ACS Applied Materials & Interfaces
·
2018
·
IF 8.097
Zengjie Fan,Jie Li,Jianli Liu,Hongjing Jiao,Bin Liu
Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease, which can cause endless suffering to the patients and severely impact their normal lives. To treat RA, the drugs in use have many serious side effects, high cost, or only focus on their anti-inflammatory mechanisms without taking joint lubrication into consideration. Therefore, in this study, we aim to construct a novel anti-RA drug composed of hyaluronic acid/curcumin (HA/Cur) nanomicelle to resolve these problems. Characterizations show that Cur is bound to HA by ester linkages and self-assembles to form a spherical nanomicelle with a diameter of around 164 nm under the main driving of the hydrophilic and hydrophobic forces. The nanomicelle enjoys excellent biocompatibility that effectively promotes the proliferation of chondrocytes. When injected to the RA rats, the nanomicelle significantly lowers the edema degree of the arthritic rats compared to other groups; more critically, a dramatic decrease in friction between the surfaces of cartilage around the joints has been found, which protects the cartilage from the RA-induced damage. Additionally, systematic mechanism investigation indicates that the nanomicelle diminishes the expression of related cytokines and vascular endothelial growth factor, finally leading to the excellent performance. The newfound nanomicelle has a potential for clinical practice of RA therapy, which will contribute significantly to alleviating the pain of patients and improving the quality of life for them.
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Food & Function
·
2019
·Vol. 10
·期 6
·3344-3355
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IF 3.241
Yaqiong Pei,Tingyang Ai,Ziyu Deng,Di Wu,Hongshan Liang,David Julian McClements,Bin Li
The impact of phytic acid on lipid digestion and curcumin bioaccessibility in oil-in-water nanoemulsions was investigated using a simulated gastrointestinal tract (GIT). The size, charge, and structural organization of the colloidal particles in the system were measured as the curcumin-loaded emulsions (7 mg curcumin per g lipid) were passed through simulated mouth (pH 6.8, 2 min), stomach (pH 2.5, 2 hours), and small intestine (pH 7.0, 2 hours) stages. After the small intestine stage, the level of free fatty acids (FFAs) generated and the bioaccessibility of curcumin were measured. The total amount of FFAs released significantly decreased with increasing phytic acid level, from 105.7 ± 5.9% (control) to 78.4 ± 6.4% (0.5% phytic acid). Conversely, curcumin bioaccessibility significantly increased from 39.4 ± 3.5% (control) to 74.7 ± 2.6% (0.5% phytic acid). The inverse relationship between lipolysis and curcumin bioaccessibility was ascribed to the impact of phytic acid on droplet flocculation and the level of free calcium ions present, which affected the production of mixed micelles capable of solubilizing the nutraceutical. The knowledge obtained here might prove beneficial for the employment of phytic acid as a multifunctional ingredient that inhibits lipid digestion while boosting nutraceutical bioavailability.
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RSC Advances
·
2015
·Vol. 5
·期 28
·21504-21510
·
IF 3.84
Xiaojuan Zhao,Fengxia Li,Qingyan Zhang,Zengbo Li,Yehong Zhou,Jun Yang,Chuan Dong,Junping Wang,Shaomin Shuang
Mn-doped ZnS quantum dots capped with 3-mercaptopropionic acid (MPA) were synthesized by a facile method in aqueous solution as a ratiometric fluorescent (I590 nm/I458 nm) probe for curcumin. Curcumin caused defect-related fluorescence quenching of the probe at 458 nm, whereas the orange transition emission of the probe at 590 nm changed only negligibly with variations in curcumin concentration. The MPA-assembled Mn-doped ZnS quantum dots were used for the simple, sensitive and non-toxic determination of curcumin. Under the optimized conditions, the response to curcumin was linear in the range 0.16–16.9 μM with a detection limit of 37 nM. The method was successfully applied to the determination of trace amounts of curcumin in urine samples with recoveries of 97.73–109.73%.
