Regenerative Biomaterials
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2015
·Vol. 2
·期 2
·97-105
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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
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药剂学
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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
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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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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
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药理学
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生物化学
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分子生物学
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Materials Science & Engineering C-Materials for Biological Applications
·
2019
·
IF 4.959
Zhiyong Song,Yang Wu,Huajuan Wang,Heyou Han
Due to their remarkable antibacterial properties, silver nanoparticles (Ag NPs) and curcumin (CCM) have been widely used in the antimicrobial field. In our study, we have fabricated the uniform and stable silver/curcumin composite nanoparticles by a facile ultrasound treatment process and the synergistic antibacterial activity were evaluated. The curcumin not only played a role of reducing agent but also acted as a capping agent. The antibacterial effects of silver/curcumin (cAgNPs) were studied by measuring the growth curve and surface plate assay based on the E. coli and B. subtilis , which showed concentration dependent bacteriostatic and bactericidal effects of cAgNPs. The presence of CCM enhance the binding of Ag to bacterial membrane and Ag + release in comparison to that without CCM, so that creating a temporary and local high Ag + concentration near the surface of the bacterium, meanwhile, generation of more reactive oxygen species, lead to membrane damage, bacterial lipases and induce leakage of intracellular contents followed by bacterial death that lead to growth inhibition of the bacteria. The antibacterial effects were characterized by scanning electron microscopy (SEM) and transmission electron microscopy (TEM), the effect which were further found to decrease by introducing antioxidant N -acetyl- l -cysteine (NAC) act as a reactive oxygen species (ROS) scavenging agent. These initial data suggest that cAgNPs have a highly antibacterial efficient and might have potential to be developed as an effective antimicrobial nanomaterial.
研究领域:
微生物学
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纳米生物学
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药理学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Shiyu Chen,Xiaoe Chen,Gaofeng Yuan
Biocompatible and degradable hydrogels are extensively utilized for the delivery and controlled release of bioactive agents. Chitosan/squid ring teeth protein (SRT) hydrogels (CH/SRTs) cross-linked by genipin were fabricated, and their gel properties and structural characteristics were analyzed across varying SRT contents. Additionally, the curcumin-release behavior of curcumin-loaded CH/SRTs (Cur-CH/SRTs) was evaluated. Results indicated that increasing SRT content enhanced the elasticity, viscosity, gel strength, hardness, and thermal stability of CH/SRTs. Specifically, the hardness and gel strength of CH/SRT3 (Chitosan: SRT, 1:1) were 207.8 % and 220.9 % higher, respectively, than those of the pure chitosan hydrogel. Higher SRT content significantly increased the curcumin encapsulation efficiency of Cur-CH/SRTs while substantially reducing curcumin release in simulated gastrointestinal fluid. Compared to the curcumin-loaded pure chitosan hydrogel, the curcumin release rate of Cur-CH/SRT3 decreased by 56.12 % after 480 min of simulated gastrointestinal digestion. These findings were attributed to reduced swelling and improved gel strength of Cur-CH/SRTs with SRT addition. Consequently, CH/SRTs demonstrate potential for applications in the controlled release of drugs and bioactive agents.
研究领域:
生物材料学
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药物递送系统
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2023
·
IF 8.2
Lan Wang,Jin Mao,Qi Zhou,Qianchun Deng,Lei Zheng,Jie Shi
The food industry has paid lots of attentions to curcumin because of its potential bioactive qualities. However, its use is severely constrained by its low bioavailability, stability and water solubility. Herein, we created sodium caseinate and carboxymethylpachymaran (CMP) nanoparticles (SMCNPs) that were loaded with curcumin. The composite nanoparticles were spherical, as characterized by SEM and TEM , the fluorescence spectroscopy, FTIR and XRD research revealed that hydrogen bonding, hydrophobic interaction and electrostatic interaction were the main drivers behind the creation of the nanoparticles. The SMCNPs exhibited lower particle size, greater dispersion and higher encapsulation rate when the mass ratio of sodium caseinate to CMP was 3:5 (particle size of 166.8 nm, PDI of 0.15, and encapsulation efficiency of 88.07 %). The composite nanoparticles had good antioxidant activity , physical stability and sustained release effect on intestinal tract during the in vitro simulation experiments, successfully preventing the early release of curcumin into gastric fluid. Finally, cytotoxicity studies told that the prepared composite nanoparticles have good biocompatibility and can inhibit the growth of tumor cells (HT-29). In conclusion, using CMP and sodium caseinate as carriers in this study may open up a fresh, environmentally friendly, and long-lasting way to construct a bioactive material delivery system.
