DRUG DELIVERY
·
2016
·
IF 4.843
Jiang Ni,Fengchun Tian,Fatima Zohra Dahmani,Hui Yang,Deren Yue,Shuwang He,Jianping Zhou,Jing Yao
The low oral bioavailability of numerous drugs has been mostly attributed to the significant effect of P-gp-mediated efflux on intestinal drug transport. Herein, we developed mixed polymeric micelles (MPMs) comprised of curcumin-carboxymethyl chitosan (CNC) conjugate, as a potential inhibitor of P-gp-mediated efflux and gastrointestinal absorption enhancer, and low-molecular-weight heparin-all-trans-retinoid acid (LHR) conjugate, as loading material, with the aim to improve the oral absorption of P-gp substrate drugs. CNC conjugate was synthesized by chemical bonding of curcumin (Cur) and carboxymethyl chitosan (CMCS) taking advantage of the inhibition of intestinal P-gp-mediated secretion by Cur and the intestinal absorption enhancement by CMCS. The chemical structure of CNC conjugate was characterized by 1H NMR with a degree of substitution of Cur of 4.52–10.20%. More importantly, CNC conjugate markedly improved the stability of Cur in physiological pH. Cyclosporine A-loaded CNC/LHR MPMs (CsA-CNC/LHR MPMs) were prepared by dialysis method, with high drug loading 25.45% and nanoscaled particle size (∼200 nm). In situ single-pass perfusion studies in rats showed that both CsA + CNC mixture and CsA-CNC/LHR MPMs achieved significantly higher Ka and Peff than CsA suspension in the duodenum and jejunum segments (p < 0.01), which was comparable to verapamil coperfusion effect. Similarly, CsA + CNC mixture and CsA-CNC/LHR MPMs significantly increased the oral bioavailability of CsA as compared to CsA suspension. These results suggest that CNC conjugate might be considered as a promising gastrointestinal absorption enhancer, while CNC/LHR MPMs had the potential to improve the oral absorption of P-gp substrate drugs.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Oncotarget
·
2017
·
IF 5.168
Na Huang,Shuai Lu,Xiao-Ge Liu,Jie Zhu,Yu-Jiong Wang,Rui-Tian Liu
Alzheimer's disease (AD) is the most common form of dementia, characterized by the formation of extracellular senile plaques and neuronal loss caused by amyloid β (Aβ) aggregates in the brains of AD patients. Conventional strategies failed to treat AD in clinical trials, partly due to the poor solubility, low bioavailability and ineffectiveness of the tested drugs to cross the blood-brain barrier (BBB). Moreover, AD is a complex, multifactorial neurodegenerative disease; one-target strategies may be insufficient to prevent the processes of AD. Here, we designed novel kind of poly(lactide-co-glycolic acid) (PLGA) nanoparticles by loading with Aβ generation inhibitor S1 (PQVGHL peptide) and curcumin to target the detrimental factors in AD development and by conjugating with brain targeting peptide CRT (cyclic CRTIGPSVC peptide), an iron-mimic peptide that targets transferrin receptor (TfR), to improve BBB penetration. The average particle size of drug-loaded PLGA nanoparticles and CRT-conjugated PLGA nanoparticles were 128.6 nm and 139.8 nm, respectively. The results of Y-maze and new object recognition test demonstrated that our PLGA nanoparticles significantly improved the spatial memory and recognition in transgenic AD mice. Moreover, PLGA nanoparticles remarkably decreased the level of Aβ, reactive oxygen species (ROS), TNF-α and IL-6, and enhanced the activities of super oxide dismutase (SOD) and synapse numbers in the AD mouse brains. Compared with other PLGA nanoparticles, CRT peptide modified-PLGA nanoparticles co-delivering S1 and curcumin exhibited most beneficial effect on the treatment of AD mice, suggesting that conjugated CRT peptide, and encapsulated S1 and curcumin exerted their corresponding functions for the treatment.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD HYDROCOLLOIDS
·
2025
·
IF 12.4
Zihang Yan,Sixing Lai,Suqi Yang,Kefan Ouyang,Yuanyuan Feng,Hao Hu,Xing Hu,Hua Xiong,Qiang Zhao
Active gelatin-based films (CUR-PLLF) incorporating V-type granular starch-curcumin complex (VGS-C) and ε-polylysine (PLL) were developed for the short-term refrigerated preservation of salmon fillets. The experiment demonstrates that the composite film (CUR-PLLF), exhibits an enhanced elongation at break by 36.67%, accompanied by a marked increase in DPPH radical scavenging activity from 2.40% to 9.07%. The water vapor permeability and oxygen permeability of CUR-PLLF film were reduced by 14.02% and 18.09%, respectively, and it can be completely degraded in soil within 14 d, demonstrating significant environmental advantages. In salmon fillets refrigeration experiments, CUR-PLLF inhibited bacterial proliferation and fat oxidation, resulting in a 17.25% reduction in Total volatile base nitrogen level, which were below the spoilage threshold of 25 mg/100 g. Additionally, the content of thiobarbituric acid-reactive substances decreased by 30.77%. These findings suggest that the developed gelatin-based film exhibits comprehensive advantages in antibacterial properties, antioxidant activity, and biodegradability, offering an efficient and environmentally friendly solution for the preservation of salmon during short-term refrigeration.
