查找使用阿拉丁产品的科研文献

Ultrasound-responsive osteopontin-targeted liposomes Co-delivering curcumin and perfluoro-n-pentane for atherosclerosis therapy

Qingfeng Luo,Yuyi Deng,Qiyuan Yang,Nanxin Zhao,Can Wang,Xingsheng Li

Osteopontin (OPN), highly expressed in foam cells, serves as a hallmark of atherosclerotic plaques and a potential target for site-specific drug delivery. In this study, we developed OPN-targeted liposomes (OPN LIP) co-loaded with curcumin and perfluoro-n-pentane (PFP) to enhance therapeutic efficacy against atherosclerosis. The liposomes exhibited uniform particle size, colloidal stability, favorable biocompatibility, and minimal cytotoxicity. In vitro experiments demonstrated efficient and time-dependent cellular uptake by ox-LDL–stimulated RAW264.7 foam cells. Upon exposure to low-intensity focused ultrasound (LIFU), the nanocarriers underwent acoustic cavitation-induced rupture, leading to rapid curcumin release and significant induction of apoptosis. OPN LIP treatment notably reduced IL-1α and TNF-α levels and aggravated apoptosis in foam cells. Transcriptomic analysis revealed modulation of inflammatory and apoptotic pathways, including TLR, NF-κB, and Mapk3 signaling. These findings highlight the potential of OPN LIP as an ultrasound-responsive, targeted nanoplatform capable of suppressing inflammation and foam cell viability, providing a promising approach for the treatment of atherosclerosis through combined physical and pharmacological strategies.

Preparation, rheological properties, and in vitro digestibility of starch-based hydrogel beads for curcumin delivery

Ping Shi,Siyu Liu,Hafiz Umer Javed,Jinming Lu,Yuansen Liu

Curcumin (CUR) possesses notable health benefits but suffers from poor solubility, instability, and low bioavailability. To address these limitations, this study developed a novel starch-chitosan composite cross-linked with citric acid (CA). The modified starch was employed in the fabrication of emulsion and emulsion gel beads, which were systematically evaluated based on rheological properties, texture, moisture distribution, and in vitro digestibility. The starch-based emulsion exhibited higher storage modulus and loss modulus compared to the emulsion. Texture analysis revealed that the hardness and adhesiveness decreased to 1.89 ± 0.13 N and 0.66 ± 0.05 N, respectively, while cohesion, elasticity, and chewiness were increased. The LF-NMR results indicated that the CA combined CS modified starch-based emulsion beads (CA/CS-SEB) had a diminished proportion of free water and a correspondingly greater proportion of bound water compared to starch-based emulsion beads (SEB). The encapsulation efficiency of the CUR-loaded beads reached 86.50 ± 0.25 %. In simulated gastrointestinal digestion, CA combined CS modified starch-based emulsion beads loaded with curcumin (CA/CS-SEB-CUR) exhibited the slowest release ratio, which decreased from 23.20 ± 0.03 % to 17.03 ± 0.77 %. These findings provide a theoretical basis for the use of modified starch and propose a viable strategy for curcumin delivery.

Solid Lipid–Threshold Guided Chitosan Coating of NLCs for Improved Gastrointestinal Stability and Curcumin Bioavailability

Chujing Wang,Zengliu Song,Xinyue Ning,Yong Wang,Jie Xiao

Chitosan-coated nanostructured lipid carriers (CS-NLCs) were engineered to overcome the gastrointestinal instability and limited absorption of glycerol distearate (GDS)/medium-chain triglyceride (MCT)-based NLCs. Using a dropwise coating method, we systematically evaluated the impact of chitosan coating on digestive stability and intestinal permeability through in vitro digestion models, Ussing chamber assays, and confocal laser scanning microscopy (CLSM). The results indicate that Chitosan coating improved NLCs’ storage stability (except G2M8 formulation). CS-NLCs exhibited more complete digestion (the maximum fatty acid released within 20   minutes versus 30   minutes for uncoated NLCs), with Turbiscan analysis demonstrating an increase in initial digestion rate compared to uncoated NLCs, though chitosan-induced flocculation reduced small intestinal permeability (52% lower apparent permeability coefficient in Ussing chambers). CLSM imaging identified a critical solid lipid threshold (>50%) for chitosan-mediated adhesion enhancement, with 80% solid lipid CS-NLCs showing 1.6-fold higher mucus adhesion due to incomplete chitosan degradation and increased particle size (from 747   nm to 16μm). Pharmacokinetic studies in rats confirmed that CS-NLCs with >50% solid lipid achieved 1.8-fold higher curcumin bioavailability versus uncoated counterparts. This study highlights the critical role of chitosan coating in optimizing the bioavailability of lipid-based nutraceuticals in the gastrointestinal tract.

