PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
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2021
·
IF 3.133
Kang Sha,Qianfang Ma,Hanitrarimalala Veroniaina,Xiaole Qi,Jiayi Qin,Zhenghong Wu
Solidification of self-microemulsifying drug delivery systems (SMEDDS) is one of the major trends to promote the transformation of self-microemulsion technology into industrialization. Here, a preliminary curcumin SMEDDS formulation was constructed to improve the druggability of curcumin, through the determination of equilibrium solubility determination, self-emulsifying grading assessment, and pseudo-ternary phase diagrams drafting. Furthermore, the optimal curcumin SMEDDS formulation consisted of 10% Ethyl oleate, 57.82% Cremophor RH 40, and 32.18% Transcutol P was obtained by the simplex lattice design. Besides, curcumin solid self-microemulsifying drug delivery system (S-SMEDDS) was developed by the extrusion and spheronization process to achieve the solidification of SMEDDS. The formulation of curcumin S-SMEDDS pellets was screened by the single factor experiment and the process parameters were investigated using the orthogonal optimization method. Subsequently, curcumin S-SMEDDS pellets were evaluated by apparent morphology characterization, redispersibility study, drug release behavior, and pharmacokinetic evaluation. Results from the pharmacokinetic study in rabbits showed that the AUC0–τ of the curcumin S-SMEDDS pellets and curcumin suspension were 5.91 ± 0.28 µg/mL·h and 2.05 ± 0.04 µg/mL·h, while the relative bioavailability was 289.30%. These studies demonstrated that S-SMEDDS pellets can be a promising strategy for curcumin industrialized outputs.
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JOURNAL OF FOOD PROCESS ENGINEERING
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2020
·Vol. 43
·期 12
·e13556
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IF 1.703
Shenghua He,Sanjiu Zhou,Weiyun Guo,Yonghui Wang,Chunhong Liu,Rongchun Wang,Fugang Xiao
In this study, rapeseed oil bodies (RPOBs) were used to prepare curcumin emulsions (CEs) in order to investigate their stability and gastrointestinal. The results showed that particle size significantly reduced ( p < .05) with increasing RPOBs concentrations from 1.0 to 6.0 wt%. Additionally, CEs showed good stability at pH 2.0–10.0. However, CEs were instable at salt concentration ranging from 100 to 500 mM and at temperatures between 35 and 95°C. CE fat droplet size after 30 min of digestion time exhibited a remarkable increase ( p < .05) compared with other times. Upon exposure to simulated intestinal fluid (SIF) conditions, CEs particle sizes gradually decreased with increasing digestion time. Then, 56% curcumin and 40 μmol/ml free fatty acids were produced from CEs after 180 min digestion time under SIF conditions. Practical applications Our findings indicate that rapeseed oil bodies as a novel carrier can be applied for the delivery-controlled release of lipophilic bioactive compounds from emulsions during gastrointestinal digestion.
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CARBOHYDRATE POLYMERS
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2020
·
IF 7.182
Jun Wang,Leyna G. Liu,Wen-Qiao Jiao,Hua Yang,Jing Liu,Dahai Liu
In order to achieve high loading and efficient delivery of curcumin, phenylboronic acid-conjugated chitosan nanoparticles were prepared by a simple desolvation method. These nanoparticles exhibited a regular spherical shape with the average size about 200−230 nm and narrow size distribution, which were kinetically stable under physiological condition. Due to boronate ester formation between curcumin and phenylboronic acid groups in the nanoparticles, and the hydrogen bonding interactions between curcumin and nanocarriers, curcumin was successfully loaded into the nanoparticles with high drug loading content. These curcumin-loaded nanoparticles showed pH and reactive oxygen species (ROS)-triggered drug release behavior. In vitro cell experiments revealed that the blank nanoparticles were completely nontoxic to cultured cells, and the curcumin-loaded nanoparticles exhibited efficient antitumor efficiency against cancer cells. Moreover, the drug-loaded nanoparticles performed an enhanced growth inhibition in three-dimensional multicellular tumor spheroids. Thus, these nanocarriers would be a promising candidate for curcumin delivery in tumor treatment.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2020
·
IF 5.162
Lihong Fan,Yuqing Lu,Xiao-kun Ouyang,Junhong Ling
Curcumin (Cur) is a natural polyphenol with beneficial biological and pharmacological activities; however, it has limited applications owing to its low solubility and light sensitivity. The protein-polysaccharide complex can effectively embed lipid-soluble drugs to increase their stability and dispensability in aqueous solutions. Soybean protein isolate (Spi) and fucoidan (Fuc) were used as a polymer matrix, and core-shell nanoparticles were prepared to encapsulate Cur via electrostatic interaction under acidic and neutral conditions. The structure of the Spi-Fuc nanoparticles was studied via Fourier-transform infrared spectroscopy, transmission electron microscopy , and scanning electron microscopy. Concurrently, we evaluated the efficacy of the nanoparticles based on stability, drug loading rate, and simulated release. Our results showed that the Spi-Fuc nanoparticles (size, approximately 236.56 nm) had a spherical, core-shell structure and that they could effectively load Cur with an embedding efficiency of >95%; moreover, the system had long-term dispersion stability. Thus, we provide a simple method for Cur delivery, which can also be potentially used for delivering lipid-soluble active ingredients.
