Current Drug Delivery
·
2024
·Vol. 22
·期 4
·479-491
·
IF 2.8
Teng Guo,Chenming Zhang,Yuling Chen,Yihan Wu,Zhenda Liu,Yongtai Zhang,Nianping Feng
BackgroundAdding a suitable surfactant can enhance the transdermal permeability of transethosomes while also leveraging its functionality as a functional material. In this study, transethosomes were prepared using D-α-tocopherol acid polyethylene glycol succinate (TPGS) as edge activators for transdermal delivery of curcumin (Cur).MethodsThe TPGS-mediated curcumin-loaded transethosomes (Cur@TES) were prepared and formulated optimally, and the optimized formulations were characterized for their morphology, particle size, entrapment efficiency (EE) and drug loading (DL). The stability and deformability of Cur@TES were investigated, while the transdermal delivery of Cur@TES was investigated through in vitro transdermal assays and fluorescence imaging. A mouse ear swelling model was performed to determine the anti-inflammatory effect of Cur@TES.ResultsCur@TES appeared round or elliptical in shape. The particle size, EE and DL for the optimized formulation were observed as 131.2 ± 7.2 nm, 97.68 ± 2.26%, and 6.58 ± 0.62%, respectively. X-ray diffraction analysis confirmed the formation of disordered structures in the inner core of the vesicles. Moreover, Cur@TES system demonstrated better stability and deformability compared to the curcumin-loaded ethosomes (Cur@ES). In vitro transdermal experiments demonstrated that Cur@TES significantly increased the amount of drug retained in the skin (P<0.05). Fluorescence imaging confirmed that the skin distribution was distinctly enhanced with the delivery by TPGS mediated transethosomes. In addition, Cur@TES showed a significant inhibitory effect on Inflammatory swelling in the mouse ear-swelling model.ConclusionTPGS-mediated transethosomes exhibit significant transdermal advantages and enhanced anti-inflammatory effects, providing a new perspective for the transdermal delivery of curcumin.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2018
·
IF 3.997
Cihui Tian,Sajid Asghar,Yurui Xu,Zhipeng Chen,Mei Zhang,Lin Huang,Junxiu Ye,Qineng Ping,Yanyu Xiao
In this study, a redox-sensitive glioma-targeting micelle system was designed to deliver curcumin (CUR) by conjugating it to hyaluronic acid (HA-s-s-CUR, HSC) via disulfide linkage. The effect of the molecular weight of HA on the physicochemical characteristics of HSC conjugates and their in vitro effects in glioma cells were also explored. These conjugates formed nano-scale micelles (209–926 nm) independently in aqueous solution. The micelles greatly increased the solubility of CUR and improved its stability, which is crucial for harnessing the therapeutic potential of this active molecule. The redox sensitivities of different HSC micelles were measured by using a dynamic light scattering method and in vitro release assay, which showed that the low (50 kDa) and medium molecular weight (200 kDa and 500 kD) HA-based conjugates were sensitive to GSH, whereas higher molecular weights (1000 kDa and 2000 kDa) did not show redox-sensitivity. Increased cytotoxicity and uptake of low and medium molecular weight-modified HSC conjugates by the glioma cells further confirmed that the sensitive micelles are more effective for intracellular drug delivery compared to the high molecular weight-modified HSC conjugates or the plain CUR . In summary, the molecular weight of HA affects the physicochemical attributes of HSC conjugates. Only HSC micelles made with HA molecules less than 500 kDa exhibit redox sensitivity.
研究领域:
药学
·
生物医学工程
✓ 已验证
DOI
高影响因子
FOOD CHEMISTRY
·
2023
·
IF 8.8
Lixin Kang,Qiufang Liang,Qayum Abdul,Arif Rashid,Xiaofeng Ren,Haile Ma
To prevent food spoilage caused by microbial infection, the development of an environmentally friendly antimicrobial preservation material is crucial. Here, the microporous γ-CD-MOFs was utilized to encapsulate the hydrophobic active substance curcumin, resulting in the preparation of a non-toxic antimicrobial material (Cur-CD-MOFs). The results revealed that curcumin encapsulation in Cur-CD-MOFs occurred primarily in the carbonyl group, benzene ring, and enolic side ring of curcumin. The Cur-CD-MOFs had a 100% bactericidal effect on Escherichia coli and Staphylococcus aureus at 4 h and 8 h, and a strong inhibitory effect on aerial mycelium of Penicillium expansum and Botrytis cinerea . Furthermore, the incorporation of Cur-CD-MOFs improved the Pul/Tre film barrier and mechanical properties. The effectiveness of Cur-CD-MOFs-Pul/Tre in retaining fruit freshness was validated using Centennial Seedless grapes. This study confirmed that Cur-CD-MOFs is a promising antibacterial material, and Cur-CD-MOFs-Pul/Tre will be a potent candidate for food preservation.
