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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2023 · IF 4.4

Yellow-emitting carbon dots as fluorescent sensors for the rapid determination of curcumin

Shen Zhang,Jinjia Bao,Ling Lv,Yongjie Bai,Yiming Zhang,Yaofang Zhang

The non-standard use of curcumin could cause some adverse drug reactions, such as diarrhea, nausea and skin allergies. Thus, the curcumin determination was fundamental to disease treatment and prevention. Herein, a facile and efficient fluorescent probe was developed based on carbon dots, which was prepared through hydrothermal method (o-phenylenediamine and N-isopropylacrylamide as the reaction raw materials). Characteristics of the as-fabricated carbon dots (NCDs) were studied through some analysis techniques, such as UV–vis absorption spectroscopy, transmission electron microscopy, Fourier transform infrared instrument, X-ray photoelectron spectroscopy and fluorescence spectrophotometer. Fluorescence quenching phenomenon could be observed after addition of curcumin. This as-prepared fluorescent probe displayed a significant response for the determination of curcumin with a satisfactorily lower detection limit of 0.017 μM and a considerable linear range of 0.5–50 μM compared to reported literatures. Because of the preeminent repeatability and anti-jamming capability, the as-developed CDs suggested mighty potentiality for actual applications of curcumin detection in real samples and temperature sensing.

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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2023 · IF 5.8

Dissolvable hybrid microneedle patch for efficient delivery of curcumin to reduce intraocular inflammation

Hui Shi,Shuo Huai,Huiling Wei,Ying Xu,Lei Lei,Hao Chen,Xingyi Li,Huixiang Ma

Intraocular inflammation seriously impairs vision, and the effectiveness of intraocular drug delivery is hampered by various physiological barriers, such as the corneal barrier. In this paper, we present a simple approach to fabricating a dissolvable hybrid microneedles (MNs) patch for the efficient delivery of curcumin to treat intraocular inflammatory disorders. Water-insoluble curcumin was first encapsulated into polymeric micelles with high anti-inflammatory capacities, and then were combined with hyaluronic acid (HA) to create a dissolvable hybrid MNs patch using a simple micromolding method. Curcumin was amorphously dispersed within the MNs patch as indicated by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) analyses. According to an in vitro drug release study, the proposed MNs patch provided sustainable drug release over 8 h. Following its in vivo topical application, the MNs patch demonstrated an extended pre-corneal retention time over 3.5 h and exhibited great ocular biocompatibility . Additionally, such MNs patch could reversibly penetrate the corneal epithelium, generating an array of microchannels on the corneal surface, thereby increasing ocular bioavailability. Of greater significance, the use of MNs patch demonstrated the improved therapeutic effectiveness in treating endotoxin-induced uveitis (EIU) in a rabbit model compared to curcumin eye drops via a significant reduction in the infiltration of inflammatory cells such as CD45 + leukocytes and CD68 + macrophages. Overall, the topical application of the MNs patch as an efficient ocular drug delivery system could potentially serve as a promising approach for treating different types of intraocular disorders.

CAS / MDL: 458-37-7
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Pharmaceutics · 2023 ·Vol. 15 ·期 5 ·1341 · IF 5.4

Pickering Emulsions Enhance Oral Bioavailability of Curcumin Nanocrystals: The Effect of Oil Types

Yuze Sheng,Qin Yu,Yanping Huang,Quangang Zhu,Zhongjian Chen,Wei Wu,Tao Yi,Yi Lu

Nanocrystals (NCs) have the potential to enhance the oral bioavailability of Class IV drugs in the Biopharmaceutical Classification System (BCS) due to the absorption of the intact crystals. The performance is compromised by the dissolution of NCs. Drug NCs have recently been adopted as solid emulsifiers to prepare nanocrystal self-stabilized Pickering emulsions (NCSSPEs). They are advantageous in high drug loading and low side effects due to the specific drug loading mode and the absence of chemical surfactants. More importantly, NCSSPEs may further enhance the oral bioavailability of drug NCs by impeding their dissolution. This is especially true for BCS IV drugs. In this study, curcumin (CUR), a typical BCS IV drug, was adopted to prepare CUR-NCs stabilized Pickering emulsions using either indigestible (isopropyl palmitate, IPP) or digestible (soybean oil, SO) oils, i.e., IPP-PEs and SO-PEs. The optimized formulations were spheric with CUR-NCs adsorbed on the water/oil interface. The CUR concentration in the formulation reached 20 mg/mL, which was far beyond the solubility of CUR in IPP (158.06 ± 3.44 μg/g) or SO (124.19 ± 2.40 μg/g). Moreover, the Pickering emulsions enhanced the oral bioavailability of CUR-NCs, being 172.85% for IPP-PEs and 152.07% for SO-PEs. The digestibility of the oil phase affected the amounts of CUR-NCs that remained intact in lipolysis and, thus, the oral bioavailability. In conclusion, converting NCs into Pickering emulsions provides a novel strategy to enhance the oral bioavailability of CUR and BCS IV drugs.Keywords:curcumin;nanocrystals;Pickering emulsions;oral bioavailability;BCS IV;lipolysis