Single molecule recognition of CD95 receptors on the surface of HepG2 cells under the curcumin

Zeling Guo,Yu Meng,Xinyu Li,Jiangting Li,Shang Zhou,Rongrong Feng,Weiting Wu,Mingjing Xu,Jinhao Liu,Xiangfu Zeng,Weidong Zhao,Haijian Zhong

Hepatocellular carcinoma (HCC) is a serious concern worldwide. The published reports showed that aberrant CD95 receptor expression plays a critical role in apoptosis in liver cancer. While curcumin has shown promise in inducing apoptosis in liver cancer cells, its direct effects on CD95 expression during this process have not been thoroughly investigated. This study aims to quantitatively assess the expression of the CD95 receptor in HepG2 cells treated with different concentrations of curcumin using techniques such as fluorescence staining, single-molecule force spectroscopy (SMFS), and single-molecule recognition imaging (SMRI). Fluorescence staining results indicate a significant increase in CD95 expression following curcumin treatment. For the first time, SMFS and SMRI techniques were used to directly reveal the binding sites of CD95 on the cell membrane, with the number of binding sites increasing as the curcumin concentration increased. Additionally, the binding force between an antibody-modified probe and CD95 was strengthened with curcumin treatment, suggesting that curcumin enhances both the quantity and affinity of CD95 binding sites. This study provides new insights into curcumin-induced CD95-mediated apoptosis in liver cancer cells and highlights the potential of AFM techniques for investigating drug mechanisms. Overall, these findings may inform innovative therapeutic strategies for liver cancer and improve drug design processes.

Ultrasonic engineering of zein-curcumin nanoparticles/sodium alginate composite films for active food packaging applications

Qiufang Liang,Panpan Cao,Haina Lu,Yunxia Du,Lixin Kang,Haile Ma,Xiaofeng Ren

Food spoilage poses a significant threat to human health and contributes to substantial global food waste. To address this issue, advancements in biopolymer-based packaging materials have garnered increasing research attention. A novel zein-curcumin nanoparticles/sodium alginate (U-ZcNPs/SA) composite films was fabricated by encapsulating curcumin (Cur) within zein nanoparticles via ultrasonic-assisted self-assembly, followed by integration into an SA matrix. Ultrasonic treatment induced structural reorganization of zein, enhancing electrostatic interactions and hydrogen bonding within the film matrix, which improved nanoparticle dispersion, mechanical properties (tensile strength: 40.51 N/mm 2 ; elongation at break: 72.23 %), and barrier performance (oxygen permeability: 2.44 g/hm 2 ). Characterization techniques (SEM, FTIR, XRD, TGA) confirmed superior interfacial compatibility, thermal stability, and amorphous structure in U-ZcNPs@SA films. Furthermore, the films demonstrated robust antibacterial activity against both Escherichia coli and Staphylococcus aureus , with inhibition zones measuring up to 11.09 cm and 10.78 cm, respectively. In the preservation experiment, the U-ZcNPs@SA film effectively extended the shelf life of grapes and strawberries by maintaining their visual quality. Notably, it significantly reduced weight loss in strawberries while suppressing their respiration rate and ethylene production. These results demonstrated that ultrasonic modification optimized the functional performance of biodegradable films, offering a sustainable strategy for active food packaging.

Antimicrobial photodynamic inactivation with curcumin against Staphylococcus saprophyticus, in vitro and on fresh dough sheet

Ziyuan Wang,Yating Jia,Wanyi Li,Min Zhang

Photodynamic inactivation (PDI), as a new non-thermal decontamination and preservation technology, exhibits the advantages of low cost, free of residue and non-microbial resistance. Curcumin (CUR) as a natural photosensitizer could effectively inactivate food spoilage bacteria at an absorbance wavelength (420–470 nm) light illumination. In this study, the in vitro influence of PDI process parameters on the inactivation of Staphylococcus saprophyticus and the antimicrobial mechanism was analyzed. Approximate 5 log CFU/ml reduction was obtained when treated with 25 μM CUR and 4.32 J/cm 2 of blue LED. Obvious cell wrinkles, cell membrane disruption, intracellular contents leakage and increased membrane permeability of S. saprophyticus cell were observed after CUR-PDI treatment. Further, generation of intracellular reactive oxygen species, along with decreased intracellular enzyme activities and increased degree of cell membrane depolarization verified cell damage. The in vivo photo-antibacterial effect (1.04 log CFU/g and 0.81 log CFU/g) was validated on fresh millet dough sheet at two initial bacterial loads (5 log CFU/g and 3 log CFU/g, respectively). These findings illustrated that CUR mediated PDI could be applied to inhibit S. saprophyticus growth and possibly prevent spoilage of fresh dough products.