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TALANTA
·
2020
·
IF 5.339
Fangzheng Yuan,Xia Wu,Hui Zhang
An intrinsic Eu(III) luminescence phenomenon of Eu(III) complex was found under near-infrared light (NIRL) excitation of xenon lamp, and the maximum excitation wavelength is about twice the excitation wavelength of its Stokes fluorescence. The NIRL excitation fluorescence was mainly originated from second order diffracted light (SODL) excitation. The Eu(III) complex was consist of Eu(III), Gd(III), 2-trifluoroacetylacetone (TTA) and cetyltrimethylammonium bromide (CTAB). Curcumin (Cur) could notably quench the luminescence intensity of the Eu(III) complex. Based on this, a sensitive method for Cur detection was developed. Under optimum conditions, the decrease extent in the fluorescence intensity at 611 nm exhibited a good linear relationship with the Cur concentration in the range of 2.0 × 10 −9 mol/L - 6.0 × 10 −8 mol/L under 746 nm excitation, the limit of detection (LOD, S/N = 3) was 5.2 × 10 −10 mol/L. While, the linear relationship and the LOD of Stokes fluorescence method ( λ ex / λ em = 360/611 nm) were found to be 1.0 × 10 −8 mol/L - 6.0 × 10 −8 mol/L and 2.6 × 10 −9 mol/L, respectively. The former method is superior to the latter one in Cur detection. Both two methods were successfully applied to determine Cur in real samples. The luminescence mechanism of Eu(III) complex under the NIRL excitation and the quenching mechanism of Cur on the Eu(III) fluorescence was also investigated.
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Pharmaceutics
·
2019
·Vol. 11
·期 11
·584
·
IF 4.773
Xiaoxiao Sun,Dongyan Yu,Zhuoyang Ying,Chuqiao Pan,Nan Wang,Fangfang Huang,Junhong Ling,Xiao-kun Ouyang
Curcumin (Cur) has anticancer activities but has poor stability, which can be improved using carrier materials. In this study, chitosan was aminated to increase the number of amino groups on its surface, modified with folic acid (FA), and then made into nanoparticles by ionic crosslinking. Owing to ion interaction, the negatively charged, non-toxic tripolyphosphate (TPP) interacted with the positively charged amino group on the aminated chitosan (AmCS) surface, producing FA-AmCS-TPP nanoparticles, which were then characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared spectrophotometry (FT-IR), and thermogravimetric analysis (TGA). Their small particle size (175.2 ± 0.99 nm) and good surface positive potential (+42.4 mV) are beneficial for carrying antitumor drugs. We subsequently investigated whether coating of Cur by AmCS allows slow drug release by FA-AmCS-TPP nanoparticles in different pH environments, and estimated the Cur loading efficiency (EE-Cur). Our results showed that the cumulative release rate of Cur at 48 h was 56.2%, and that the EE-Cur reached 94.26 ± 0.91% with nanoparticles composed of 0.10 g AmCS, 10.0 mg FA, 10.0 mg TPP, and 15.0 mg Cur. Additionally, cytotoxicity experiments showed that the Cur/FA-AmCS-TPP nanoparticles had good targeting ability for tumor cells. Therefore, the non-toxic targeted composite nanoparticles had potential as a new antitumor agent that can overcome the limitations of Cur.Keywords:aminated chitosan;folic acid;nanoparticles;targeted delivery;curcumin