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Food Bioscience
·
2023
·
IF 5.2
Hengju Ge,Jiaxin Li,Yang Xu,Jiahong Xie,Naymul Karim,Fujie Yan,Jianling Mo,Wei Chen
Curcumin (CUR), the main compound extracted from Curcuma longa , has various biological actions, including hepatoprotective, anti-infective, anti-inflammatory, antioxidant, and neurotrophic properties. But it has not yet been clarified how CUR affects the accumulation of fatty in hepatic cells. Our study uncovered that CUR decreased the lipid deposition in free fat acids (FFAs)-treated hepatocytes, which could be blocked by Compound C (an AMPK inhibitor). This result suggests that protective effect was associated with the AMPK pathway activation. MiR-3666 directly targets the AMPK gene, and overexpression of miR-3666 greatly weakens the hypolipidemic effect of CUR. Our results showed that CUR reduced FFAs-induced lipid deposition by targeting miR-3666. This boosted AMPK phosphorylation and inhibited its downstream targets, including ACC and SREBP1 . These findings together confirm that CUR-mediated inhibition of miR-3666 to activate the AMPK pathway is a potential alternative for alleviation of hepatic lipid deposition.
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Food Chemistry-X
·
2023
·
IF 6.1
Guangyi Kan,Ye Zi,Li Li,Huan Gong,Jiawei Peng,Xichang Wang,Jian Zhong
Herein, pH-cycle method was explored to prepare curcumin-encapsulated hydrophilic bovine bone gelatin (BBG/Cur) nanoparticle and then the obtained nanoparticle was applied to stabilize fish oil-loaded Pickering emulsion. The nanoparticle had a high encapsulation efficiency (93.9 ± 0.5 %) and loading capacity (9.4 ± 0.1 %) for curcumin. The nanoparticle-stabilized emulsion had higher emulsifying activity index (25.1 ± 0.9 m 2 /g) and lower emulsifying stability index (161.5 ± 18.8 min) than BBG-stabilized emulsion. The pH affected the initial droplet sizes and creaming index values of the Pickering emulsions: pH 11.0 < pH 5.0 ≈ pH 7.0 ≈ pH 9.0 < pH 3.0. Curcumin provided obvious antioxidant effect for the emulsions, which was also dependent on pH. The work suggested pH-cycle method could be used to prepare hydrophobic antioxidant-encapsulated hydrophilic protein nanoparticle. It also provided basic information on the development of protein nanoparticles for Pickering emulsion stabilization.
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International Journal of Nanomedicine
·
2022
·
IF 7.033
Jiangxiu Niu,Ming Yuan,Zhaowei Zhang,Liye Wang,Yanli Fan,Xianghui Liu,Xianming Liu,Huiyuan Ya,Yansong Zhang,Yang Xu
Background The poor skin permeation and deposition of topical therapeutic drugs is a major issue in topical drug delivery, improving this issue is conducive to improving the topical therapeutic effect of drugs. Methods In this study, octadecylamine modified hyaluronic acid (OHA) copolymer was synthesized by amide reaction technique to prepare curcumin (CUR)-loaded micelles (CUR-M) for topical transdermal administration. CUR-M was successfully prepared by dialysis, and the formulation was evaluated for particle size, zeta potential, surface morphology, entrapment effciency (EE%), drug loading (DL), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and the in vitro drug release. Additionally, in vitro skin permeation and retention, in vivo topical analgesic and anti-inflammatory activity, and skin irritation were assessed. Results The mean drug loading (DL), drug entrapment efficiency (EE), hydrodynamic diameter and zeta potential of CUR-M were 8.26%, 90.86%, 165.64 nm and −26.85 mV, respectively. CUR-M was characterized by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR), it was found that there was an interaction between CUR and OHA, and CUR existed in CUR-M in an amorphous form. CUR-M exhibited sustained release in 48 h and good stability at 4 °C for 21days. CUR-M could significantly increase the skin penetration and retention of CUR and had better analgesic and anti-inflammatory activities in vivo when compared with CUR solution. Hematoxylin-eosin staining results revealed that the transdermal penetration mechanism of CUR-M might be related to the hydration of stratum corneum by HA. In addition, CUR-M showed no skin irritation to mouse skin. Conclusion CUR-M might be a promising and safe drug delivery system for the treatment of topical diseases.
