Nanomaterials
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2018
·Vol. 8
·期 3
·167
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IF 3.504
Muyang Yang,Lixia Yu,Ruiwei Guo,Anjie Dong,Cunguo Lin,Jianhua Zhang
Synergistic combination therapy by integrating chemotherapeutics and chemosensitizers into nanoparticles has demonstrated great potential to reduce side effects, overcome multidrug resistance (MDR), and thus improve therapeutic efficacy. However, with regard to the nanocarriers for multidrug codelivery, it remains a strong challenge to maintain design simplicity, while incorporating the desirable multifunctionalities, such as coloaded high payloads, targeted delivery, hemodynamic stability, and also to ensure low drug leakage before reaching the tumor site, but simultaneously the corelease of drugs in the same cancer cell. Herein, we developed a facile modular coassembly approach to construct an all-in-one multifunctional multidrug delivery system for the synergistic codelivery of doxorubicin (DOX, chemotherapeutic agent) and curcumin (CUR, MDR modulator). The acid-cleavable PEGylated polymeric prodrug (DOX-h-PCEC), tumor cell-specific targeting peptide (CRGDK-PEG-PCL), and natural chemosensitizer (CUR) were ratiometrically assembled into in one single nanocarrier (CUR/DOX-h[email protected]NPs). The resulting CUR/DOX-h[email protected]NPs exhibited several desirable characteristics, such as efficient and ratiometric drug loading, high hemodynamic stability and low drug leakage, tumor intracellular acid-triggered cleavage, and subsequent intracellular simultaneous drug corelease, which are expected to maximize a synergistic effect of chemotherapy and chemosensitization. Collectively, the multifunctional nanocarrier is feasible for the creation of a robust nanoplatform for targeted multidrug codelivery and efficient MDR modulation.Keywords:modular coassemble;synergistic codelivery;polymeric prodrug;stimulisensitive release;biocompatibility
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2018
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IF 3.412
Shengfeng Peng,Ziling Li,Liqiang Zou,Wei Liu,Chengmei Liu,David Julian McClements
There is great interest in developing colloidal delivery systems to enhance the water solubility and oral bioavailability of curcumin, which is a hydrophobic nutraceutical claimed to have several health benefits. In this study, a natural emulsifier was used to form sophorolipid-coated curcumin nanoparticles. The curcumin was loaded into sophorolipid micelles using a pH-driven mechanism based on the decrease in curcumin solubility at lower pH values. The sophorolipid-coated curcumin nanoparticles formed using this mechanism were relatively small (61 nm) and negatively charged (−41 mV). The nanoparticles also had a relatively high encapsulation efficiency (82%) and loading capacity (14%) for curcumin, which was present in an amorphous state. Both in vitro and in vivo studies showed that the curcumin nanoparticles had an appreciably higher bioavailability than that of free curcumin crystals (2.7–3.6-fold), which was mainly attributed to their higher bioaccessibility. These results may facilitate the development of natural colloidal systems that enhance the oral bioavailability and bioactivity of curcumin in food, dietary supplements, and pharmaceutical products.
