查找使用阿拉丁产品的科研文献

Enhancing stability of curcumin-loaded casein nanoparticles by adding liposomal nanoparticles

Meiqi Liu,Shengfeng Peng,David Julian McClements,Lingli Chen,Suyun Lin,Wenjun Wang

Curcumin (Cur) is a natural polyphenol found in turmeric. Its application as a functional ingredient in foods, supplements, and pharmaceuticals is dramatically limited due to its poor stability, water solubility, and bioavailability. The purpose of this research was to enhance the performance of curcumin using advanced encapsulation technologies. Curcumin-loaded casein nanoparticles (CCNP) were prepared using the pH-driven method, and then different concentrations of liposomes (LP) were added to assess their impact on the stability of this delivery system. Then, CCNP, curcumin liposome nanoparticles (CLP), and the optimal ratio of CCNP/LP complexes were selected for thermal and storage stability studies. Their formation mechanism was studied by atomic force microscopy (AFM), isothermal titration calorimetry (ITC), and Fourier transform infrared (FTIR) methods. Furthermore, the impact of pH and salt (NaCl) on their stability was also investigated. The results show that LP can adsorb onto the surfaces of CCNP through hydrogen bonding and electrostatic attractive interactions at certain concentrations, which reduces the surface hydrophobicity of the nanoparticles, thereby improving their resistance to environmental stresses. This study provides information that can be used to improve the bioavailability of curcumin.

Microfluidic Formulation of Curcumin-Loaded Multiresponsive Gelatin Nanoparticles for Anticancer Therapy

Yu Xia,Ruicheng Xu,Siyuan Ye,Jiaxuan Yan,Piyush Kumar,Peng Zhang,Xiubo Zhao

Current anticancer research shows that a combination of multiple treatment methods can greatly improve the killing of tumor cells. Using the latest microfluidic swirl mixer technology, combined with chemotherapy and photothermal-ablation therapy, we developed multiresponsive targeted antitumor nanoparticles (NPs) made of folate-functionalized gelatin NPs under 200 nm in size and with encapsulated CuS NPs, Fe3O4 NPs, and curcumin (Cur). By exploring gelatin’s structure, adjusting its concentration and pH, and fine-tuning the fluid dynamics in the microfluidic device, the best preparation conditions were obtained for gelatin NPs with an average particle size of 90 ± 7 nm. The comparative targeting of the drug delivery system (DDS) was demonstrated on lung adenocarcinoma A549 cells (low level of folate receptors) and breast adenocarcinoma MCF-7 cells (high level of folate receptors). Folic acid helps achieve targeting and accurate delivery of NPs to the MCF-7 tumor cells. The synergistic photothermal ablation and curcumin’s anticancer activity are achieved through infrared light irradiation (980 nm), while Fe3O4 is guided with an external magnetic field to target gelatin NPs and accelerate the uptake of drugs, thus efficiently killing tumor cells. The method described in this work is simple, easy to repeat, and has great potential to be scaled up for industrial production and subsequent clinical use.

Chitosan Nanoparticles for Pulmonary Delivery of Curcumin/Nintedanib to Treat Pulmonary Fibrosis

Mengya Jin,Jinming Liu,Mengliu Shao,Shaoqin He,Yue He,Qingliang Yang,Gensheng Yang

Background/Objective Pulmonary fibrosis is a chronic, progressive lung disease with a high mortality rate. Currently, the treatment options for IPF involve the oral administration of nintedanib (NDNB); however, these therapies are hampered by low oral bioavailability. This study aimed to develop chitosan-based nanoparticles for pulmonary delivery to enhance the therapeutic effects of curcumin (Cur) and NDNB.Methods We successfully prepared and optimized Cur-loaded chitosan nanoparticles (Cur/CS-VES NPs) and NDNB-loaded chitosan nanoparticles (NDNB/CS-PGA NPs) through a standardized process. In vitro, Calu-3 and HFL1 cells were treated to evaluate the biocompatibility of chitosan nanocarrier materials and the antifibrotic activity of drug-loaded nanoparticles, respectively. In vivo, the bleomycin-induced rat models of pulmonary fibrosis were established to study the efficacy of chitosan nanoparticles.Results In vitro experiments indicated that the drug-loaded chitosan nanoparticles exhibited good stability and low cytotoxicity. In vivo pharmacodynamic studies revealed that, compared with oral administration of Cur or NDNB alone, the pulmonary delivery of Cur/CS-VES NPs and NDNB/CS-PGA NPs effectively inhibited the progression of pulmonary fibrosis, improved lung function, reduced levels of inflammatory factors, and mitigated pathological lesions in the lungs. These findings suggest that chitosan-based nano-particles have promising potential as pulmonary inhalation agents for the treatment of pulmonary fibrosis.Conclusion These findings highlight the great potential of chitosan-based nanoparticles as a therapeutic strategy for treating IPF and related pulmonary fibrosis with pulmonary delivery pathways.

