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FOOD CHEMISTRY · 2023 · IF 8.8

Nanoparticle encapsulation using self-assembly abietic acid to improve oral bioavailability of curcumin

Ying Han,Hua Zhang,Haitian Zhao,Shiyao Fu,Ruiling Li,Zhili Wang,Yangxin Wang,Weihong Lu,Xin Yang

This research constructed composite nanoparticles ( NP s) using abietic acid ( AA ) as a carrier for significantly enhancing the bioavailability of curcumin ( CCM ). CCM -loaded AA NPs were synthesized using a low-energy microemulsification method, and the obtained nanoparticles had a spherical morphology with an average diameter of 458.66 nm, a narrow size distribution and a negative surface charge of −19.13 mV. The encapsulation efficiency of CCM was 17.98 %, while its solubility was 20-fold that of free curcumin. FITR, UV, and MD revealed hydrogen bonds and hydrophobic forces between AA and CCM . The   in-vitro   release profile showed sustainable release of CCM in simulated gastric and intestinal fluids up to 2 h at 37 °C. In cellular studies, CCM -loaded AA NPs with the same CCM concentration exhibited greater bioaccessibility and bioavailability than free CCM . These data suggested a possible utilization of AA NPs in improving water solubility, bioavailability and activity of lipophilic bioactive food factors.

CAS / MDL: 3326-32-7
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CARBOHYDRATE POLYMERS · 2023 · IF 11.2

Biodegradable cellulose/curcumin films with Janus structure for food packaging and freshness monitoring

Weiquan Wang,Xuewen Liu,Fan Guo,Yuxuan Yu,Jinqing Lu,Yiling Li,Qiaoyun Cheng,Jinping Peng,Goubin Yu

The development of renewable, hydrophobic, and biodegradable intelligent packaging materials as an alternative to petroleum-based plastic products has become a new research focus in recent years, but remains a challenge. Herein, regenerated cellulose/curcumin composite films were fabricated by dispersing hydrophobic curcumin uniformly in a hydrophilic cellulose matrix using an aqueous alkali/urea solvent based on the pH-driven principle of curcumin. In addition, a unilateral hydrophobic modification was carried out using chemical vapor deposition of methyltrichlorosilane to obtain Janus structure. The composite films exhibited high transparency in the visible light spectrum , excellent antioxidation, thermal stability , mechanical strength , gas barrier properties, and antibacterial activity . Furthermore, the films demonstrated the capability to lower the overall levels of volatile basic nitrogen in stored fish. The color of the films shifted from a pale yellow to a reddish-brown over time during storage. The composite films can be completely degraded after approximately 98 days in soil with an average environmental temperature of 29 °C. This work provided a facile strategy to prepare biodegradable cellulose/curcumin films with Janus structure as packaging materials which could preserve the freshness of food products while offering visual monitor of their freshness in real-time.

CAS / MDL: 1310-66-3
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PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY · 2021 · IF 3.133

Formulation optimization of solid self-microemulsifying pellets for enhanced oral bioavailability of curcumin

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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CARBOHYDRATE POLYMERS · 2020 · IF 7.182

Phenylboronic acid-conjugated chitosan nanoparticles for high loading and efficient delivery of curcumin

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 · 2020 · IF 5.162

Development and characterization of soybean protein isolate and fucoidan nanoparticles for curcumin encapsulation

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.

CAS / MDL: 458-37-7 7558-79-4
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JOURNAL OF FOOD PROCESS ENGINEERING · 2020 ·Vol. 43 ·期 12 ·e13556 · IF 1.703

Investigation of curcumin emulsion stability and gastrointestinal digestion prepared with rapeseed oil body

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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TALANTA · 2020 · IF 5.339

Luminescence of Eu (III) complex under near-infrared light excitation for curcumin detection

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.

CAS / MDL: 7365-45-9 326-91-0
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2019 · IF 2.606

Mucus-penetrating polymeric nanoparticles for oral delivery of curcumin to inflamed colon tissue

Xin Zhou,Yao Liu,Yamei Huang,Ya Ma,Jun Lv,Bo Xiao

Oral nanotherapeutics have been proven to have great potential in the treatment of ulcerative colitis (UC). However, their therapeutic efficacies are mainly restricted by the lack of mucus-penetrating capacity. To overcome this obstacle, we functionalized the surface of curcumin (CUR)-loaded polymeric nanoparticles (NPs) with various amounts of pluronic F127 (PF127). The obtained NPs (NPs-I, NPs-II, NPs-III and NPs-IV) had hydrodynamic particle sizes around 250  nm with highly monodisperse size distributions, negatively charged surfaces and constant CUR release properties. It was found that the functionalization with PF127 notably improved the mucus-penetrating ability of NPs. Further cell experiments revealed that they showed negative cytotoxicities, and PF127-functionalized NPs (NPs-II, NPs-III and NPs-IV) yielded remarkably higher internalization rates of CUR in macrophages as compared to NPs without PF127 modification (NPs-I). Interestingly, NPs-III exhibited notably stronger capacity to decrease the secretion of TNF-α from macrophages when they were compared with other NPs. Finally, mouse experiments demonstrated that NPs-III achieved the best therapeutic efficacy against UC among all the tested NPs. Our results clearly suggest that PF127-functionalized polymeric NPs with desirable compositional proportions are promising and efficient nanotherapeutics for UC therapy.