CAS / MDL: 8049-47-6
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E-POLYMERS · 2023 ·Vol. 23 ·期 1 · IF 3.7

Melt-blended PLA/curcumin-cross-linked polyurethane film for enhanced UV-shielding ability

Xuya Fu,Tao Zhang,Wenshuo Zhang,Yuye Zhong,Shuliang Fang,Guannan Wang,Ying Li,Yajun Deng,Xinghai Liu,Houbin Li

Biomass films with ultraviolet (UV)-shielding ability have attracted considerable attention. Curcumin was introduced into castor oil-based polyurethane (CCPU) as a chain extender, which was melt with polylactic acid (PLA) as a reinforcement to obtain biomass UV-shielding film. The excellent UV absorption and antioxidant qualities of curcumin contributed to the impressive UV-shielding capacity (97.6% UV radiation absorption) and antioxidant (51% free radical scavenging) of PLA/CCPU-20 film. In the scanning electron microscopic images of film fracture, the mixing of CCPU elastomer into the PLA matrix caused the blend films to exhibit significant toughening fracture characteristics compared to the pure PLA film. The excellent thermal stability, low water swelling degree, and low water solubility of PLA/CCPU blend films were maintained after CCPU was added to the PLA matrix. Therefore, the PLA/CCPU blend films can be considered as a potential packaging material because of its favorable UV-shielding properties and film stability. Graphical abstract Schematic for the preparation of the PLA/CCPU blend films.

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CARBOHYDRATE POLYMERS · 2023 · IF 11.2

Preparation and characterization of curcumin/chitosan conjugate as an efficient photodynamic antibacterial agent

Lingyu Zhao,Xiaowei Ding,Imran Mahmood Khan,Lin Yue,Yin Zhang,Zhouping Wang

Curcumin (Cur) is a natural pigment with excellent biological activity. The poor stability and insolubility of Cur in water severely limit its application. Therefore, to overcome these dilemmas which are big hindrances in their application, a novel derivative (COCS-Cur) was prepared by the esterification reaction of carboxylated chitosan (COCS) and Cur. The structure and properties of conjugate were determined through a series of characterizations. The derivatives had excellent solubility as well as stability. In addition, antioxidant and photodynamic antibacterial experiments proved that COCS-Cur had the excellent free radical scavenging ability and photodynamic antibacterial activity . The derivatives presented a better antibacterial effect on Staphylococcus aureus ( S. aureus ) than Escherichia coli ( E. coli ). Noteworthy, the COCS-Cur derivatives showed no obvious toxicity which makes them a stronger contender and potential antimicrobial agent or functional nutrient for application in the food industry.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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International Journal of Nanomedicine · 2023 · IF 8

Cyclic hexapeptide-conjugated nanoparticles enhance curcumin delivery to glioma tumor cells and tissue

Xuemei Zhang,Xuejuan Li,Hongchen Hua,Aiping Wang,Wanhui Liu,Youxin Li,Fenghua Fu,Yanan Shi,Kaoxiang Sun

