CARBOHYDRATE POLYMERS
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2021
·
IF 9.381
Tiantian Wei,Yin Zhang,Meng Lei,Yanru Qin,Zhongjie Wang,Zhimeng Chen,Liefeng Zhang,Yongqiang Zhu
Herein, a pH-responsive cyclodextrin derivative (R6H4-CMβCD) with cell-penetrating ability was successfully synthesized, and curcumin-loaded nanoparticles (R6H4-CMβ [email protected] NPs, RCCNPs) were developed to improve its efficacy in hepatoma. RCCNPs could improve the cell uptake compared with CMβ [email protected] NPs (CCNPs) and were internalized into cells mainly through endocytosis mediated by reticulin and macropinocytosis . Furthermore, the accumulation of RCCNPs in hepatoma cells at pH 6.4 was higher than that at pH 7.4, indicating a pH-responsive uptake. Additionally, RCCNPs could escape from the lysosomes via the “proton sponge effect”, and a high apoptosis rate was detected. Importantly, in vivo experiments revealed that orally administered RCCNPs could exert excellent anti-cancer effects in tumor-bearing mice. Hematoxylin-eosin staining did not show significant histological changes in the major organs. Thus, our findings indicate the potential of R6H4-CMβCD as a nanopharmaceutical material, and RCCNPs as an effective delivery system for oral curcumin in cancer management.
研究领域:
药学
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纳米技术
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癌症研究
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药物递送系统
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DOI
PubMed
高影响因子
Journal of Biomedical Nanotechnology
·
2014
·Vol. 10
·期 8
·1458-1468
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IF 7.578
Li Xingyi,Chen Tongke,Xu Lu,Zhang Zhaoliang,Li Lingli,Chen Hao
Poor water solubility as well as poor bioavailability of curcumin has greatly hindered its applications in cancer therapy. In the present study, a highly water soluble curcumin nano-formulation was developed and its in vivo anti-cancer efficiency in nude BALB/c mouse model was
evaluated. Unlike native curcumin, the developed curcumin micelles were quickly dissolved into aqueous solution with significant improvement of water solubility (∼104 fold increasement compared to its native form). The developed curcumin micelles had a narrow size distribution
(18–28 nm) with high drug encapsulation efficiency (85%–95%). The developed curcumin micelles were characterized by X-raydiffraction (XRD), Differential scanning calorimetric (DSC), and Fluorescence spectral analysis. We observed the enhanced stability of curcumin in micelles formulation
in phosphate buffer solution (PBS). In vitro cytotoxicity assay indicated that the curcumin micelles was comparatively more effective than native curcumin against various cancer cell lines due to the enhanced cellular uptake of curcumin yet resulting in the apoptosis of cancer cells.
Western blotting study revealed that the induction apoptosis of S-65 cancer cells by curcumin micelles was mainly due to the down-regulation of p-Rb, Blc-2, p-AKT expression and caspase-9 activation. In vivo anti-tumor test in nude BALB/c mouse bearing S-65 xenografts indicated the
intraperitoneal injection of curcumin micelles (25 mg/kg) could significantly inhibit tumor growth as compared with native curcumin treatment (p < 0.05), which was accompanied by significantly increased apoptosis of tumor cells and diminished vascular endothelial growth factor expression
in tumor tissue (p < 0.05).