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Pharmaceutics · 2019 ·Vol. 11 ·期 11 ·584 · IF 4.773

Fabrication of Ion-Crosslinking Aminochitosan Nanoparticles for Encapsulation and Slow Release of Curcumin

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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COLLOIDS AND SURFACES B-BIOINTERFACES · 2019 · IF 3.973

Improvement on stability, loading capacity and sustained release of rhamnolipids modified curcumin liposomes

Ce Cheng,Zhihua Wu,David Julian McClements,Liqiang Zou,Shengfeng Peng,Wei Zhou,Wei Liu

A novel cholesterol-free curcumin delivery system was fabricated by rhamnolipids modified liposomes (RL-Lps). The incorporation of the rhamnolipids increased the sphericity, reduced the size, and decreased the polydispersity of the liposomes compared with pure liposomes (Lps). Analysis of the environmental stability of the RL-Lps showed they have good long-term stability over a wide range of pH (2–3 and 5–8), ionic strengths (0–200 mM), and accelerated centrifugal conditions. The curcumin-loaded rhamnolipids modified liposomes (Cur-RL-Lps) could be prepared with a relatively high loading efficiency (LE > 90%) and loading capacity (LC > 3.5%). The thermal and photochemical stability of the curcumin was improved after encapsulation in the Cur-RL-Lps. In vitro release studies indicated that the sustained release of the curcumin was prolonged when rhamnolipids were incorporated into the liposomes. This study shows that rhamnolipids have great potential for liposomal delivery system suitable for utilization in functional foods, dietary supplements, and pharmaceutical preparations.

CAS / MDL: 458-37-7
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JOURNAL OF NON-CRYSTALLINE SOLIDS · 2018 · IF 2.488

Preparation, characterization, release and antioxidant activity of curcumin-loaded amorphous calcium phosphate nanoparticles

Xia Guo,Wenfeng Li,Heping Wang,Yan-Ying Fan,Huifang Wang,Xianghua Gao,Baolong Niu,Xuechen Gong

In the study, amorphous calcium phosphate (ACP) nanoparticles were prepared by the coprecipitation method to optimize release profile of curcumin (Cur) and avoid burst releases, which were used to overcome the weakness of Cur, such as poor chemical stability and bioavailability. To find the best preparation condition, the influence of reaction concentration, temperature, time and pH on crystal phase of the samples was investigated by XRD and FTIR. The results showed that amorphous calcium phosphate (ACP) was obtained, when pH value and the concentration of PO 4 3− were 8 and 0.024 mM, prepared at 30 °C for 10 min. In vitro drug release assay, ACP nanoparticles showed high loading capacity of Cur and favorable pH-responsive drug release properties. Furthermore, the Cur-load ACP nanoparticles showed an excellent ability to scavenge free radical and damage A549 cells, resulting in a high antioxidant properties and low cell viability. Therefore, the as-prepared nanoparticles have promising applications in the food and biomedical fields.

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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2019 · IF 4.784

Mesenchymal stem cells-curcumin loaded chitosan nanoparticles hybrid vectors for tumor-tropic therapy

Menglu Xu,Sajid Asghar,Shuang Dai,Yajing Wang,Shanshan Feng,Liang Jin,Feng Shao,Yanyu Xiao

The combination of controlled release technology and targeted drug delivery has become a promising strategy for cancer therapy. In this study, cell-nanoparticle hybrid vector was constructed using mesenchymal stem cells as the targeting cellular carrier and biotinylated chitosan polymer nanoparticles as the drug depot. Drug-loaded nanoparticles (hydrodynamic size =377.0 ± 14.6 nm and zeta potential = 9.6 ± 1.9 mV) were prepared by encapsulating hydrophobic model drug curcumin into biotinylated chitosan polymer. The biotin-modified nanoparticles were anchored on biotinylated mesenchymal stem cells surface by biotin-avidin binding, achieving an upload of 54.73 ± 3.95 pg/cell. The anchorage of nanoparticles on mesenchymal stem cells had no effect on their viability and homing property. Biotin-avidin binding lasted over 48 h, which could be sufficient for cell-directed tumor-tropic delivery. The in vitro and in vivo anti-tumor results advocate that cell-nanoparticle hybrid vector could prove beneficial in pulmonary melanoma metastasis therapy.

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