✓ 已验证
产品关联
DOI
高影响因子
FOOD RESEARCH INTERNATIONAL
·
2025
·
IF 8
Jingbo Liu,Yang Liu,Shanglin Li,LongJiang Tian,Yajuan Li,Chunmei Liu,Sitong Ma,Ting Zhang,Meng Yang,Zhiyang Du
Efficient oral coassembly strategies have attracted increasing attention for the preferable co-delivery of multiple nutraceuticals. Inspired by superior transport tendencies of the intestinal glucose transporter 2 (GLUT2) to fructose-modified biopolymers, this study fabricated the coassemblies consisting of fructose-modified chitosan (Fru-CS) shell and disulfonic acid-modified γ-cyclodextrin (BA-γ-CD) core to effectively co-deliver hydrophilic egg white oligopeptides (EWOP) and hydrophobic curcumin (Cur). The non-covalent interactions-driven coassemblies exhibited the admirable nanoscale colloidal features and nutraceuticals (EWOP/Cur) co-loading capacity (20.6–25.5 > > 10 %). Besides, the coassemblies introduced the outstanding application synergism (> 15 % enhancement) to nutraceuticals under multi-dimensional scenarios ( e.g. , digestion, heat, UV-light, and antioxidant). Notably, the outer Fru-CS-coated coassemblies could dramatically improve the intact absorption efficiency (2.5–7.9 times) of nutraceuticals mainly via GLUT2-oriented transcytosis and cooperate with BA-γ-CD to achieve better gastrointestinal retention and mucus permeation. This work offers a facile and effective co-assembly strategy for oral co-delivery of nutraceuticals for food processing and healthcare.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Meiying Liu,Tongsheng Huang,Yiping Liu,Lihua Chen,Shijie Liao,Xinxin Gong,Mubarak G. Bello,Weifeng Zhu,Shaorong Huang,Xiaoyong Zhang
Zein and its complexes have been considered as promising carriers for encapsulating and delivering various biological active ingredients, however, there still have some issues about Zein-based drug delivery systems should be considered, including poor colloidal stability, low drug encapsulation efficiency as well as rapid initial drug release, and uncontrollable release. In this work, we reported for the first time that hyperbranched polymers (HPG) functionalized Zein with terminal alkyne (Zein-HPG-PA) can be used for loading anticancer agent curcumin (CUR) via a facile phenol-yne click reaction. The resultant product (Zein-HPG-PA@CUR) displays high drug loading capacity, small particle size and excellent water dispersibility. More importantly, almost no CUR was released from Zein-HPG-PA@CUR under pH 7.4 and the cargo will be gradually released under acidic environment. As compared with free CUR, Zein-HPG-PA@CUR shows considerable cytotoxicity towards MDA-MB-231 cells under dark environment, while the cytotoxicity was significantly enhanced upon light-irradiation, implying great potential of Zein-HPG-PA@CUR for cancer treatment. Considered the above aspects, we believe that this work should be of significant impact on the biomedical applications of Zein, especially for fabrication of Zein-based responsive drug delivery systems.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF FOOD ENGINEERING
·
2024
·
IF 5.3
Luping Wang,Peng Wu,Zejun Hu,Yiqing Chen,Xia Jin,Ruoxuan Deng,Timothy V. Kirk,Xiao Dong Chen
Plant proteins, serving as an environmentally friendly and cost-effective alternative to animal proteins, have gained widespread usage in encapsulating various bioactive compounds like curcumin. However, understanding how plant protein-based microcapsules compare to those made with animal proteins in terms of disintegration, release, and absorption in the gastrointestinal tract (GIT) remains limited. This study aims to investigate the impact of soy protein isolate (SPI) and whey protein isolate (WPI) as wall materials on the release, stability, and absorption of curcumin. Spray-dried SPI-based microcapsules (SPI–C) exhibited significantly lower encapsulation efficiency (77.1%) and loading efficiency (3.6%) compared to WPI-based microcapsules (WPI–C) (97.6% and 9.6%, respectively). Structural analysis revealed pleated hollow spherical structures for SPI-C and a concave surface with a single-chamber structure for WPI-C. SPI-C demonstrated higher proteolysis (55.8% vs . 