Dual Targeting pH-Sensitive Co-Delivery Curcumin and β-Elemene Nanomedicine for Breast Cancer Therapy

Liu Mengna,Wu Jun,Wang Kaili,Yuan Dehao,Wang Yinan,Cheng Haoran,Zhao Feng,Fan Huaying,Xu Hui,Chen Daquan

In this paper, for the sake of improving the bioavailability and tumor targeting ability of curcumin (cur), we reported a nanoplatform self-assembled from Folic acid-Adipic dihydrazide-oligomeric hyaluronic acid (FA-ADH-oHA) as drug carrier, curcumin and β-elemene as loaded model drug for dual targeting to breast cancer cells. We used pH sensitive Folic acid-Adipic dihydrazide (FA-ADH) as hydrophobic moieties, HA as the target of cancer stem cells CD44 receptor. The structure characteristic of this smart multifunctional dual targeting nano-sized carrier was measured by 1H-NMR. Cur, an anticancer drug, was successfully loaded into FA-ADH-oHA micelles by self-assembly with a hydrodynamic diameter of 216.4 ± 0.5 nm. Triggered by faintly acidic tumor microenvironment, more encapsulated curcumin and β-elemene could be released from the FA-ADH-oHA micelles in tumor environment than in the pH 7.3 environment. To sum up, the novel polymeric carrier based on pH sensitive and dual drug-targeting strategies was a prospective delivery platform to enhance therapeutic efficiency and decrease toxic side effect in breast cancer therapy.

Synthesis Characterization of Platinum (IV) Complex Curcumin Backboned Polyprodrugs: In Vitro Drug Release Anticancer Activity

Honglei Zhang,Yanjuan Wu,Xiao Xu,Chen Chen,Xiukun Xue,Ben Xu,Tianduo Li,Zhaowei Chen

The conventional mono-chemotherapy still suffers from unsatisfied potency for cancer therapy due to tumor heterogeneity and the occurrence of drug resistance. Combination chemotherapy based on the nanosized drug delivery systems (nDDSs) has been developed as a promising platform to circumvent the limitations of mono-chemotherapy. In this work, starting from cisplatin and curcumin (Cur), we prepared a dual drug backboned shattering polymeric nDDS for synergistic chemotherapy. By in situ polymerization of the Cur, platinum (IV) complex-based prodrug monomer (DHP), L-lysine diisocyanate (LDI), and then conjugation with a hydrophilic poly (ethylene glycol) monomethyl ether (mPEG) derivative, a backbone-type platinum (IV) and Cur linkage containing mPEG-poly(platinum-co-Cur)-mPEG (PCPt) copolymer was synthesized. Notably, the platinum (IV) (Pt (IV)) and Cur were incorporated into the hydrophobic segment of PCPt with the fixed drugs loading ratio and high drugs loading content. The batch-to-batch variability could be decreased. The resulting prodrug copolymer then self-assembled into nanoparticles (PCPt NPs) with an average diameter around 100 nm, to formulate a synergetic nDDS. Importantly, PCPt NPs could greatly improve the solubility and stability of Cur. In vitro drug release profiles have demonstrated that PCPt NPs were stable in PBS 7.4, rapid burst release was greatly decreased, and the Pt and Cur release could be largely enhanced under reductive conditions due to the complete dissociation of the hydrophobic main chain of PCPt. In vitro cell viability test indicated that PCPt NPs were efficient synergistic chemotherapy units. Moreover, PCPt NPs were synergistic for cisplatin-resistant cell lines A549/DDP cells, and they exhibited excellent reversal ability of tumor resistance to cisplatin. This work provides a promising strategy for the design and synthesis of nDDS for combination chemotherapy.Keywords:nanosized drug delivery system;dual drug;backboned;combination chemotherapy;polyprodrug

Facile preparation of thermosensitive and water-soluble fluorescent polymer containing curcumin and its cell imaging

Qingmin Yang,Hongmei Liu,Jiarun Cheng,Chaoying Hu,Shuchen Zhang,Xiaomeng Li,Hongchi Zhao,Libin Bai,Sujuan Wang,Yonggang Wu