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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2024
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IF 3.1
Hualu Wu,Saili Xie,Xiaohai Chen,Hailun Xia,Yuxin Shen,Ren-ai Xu,Wei Tan,Ruanjuan Zhan
Fuzuloparib is a novel orally bioactive poly-ADP-ribose polymerase inhibitor (PARPi), which was approved by the Chinese Regulatory Agency (CRA) in 2020 for the treatment of platinum-sensitive recurrent ovarian, fallopian tube, and primary peritoneal cancers. This study firstly presents a rapid and accurate ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for analyzing the levels of fuzuloparib and its major metabolite (SHR165202), and to investigate drug-drug interaction between fuzuloparib and curcumin in vitro and in vivo studies. After protein precipitation with acetonitrile, mobile phase consisted of acetonitrile and 0.1 % formic acid with a gradient elution was used to successfully separate fuzuloparib, SHR165202 and talazoparib (internal standard, IS). The results indicated that fuzuloparib and SHR165202 had good linearity over the calibration range of 2–50 ng/mL and 1–20 ng/mL, respectively. The precision, accuracy, stability, matrix effect, and extraction recovery required for methodological validation all complied with the requirements of the Bioanalytical Method Validation Guidelines. In vitro microsome incubation experiments, curcumin exhibited inhibitory effect on fuzuloparib in both rat liver microsomes (RLM) and human liver microsomes (HLM) with half-maximal inhibitory concentration (IC 50 ) value of 10.54 μM and 47.64 μM, respectively, and the corresponding mechanism was non-competitive. Furthermore, the inhibitory mechanism of curcumin on fuzuloparib was validated through molecular docking. In pharmacokinetic experiments in rats, curcumin significantly altered the plasma exposure of fuzuloparib, resulting in significant increases in AUC (0-t) and C max of fuzuloparib and a significant decrease in CL z/F . Moreover, the metabolite SHR165202 showed significant increases in AUC (0-t) , AUC (0-∞) , T max and C max and a significant decrease in CL z/F . This further supports the notion that curcumin could inhibit the metabolism of fuzuloparib. Therefore, when co-administering fuzuloparib and curcumin in clinic, it is recommended to monitor plasma levels of fuzuloparib and pay close attention to adverse effects. If necessary, the dose of fuzuloparib needs to be reduced.
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Scientific Reports
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2024
·Vol. 14
·期 1
·1-15
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IF 3.8
Chen Linli,Guo Xiaojing,Lin Wen,Huang Yingying,Zhuang Suling,Li Qianfeng,Xu Jianhua,Ye Shengnan
Lytic induction therapy was devised to selectively combat malignancies associated with Epstein–Barr virus (EBV) by triggering viral reactivation from latency. At present, the major challenges of lytic induction therapy are to maximize reactivating efficiencies and meanwhile minimize infectious virion production. C210, a novel curcumin derivative with potent Hsp90 inhibitory activity, was explored for EBV-reactivating and virion-producing effects in EBV-positive nasopharyngeal carcinoma (NPC) and gastric carcinoma (GC) cell lines. And the molecular mechanisms underlying these effects were determined. Follow C210 treatment, EBV lytic RNAs and proteins were upregulated, but infectious virions were not produced. Knockdown of heat shock protein 90 (Hsp90) induced expression of lytic RNAs and proteins, and diminished C210-driven EBV lytic induction. Pretreatment with an X box binding protein 1 (XBP1) inhibitor reduced C210-induced EBV lytic RNA. Furthermore, we demonstrated that C210 inhibited the binding of Hsp90 with its clients, signal transducer and activator of transcription 3 (STAT3) and xeroderma pigmentosum group B-complementing protein (XPB), which subsequently promoted their proteasomal degradation. Degradation of STAT3 by C210 enhanced the EBV-reactivating and anticancer capacity of suberoylanilide hydroxamic acid (SAHA). Depletion of XPB blocked SAHA-induced expression of late viral genes and production of infectious virions. These results elucidate a novel Hsp90 inhibitor targeting EBV lytic phase and extend the research on lytic induction strategy, which may offer reference value in the treatment of EBV-positive malignancies.
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INDUSTRIAL CROPS AND PRODUCTS
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2024
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IF 5.6
Wei Tan,Yin Tian,Chunlong Zuo,Yongli Zhang,Xiaoyu Liu,Ziyin Ye,Lu Bai,Yuanlin Ren,Xiaohui Liu
With the depletion of petrochemical resources and the escalating severity of white pollution, replacing petrochemical resources with bio-based resources aligns with sustainable development strategy. In this work, a novel biomass flame retardant (PCDAC) derived from curcumin was intercalated into expandable graphite (EG) to construct an intrinsically intumescent flame retardant system (EG@PCDAC), which was then melt blended with polylactic acid (PLA) to fabricate flame retardant, anti-dripping and smoke suppressive PLA composite (PLA/EG@PCDAC). The residual char of PLA/EG@PCDAC was 14.27 wt% under N 2 atmosphere, while reaching UL-94 V–0 rating. Furthermore, the peak heat release rate and total heat release of PLA/EG@PCDAC were reduced by 46.95 % and 19.02 % compared with original PLA, and the total smoke production and peak smoke production rate also decreased by 20.74 % and 72.09 %, respectively. This work offered green and feasible inspiration for exploring biomass flame retardants and renewable PLA-based functional materials.