研究领域:
药学
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肿瘤学
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纳米技术
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药理学
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DOI
PubMed
高影响因子
Frontiers in Pharmacology
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2021
·
IF 5.811
Wang Peijian,Li Hui,Lin Zhexuan,Luo Hongjun,Luo Wenhong
The poor bioavailability and rapid metabolism of curcumin (CUR) restrict its clinical application. Piperine (PIP), which was extracted from natural compounds, can increase the plasma concentration of curcumin in humanidad. As an artificial synthetic piperine analog, silepcimide (ILE) has significant advantages because of the low price and simple synthesis process. In this study, a simple and rapid HPLC-UV method was developed for determination of the plasma concentration of CUR, PIP,ILE and dihydrocurcumin (DHC, a metabolite of CUR) simultaneously. Meanwhile, the effects of PIP and ILE on the plasma concentration and pharmacokinetics of DHC in SD rats was studied to explore whether ILE could serve as a CUR bioavailability enhancer. The metabolic pathway of CUR was studied by comparing the differences of CUR plasma concentration between intravenous injection and oral administration over the same time period, and reacting with small intestine homogenate without microbes of SD rats. The results of drug-time curve showed that combined administration of ILE and CUR had significant effect on plasma concentrations of DHC. Repeated administration of PIP or ILE could significantly increase the plasma concentration of DHC. Plasma CUR could be detected in the samples of from intravenous injection of CUR rats, whereas, it couldn’t be detected in the plasma sample form oral administration rats. CUR incubated with intestinal homogenate without intestinal bacteria could not be transformed into DHC. In conclusion, our results show that ILE can improve the bioavailability of CUR. Additionally, it was inferred that most of the CUR was reduced to DHC by NADPH when it was absorbed from gastrointestinal tract, and our results demonstrated that this pathway might be mediated by gastrointestinal microorganisms.
研究领域:
药理学
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药物学
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药物代谢
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DOI
PubMed
高影响因子
Current Research in Food Science
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2022
·
IF 6.269
Sheng Lin,Xixi Cai,Huimin Chen,Yizhou Xu,Jiulin Wu,Shaoyun Wang
The poor water solubility, bioavailability and stability of bioactive compounds have become the bottleneck restricting their wide application, thus developing a functional carrier to realize the efficient encapsulation and activity improvement of active hydrophobic substances has become a research hotspot. In this work, a functional glycosylated fish gelatin (called FG-COS conjugates) carrier based on fish gelatin (FG) and chitooligosaccharide (COS) via Maillard reaction was developed. The functional carrier exhibited good antioxidant activity and high encapsulation of curcumin (Cur). Enhanced antioxidant effect of Cur loaded in FG-COS conjugates (called FG–COS–Cur nanoparticles) was achieved, showing remarkable UV protection on Cur and enhanced intracellular antioxidant activity of FG–COS–Cur nanoparticles. Remarkably, FG–COS–Cur nanoparticles increased the cell viability of H 2 O 2 -induced oxidative damage Caco-2 cells, drastically reduced the levels of reactive oxygen species (ROS) and lactate dehydrogenase (LDH), and significantly increased intracellular antioxidant enzyme activities, which all exhibited a dose-response relationship. These findings suggested that the FG-COS conjugates with intrinsic antioxidant activity could effectively encapsulate Cur and improved bioavailability for hydrophobic active molecules in functional food field.
研究领域:
食品科学
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药学
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生物技术
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营养学
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DOI
PubMed
高影响因子
Drug Delivery and Translational Research
·
2020
·Vol. 10
·期 5
·1520-1530
·
IF 2.664
Cheng Ziting,Lin Hua,Wang Zhen,Yang Xiaoyu,Zhang Mei,Liu Xuechun,Wang Bingjie,Wu Zhenfeng,Chen Daquan
In order to improve the bioavailability of curcumin (Cur) and patient compliance, a type of novel hyaluronic acid (HA) composite microneedles containing Cur-loaded micelles was designed in this paper. On the one hand, the microneedles matrix solution was prepared by screening the optimal concentration of HA and the better proportion of HA to sodium carboxymethyl starch (CMS-Na). On the other hand, the amphiphilic polymer, named as Quercetin-Dithiodipropionic Acid-Oligomeric Hyaluronic Acid (Que-DA-oHA), was synthesized and characterized using 1 H-NMR. Subsequently, the dialysis method was used to prepare Cur-loaded Que-DA-oHA micelles with an average size of 172.6 ± 11.4 nm and zeta potential of − 33.71 ± 0.45 mV. A micromolding process was used to prepare the micelle-loaded HA composite microneedles. It had been found that when the concentration of HA was 200 mg/mL and the mass ratio of HA to CMS-Na was 2:1, the prepared HA composite microneedles had good mechanical strength. In-skin dissolution kinetics showed that the micelle-loaded HA composite microneedles could dissolve quickly in the skin. In vitro permeation study indicated that the microneedles delivered 74.7% of their drug load over 6 h, which exhibited remarkable drug permeation properties in a short time. Here, we creatively combined micellar technology with microneedle technology to rapidly deliver Cur transdermally for diseases treatment such as melanoma.