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Biomed Research International
·
2013
·
IF 0
Li Lv,Yuanyuan Shen,Min Li,Xiaofen Xu,Mingna Li,Shengrong Guo,Shengtang Huang
A novel 4-arm poly(ethylene glycol)-block-poly(anhydride-esters) amphiphilic copolymer (4-arm PEG-b-PAE) was synthesized by esterization of 4-arm poly(ethylene glycol) and poly(anhydride-esters) which was obtained by melt polycondensation of α-, ω-acetic anhydride terminated poly(L-lactic acid). The obtained 4-arm PEG-b-PAE was characterized by 1H-NMR and gel permeation chromatography. The critical micelle concentration of 4-arm PEG-b-PAE was 2.38 μg/mL. The curcumin-loaded 4-arm PEG-b-PAE micelles were prepared by a solid dispersion method and the drug loading content and encapsulation efficiency of the micelles were 7.0% and 85.2%, respectively. The curcumin-loaded micelles were spherical with a hydrodynamic diameter of 151.9 nm. Curcumin was encapsulated within 4-arm PEG-b-PAE micelles amorphously and released from the micelles, faster in pH 5.0 than pH 7.4, presenting one biphasic drug release pattern with rapid release at the initial stage and slow release later. The hemolysis rate of the curcumin-loaded 4-arm PEG-b-PAE micelles was 3.18%, which was below 5%. The IC50 value of the curcumin-loaded micelles against Hela cells was 10.21 μg/mL, lower than the one of free curcumin (25.90 μg/mL). The cellular uptake of the curcumin-loaded micelles in Hela cell increased in a time-dependent manner. The curcumin-loaded micelles could induce G2/M phase cell cycle arrest and apoptosis of Hela cells.
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Nanoscale
·
2017
·Vol. 9
·期 34
·12533-12542
·
IF 7.367
Cheng Gao,Fan Tang,Guiyi Gong,Jianxiang Zhang,Maggie P. M. Hoi,Simon M. Y. Lee,Ruibing Wang
In order to realize a combination of chemotherapy and selective drug release into tumor cells, novel pH-sensitive prodrugnanoparticles were designed and prepared via the self-assembly of a synthetic amphiphilic macromolecular prodrug for the selective co-delivery of doxorubicin (Dox) and curcumin (Cur). Dox was covalently conjugated to the oxidized sodium alginate through a Schiff base reaction to produce an amphiphilic macromolecular prodrug, and the prodrug was subsequently self-assembled into nanoparticles (Dox-NPs) in an aqueous solution, which were responsive to the acidic environment in tumor cells. Additionally, a second chemotherapeutic agent, Cur, was encapsulated in the core of nanoparticles (Cur–Dox-NPs) via hydrophobic effects, with a significant drug loading capacity. Cur–Dox-NPs exhibited an efficient release of both Dox and Cur in acidic media and further studies of their intracellular uptake and drug release confirmed that Dox-NPs were easily taken up by cells and selectively released the drug into the human breast cancer cell line MCF-7. In vitro cytotoxicity studies of the NPs showed a remarkable efficacy against MCF-7 cell lines, whereas an improved safety profile was observed in the human breast epithelial cell line MCF-10A. Furthermore, in vivo studies in zebrafish further confirmed an efficient absorption of Dox-NPs. In vivo cardiotoxicity experiments on a zebrafish model showed that Dox-NPs exhibited an improved cardiotoxicity profile in comparison with free Dox. This study demonstrated that this novel pH-sensitive prodrug-nanoparticle system may provide a simple and efficient platform for the selective co-delivery of multiple drugs to tumor cells.
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Scientific Reports
·
2016
·Vol. 6
·期 1
·1-14
·
IF 5.228
Liu Dandan,Li Jinyu,Pan Hao,He Fengwei,Liu Zhidong,Wu Qingyin,Bai Chunping,Yu Shihui,Yang Xinggang
The transient precorneal retention time and low penetration capacity into intraocular tissues are the key obstacles that hinder the ophthalmic drug delivery of many therapeutic compounds, especially for drugs with poor solubility and permeability. To break the stalemate, N-acetyl-L-cysteine functionalized chitosan copolymer (CS-NAC), which exhibit marked bioadhesion and permeation enhancing effect, was synthesized. The curcumin encapsulated NLC (CUR-NLC) was produced and optimized followed by surface absorption of CS-NAC. After coating, changed particle size from 50.76 ± 2.21 nm to 88.64 ± 1.25 nm and reversed zeta potential from −20.38 ± 0.39 mV to 22.51 ± 0.34 mV was observed. The in vitro CUR release from NLC was slower than that of CUR-NLC and chitosan hydrochlorides (CH) coated NLC due to the inter and/or intramolecular disulfide formation of thiomers on the surface of nanocarriers. The modification also significantly enhanced transcorneal penetration compared with CH-NLC and the uncoated ones. The effect on bioadhesion and precorneal retention were evaluated by in vivo imaging technique and ocular pharmacokinetics studies revealing that the clearance of the formulations was significantly delayed in the presence of CS-NAC and the effect was positively related to the degree of thiolation. In summary, CS-NAC-NLC presented a series of notable advantages for ophthalmic drug application.