Formation of Curdlan–Curcumin helically structured nanogels for targeted anti-inflammatory nanotherapy

Menghe Li,Qunjie Chen,Ru Yang,Yifei Wang,Qiuying Liu,Chaoxi Wu

Curdlan possesses intrinsic macrophage-binding ability, making it a promising platform for targeted drug delivery. However, constructing curdlan–drug complexes with well-defined structures and predictable biological functions remains challenging due to difficulties in controlling curdlan conformations. In this study, we developed a self-assembling nanogel system composed of low-molecular-weight curdlan (LCD) and curcumin. Molecular dynamics simulations and circular dichroism analyses revealed two interaction modes—curcumin bound to the triple-helix surface and encapsulated within the single-helix core—which together drive the spontaneous formation of stable LCD–curcumin nanogels. FTIR, DSC, SEM, and DLS characterizations confirmed their structural integrity and preserved helical organization. Cell-based evaluations showed that the nanogels mitigated curcumin cytotoxicity, enhanced its anti-inflammatory activity, and promoted uptake by RAW264.7 macrophages. Studies in a mouse model of ulcerative colitis demonstrated improved curcumin bioavailability, stronger therapeutic effects, and good systemic safety. Overall, these results indicate that LCD–curcumin nanogels possess controlled helical structures and potent anti-inflammatory properties, highlighting their potential as an effective nanomedicine for inflammatory disorders.

Selective Targeting of Cancer Cells by Oxidative Vulnerabilities with Novel Curcumin Analogs

Pignanelli Christopher,Ma Dennis,Noel Megan,Ropat Jesse,Mansour Fadi,Curran Colin,Pupulin Simon,Larocque Kristen,Wu Jianzhang,Liang Guang,Wang Yi,Pandey Siyaram

Recently, research has focused on targeting the oxidative and metabolic vulnerabilities in cancer cells. Natural compounds like curcumin that target such susceptibilities have failed further clinical advancements due to the poor stability and bioavailability as well as the need of high effective doses. We have synthesized and evaluated the anti-cancer activity of several monocarbonyl analogs of curcumin. Interestingly, two novel analogs (Compound A and I) in comparison to curcumin, have increased chemical stability and have greater anti-cancer activity in a variety of human cancer cells, including triple-negative, inflammatory breast cancer cells. In particular, the generation of reactive oxygen species was selective to cancer cells and occurred upstream of mitochondrial collapse and execution of apoptosis. Furthermore, Compound A in combination with another cancer-selective/pro-oxidant, piperlongumine, caused an enhanced anti-cancer effect. Most importantly, Compound A was well tolerated by mice and was effective in inhibiting the growth of human triple-negative breast cancer and leukemia xenografts in vivo when administered intraperitoneally. Thus, exploiting oxidative vulnerabilities in cancer cells could be a selective and efficacious means to eradicate malignant cells as demonstrated by the curcumin analogs presented in this report with high therapeutic potential.

Uptake enhancement of curcumin encapsulated into phosphatidylcholine-shielding micelles by cancer cells

Lei Huang,Mengtan Cai,Xiaoxiong Xie,Yuanwei Chen,Xianglin Luo

Curcumin liposomes prepared with milk fat globule membrane phospholipids and soybean lecithin

Hong-Hao Jin,Qun Lu,Jian-Guo Jiang

Using thin film ultrasonic dispersion method, the curcumin liposomes were prepared with milk fat globule membrane (MFGM) phospholipids and soybean lecithins, respectively, to compare the characteristics and stability of the 2 curcumin liposomes. The processing parameters of curcumin liposomes were investigated to evaluate their effects on the encapsulation efficiency. Curcumin liposomes were characterized in terms of size distribution, ζ-potential, and in vitro release behavior, and then their storage stability under various conditions was evaluated. The curcumin liposomes prepared with MFGM phospholipids had an encapsulation efficiency of about 74%, an average particle size of 212.3   nm, and a ζ-potential of −48.60   mV. The MFGM liposomes showed higher encapsulation efficiency, smaller particle size, higher absolute value of ζ-potential, and slower in vitro release than soybean liposomes. The retention rate of liposomal curcumin was significantly higher than that of free curcumin. The stability of the 2 liposomes under different pH was almost the same, but MFGM liposomes displayed a slightly higher stability than soybean liposomes under the conditions of Fe 3+ , light, temperature, oxygen, and relative humidity. In conclusion, MFGM phospholipids have potential advantages in the manufacture of curcumin liposomes used in food systems.