Graphical abstract
研究领域:
药学
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纳米技术
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药物递送系统
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生物医学工程
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DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2017
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IF 4.3
Cihui Tian,Sajid Asghar,Yifan Wu,Zhipeng Chen,Xin Jin,Lining Yin,Lin Huang,Qineng Ping,Yanyu Xiao
The expression of multiple receptors on intestinal epithelial cells enables an actively targeted carrier to significantly enhance the oral delivery of payloads. Conjugating the receptors’ ligands on the surfaces of a particulate-delivery system allows site-specific targeting. Here, we used taurocholic acid (TCA) as a ligand for uptake of nanostructured lipid carriers (NLCs) mediated by a bile-acid transporter to improve oral bioavailability of curcumin (Cur). First, synthesis of TCA–polyethylene glycol 100–monostearate (S100-TCA) was carried out. Then, the physical and chemical properties of S100-TCA-modified Cur-loaded NLCs (Cur-TCA NLCs) with varying levels of S100-TCA modifications were investigated. Small particle size (<150 nm), high drug encapsulation (>90%), drug loading (about 3%), negative ζ-potential (−7 to −3 mV), and sustained release were obtained. In situ intestinal perfusion studies demonstrated improved absorption rate and permeability coefficient of Cur-TCA NLCs. Depending on the degree of modification, Cur-TCA NLCs displayed about a five- to 15-fold higher area under the curve in rats after oral administration than unmodified Cur NLCs, which established that the addition of S100-TCA to the NLCs boosted absorption of Cur. Further investigations of TCA NLCs might reveal a bright future for effective oral delivery of poorly bioavailable drugs.
研究领域:
药学
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药物递送系统
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药代动力学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2021
·
IF 5.875
Yuanyuan Chen,Die Jia,Qiming Wang,Yueru Sun,Zhenan Rao,Xiaojuan Lei,Jichun Zhao,Kaifang Zeng,Zhigang Xu,Jian Ming
Curcumin (Cur), a hydrophobic active pharmaceutical ingredient with high anticancer activity, has poor water solubility and low bioavailability. Although many delivery systems have been developed to improve their bioavailability, some limitation such as low drug loading efficiency and poor stability are still remained. The metal-polyphenol networks (MPNs) delivery system designed in this subject solved above problems and effectively improved the anticancer activity of Cur. The synthesized [email protected] (III) is consisting of epigallocatechin gallate (EGCG), iron chloride (FeCl 3 ) and Cur, and the well-designed structure endow [email protected] (III) high loading efficiency, good water solubility and stability. After the [email protected] (III) nanoparticles were internalized by MCF-7 cells, the Cur could be released in endo/lysosomal microenvironment (pH = 5.0), and the Cur delivery in the deep tumor could be realized. The distribution of [email protected] (III) in MCF-7 cells was analyzed by laser confocal, and [email protected] (III) could effectively deliver more Cur into MCF-7 cells in comparison with free Cur. In addition, the results of flow cytometry and western blot further indicated that [email protected] (III) had a stronger ability to induce apoptosis than free Cur. Transwell cell migration and invasion experiments showed that Cur and EGCG-Fe(III) had a synergistic effect in inhibiting MCF-7 cell migration and invasion. In vitro hemolysis and in vivo experiments showed that the [email protected] (III) had negligible effect on the blood environment and a great tumor-inhibition efficacy, indicating that the MPNs delivery system had a good blood compatibility and antitumor activity. Our results indicated that MPNs-coated Cur nanoparticle could be a new form of Cur delivery system for anticancer application.