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Biomedical Materials
·
2024
·Vol. 19
·期 2
·025021
·
IF 3.9
Peng Ding,Xiaoyue Ding,Jingyu Li,Wei Guo,Oseweuba Valentine Okoro,Mahta Mirzaei,Yanfang Sun,Guohua Jiang,Amin Shavandi,Lei Nie
The increased demand for improved strategies for wound healing has, in recent years, motivated the development of multifunctional hydrogels with favorable bio-compatibility and antibacterial properties. To this regard, the current study presented the design of a novel self-healing composite hydrogel that could perform as wound dressing for the promotion of wound healing. The composite hydrogels were composed of polyvinyl alcohol (PVA), borax and chitosan functionalized with sialic acid (SA-CS) and curcumin loaded pluronic F127 micelles. The hydrogels were formed through the boronic ester bond formation between PVA, SA-CS and borax under physiological conditions and demonstrated adjustable mechanical properties, gelation kinetics and antibacterial properties. When incubating with NIH3T3 cells, the hydrogels also demonstrated good biocompatibility. These aspects offer a promising foundation for their prospective applications in developing clinical materials for wound healing.
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FOOD HYDROCOLLOIDS
·
2024
·
IF 11
Pu Zheng,Xinru Chen,Chunyang Zhao,Jialong Wang,Jianhong Zhang,Xiong Hu,Wenchao Geng,Qianqian Zhao
The Cyclodextrin (CD) encapsulation technology can significantly enhance the water solubility of Curcumin (CUR) and effectively protect it against chemical degradations. In the current study, a combination of experimental and multi-scale computational approaches was used to investigate the binding mechanism between CUR and β-CDs (β-CD, 2-HP-β-CD, Me-β-CD, and DM-β-CD). Phase solubility studies showed that β-CDs exhibited a strong binding affinity with CUR and significantly enhanced its solubility. SEM, PXRD, DSC, and TG analysis confirmed the formation of inclusion complexes, resulting in the transition of CUR from crystalline to an amorphous state. FTIR, 1 H, and 13 C NMR spectra deduced that CUR may have multiple binding conformations with β-CDs. The rationality of molecular dynamics simulation systems was confirmed by comparing the simulated IR spectrum from quantum mechanics with the experimental IR spectrum. MM-PBSA and umbrella sampling simulation calculated the binding free energy of the CUR/CD inclusion complexes, ranking Me-β-CD > DM-β-CD > 2-HP-β-CD > β-CD, and clarified that van der Waals interaction played a major role in stabilizing the inclusion complexes. RDF analysis confirmed that the release of high-energy water molecules drove the formation of the CUR/CD inclusion complex, and the β-CD substituents affected their exterior hydration layer. Additionally, principal component analysis (PCA) and non-covalent interaction analysis revealed three CUR/CD binding modes: bead-on-string, terminal insertion, and V-shaped-folding. The research strategy adopted here can serve as a paradigm for investigating the encapsulation mechanism of poorly soluble drugs with CDs.
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FOOD CHEMISTRY
·
2024
·
IF 8.5
Shen Long,Meng-Jie Yu,Ran Feng,Han Tao,Bao Zhang
In this study, a novel dextrin-based micelle (OSAD-SH), dual-modified with octenyl succinic anhydride (OSA) and cysteamine, has been developed to address the acid instability issues of micelles modified only by OSA and designed for curcumin delivery. The chemical structure of OSAD-SH was characterized and the physical properties of the micelles were evaluated. Results displayed that OSAD-SH micelles exhibit strong self-assembly properties, appearing as spheres with diameters ranging from 92.41 to 194.20 nm. Blank micelles with good dilution resistance, acid, thermal, and ionic strength stability. The curcumin encapsulated by the micelles is in an amorphous state. In vitro release experiments demonstrated that curcumin released from OSAD-SH micelles exhibits intestinal targeting. The Ritger-Peppas model effectively predicted the release behavior of curcumin, indicating that the release mechanism follows super case-II transport. The OSAD-SH micelle could be a promising nanocarrier for improving the physicochemical properties of curcumin in food fields.
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LWT-FOOD SCIENCE AND TECHNOLOGY
·
2024
·
IF 6
Dehua Wang,Biqian Wei,Yi Zhang,Tongxin Xie,Jing Yu,Yong Xue,Biao Kong,Changhu Xue,Qingjuan Tang
Excessive salt consumption is strongly linked to the chronic diseases development, highlighting the urgent need for effective salt-reduction strategies in food products. However, reducing salt content often compromises both food preservation and flavor. In this study, we hypothesized that curcumin could enhance the flavor perception of sodium chloride while compensating for its antimicrobial effect in reduced-salt applications. To test this, we developed a curcumin/γ-cyclodextrin/sodium chloride complex (IC), using γ-cyclodextrin as a carrier, and evaluated its antimicrobial and flavor-enhancing properties. The complex's formation was confirmed through various analytical techniques. Results from electronic tongue and sensory evaluations demonstrated that the IC enhanced the perception of saltiness and imparted unique aromatic characteristics compared to standard sodium chloride. GC-IMS analysis identified key aroma contributors, such as aldehydes and alcohols. Additionally, antimicrobial tests revealed that the IC efficiently mediated the sono/photodynamic inactivation of Shewanella putrefaciens and Vibrio parahaemolyticus . In summary, the IC offers a multifunctional approach, enhancing flavor, reducing salt, and enabling antimicrobial activity, while promoting practical uses of sono/photodynamic technology in low-sodium foods.
