Drug Delivery and Translational Research
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2020
·Vol. 10
·期 5
·1520-1530
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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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International Journal of Nanomedicine
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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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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
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癌症研究
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纳米技术
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药物递送系统
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RESPIRATORY PHYSIOLOGY & NEUROBIOLOGY
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2018
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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
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睡眠医学
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PROGRESS IN ORGANIC COATINGS
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2026
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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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JOURNAL OF MATERIALS RESEARCH
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2026
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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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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2023
·
IF 8.2
Qianyu Sun,Tianzhong Yuan,Gang Yang,Daliang Guo,Lizheng Sha,Rendang Yang
The solubility of cyclodextrin metal-organic frameworks (CD-MOFs) in aqueous media making it not suitable as sustained-release drug carrier. Here, curcumin-loaded CD-MOFs (CD-MOFs-Cur) was embedded in chitosan- graft -poly(lactic acid) (CS-LA) via a solid-in-oil-in-oil (s/o/o) emulsifying solvent evaporation method forming the sustained-release composite microspheres . At CS-LA concentration of 20 mg/mL, the composite microspheres showed good sphericity. The average particle size of CS-LA/CD-MOFs-Cur (2:1), CS-LA/CD-MOFs-Cur (4:1) and CS-LA/CD-MOFs-Cur (6:1) composite microspheres was about 9.3, 12.3 and 13.5 μm, respectively. The above composite microspheres exhibited various degradation rates and curcumin release rates. Treating in HCl solution (pH 1.2) for 120 min, the average particle size of above microspheres reduced 28.19 %, 24.34 % and 6.19 %, and curcumin released 86.23 %, 78.37 % and 52.57 %, respectively. Treating in PBS (pH 7.4) for 12 h, the average particle size of above microspheres reduced 30.56 %, 26.56 % and 10.66 %, and curcumin released 68.54 %, 54.32 % and 31.25 %, respectively. Moreover, the composite microspheres had a favorable cytocompatibility, with cell viability of higher than 90 %. These composite microspheres open novel opportunity for sustained drug release of CD-MOFs.
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PHOTOCHEMISTRY AND PHOTOBIOLOGY
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2023
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IF 3.3
Qing Guo,Peiyuan Li,Ying Zhang,Hongjun Yan,Qiuyan Yan,Rixiang Su,Wei Su
Combined photothermal therapy (PTT) and photodynamic therapy (PDT) has emerged as a novel and effective antibacterial strategy. In order to endow titanium (Ti) with antibacterial properties, the Ti-PDA-Cur composite was prepared using the excellent adhesion properties of polydopamine (PDA) to load curcumin (Cur) on the surface of Ti. The Ti-PDA-Cur coating can produce singlet oxygen ( 1 O 2 ) and heat under 405 + 808 nm light irradiation, which can effectively kill Staphylococcus aureus and Escherichia coli . Moreover, the cytotoxicity and hemolysis rate of Ti-PDA-Cur were low, indicating its good biocompatibility. Therefore, this study provided a new strategy for the development of new Ti implants.
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International Journal of Nanomedicine
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2023
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IF 8
Lin Sheng,Yumeng Wei,Chao Pi,Ju Cheng,Zhilian Su,Yuanyuan Wang,Tao Chen,Jie Wen,Yuxun Wei,Jingwen Ma,Jia Tang,Huiyang Liu,Zerong Liu,Hongping Shen,Ying Zuo,Wenwu Zheng,Ling Zhao
Purpose The early stage of this study verified that a turmeric extract (TUR) including 59% curcumin (CU), 22% demethoxycurcumin (DMC), and 18% bisdemethoxycurcumin (BDMC), could enhance the stability of CU and had greater antidepressant potential in vitro. The objective of the study was to develop a nano-delivery system containing TUR (TUR-NE) to improve the pharmacokinetic behavior of TUR and enhance its antidepressant effect.Methods The antidepressant potential of TUR was explored using ABTS, oxidative stress-induced cell injury, and a high-throughput screening model. TUR-NE was fabricated, optimized and characterized. The pharmacokinetic behaviors of TUR-NE were evaluated following oral administration to normal rats. The antidepressant effect of TUR-NE was assessed within chronic unpredictable mild stress model (CUMS) mice. The behavioral and biochemical indexes of mice were conducted.Results The results depicted that TUR had 3.18 and 1.62 times higher antioxidant capacity than ascorbic acid and CU, respectively. The inhibition effect of TUR on ASP+ transport was significantly enhanced compared with fluoxetine and CU. TUR-NE displayed a particle size of 116.0 ± 0.31 nm, polydispersity index value of 0.121 ± 0.007, an encapsulation rate of 98.45%, and good release and stability in cold storage. The results of pharmacokinetics indicated the AUC(0-t) of TUR-NE was 8.436 and 4.495 times higher than that of CU and TUR, while the Cmax was 9.012 and 5.452 times higher than that of CU and TUR, respectively. The pharmacodynamic study confirmed that the superior antidepressant effect of TUR-NE by significantly improving the depressant-like behaviors and elevating the content of 5-hydroxytryptamine in plasma and brain in CUMS mice. TUR-NE showed good safety with repeated administration.Conclusion TUR-NE, which had small and uniform particle size, enhanced the bioavailability and antidepressant effect of TUR. It could be a promising novel oral preparation against depression.