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COLLOIDS AND SURFACES B-BIOINTERFACES
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2024
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IF 5.4
Mengyi Zhang,Ju Liang,Ying Liang,Xuening Li,Wenlan Wu
In the realm of intracellular drug delivery, overcoming the barrier of endosomal entrapment stands as a critical factor influencing the effectiveness of nanodrug delivery systems. This study focuses on the synthesis of an acid-sensitive fatty acid derivative called imidazole-stearic acid (IM-SA). Leveraging the proton sponge effect attributed to imidazole groups, IM-SA was anticipated to play a pivotal role in facilitating endosomal escape. Integrated into the lipid core of solid lipid nanoparticles (SLNs), IM-SA was paired with hyaluronic acid (HA) coating on the surface of SLNs loading with curcumin (CUR). The presence of IM-SA and HA endowed HA-IM-SLNs@CUR with dual functionalities, enabling the promotion of endosomal escape, and specifical targeting of liver cancer. HA-IM-SLNs@CUR exhibited a particle size of ~228 nm, with impressive encapsulation efficiencies (EE) of 87.5% ± 2.3% for CUR. Drugs exhibit significant pH sensitive release behavior. Cellular experiments showed that HA-IM-SLN@CUR exhibits enhanced drug delivery capability. The incorporation of IM-SA significantly improved the endosomal escape of HA-IM-SLN@CUR, facilitating accelerated intracellular drug release and increasing intracellular drug concentration, exhibiting excellent growth inhibitory effects on HepG2 cells. Animal experiments revealed a 3.4-fold increase in CUR uptake at the tumor site with HA-IM-SLNs@CUR over the free CUR, demonstrating remarkable tumor homing potential with the tumor growth inhibition rate of 97.2%. These findings indicated the significant promise of HA-IM-SLNs@CUR in the realm of cancer drug delivery.
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FOOD HYDROCOLLOIDS
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2025
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IF 12.4
Liwei Zhao,Taijiao Xiang,Jiaoyu Wang,Ziming Xu,Danli Wang,Tinglan Yuan,Ling Li,Haina Yuan,Gongshuai Song,Mengna Zhang,Jinyan Gong
Protein-based emulsion gels with transglutaminase (TG)-catalyzed crosslinking exhibit great potential for delivering hydrophobic bioactive substances. However, effects of TG-catalyzed crosslinking modifications under different reaction times on the structural and textural characterization, stability, and delivery behavior have rarely been reported. This study investigated the effect of TG-catalyzed crosslinking on the physicochemical, structural, and functional properties of β-lactoglobulin (β-LG) - camellia oil (CAO) emulsion gels by cold-gelation under different reaction times. Results revealed that prolonged reaction times could improve the formation of intramolecular and intermolecular covalent bonds between lysine and glutamine residues. Rheological analysis showed an increase in both the storage modulus (G’) and loss modulus (G’’), indicating enhanced the gel elasticity and stability. Furthermore, the oxidative stability, the water-holding capacity, and functional stability (freeze-thaw, UV-light, thermal, and salt stability) of the emulsion gels were enhanced by the TG-catalyzed crosslinking. In the in vitro digestion process, the encapsulation efficiency and bioaccessibility of curcumin (Cur) were enhanced in the TG-catalyzed crosslinking β-LG-CAO emulsion gel system when the reaction time exceeded 3 h. The dense gel structure, improved stability, and great Cur delivery behavior of the emulsion gel could be formed by TG-catalyzed crosslinking at 4 h. This study benefited the encapsulation and release behavior of Cur in oil-in-water emulsions and the application in food and nutraceutical products.