44.1%) during in vitro digestion, leading to greater curcumin release ratio (67.9% vs . 59.2%) and digestive stability (97.9% vs . 93.7%) compared to WPI-C. Notably, SPI-C exhibited higher apparent permeability (0.97 × 10 −6 cm/s) to the ex vivo rat small intestine than WPI-C (0.44 × 10 −6 cm/s). These findings suggest improved gastrointestinal stability and absorption of curcumin encapsulated by SPI, indicating the potential for enhanced utilization of plant-derived proteins in encapsulating bioactive compounds.
✓ 已验证
产品关联
DOI
高影响因子
Drug Design Development and Therapy
·
2023
·
IF 4.8
Chengguang Zhao,Yali Zhang,Peng Zou,Jian Wang,Wenfei He,Dengjian Shi,Huameng Li,Guang Liang,Shulin Yang
A novel class of asymmetric mono-carbonyl analogs of curcumin (AMACs) were synthesized and screened for anti-inflammatory activity. These analogs are chemically stable as characterized by UV absorption spectra. In vitro, compounds 3f, 3m, 4b, and 4d markedly inhibited lipopolysaccharide (LPS)-induced expression of pro-inflammatory cytokines tumor necrosis factor-α and interleukin-6 in a dose-dependent manner, with IC50 values in low micromolar range. In vivo, compound 3f demonstrated potent preventive and therapeutic effects on LPS-induced sepsis in mouse model. Compound 3f downregulated the phosphorylation of extracellular signal-regulated kinase (ERK)1/2 MAPK and suppressed IκBα degradation, which suggests that the possible anti-inflammatory mechanism of compound 3f may be through downregulating nuclear factor kappa binding (NF-κB) and ERK pathways. Also, we solved the crystal structure of compound 3e to confirm the asymmetrical structure. The quantitative structure–activity relationship analysis reveals that the electron-withdrawing substituents on aromatic ring of lead structures could improve activity. These active AMACs represent a new class of anti-inflammatory agents with improved stability, bioavailability, and potency compared to curcumin. Our results suggest that 3f may be further developed as a potential agent for prevention and treatment of sepsis or other inflammation-related diseases.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2025
·
IF 4.5
Jiaxin Wu,Leyan Wang,Han Lu,Yujia Huo,Zhaoyang Guo,Yuanyuan Cheng,Yunan Li,Yinsong Wang,Chunyu Li
Inflammatory bowel disease (IBD) management remains challenging due to the inadequate efficacy and systemic toxicity of conventional therapies. Herein, we developed an inulin hydrogel loaded with self-assembled nanoparticles of curcumin and glycyrrhizic acid (CURG@IN) for IBD treatment. CURG@IN exhibited remarkable gel characteristics and enzyme-responsive drug release behavior. In vitro, CURG@IN demonstrated potent antioxidant capabilities, effectively protecting cells from oxidative injury, facilitating wound healing of epithelial cells, and regulating macrophage polarization. Additionally, it exerted inhibitory effects on the NF-κB pathway, thereby reducing the production of inflammatory cytokines. In DSS-induced colitis mice, oral CURG@IN significantly ameliorated disease activity index and restored colonic histological architecture. Gut barrier integrity was reinforced through upregulation of tight junction proteins, while microbiota analysis revealed significant restoration of microbial homeostasis. Notably, no significant toxicity was observed during treatment. Collectively, this oral therapeutic strategy provides a multimechanistic approach combining anti-inflammatory, antioxidative, and microbiota-modulating effects for safe IBD therapy, with the potential for clinical application.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2020