Glioma has one of the highest mortality rates among primary brain tumors. The clinical treatment for glioma is very difficult due to its infiltration and specific growth locations. To achieve improved drug delivery to a brain tumor, we report the preparation and in vitro and in vivo evaluation of curcumin nanoparticles (Cur-NPs). The cyclic hexapeptide c(RGDf(N-me) VK)-C (cHP) has increased affinity for cells that overexpress integrins and was designed to target Cur-NPs to tumors. Functional polyethyleneglycol-modified poly(d,l-lactide-co-glycolide) (PEG-PLGA) conjugated to cHP was synthesized, and targeted Cur-NPs were prepared using a self-assembly nanoprecipitation process. The physicochemical properties and the in vitro cytotoxicity, accuracy, and penetration capabilities of Cur-NPs targeting cells with high levels of integrin expression were investigated. The in vivo targeting and penetration capabilities of the NPs were also evaluated against glioma in rats using in vivo imaging equipment. The results showed that the in vitro cytotoxicity of the targeted cHP-modified curcumin nanoparticles (cHP/Cur-NPs) was higher than that of either free curcumin or non-targeted Cur-NPs due to the superior ability of the cHP/Cur-NPs to target tumor cells. The targeted cHP/Cur-NPs, c(RGDf(N-me)VK)-C-modified Cur-NPs, exhibited improved binding, uptake, and penetration abilities than non-targeting NPs for glioma cells, cell spheres, and glioma tissue. In conclusion, c(RGDf(N-me)VK)-C can serve as an effective targeting ligand, and cHP/Cur-NPs can be exploited as a potential drug delivery system for targeting gliomas.

CAS / MDL: 298-93-1
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International Journal of Nanomedicine · 2023 · IF 8

Dual targeting curcumin loaded alendronate-hyaluronan- octadecanoic acid micelles for improving osteosarcoma therapy

Yanhai Xi,Tingwang Jiang,Yinglan Yu,Jiangmin Yu,Mintao Xue,Ning Xu,Jiankun Wen,Weiheng Wang,Hailong He,Yan Shen,Daquan Chen,Xiaojian Ye,Thomas J Webster

Introduction Curcumin (CUR) is a general ingredient of traditional Chinese medicine, which has potential antitumor effects. However, its use clinically has been limited due to its low aqueous solubility and bioavailability. In order to improve the therapeutic effect of CUR on osteosarcoma (i.e., bone cancer), a multifunctional micelle was developed here by combining active bone accumulating ability with tumor CD44 targeting capacity.Methods The CUR loaded micelles were self-assembled by using alendronate-hyaluronic acid-octadecanoic acid (ALN-HA-C18) as an amphiphilic material. The obtained micelles were characterized for size and drug loading. In addition, the in vitro release behavior of CUR was investigated under PBS (pH 5.7) medium containing 1% Tween 80 at 37℃. Furthermore, an hydroxyapatite (the major inorganic component of bone) affinity experiment was studied. In vitro antitumor activity was evaluated. Finally, the anti-tumor efficiency was studied.Results The size and drug loading of the CUR loaded ALN-HA-C18 micelles were about 118 ± 3.6 nm and 6 ± 1.2%, respectively. CUR was released from the ALN-HA-C18 micelles in a sustained manner after 12 h. The hydroxyapatite affinity experiment indicated that CUR loaded ALN-HA-C18 micelles exhibited a high affinity to bone. CUR loaded ALN-HA-C18 micelles exhibited much higher cytotoxic activity against MG-63 cells compared to free CUR. Finally, CUR loaded ALN-HA-C18 micelles effectively delayed anti-tumor growth properties in osteosarcoma bearing mice as compared with free CUR.Conclusion The present study suggested that ALN-HA-C18 is a novel promising micelle for osteosarcoma targeting and delivery of the hydrophobic anticancer drug CUR.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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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 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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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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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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JOURNAL OF APPLIED POLYMER SCIENCE · 2017 ·Vol. 135 ·期 15 ·46127 · IF 1.86

PMMA@SCNC composite microspheres prepared from pickering emulsion template as curcumin delivery carriers

Hongxia Liu,Changbing Zhou,Xinyue Liu,Yang Xu,Simin Geng,Yunhua Chen,Chun Wei,Chuanbai Yu

We demonstrate a facile route to prepare novel composite microspheres based on Pickering emulsion template stabilized by cellulose nanocrystals prepared from sisal fiber (SCNCs). The oil phase of the Pickering emulsions contains hydrophobic drug curcumin and poly(methyl methacrylate) (PMMA). Curcumin loaded PMMA composite microspheres coated by SCNCs (Cur-loaded PMMA@SCNC CMs) were obtained after the evaporation of dichloromethane. The structure and morphology of CMs were characterized by polarized optical microscope (POM), confocal laser scanning microscope, scanning electric microscope, and Fourier transform infrared spectroscopy. The stability and release kinetics of curcumin were evaluated based on spectrophotometric measurements. Overall, these results show that Cur-loaded PMMA@SCNC CMs display long-term photostability and good encapsulating ability for curcumin. This work offers an effective route of preparing new functional microsphere for the delivery of bioactive compounds. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2018 , 135 , 46127.

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