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Polymers
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2025
·Vol. 17
·期 7
·830
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IF 4.9
Hashimu Juma,Cunshi Zhao,Qingbo Wang,Yunfeng Guo,Xinyan Fan,Wuming Fan,Linlin Zhao,Jiayi Sun,Dong Wang,Yonggui Wang
Polybutylene adipate-terephthalate (PBAT) offers a convincing ecological alternative to the traditional fossil-based plastics due to its biodegradability and robust mechanical properties. The objective of this study is to develop PBAT-based bio-composite films through incorporating functionalized cellulose nanocrystals (CNC) and curcumin (CUR). In order to improve the interfacial compatibility with the PBAT matrix and co-doping with CUR, CNC was modified using dodecyl succinic anhydride (DxCNC). In this ternary bio-composite system, CUR functioned as a bio-based antioxidant and antimicrobial agent. The presence of CUR also provides excellent UV-shielding properties, whereas the DxCNC effectively enhances the controlled release of CUR. The synergistic effect between DxCNC and CUR in boosting antimicrobial properties, with the inhibition values forE. coliandS. aureusreached 1.82 log CFU/cm2and 2.12 log CFU/cm2, respectively. These findings indicate DxCNC/CUR/PBAT ternary composite films as a promising material for eco-friendly packaging products.
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CHEMICAL ENGINEERING JOURNAL
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2025
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IF 13.2
Xiaolei Guo,Lin Yang,Nan Sheng,Xirui Long,Zhen Li,Feng Luo,Jiehua Li,Hong Tan
Oral ulcers severely affect the patient’s mood, diet, and language activities and are mainly treated by topical administration of a patch. However, the currently commercially available patches have a limited treatment effect because of the short action time in the oral cavity. In this study, we present a novel adhesive patch made from trifunctional polycaprolactone crosslinked waterborne polyurethane (CDCPU) loaded with curcumin for treating oral ulcers. The long-chain triol cross-linking points in the polyurethane can limit water entry, while stabilizing the curcumin loading in the emulsion. Meanwhile, the interaction between curcumin and polyurethane improved the anti-swelling (swelling rate of 37.7 ± 4.9 %), water resistance (water absorption rate of 66.6 ± 5.6 %), and mechanical properties of the patch. The adhesion strength of the CDCPU patch to porcine oral mucosa and skin was 11.3 ± 1.7 kPa and 14.7 ± 2.5 kPa, respectively. The addition of curcumin provides the CDCPU patch with effective antibacterial and antioxidant functions. Moreover, the CDCPU patch was effective in promoting mucosal epithelialization and ulcer healing in a rat oral ulcer model. The development of this adhesive patch provides a new strategy for the treatment of oral ulcers.