Delivering curcumin and gemcitabine in one nanoparticle platform for colon cancer therapy

Manhong Tan,Jia Luo,Ying Tian

As gemcitabine and curcumin have different targets in colon cancer cells, combination of them may bring benefits. Here, curcumin and gemcitabine were formulated into a biodegradable polymer platform for combination therapy for treatment of colon cancer. In doing so, a FDA approved biodegradable polymer mPEG-PLA (methoxyl-polyethylen glycol-block-polylactide) was chosen as a drug carrier. At first, a mPEG-PLA/Gem conjugate was designed. Thereafter, simply using this drug conjugate to encapsulate curcumin, polymeric micelles loaded with both curcumin and gemcitabine were obtained. Varying the feed ratio of the two drugs, a series of micelles with different ratios of curcumin and gemcitabine could be prepared. The as-prepared dual drug loaded nanoparticles showed spherical structures with mean diameters ranging from 118 nm to 149 nm by DLS. In vitro, M(Cur/Gem) almost showed greater synergy than free combination of curcumin/gemcitabine. In vivo, better antitumor effect and lower systemic toxicity of M(Cur/Gem) were observed on a murine xenograft model. The present study provides the possibility of combining curcumin and gemcitabine in a nanoparticle formulation, and translation of this combination may bring benefits for future clinical use.

Galactosamine-modified PEG-PLA/TPGS micelles for the oral delivery of curcumin

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.

Identification of Curcumin Targets in the Brain of Epileptic Mice Using DARTS

Ninan Zhang,Ruifan Lin,Honglin Xu,Xianghong Jing,Hongwei Zhou,Xiaoxiao Wen,Qi Xie

Curcumin, a compound derived from turmeric, is traditionally utilized in East Asian medicine for treating various health conditions, including epilepsy. Despite its involvement in numerous cellular signaling pathways, the specific mechanisms and targets of curcumin in epilepsy treatment have remained unclear. Our study focused on identifying the primary targets and functional pathways of curcumin in the brains of epileptic mice. Using drug affinity responsive target stabilization (DARTS) and affinity chromatography, we identified key targets in the mouse brain, revealing 232 and 70 potential curcumin targets, respectively. Bioinformatics analysis revealed a strong association of these proteins with focal adhesions and cytoskeletal components. Further experiments using DARTS, along with immunofluorescence staining and cell migration assays, confirmed curcumin’s ability to regulate the dynamics of focal adhesions and influence cell migration. This study not only advances our understanding of curcumin’s role in epilepsy treatment but also serves as a model for identifying therapeutic targets in neurological disorders.

Oral Administration of Metal-Phenolic-Inspired Curcumin Self-Assemblies for Colitis Alleviation

Xiaojuan Chen,Weiyi Sun,Bin Zhou,Bin Li,Hongshan Liang

Natural bioactive compounds hold promise for ulcerative colitis (UC) but are limited by their poor bioavailability and efficacy. Herein, we propose an interdisciplinary strategy termed “natural bioactive compound-nanotechnology-multipronged modulation” to develop an oral, biocompatible nanoparticle system (CTAl NPs) via a self-assembly strategy. Curcumin (Cur) was successfully encapsulated within a tannic acid (TA) and Al3+ coordination network through hydrogen bonding, π–π stacking, and coordination interactions. The resulting CTAl NPs confer therapeutic benefits through three synergistic mechanisms, including potent anti-inflammatory and antioxidant activities, restoration of immune homeostasis, and reinforcement of the intestinal barrier. These effects stem from the complementary functionalities of each component: TA–Al3+ coordination confers mucosal adhesion and immune modulation, while Cur contributes intrinsic anti-inflammatory activity. This tricomponent system demonstrates enhanced efficacy, offering a facile, safe, and efficient approach for UC management and broader insight into treating inflammation-related disorders.

Curcumin Cocrystals with Bipyridyl-like Coformers: Crystal Structures, Characterization, and Enhanced Dissolution

Jun-Feng Hong,Qian-Hua Fu,Xue-Jie Qi,Xi Wang

Curcumin (Cur) exhibits broad pharmacological activities, but its clinical application is limited by the extremely low solubility. Cocrystallization has emerged as an effective approach to improve physicochemical properties of drugs without altering their chemical structure and intrinsic bioactivity. The Cur cocrystal with 4,4′-bipyridine (Bpy) has demonstrated enhanced solubility facilitated by weaker O–H···N hydrogen bonds, in contrast to the O–H···O bonds formed with hydroxyl coformers (CCFs). Herein, three Bpy-analogous CCFs, 1,2-bis(4-pyridyl)ethane (Bpa), 1,2-bis(4-pyridyl)ethylene (Bpe), and 1-(4-pyridyl)piperazine (Pyp), were selected to construct novel cocrystals with Cur, which were successfully synthesized and thoroughly characterized by single-crystal X-ray diffraction and complementary analytical techniques. Structural analysis revealed that all three cocrystals form similar 1D chains via O–H···N hydrogen bonds between Cur and the CCFs. Powder dissolution studies revealed that all cocrystals present “spring-and-parachute” profiles, with Cur–Bpa and Cur–Pyp exhibiting enhanced solubility, whereas Cur–Bpe showed unexpectedly reduced equilibrium solubility. Their different dissolution behaviors are rationalized by lattice energy (as reflected in melting point) and CCF basicity.