometric method was employed to detect lipid peroxidation. To mimic the interaction of P-curcumin on cell membranes with Aβ, liposomes were prepared by thin film method. Finally, the interactions between free P-curcumin and P-curcumin cultivated on liposomes and Aβ were determined via spectrophotometry. Results: A novel derivative, palmitic acid curcumin ester was prepared and characterized. This curcumin, cultivated on the membranes of neurocytes, may prevent Aβ-mediated ROS production and may inhibit the direct interaction between Aβ and the cellular membrane. Furthermore, P-curcumin could scavenge Aβ-mediated ROS as curcumin in vitro and in vivo, and had the potential to prevent lipid peroxidation. Morphological analyses showed that P-curcumin was better than curcumin at protecting cell shape. To examine P-curcumin’s ability to attenuate direct interaction between Aβ and cell membranes, the binding affinity of Aβ to curcumin and P-curcumin was determined. The association constants for free P-curcumin and curcumin were 7.66 × 104 M-1 and 7.61 × 105 M-1, respectively. In the liposome-trapped state, the association constants were 3.71 × 105 M-1 for P-curcumin and 1.44× 106 M-1 for curcumin. With this data, the thermodynamic constants of P-curcumin association with soluble Aβ (ΔH, ΔS, and ΔG) were also determined. Conclusion: Cultivated curcumin weakened the direct interaction between Aβ and cell membranes and showed greater neuroprotective effects against Aβ insult than free curcumin
研究领域:
神经科学
·
药理学
·
生物化学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）