研究领域:
食品科学
·
生物技术
✓ 已验证
DOI
高影响因子
JOURNAL OF FOOD SCIENCE
·
2021
·Vol. 86
·期 8
·3550-3562
·
IF 3.167
Ying Cai,Jingwei Guan,Wen Wang,Li Wang,Jianyu Su,Liming Fang
Food packaging materials, especially biodegradable polymer composites incorporated with natural antimicrobial agents with excellent antibacterial activities, are in high demand and attracted immense attention. Herein, a polycaprolactone/curcumin@zeolitic imidazolate framework-8 (PCL/Cur@ZIF-8) composite film with enhanced antibacterial activity was developed. Curcumin, a natural photosensitizer, was loaded in the highly porous nanocrystals ZIF-8 to improve its poor water solubility and stability. The integral structure of Cur@ZIF-8 was maintained well in the PCL matrix even at the highest loading of 35% (w/w), and all composite films had good light transmittance at 420–430 nm. The PCL/Cur@ZIF-8 composite films responded to the acidic growth environment of bacteria by releasing zinc ions and curcumin molecules. Furthermore, upon blue light irradiation (420–430 nm, 2.2 mW/cm 2 ), curcumin molecules generated singlet oxygen. With the synergistic effects of zinc ions and singlet oxygen, the composite films exhibited a 99.9% reduction of Escherichia coli and Staphylococcus aureus strains when the amount of Cur@ZIF-8 loading was more than 15% (w/w), as well as a strong anti-adhesion effect on bacteria. Moreover, bacterial resuscitation tests indicated that the composite films exhibited 99.9% reduction in the adhered bacteria population through treatment with photodynamic sterilization. This is the first study presenting that the incorporated curcumin ZIF-8 nanoparticles in the matrix of polymer are pH and light responsive for anti-adhesion of bacteria, which is of great potential application as antibacterial packaging material for the food industry. Practical Application A novel, biodegradable, pH, and light-responsive composite film was developed for antibacterial activity. Natural photosensitizer curcumin was encapsulated in ZIF-8 nanocrystals (Cur@ZIF-8) as the antimicrobial agent. With the synergistic effects of Zn 2+ and singlet oxygen, the composite film exhibited a 99.9% reduction of Escherichia coli and Staphylococcus aureus strains, and a strong anti-adhesion property toward bacteria. This composite film is of great potential application as an antibacterial packaging material that enhances the shelf life of fruits, meat, and so on.
研究领域:
食品科学
·
材料科学
·
生物医学工程
✓ 已验证
DOI
高影响因子
FOOD CHEMISTRY
·
2020
·
IF 6.306
Guohuan Huang,Yuping Yan,Danxia Xu,Jia Wu,Chuanhui Xu,Lihua Fu,Baofeng Lin
Food spoilage is one of the biggest concerns for food safety worldwide. Here, we describe the construction of a carrier for biological agents by chemical combination of porous nanoMOFs and carboxymethylated filter paper (CMFP). When curcumin was encapsulated in nanoMOFs@CMFP, they showed the ability to act as super-long-acting food preserving agents with controllable release of curcumin. Although only 22.3% of curcumin was released into water in 600 h, 65.8% was released into PBS in the same time, and the release into PBS could be tuned by adding citric acid at the time of greatest requirement. Furthermore, the chemical stability of curcumin in nanoMOFs@CMFP was >4.9 times greater than for free curcumin. The outstanding antioxidant and antimicrobial activity of curcumin-loaded nanoMOFs@CMFP paste was demonstrated by prolonging the shelf life of pitayas, which illustrates its potential for development as long-acting and stable preserving paste for use in food preservation.
研究领域:
食品科学
·
材料科学
·
生物学
✓ 已验证
DOI
高影响因子
JOURNAL OF CHEMICAL RESEARCH
·
2024
·
IF 1
Haodong Zhou,Yulan Zhu,Xianfeng Huang
PDE4 is a potential target for treating mental diseases including depression, Alzheimer’s disease and schizophrenia involving in the hydrolysis of cAMP. Curcumin is well-known for its potential as a neuroprotective compound against depression. It was able to inhibit PDE4 with IC50 value in the range of 10 to 20 μM with low selectivity. However, curcumin itself cannot be used clinically because of its poor drug-like properties. Herein, a series of new curcumin derivatives were designed and synthesized. Their PDE4 inhibitory activities and antidepressant effects in vivo were also evaluated. Consequently, most of these curcumin derivatives demonstrated good inhibitory activities against PDE4. Furthermore, compound 4e exhibited the most potent activity at nanomolar level (IC50 value: 23 nM). It also could improve depression-like behaviors induced by chronic stress including sugar forced swimming and water consumption tests in vivo.