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Frontiers in Bioengineering and Biotechnology
·
2022
·
IF 6.064
Jiang Mingyue,Chen Le,Chen Bo,Yu Qinghua,Zhang Xianming,Jing Weihong,Ma Limei,Deng Tao,Yang Zhangyou,Yu Chao
Curcumin (CUR) is a natural bioactive compound that has attracted attention as a “golden molecule” due to its therapeutic properties against several types of tumors. Nonetheless, the antitumor application of CUR is hampered due to its extremely low aqueous solubility and chemical instability. Herein, a novel type of CUR-loaded polymeric micelles with intracellular K+-responsive controlled-release properties is designed and developed. The polymeric micelles are self-assembled by poly (N-isopropylacrylamide-co-acryloylamidobenzo-15-crown-5-co-N, N-dimethylacrylamide)-b-DSPE (PNDB-b-DSPE) block copolymers, and CUR. CUR is successfully loaded into the micelles with a CUR loading content of 6.26 wt%. The proposed CUR-PNDB-DSPE polymeric micelles exhibit a significant CUR release in simulated intracellular fluid due to the formation of 2 : 1 ‘‘sandwich’’ host–guest complexes of 15-crown-5 and K+, which lead to the hydrophilic outer shell of micelles to collapse and the drug to rapidly migrate out of the micelles. In vitro, the B16F10 cell experiment indicates that CUR-PNDB-DSPE micelles exhibit a high cellular uptake and excellent intracellular drug release in response to the intracellular K+ concentration. Moreover, CUR-PNDB-DSPE micelles show high cytotoxicity to B16F10 cells compared to free CUR and CUR-PEG-DSPE micelles. The polymeric micelles with intracellular K+-responsive controlled release properties proposed in this study provide a new strategy for designing novel targeted drug delivery systems for CUR delivery for cancer treatment.
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MATERIALS & DESIGN
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2022
·
IF 9.417
Liangjun Zhang,Haihan Xia,Song Du,Nan Zhao,Xiaoxun Zhang,Qiong Pan,Senlin Xu,Zhicheng He,Zeng Yi,Jin Chai
Hyperinflammation can lead to tissue injury, organ failure, and even fatalities by overproducing proinflammatory cytokines. The long-term safety and outstanding anti-inflammatory ability of natural products have attracted much attention, but the low solubility and bioavailability limit their application. In this study, PGDE was conjugated with aromatic hydroxy groups of curcumin, resveratrol, and quercetin to prepare polyphenolic nano-assemblies. The nano-assemblies showed a comparable capacity for scavenging DPPH and ABTS free radicals with curcumin. The modification not only decreased the cytotoxicity of curcumin but also the anti-inflammation activity was preserved successfully. In vivo tests, NCAs were preferentially located at the inflammatory sites and performed effective therapeutic effects on acute and chronic inflammation models including sepsis, IBD, and liver fibrosis models. The anti-inflammatory activities were primarily realized by suppressing the overproduction of TNF-α, IL-6 and IL-β cytokines, and down-regulating the ROS-related NOX-1 and NOX-4. Additionally, NCAs inhibited the activation of the TGF-α/Smad pathway and decreased the production of α-SMA to alleviate collagen deposition in fibrosis mice. This study described a simple method for preparing nano-assemblies of insoluble polyphenols via the carrier-free self-assembly method, which improved the therapeutic effect on inflammatory diseases and broadened the application field of insoluble natural active polyphenols.
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JOURNAL OF PHARMACEUTICAL SCIENCES
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2022
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IF 3.784
Jiawei Han,Yuanfeng Wei,Luyuan Li,Yutong Song,Zunting Pang,Shuai Qian,Jianjun Zhang,Yuan Gao,Weili Heng
In the previous study, the development of amorphous curcumin (CUR) aimed to enhance the solubility/dissolution of CUR by disrupting its crystal lattice, but it unexpectedly showed a decreased dissolution than its crystalline counterpart on account of gel formation in its dissolution process. Whether such gelation could be eliminated by co-amorphous strategy was answered in this study. Herein, CUR by co-amorphization with chlorogenic acid (CHA) was successfully prepared using quench cooling. The formed co-amorphous material (namely CUR-CHA CM) eliminated the gelation and hence performed superior dissolution performance than crystalline/amorphous CUR. Meanwhile, it exhibited higher physical stability than amorphous CUR during dissolution as well as under long-term/accelerated conditions. To further study the such enhancement mechanism, the internal molecular interactions were investigated for CUR-CHA CM in the solid state as well as in aqueous solution. FTIR and solid-state 13 C NMR spectra confirmed that intermolecular hydrogen bonds formed between CUR and CHA after co-amorphization. Furthermore, the nucleation of CUR was significantly inhibited by CHA in an aqueous solution, thus maintaining the supersaturated dissolution for a long time. The present study offers a feasible strategy to eliminate gelation and enhance stability of amorphous solids by co-amorphization and crystallization inhibition.
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