Curcumin-laden amphiphilic chitosan microemulsion with enhanced transdermal delivery, skin compatibility and anti-arthritic activity

Jie Zhang,Zetao Wang,Muheng Liao,Shuxian Li,Qi Feng,Xiaodong Cao

Transdermal administration can avoid the first-pass effect of liver, improve the bioavailability of drugs and the adaptability of patients. However, there are still many problems, such as low load efficiency, short drug half-life, unfavorable transdermal efficiency, poor skin compatibility, which hinder the development of transdermal administration. In order to solve the above problems, amphiphilic chitosan microemulsion (AC-ME) is developed by using chitosan with hydrophilic carboxyl groups and hydrophobic long alkane chains as surfactant. AC-ME is efficient for drug loading and transdermal delivery , which is demonstrated by extremely high drug loading, improved drug stability and excellent transdermal efficiency. Specifically, the loading amount of curcumin (Cur) can reach up to 3.41 ± 0.13 mg/mL, an increase of approximately 30,000 times compared to its water solution. The light stability of Cur is improved from 43% to 75%. The transdermal process and skin retention of Cur exhibit 1.76-fold and 5.29-fold increase, respectively. Moreover, AC-ME is skin-compatible and does not damage skin structure. Finally, AC-ME can improve the therapeutic effect of Cur and exhibit superb anti-inflammatory effect in the rheumatoid arthritis (RA) model of mice. In a word, AC-ME would be a promising drug carrier for transdermal drug delivery.

Development of oral curcumin based on pH-responsive transmembrane peptide-cyclodextrin derivative nanoparticles for hepatoma

Tiantian Wei,Yin Zhang,Meng Lei,Yanru Qin,Zhongjie Wang,Zhimeng Chen,Liefeng Zhang,Yongqiang Zhu

Herein, a pH-responsive cyclodextrin derivative (R6H4-CMβCD) with cell-penetrating ability was successfully synthesized, and curcumin-loaded nanoparticles (R6H4-CMβ [email protected] NPs, RCCNPs) were developed to improve its efficacy in hepatoma. RCCNPs could improve the cell uptake compared with CMβ [email protected] NPs (CCNPs) and were internalized into cells mainly through endocytosis mediated by reticulin and macropinocytosis . Furthermore, the accumulation of RCCNPs in hepatoma cells at pH 6.4 was higher than that at pH 7.4, indicating a pH-responsive uptake. Additionally, RCCNPs could escape from the lysosomes via the “proton sponge effect”, and a high apoptosis rate was detected. Importantly, in vivo experiments revealed that orally administered RCCNPs could exert excellent anti-cancer effects in tumor-bearing mice. Hematoxylin-eosin staining did not show significant histological changes in the major organs. Thus, our findings indicate the potential of R6H4-CMβCD as a nanopharmaceutical material, and RCCNPs as an effective delivery system for oral curcumin in cancer management.

Curcumin encapsulated PLGA-chitosan nanocarrier: Fabrication, characterization, and in vitro differentiation evaluation on PC12 cells

Renzhang Liang,Cuilian Yu,Dong Ma,Xiaohan Cao,Liying Bai,Yulan Li,Jingxian Zhang,Jiayue Liu,Xia Qiao,Bingren Tian

Curcumin, a polyphenolic compound, demonstrates neuroprotective potential through its antioxidant, anti-inflammatory, and anti-amyloid activities. To enhance its delivery, we fabricated poly(lactic-co-glycolic acid) (PLGA) nanoparticles encapsulating curcumin and stabilized them with chitosan. Successful formulation was confirmed by FTIR, XRD, and SEM analyses. Zeta potential measurement confirmed a surface charge reversal from -28.1 mV (uncoated PLGA) to + 14.7 mV after chitosan coating. The nanoparticles exhibited favorable drug loading (4.09 ± 0.02 % to 5.67 ± 0.01 %) and encapsulation efficiency (14.33 ± 0.08 % to 19.85 ± 0.04 %), and provided a sustained release profile (>24 h) enhanced by chitosan. The curcumin encapsulated PLGA-chitosan nanocarriers demonstrated potent antioxidant activity (>80 % DPPH scavenging at 0.75 mg/mL) and no significant cytotoxicity against PC12 cells at concentrations up to 80 μg/mL. In HCT116 cells, the chitosan coating enhanced cellular uptake and cytoplasmic distribution. Crucially, the nanocarriers promoted PC12 cells differentiation, resulting in a high proportion of neurite-bearing cells. These findings indicate that the designed chitosan-coated PLGA nanoparticles are a promising delivery system for promoting neuronal differentiation.