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Journal of Biomedical Nanotechnology
·
2017
·Vol. 13
·期 12
·1631-1646
·
IF 4.521
Wang Jiao,Liu Qiang,Yang Linnan,Xia Xiaofei,Zhu Rongrong,Chen Shengguang,Wang Mei,Cheng Liming,Wu Xianzheng,Wang Shilong
Cervical cancer is the fourth most common cancer in women worldwide, and existing treatments cause severe side effects and great burdens. Thus, the development of safe, inexpensive therapeutic agents is necessary. Curcumin (Cur), a well-known natural product, exerts promising anti-cancer
activities against various cancer types. However, its therapeutic efficacy is severely restrained due to rapid degradation, poor aqueous solubility, and low bioavailability. The objective of this study was to investigate the therapeutic potential of novel curcumin-loaded TPGS/F127/P123 mixed
polymeric micelles (Cur@NPT100) for cervical cancer treatment. The Cur@NPT100 exhibited an average size of approximately 19 nm, a zeta potential of around –4 mV, a drug loading of 8.18 ± 0.36%, and an encapsulation efficiency of 79.38 ± 4.65%. Unlike free Cur, Cur@NPT100
are readily dispersed in aqueous medium, showing enhanced stability and a sustained release profile over a 6-day period. In vitro cell culture experiments revealed that TPGS/F127/P123 mixed polymeric micelles (NPT100) based nanocarriers substantially promoted the selective cellular
uptake of Cur into HeLa cells rather than by non-cancerous NIH3T3 cells, inducing higher cytotoxicity and greater apoptosis and significantly increasing the percentage of cells arrested at the G2/M phase of the cell cycle. Additionally, the Cur@NPT100 facilitated more Cur accumulation in the
mitochondria and decreased the mitochondrial membrane potential. In addition, western blot assays demonstrated that Cur@NPT100 were more potent than free Cur at activating the mitochondria-mediated apoptosis pathway. In vivo results further confirmed that Cur@NPT100 exhibited a much higher
antitumor efficacy than free Cur and had excellent biocompatibility. In conclusion, Cur@NPT100 might be an effective therapeutic agent for cervical cancer.
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ACS Applied Materials & Interfaces
·
2024
·
IF 8.3
Xianmou Fan,Jun Huang,Wanjun Zhang,Zhihong Su,Jin Li,Zeyong Wu,Peihua Zhang
The treatment of diabetic chronic wounds is still faced with great challenges, mainly due to wound infection, excessive inflammation, and peripheral vascular disease in the wound area. Therefore, it is of great importance to develop a novel multifunctional hydrogel with high efficiency to accelerate diabetic wound healing. Curcumin (Cur), a Chinese herbal, has shown great potential in enhancing the healing of diabetic chronic wounds because of its immunomodulatory and pro-angiogenic properties. However, its low aqueous solubility, poor bioavailability, and chemical instability have limited its clinical applications. To address these current bottlenecks, novel poly(vinyl alcohol) (PVA)–chitosan (CS)/sodium alginate (SA)–Cur (PCSA) hydrogels were prepared for the first time, and they demonstrated all of the above intriguing performances by the Michael addition reaction of CS and Cur. PCSA hydrogels show multiple dynamic bonds, which possess strong mechanical properties (tensile stress: ∼0.980 MPa; toughness: ∼258.45 kJ/m3; and compressive strength: ∼7.38 MPa at strain of 80%). These intriguing performances provided an optimal microenvironment for cell migration and proliferation and also promoted the growth of blood vessels, leading to early angiogenesis. Importantly, the experimental results demonstrated that PCSA hydrogels can effectively transform pro-inflammatory M1 macrophages into anti-inflammatory M2 macrophages without the need for additional ingredients in vitro. Benefiting from these characteristics, a full-thickness diabetic wound in a rat model demonstrated that PCSA hydrogels can effectively accelerate wound healing via ROS-scavenging, downregulation of IL-1β, and upregulation of CD31 expression, resulting in angiogenesis and collagen deposition. This strategy not only provides a simple and safe Cur-based hydrogel for diabetic wound healing but also highlights the significant potential for the development of high-performance biomaterials for promoting diabetic wound healing using traditional Chinese medicine.
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