研究领域:
药理学
·
神经科学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Chunwei Du,Fan Jiang,Wenxuan Hu,Wupeng Ge,Xiuzhu Yu,Shuang-kui Du
Starch nanoparticles (SNPs) were produced by nanoprecipitation combined with ultrasonication with the use of different starches (corn, potato and sago starch) and used to stabilize Pickering emulsions. The orthogonal experiment was used to optimize preparation conditions of gelatinization pretreatment duration of 30 min, ultrasonic power of 600 W, and ultrasonic time of 40 min. Compared with native starch, the SNPs were spherical in shape and displayed a V -type crystalline structure with low relative crystallinity and higher degree of double-helix. Compared with native starch-Pickering emulsion, the SNP-Pickering emulsion had a smaller droplet size, more uniform distribution, clearer oil/water interface, and higher static stability of droplets. The sago SNP-Pickering emulsion had the great gelatinous structure and emulsion stability. In addition, the SNP-Pickering emulsion had the better loading efficiency and controlled release performance of curcumin . Meanwhile, the bioavailability of curcumin in sago SNP-Pickering emulsion was highest.
研究领域:
食品科学
·
材料科学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2021
·
IF 5.875
Siyu Sun,Xiyou Du,Manfei Fu,Abdur Rauf Khan,Jianbo Ji,Weidong Liu,Guangxi Zhai
In this study, galactosamine-modified poly(ethylene glycol)-poly(lactide) (Gal-PEG-PLA) polymers were synthesized and Gal-PEG-PLA/D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) micelles named as GPP micelles were designed to promote the oral absorption of a hydrophobic drug, curcumin (CUR). CUR-loaded Gal-PEG-PLA/TPGS micelles (CUR@GPP micelles) were fabricated using the thin-film dispersion method. CUR@GPP micelles had a size of about 100 nm, a near-neutral zeta potential , drug loading (DL) of 14.6%, and sustained release properties. GPP micelles with high Gal density (GPP3 micelles) were superior in facilitating uptake in epithelial cells and improving intestinal permeation. In situ intestinal absorption studies suggested that the jejunum and ileum were the best absorption segments in the intestinal tract. Additionally, biodistribution results revealed that GPP3 micelles could be remarkably taken up by the jejunum and ileum. Pharmacokinetics revealed that the maximum plasma concentration (C max ) and the area under the plasma concentration-time curve from 0 to 24 h (AUC 0–24 ) for CUR@GPP3 micelles were both significantly increased, and that the relative bioavailability of CUR@GPP3 micelles to CUR-loaded mPEG-PLA/TPGS micelles (CUR@PP micelles) was 258.8%. Furthermore, CUR-loaded micelles could reduce damage to the liver and intestinal tissues. This study highlights the importance of Gal content in the design of targeting nanocarrier Gal-modified micelles, which have broad prospects for oral delivery of hydrophobic drugs. Therefore, they could serve as a promising candidate for targeted delivery to the liver.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
DOI
高影响因子
Acupuncture and Herbal Medicine
·
2023
·Vol. 3
·期 4
·343
·
IF 0
Liu Rui,Liu Zhongyan,Guo Xueli,Kebebe Dereje,Pi Jiaxin,Guo Pan
Objective: Inhibition of tumor angiogenesis has become a new targeted tumor therapy. In this study, we established a micellar carrier with a tumor neovascularization-targeting effect modified by the neovascularization-targeting peptide NGR. Methods: The targeted polymer poly(ethylene glycol)-b-poly(lactide-co-glycolide) (PEG-PLGA) modified with Asn–Gly–Arg (NGR) peptide was prepared and characterized by 1 H nuclear magnetic resonance and Fourier-transform infrared spectrometry. NGR-PEG-PLGA was used to construct curcumin (Cur)-loaded micelles by the solvent evaporation method. The physicochemical properties of the micelles were also investigated. Additionally, we evaluated the antitumor efficacy of the polymer micelles (PM) using in vitro cytology experiments and in vivo animal studies. Results: The particle size of Cur-NGR-PM was 139.70 ± 2.51 nm, and the drug-loading capacity was 14.37 ± 0.06%. In vitro cytological evaluation showed that NGR-modified micelles showed higher cellular uptake through receptor-mediated endocytosis pathways than did unmodified micelles, leading to the apoptosis of tumor cells. Then, in vivo antitumor experiments showed that the modified micelles significantly inhibited tumor growth and were safe. Conclusions: NGR-modified micelles significantly optimized the therapeutic efficacy of Cur. This strategy offers a viable avenue for cancer treatment. Export
研究领域:
药剂学
·
肿瘤学
·
生物医学工程
·
分子生物学
✓ 已验证
DOI
CARBOHYDRATE POLYMERS
·
2016
·
IF 4.219
Yurui Xu,Sajid Asghar,Liu Yang,Hongying Li,Zhilin Wang,Qineng Ping,Yanyu Xiao
Curcuminoid (Cur) loaded polysaccharide nanoformulations with blood-brain barrier (BBB) penetration and brain targeting properties, based on hyaluronic acid (HA) and chitosan hydrochloride (CSH) (Lf-Cur-PSNPs) were developed as a novel delivery system for malignant glioma. Formulations were investigated for physicochemical characteristics, cytotoxicity, uptake, and BBB penetration. The results showed that Lf M -Cur-PSNPs (concentration of Lf was 0.5 mg/mL) were preferentially taken up by brain capillary endothelial cells than Cur-PSNPs at any time. After crossing the BBB, Lf M -Cur-PSNPs remained largely intact and were more effective in targeting glioma cells (C6). In vivo imaging studies in mice exposed Lf M -PSNPs could effectively permeate BBB and preferentially accumulate in the brain (2.39 times greater than PSNPs). Moreover, PSNPs were detected in brain up to 72 h. This data indicates that Lf-Cur-PSNPs could effectively target and accumulate within the gliomas after enhanced permeation through BBB, thus should be further explored for their potential in CNS maliganancies.