·Vol. 21
·期 5
·1-13
·
IF 2.401
Liu Dandan,Qiao Sen,Cheng Bingchao,Li Dongyang,Chen Jisuan,Wu Qingyin,Pan Hao,Pan Weisan
Despite that either non-covalent or covalent attachment of hydrophilic polymers or surfactants onto nanodiamonds (NDs) could overcome the shortcomings of being a drug delivery system, it is hard to draw a definite conclusion which strategy is more effective. Hence, with the purpose of comparing the influence of different coating approach of NDs on the oral delivery efficiency of water-insoluble model drug curcumin (CUR), NDs were firstly modified with d -α-tocopheryl polyethylene glycol 1000 succinate (TPGS) via non-covalent or covalent conjugation method, and then loaded with CUR (CUR@NDs-COOH/TPGS or CUR@NDs-TPGS). In comparison with the core-shell-structured CUR@NDs-COOH/TPGS, CUR@NDs-TPGS were irregular in shape with dense TPGS film, and exhibited smaller size, more negatively potential, and higher drug loading efficiency. The covalent connection group also showed higher anti-cancer activity, cellular uptake, and permeability through the Caco-2 cell monolayers, as well as favorable distribution, penetration, and retention in rat intestines. The oral bioavailability study in rats demonstrated that CUR@NDs-TPGS showed significantly greater C max and AUC 0− t in contrast with CUR suspension and the TPGS-coated ones, respectively. The findings illustrated that covalent grafting TPGS onto the surface of NDs possesses better efficacy and biocompatibility on oral delivery of poorly soluble drug CUR than pristine and non-covalent coated nanoparticles.
✓ 已验证
DOI
PubMed
高影响因子
MOLECULES
·
2022
·Vol. 27
·期 12
·3940
·
IF 4.927
Dongge Yin,Xueling Hu,Mengru Cai,Kaixin Wang,Hulinyue Peng,Jie Bai,Yvchen Xv,Tingting Fu,Xiaoxv Dong,Jian Ni,Xingbin Yin
Curcumin (CUR) has a bright future in the treatment of cancer as a natural active ingredient with great potential. However, curcumin has a low solubility, which limits its clinical application. In this study, IRMOF-10 was created by the direct addition of triethylamine, CUR was loaded into IRMOF-10 using the solvent adsorption method, and the two were characterized using a scanning electron microscope (SEM), X-ray diffraction (XRD), dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TG) methods, and Brunauer–Emmett–Teller (BET) analysis. We also used the MTT method, 4′,6-diamidino-2-phenylindole (DAPI) staining, the annexin V/PI method, cellular uptake, reactive oxygen species (ROS), and the mitochondrial membrane potential (MMP) to perform a safety analysis and anticancer activity study of IRMOF-10 and[email protected]on HepG2 cells. Our results showed that[email protected]had a CUR load of 63.96%, with an obvious slow-release phenomenon. The CUR levels released under different conditions at 60 h were 33.58% (pH 7.4) and 31.86% (pH 5.5). Cell experiments proved that IRMOF-10 was biologically safe and could promote curcumin entering the nucleus, causing a series of reactions, such as an increase in reactive oxygen species and a decrease in the mitochondrial membrane potential, thereby leading to cell apoptosis. In summary, IRMOF-10 is an excellent drug carrier and[email protected]is an effective anti-liver cancer sustained-release preparation.Keywords:MOFs;IRMOF-10;curcumin;HepG2 cells
✓ 已验证
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2016
·
IF 4.219
Jinyu Li,Dandan Liu,Guoxin Tan,Zhinan Zhao,Xinggang Yang,Weisan Pan