研究领域:
药学
·
癌症研究
·
纳米技术
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY
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2018
·
IF 1.792
Bo Wang,Wenyang Li,Hongyu Jin,Xinshi Nie,Hui Shen,Erran Li,Wei Wang
Chronic intermittent hypoxia (CIH) is one of the main features of obstructive sleep apnea (OSA), which is also commonly associated with neurocognitive impairments. The present study aimed to elucidate the beneficial effect of curcumin on CIH-induced brain injuries. Male balb/c mice (6 ∼ 8 weeks) were exposed to normoxia or a pattern of CIH (8 h/day, cycles of 180 s each, hypoxia: 5% O 2 for 50 s, reoxygenation: 21% O 2 for 50 s) for 10 weeks, along with daily curcumin treatment (50, 100, or 200 mg/kg, intragastrically) or its vehicle. The results showed that CIH induced significant brain edema, as well as neuronal apoptosis and astrogliosis in the cerebral cortex, brainstem, and cerebellum regions of brain. In addition, increased astrocytic AQP4 expression and activation of p38 MAPK pathway were observed after CIH exposure. Curcumin dose-dependently mitigated the brain edema and relevant cell alterations, showing a neuroprotective effect in CIH-induced brain injury. Together, these results suggest curcumin ameliorates the CIH-induced brain injuries, including brain edema, neuronal death and astrogliosis. The beneficial role of curcumin is mediated partially by regulating AQP4 and p38 MAPK pathway.
研究领域:
神经科学
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药理学
·
睡眠医学
✓ 已验证
DOI
PubMed
高影响因子
PROGRESS IN ORGANIC COATINGS
·
2026
·
IF 7.9
Xing-Yu Lei,Liang Ma,Qi Xu,Hui-Jing Li,Yan-Chao Wu
Biofouling poses a great challenge to marine facilities and causes serious economic losses, making the development of green and non-toxic anti-fouling coatings a high priority. In this study, leveraging the broad-spectrum bacteriostatic and economic properties of the natural product curcumin (Cur), it was chemically grafted onto the surface of xanthate-functionalized silica nanoparticles with the hydrophilic monomer vinylpyrrolidone (NVP) using a reversible addition-fragmentation chain transfer (RAFT) polymerization strategy. The resulting modified particles were incorporated as active fillers into a terminal hydroxy-polydimethylsiloxane (PDMS) matrix, successfully constructing a functional coating labeled PDMS/SiO 2 -X. This coating exhibits a synergistic antifouling mechanism combining self-polishing, static antifouling agent mitigation and dynamic fouling release. The presence of modified silica significantly improves the mechanical properties of the coating. The low surface energy surface imparts excellent fouling-release characteristics, while the hydrolysis of ester bond enables the sustained release of Cur to achieve efficient bacterial inhibition. Additionally, NVP effectively resists protein adhesion by forming a hydration layer. A 180-day real-sea field test verifies the long-lasting and stable antifouling performance of the coating. This work provides a new idea for developing highly efficient and environmentally friendly marine antifouling coatings.