研究领域:
药剂学
·
神经科学
·
肿瘤学
✓ 已验证
DOI
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2013
·
IF 2.906
Yanyu Xiao,Xi Chen,Liu Yang,Xieting Zhu,Lang Zou,Fanfei Meng,Qineng Ping
Curcuminoid, a dietary polyphenolic compound, has poor water solubility and low bioavailability following oral administration. The aim of this study was to develop a formulation of curcuminoid-loaded microemulsion (Cur-ME) to improve its oral bioavailability. The optimized Cur-ME formulation was prepared by using labrafac lipophile WL 1349, cremophor RH 40, and glycerine as the oil phase, the surfactant, and the cosurfactant, respectively. Pharmacokinetics and bioavailability of curcuminoid suspension and Cur-ME were evaluated and compared in rats. Plasma bisdemethoxycurcumin (BDMC), treated as the representing component of curcuminoid, was determined by high-performance liquid chromatography with fluorescence detector. After gavage administration of curcuminoid suspension, the plasma BDMC level was very low, below 5 ng/mL, whereas for Cur-ME, double peak of maximum concentrations were observed. The relative bioavailability of Cur-ME was enhanced in an average of 9.6-fold that of curcuminoid suspension. It was concluded that the bioavailbility of curcuminoid was enhanced greatly by the microemulsion.
研究领域:
药剂学
·
药物代谢动力学
·
生物医学工程
✓ 已验证
DOI
高影响因子
Current Drug Delivery
·
2024
·
IF 2.8
Zhang Ziyi,Tian Jinyuan,Xu Xiaoqing,Shi Wei,Qi Yajuan,Liu Zhanjun
Introduction: Polymer prodrug nanoparticles have become an emerging drug delivery
system in cancer therapy due to their high drug loading. However, their poor drug release and lack of
tumor cell targeting limit their clinical application.
Objective: This study aimed to prepare targeted and reduction-reactive polyprodrug nanocarriers
based on curcumin (CUR) for co-delivery of doxorubicin (DOX), labeled as DOX/HAPCS NPs, and
to investigate their anticancer activity.
Methods: The polymer was synthesized and characterized by chemical method. The drug loading
and drug release behavior of DOX and CUR in polymer nanoparticles were determined. Moreover,
the antitumor effects of polymer nanoparticles were evaluated using an MTT experiment and tumor
inhibition experiment, and the synergistic effect of co-delivered DOX and CUR was explored.
Results: The particle size of DOX/HAPCS NPs was 152.5nm, and the potential was about -26.74
mV. The drug-carrying capacity of DOX and CUR was about 7.56% and 34.75%, respectively, indicating
high drug-carrying capacity and good stability. DOX and CUR released over 90% within 24
hours in the tumor environment. Compared with free DOX, DOX/HAPCS NPs demonstrated significantly
enhanced cell and tumor inhibitory effects (P<0.05) in vivo and in vitro and changed drug
distribution to avoid toxic side effects on normal tissues. The combined index showed that DOX and
CUR showed synergistic anticancer effects at a set ratio.
Conclusion: The prepared reduction-responsive targeted polymer nanomedical DOX/HAPCS NPs
exhibited a synergistic anti-cancer effect, with high drug loading capacity and the ability to release
drugs in proportion, making it a promising polymer nanoparticle drug delivery system.
研究领域:
药剂学
·
肿瘤学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）