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JOURNAL OF MOLECULAR STRUCTURE
·
2022
·
IF 3.841
Fangzhou Wen,Peiyuan Li,Ying Zhang,Haiyi Zhong,Hongjun Yan,Wei Su
Carbon quantum dots with good biocompatibility can be used as nanomaterial carriers to improve the bioavailability of curcumin. In this paper, green tea was used as raw material to provide a green synthesis method for preparing carbon dots nanoparticles, and Curcumin was loaded to prepare carbon quantum dots/Curcumin nanocomposites (CQDs/Cur). A series of characterization methods were used to study the morphology and chemical structure of composite nanoparticles. The tea carbon dots had the characteristics of excitation wavelength dependence, salt solution stability and light stability. Finally, the antioxidant activities of CQDs/Cur nanocomposites were investigated by DPPH, ABTS •+ , hydroxyl radical, metal ion chelating and reducing power assays. The compound system not only improved the antioxidant performance of curcumin, but also retained the antibacterial activity of curcumin. These results suggested that tea carbon quantum dots loaded with curcumin had the potential to be developed as natural antioxidants and antibacterial agents.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2012
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IF 2.823
Shili Song,Zhen Wang,Yuhua Qian,Lijie Zhang,Erfeng Luo
Curcumin-loaded alginate beads, which contain different food emulsifiers, have been prepared using CaCl2 as the cross-linking agent. The controlled release of the curcumin from the beads was investigated at room temperature. For calcium alginate/Span-80/Tween-80 (A/S/T) formulations, almost all of the curcumin loaded in the beads was released into the medium within about 20 h, and the release rates could be regulated by changing the concentration of both Tween-80 and Span-80. However, for the systems of calcium alginate/Q-12A/F-18A (A/Q/F), about 60% of the curcumin loaded in the beads was released at the end of experiments. The studies of scanning electron microscopy indicated that the microstructure of the walls of beads could significantly vary with the concentration or type of emulsifiers. The Fourier transform infrared spectral measurements confirmed that the interactions between calcium alginate and polyglycerol fatty acid esters were stronger than that between calcium alginate and Tween-80/Span-80. The results of swelling studies demonstrated that the initial rates of water uptake for A/Q/F beads were higher than that for A/S/T beads. Moreover, the data of release rates were fitted by an empirical equation, which showed that the release mechanism of curcumin from the alginate gels varied with the composition of emulsifiers for the A/S/T systems. This work provides an important insight into the effect of food emulsifiers on the release rates of the curcumin from calcium alginate beads and will be helpful for the application of the systems in controlled release of other hydrophobic drug.