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MICROCHIMICA ACTA
·
2023
·Vol. 190
·期 9
·1-11
·
IF 5.7
Liu Yujie,Gao Ran,Liu Xingcen,Zheng Jinhua,Wu Xia
Curcumin (Cur) possesses diverse biological and pharmacologic effects. It is widely used as a food additive and therapeutic medicine. A study to determine a sensitive detection method for Cur is necessary and meaningful. In this work, double rare earth ions co-doped fluorescent coordination polymer nanoparticles (CPNPs) were developed for the Cur detection. The CPNPs were synthesized by using adenosine monophosphate (AMP) as bridge ligands via coordination self-assembly with Ce 3+ and Tb 3+ . The AMP-Ce/Tb CPNPs exhibited the characteristic green fluorescence of Tb 3+ and had high luminescence efficiency. Under the optimal conditions, the fluorescence intensity of AMP-Ce/Tb CPNPs could be significantly quenched by Cur. The fluorescence quenching extent at λ ex / λ em of 300 nm/544 nm showed a good linear relationship with the Cur concentration in the range of 10 to 1000 nM. The detection limit was as low as 8.0 nM ( S/N = 3). This method was successfully applied to the determination of Cur in real samples with satisfactory results. The luminescence mechanism of AMP-Ce/Tb CPNPs and the fluorescence quenching mechanism of the CPNPs by Cur were both examined. Graphical abstract
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2023
·
IF 8.2
Chenmin Zheng,Yufan Huang,Xiaojing Liang,Bihua Shen,Guoguang Zhang,Peng Fei
Pickering emulsion gels represent a novel class of non-toxic and biocompatible emulsions, offering extensive applications in the pharmaceutical and food additive sectors. This study delineates the synthesis of Pickering emulsion gels utilizing native and amidated pectin samples. Phenylalanine amidated pectin (AP) was procured via an ultra-low temperature enzyme method, while the control group (LP) adhered to an identical procedure without papain catalysis. Experimental outcomes revealed that the AP Pickering emulsion gel manifested superior stability compared to pectin emulsion samples (PE and LP). The Pickering emulsion gel from 5 % amidated pectin (5AP) retained stability throughout a 14-day emulsion stability assessment. Furthermore, all emulsion samples were evaluated for their capacity to deliver and sustain curcumin within an in vitro digestion simulation. Rheological properties and oil droplet size results indicated that the 5AP Pickering emulsion gel exhibited optimal cream index and emulsion stability, effectively inhibiting premature water-oil stratification within the emulsion and augmenting curcumin bioaccessibility. Within the in vitro digestion simulation, the 5AP Pickering emulsion gel demonstrated the highest curcumin bioaccessibility, measured at 17.96 %.
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International Journal of Electrochemical Science
·
2023
·
IF 1.5
Jianwen Xiong,Wei Tan,Jinyuan Cai,Kailing Lu,Xiyu Mo
A novel photoelectrochemical (PEC) sensor based on a nickel phthalocyanine-based metal organic framework (NiPc–Ni MOF) was prepared and used to detect Curcumin. The photosensitive material NiPc–Ni MOF was synthesized and characterized via scanning electron microscopy, transmission electron microscopy, and X-ray diffraction. Under white light irradiation, the NiPc–Ni MOF composite modified indium tin oxide glass electrode showed a good photocurrent response to the detection of Curcumin. The experimental conditions of a light source, pH, bias voltage, modifier concentration, and coating amount were optimized. The improved PEC sensor showed a linear range of 0.0025–16 μM and a detection limit of 0.8 nM. Moreover, the PEC sensor exhibited good stability, selectivity, and reproducibility. Finally, the PEC sensor was used to detect Swisse Curcumin tablets with satisfactory results. The method presented in this study is a new strategy for detecting Curcumin.
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