To develop a potential nanocarrier for the topical ocular administration of curcumin (CUR), a novel thiolated chitosan was synthesized by the covalent binding between N -acetyl- l -cysteine (NAC) and chitosan (CS) to surface modify the nanostructured lipid carrier loaded CUR (CUR-NLC). And the superiorities of the CS-NAC co polymer coated CUR-NLC over chitosan oligosaccharides (COS) or carboxymethyl chitosan (CMCS) modification were also verified in detail. As expected, the increment in particle size and the reversal of zeta potential occurred after surface decorating, and the most prominent electropositivity was obtained for the CS-NAC-CUR-NLC group. Additionally, the utilization of the CS-NAC coating demonstrated an effectively controlled release over 72 h and attained a 6.4 and 18.8 fold increase in apparent permeability coefficients (P app ) compared with the CUR-NLC and the self-made eye drops, respectively. Meanwhile, the clearance rate of the NLC labeled with Rhodamine B was significantly delayed in the presence of CS-NAC. By contrast, CS-NAC-CUR-NLC was superior to the COS and CMCS coated ones in view of in vitro release, drug permeability and corneal retention. Moreover, the results of the in-vivo and in-vitro characteristics demonstrated that the promoting effect of CMCS coating was relatively weaker than COS coated ones. Ocular irritation test was executed on the CS-NAC-CUR-NLC, neither a sign of toxicity nor irritation to the external ocular tissues was observed. In conclusion, CS-NAC-CUR-NLC possesses a greater potential as an ocular drug-delivery system comparing with the COS-CUR-NLC and CMCS-CUR-NLC.
研究领域:
药剂学
·
生物材料
·
眼科
✓ 已验证
DOI
高影响因子
ULTRASONICS SONOCHEMISTRY
·
2026
·
IF 10.2
Zijun Wang,Huan Li,Hanlu Yu,Xinyao Wang,Jia Guo,Jia Qing,Haiying Yang,Xiaoqing Xiao,Rongrong Wang,Yang Shan,Shenghua Ding
Curcumin (Cur) is a hydrophobic phenolic compound with superior biological activity, but the limited water solubility, chemical instability, and poor bioaccessibility of curcumin restrict its application. This study developed pea protein isolate (PPI)-folic acid (FA) covalent complexes as nanocarriers for the encapsulation, protection, and precise delivery of curcumin. The results of SDS-PAGE, XPS, and FTIR demonstrated that covalent complexation between PPI and FA was formed through an ultrasound-assisted free radical grafting method. Notably, ultrasonication for 15 min (PPI-FA-US15) achieved a higher FA loading capacity (44.78 ± 0.37 µg/mg) than the traditional free radical grafting for 24 h (36.45 ± 0.43 µg/mg). The ultrasonic treatment and covalent complexation of FA greatly improved the solubility of PPI (from 61.34 ± 0.67% to 97.02 ± 0.88%). Curcumin was efficiently encapsulated within the core of PPI-FA-US15 conjugates to form PPI-FA15-Cur nanocomplexes by hydrogen bonding and hydrophobic interaction. The complexation of FA improved the binding affinity of PPI for curcumin. PPI-FA15-Cur demonstrated a 1.97-fold superior loading capacity for curcumin compared to PPI-Cur. Meanwhile, PPI-FA15-Cur displayed a spherical morphology, and maintained a stable particle size distribution during 77-d storage. The heating stability, photochemical stability and antioxidant property of curcumin were significantly improved. Furthermore, in vitro digestion studies demonstrated that PPI-FA15-Cur showed a sustained release of curcumin. The bioaccessibility of curcumin within PPI-FA15-Cur was about 4.75-fold and 1.11-fold higher than that of free curcumin and PPI-Cur, respectively. This study provides a promising approach for developing plant protein-based carriers that enable precise delivery of curcumin in functional foods.
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）