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Nanomaterials
·
2024
·Vol. 14
·期 5
·389
·
IF 4.4
Feng Gao,Wenyu Liang,Qixin Chen,Bairu Chen,Yuchen Liu,Zhibo Liu,Xu Xu,Rongrong Zhu,Liming Cheng
Disordered reactive oxygen/nitrogen species are a common occurrence in various diseases, which usually cause cellular oxidative damage and inflammation. Despite the wide range of applications for biomimetic nanoparticles with antioxidant or anti-inflammatory properties, designs that seamlessly integrate these two abilities with a synergistic effect in a simple manner are seldom reported. In this study, we developed a novel PEI-Mn composite nanoparticle (PM NP) using a chelation method, and the curcumin was loaded onto PM NPs via metal–phenol coordination to form PEI-Mn@curcumin nanoparticles (PMC NPs). PMC NPs possessed excellent dispersibility and cytocompatibility, was engineered to serve as an effective nanozyme, and exhibited specific SOD-like and CAT-like activities. In addition, the incorporation of curcumin granted PMC NPs the ability to effectively suppress the expression of inflammatory cytokines in microglia induced by LPS. As curcumin also has antioxidant properties, it further amplified the synergistic efficiency of ROS scavenging. Significantly, PMC NPs effectively scavenged ROS triggered by H2O2in SIM-A9 microglia cells and Neuro-2a cells. PMC NPs also considerably mitigated DNA and lipid oxidation in Neuro-2a cells and demonstrated an increase in cell viability under various H2O2concentrations. These properties suggest that PMC NPs have significant potential in addressing excessive ROS and inflammation related to neural diseases.Keywords:nanozyme;ROS scavenging;anti-inflammatory;neuroprotective
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LWT-FOOD SCIENCE AND TECHNOLOGY
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2025
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IF 6.6
Limin Wang,Qianfei Jia,Yuan Li,Hui Zhao,Zijian Wu
This study investigated the chitosan (CS)-octenyl succinic anhydride (OSA) starch complex as a stabilizer for Pickering emulsions. The effects of OSA concentration (0.5wt%-2.5wt%) and viscosity (OSA1, OSA2, OSA3) on the stability and physiochemical properties of emulsion were examined. The results showed that CS-OSA with 2.0wt% concentration OSA stabilized emulsion exhibited optimal emulsifying capacity. Contact angle analysis, Fourier transform infrared spectrometer (FTIR) and X-difference diffractometer (XRD) were utilized to explore the stabilized mechanism of CS-OSA on emulsion, results confirmed the CS and OSA interactions, and strong adsorption of CS-OSA particles at the oil-water interface. Furthermore, CS-OSA stabilized emulsion loading curcumin were assessed, results showed that curcumin loaded emulsion exhibited high stability and better antioxidant capacity than free CS during 10-day storage. The overall study offers valuable insights into the utilization of CS-OSA emulsifiers in delivery application for lipophilic bioactive molecules.
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CHINESE JOURNAL OF CHEMISTRY
·
2016
·Vol. 34
·期 7
·657-661
·
IF 1.872
Zhengyi Li,Jinbei Yan,Yue Yin,Zhihui Zhang,Zhiming Wang,Defeng Xu,Xiaoqiang Sun
A simple and nontoxic fluorescent chemosensor of di- O -methyl curcumin has been prepared from curcumin. The sensor exhibited selective and sensitive fluorescent responses toward Al 3+ over a wide range of metal ions, such as Mn 2+ , Ce 3+ , Pt 2+ , Sn 4+ , Hg + , Sb 3+ , K + , Ca 2+ , Mg 2+ , Ba 2+ , Cu 2+ , Ni 2+ , Na + , NH 4 + , Ag + , Pb 2+ , Zn 2+ , Fe 2+ , Fe 3+ , Hg 2+ and Cr 3+ in ethanol/water. The free ligand showed quite weak fluorescence emission due to the isomerization of CO double bond in the excited state, however, after addition of Al 3+ , fluorescence emission results in a prominent fluorescence enhancement.
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Nanoscale
·
2016
·Vol. 8
·期 5
·3040-3048
·
IF 7.76
Xiao Xi Yang,Chun Mei Li,Cheng Zhi Huang
Interactions between nanoparticles and viruses have attracted increasing attention due to the antiviral activity of nanoparticles and the resulting possibility to be employed as biomedical interventions. In this contribution, we developed a very simple route to prepare uniform and stable silver nanoparticles (AgNPs) with antiviral properties by using curcumin, which is a member of the ginger family isolated from rhizomes of the perennial herb Curcuma longa and has a wide range of biological activities like antioxidant, antifungal, antibacterial and anti-inflammatory effects, and acts as reducing and capping agents in this synthetic route. The tissue culture infectious dose (TCID50) assay showed that the curcumin modified silver nanoparticles (cAgNPs) have a highly efficient inhibition effect against respiratory syncytial virus (RSV) infection, giving a decrease of viral titers about two orders of magnitude at the concentration of cAgNPs under which no toxicity was found to the host cells. Mechanism investigations showed that cAgNPs could prevent RSV from infecting the host cells by inactivating the virus directly, indicating that cAgNPs are a novel promising efficient virucide for RSV.
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