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产品关联
DOI
高影响因子
JOURNAL OF MATERIALS RESEARCH
·
2026
·
IF 2.9
Li Jie,Li Xiaojuan,Wang Xinran,Liu Xinyu,Wang Yingfeng,Wu Dingsheng,Feng Quan,Xu Zhenzhen,Chen Lei,Sheng Mingfei,Yin Maoli
Addressing limitations of conventional dressings in real-time monitoring and active repair, this study developed a smart, multifunctional nanofiber membrane by electrospinning curcumin (Cur) into a polyvinyl alcohol (PVA) matrix. The PVA/Cur membranes integrated antibacterial, antioxidant, and pH-responsive colorimetric properties. Increasing Cur content (0–1.5 wt%) reduced fiber diameter and enhanced hydrophilicity. The PVA/Cur1.0 membrane exhibited optimal mechanical properties (2.84 MPa tensile strength, 43.31% elongation). Biologically, PVA/Cur1.5 achieved a > 5-log reduction within 10 min and over 70% DPPH radical scavenging. Leveraging Cur's pH sensitivity, the dressing enabled visual wound monitoring via a distinct color transition from yellow (acidic, pH 4–6) to reddish-brown (alkaline, pH 7.5–8.9), synchronized with pH-triggered Cur release. Excellent biocompatibility was confirmed (hemolysis < 3%, fibroblast viability > 85%). This work presents an integrated strategy for a smart theragnostic dressing, merging real-time diagnosis and active therapy to advance beyond passive wound care. Graphical
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产品关联
DOI
高影响因子
ACS Applied Nano Materials
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2022
·
IF 6.14
Seojin Jung,Seokhee Chang,Na-Eun Kim,Seong-O Choi,Yoon-Jae Song,Yue Yuan,Jooyoun Kim
A feasible strategy of on-demand drug delivery for the treatment of dermal inflammation under low-pH conditions is proposed, employing zeolitic imidazolate framework-8 (ZIF-8) as a pH-responsive nanoparticle and curcumin (CCM) as a model drug. To overcome the low bioavailability of topically treated drug, a microneedle (MN) form is used to incorporate CCM and ZIF-8. Taking advantage of the fact that ZIF-8 degrades under acidic conditions, CCM is embedded in porous ZIF-8 nanoparticles such that CCM is released when ZIF-8 comes into contact with an acidic dermal fluid at the inflammation site, and this CCM-encapsulated ZIF-8 (CCMZIF) is incorporated into water-dissolvable poly(vinyl pyrrolidone) MN. The ZIF-8 shows a high loading capacity (∼40.5%) of CCM through chemical bonding and physical adsorption. From in vitro tests with both a buffered solution and porcine skin, CCM from the CCMZIF MN is released in a higher amount at pH 5.0 than at pH 7.4, demonstrating the capability of the pH-responsive release of the drug when needed at inflammatory sites. The analytical investigation conducted here reveals that an acidic environment triggers the structural degradation of ZIF-8, allowing the release of the chemically bonded CCM. Cytotoxicity and stability tests demonstrate the good biocompatibility and bioavailability of ZIF-8. This study highlights the analytical discussion of the encapsulation and release mechanism of CCM in a ZIF-8-implemented MN drug delivery platform. The results demonstrate an advanced on-demand therapeutic strategy for skin disorder treatment.
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DOI
高影响因子
INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY
·
2022
·Vol. 58
·期 4
·1728-1740
·
IF 3.612
Chunling Zhang,Yushu Zhang,Qiangsheng Fang,Rui Li,Yuan Yuan,Hong Zhuang
Summary Antimicrobial photodynamic therapy (aPDT) is an effective method in the field of sterilisation. Singlet oxygen ( 1 O 2 ) is an important substance in photodynamic sterilisation that needs to be detected. It involves energy transfer from an excited photosensitiser to surrounding oxygen molecules to produce cytotoxic 1 O 2 species, a process termed as type II reaction. Traditional photodynamic sterilisation for fresh produce generally involves only a single photosensitiser and uses nanoemulsions coating to make the photosensitiser work better. This allows the emulsion to produce only a limited amount of reactive oxygen species (ROS) in the presence of light, such that the bactericidal effect is limited. We have innovatively compounded two photosensitisers and stored them as nanoemulsions. The composite photosensitiser produces relatively higher ROS and the nanoemulsions have good stability as well as rheological properties, and the photosensitisers are well coated in the emulsions. In summary, nanoemulsions based on composite photosensitisers showed synergistic activity in controlling the growth of Staphylococcus aureus , which provides a novel approach for raw sterilisation to maintain food safety.
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）