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RSC Advances
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2017
·Vol. 7
·期 42
·25978-25986
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IF 3.108
Ce Cheng,Shengfeng Peng,Ziling Li,Liqiang Zou,Wei Liu,Chengmei Liu
The poor water solubility and bioavailability of curcumin can be improved by encapsulating it into liposomes. However, the existing encapsulation technologies, such as the thin film method and the ethanol injection method, are complex and require the use of organic solvents. In this study, an organic solvent-free and easily scalable encapsulation technique was studied by utilizing the pH-dependent solubility properties of curcumin. Phospholipid was dissolved in water to form liposomes. Curcumin was deprotonated and dissolved under alkaline conditions and then encapsulated into the liposomes after acidification. Morphological observation and X-ray diffraction analysis confirmed that curcumin liposomes had been successfully prepared. Curcumin liposomes prepared by the pH-driven method were stable during storage. During in vitro digestion, curcumin liposomes prepared by the pH-driven method showed similar bioaccessibility to those prepared by the thin film method and higher bioaccessibility than those prepared by the ethanol injection method. The pH-driven method, which is organic solvent-free and easily scalable for industrial production, is thus a promising method for the preparation of curcumin liposomes.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2024
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IF 7.7
Fang Zhu,Yanru Hu,Lihui Meng,Wenchao Li,Bin Xie,Zilin Zhou,Shuojie Cui,Meng Wang,Youfa Wang,Zebin Chen,Qingzhi Wu
The preparation of biodegradable and antibacterial hydrogels has important clinical value. In this work, a novel strategy has been developed to prepare degradable hydrogel dressings without chemical crosslinking agent using methacrylate anhydride (MA)-modified amylopectin (APMA) and polyacrylamide (PAM). After introducing C C bonds, APMA/PAM hydrogels can be formed under light irradiation. This strategy improves the gelling ability of AP and degradation properties of the hydrogel by avoiding the addition of crosslinking agent. The degradation rate of APMA/PAM hydrogel is 74.04 ± 0.69 % within 12 weeks, while that of APMA/PAM hydrogel containing crosslinking agent is only 38.5 ± 0.1 %. The APMA/PAM hydrogel loading curcumin (Cur) (APMA/PAM-Cur) exhibits high antibacterial efficiency of 98.29 ± 0.41 % and 97.18 ± 0.81 % against S. aureus and E. coli , respectively, with light irradiation. Animal experiments show that the APMA/PAM-Cur hydrogel reduces the infiltration of inflammatory factors, increases the density of collagen, and makes the newly formed granulation tissue thicker and tighter. This study not only proves the promising potential of the APMA/PAM-Cur hydrogel as degradable and antibacterial wound dressing for clinical treatment, but also provides a new strategy for developing low-cost, degradable, and antibacterial wound dressings and reducing antibiotic abuse and environmental pollution caused by medical waste.
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MOLECULAR NEUROBIOLOGY
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2024
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IF 4.6
Chen Jinglin,Wei Yumeng,Li Nong,Pi Chao,Zhao Wenmei,Zhong Yueting,Li Wen,Shen Hongping,Yang Yan,Zheng Wenwu,Jiang Jun,Liu Zerong,Liu Kezhi,Zhao Ling
The aim of this study was to develop a novel antidepressant with high activity. Based on the findings of molecular docking, eight novel curcumin analogues were evaluated in vitro to check for antidepressant efficacy. Among them, CACN136 had the strongest antidepressant effect. Firstly, CACN136 had a stronger 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonate) radical ion scavenging ability (IC 50 : 17.500 ± 0.267 μg/mL) compared to ascorbic acid (IC 50 : 38.858 ± 0.263 μg/mL) and curcumin (27.189 ± 0.192 μg/mL). Secondly, only CACN136 demonstrated clear protective effects on cells damaged by glutamate and oxidative stress at all concentrations. Finally, only CACN136 showed ASP + inhibition and was more effective than fluoxetine hydrochloride (FLU) at low concentrations. To further confirm the antidepressant effect of CACN136 in vivo, the CUMS model was established. Following 28 days of oral administration of CUMS mice, CACN136 increased the central area residence time in the open-field test, significantly increased the sucrose preference rate in the sucrose preference test ( P < 0.001) and significantly reduced the immobility period in the tail suspension test ( P < 0.0001), all of which were more effective than those of FLU. Subsequent research indicated that the antidepressant properties of CACN136 were linked to a decrease in the metabolism of 5-HT and the modulation of oxidative stress levels in vivo. In particular, the activation of the Keap1-Nrf2/BDNF-TrkB signaling pathway by CACN136 resulted in elevated levels of antioxidant enzymes, enhancing the antioxidant capability in mice subjected to CUMS. In conclusion, CACN136 has the potential to treat depression and could be an effective antidepressant. Graphical Abstract
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