AAPS PHARMSCITECH
·
2025
·Vol. 26
·期 4
·1-17
·
IF 4
Luo Zhilin,Sun Yao,Cai Shihao,Liu Hongting,Zhao Conglu,Xu Xiang,Xu Aiguo,Zhou Honggang,Yang Cheng,Gu Xiaoting,Ai Xiaoyu
Idiopathic Pulmonary Fibrosis (IPF) is a rare and serious chronic interstitial lung disease that may endanger the lives of patients. The median survival time of patients with idiopathic pulmonary fibrosis is short, and the mortality rate is higher than that of many types of cancer. At present, pirfenidone (PFD) and nintedanib (NDNB) have been approved by FDA for IPF, but they can only delay the process of pulmonary fibrosis and cannot cure the disease. Therefore, it is urgent to develop other drugs with the effect of improving pulmonary fibrosis. Ellagic acid (EA) can inhibit the Wnt-signaling pathway and has an effect in treating pulmonary fibrosis induced by bleomycin (BLM) in mice. However, its solubility is poor, resulting in its low bioavailability and limited therapeutic benefits, so its clinical application has been limited. Herein, based on the characteristics of nano-drug lung delivery system, chitosan (CS) was selected as the carrier, and ellagic acid-loaded chitosan nanoparticles (EA-CS-NPs) were prepared by ionic gelation method. The EE% and DL% of prepared EA-CS-NPs was 73.73 ± 4.52% and 6.23 ± 1.09%, the particle size was 119.6 ± 5.51 nm (PDI = 0.234 ± 0.017), the zeta potential was 29.833 ± 0.503 mV. The morphology of the nanoparticles was observed by TEM microscope, which was round, uniform dispersion, indicating that the preparation process is stable and feasible. The toxicity experiment showed that EA-CS-NPs maintained 80% cell viability, significantly higher than that of the NDNB group, indicating lower toxicity and better inhibitory effects on TGF-β1-stimulated MLg and NIH-3T3 cells. Wound healing assay results showed that the inhibitory effect of EA-CS-NPs on cell migration was more pronounced than that of EA in the same amount of EA-containing drugs. Drug uptake experiments revealed that EA-CS-NPs significantly enhanced drug uptake in MLg and NIH-3T3 cells. In vivo , Cy7-CS-NPs exhibited higher fluorescence intensity in rat lungs compared to Cy7 solution, indicating better lung retention. The in vivo efficacy test showed that compared with the EA group, EA-CS-NPs could better reduce the area of pulmonary fibrosis and collagen deposition, improve lung function, and have a longer retention time in the lung. In summary, our results revealed that EA-CS-NPs may be a good choice for the treatment of pulmonary fibrosis. Graphical
研究领域:
药剂学
·
呼吸病学
·
纳米医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Analytical Methods
·
2024
·
IF 2.7
Junwei Yang,Si Zhou,Haijiao Zheng,Qiong Jia
One of the most crucial and prevalent post-translational modifications is the phosphorylation of proteins. The study and examination of protein phosphorylation hold immense importance in comprehending disease mechanisms and discovering novel biomarkers. However, the inherent low abundance, low ionization efficiency, and coexistence with non phosphopeptides seriously affect the direct analysis of phosphopeptides by mass spectrometry. In order to tackle these problems, it is necessary to carry out selective enrichment of phosphopeptides prior to conducting mass spectrometry analysis. Herein, magnetic chitosan nanoparticles were developed by incorporating arginine, and were then utilized for phosphopeptide enrichment. A tryptic digest of β-casein was chosen as the standard substance. After enrichment, combined with matrix assisted laser desorption ionization time of flight mass spectrometry (MALDI-TOF MS), the detection limit of the method was 0.4 fmol. The synthesized magnetic material demonstrated great potential in the detection of phosphopeptides in complex samples, as proven by its successful application in detecting phosphopeptides in skim milk and human saliva samples.
研究领域:
生物化学
·
蛋白质组学
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2021
·
IF 6.953
Zhendong Ding,Mengmiao Mo,Kai Zhang,Yongguang Bi,Fansheng Kong
In this study, proanthocyanidin-loaded chitosan nanoparticles (PC-CS-NPs) were produced using ionotropic gelation and characterized using Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and dynamic light scattering (DLS). The synthesized nanoparticles were smaller than 300 nm and had a spherical shape, smooth topography and homogenous morphology as observed through scanning electron microscopy (SEM). In vitro release study showed that proanthocyanidins (PC) had a sustainable release from PC-CS-NPs in different buffer media. PC-CS-NPs had higher or comparable potency in scavenging DPPH and ABTS free radicals as compared to native drugs. Furthermore, PC-CS-NPs also inhibited the growth of four bacteria species, whose degree of inhibition depended on the bacterial strain . The results of SEM confirmed the changes in the microstructure of bacteria. Our findings support the use of chitosan nanoparticles to encapsulate PC and improve its bioactivity in food products.
研究领域:
食品科学
·
生物医学工程
·
药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Shuang Cai,Linlin Wang,Xilong Cui,Xinshu Zou,Sidi Zheng,Fanhui Liu,Chun Shi,Yanhua Li,Zhiyun Zhang
The multi-drug resistance of methicillin-resistant Staphylococcus aureus (MRSA) and complex wound microenvironment challenge the repair of MRSA infected wound. Herein, in this study, α-tocopherol modified glycol chitosan (TG) nanoparticles encapsulated with phytochemical rhein (Rhein@TG NPs) were prepared for comprehensive anti-infection and promotion of MRSA infected wound healing. Rhein@TG NPs could not only specifically release rhein in the infection site in response to low pH and lipase of infectious microenvironment, but also up-regulated M1 macrophage polarization in the infection stage, thus achieving synergistically bacterial elimination with low possibility of developing resistance. Additionally, the NPs reduced the levels of pro-inflammatory factors in the post-infection stage, scavenged the ROS, promoted cell migration and angiogenesis, which significantly improved the microenvironment of infected wound healing. Therefore, this antibiotic-free NPs enabling anti-infection and promotion of wound healing provides a new and long-term strategy for the treatment of MRSA infected wound.
研究领域:
纳米技术
·
药学
·
伤口愈合
·
微生物学
·
免疫学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Scientific Reports
·
2024
·Vol. 14
·期 1
·1-13
·
IF 3.8
Mu Dehong,Zhou Li,Shi Lingyu,Liu Ting,Guo Ying,Chen Hao,Luo Hongping,Ma Junhao,Zhang Hui,Xiong Peizheng,Tian Li
Allergic rhinitis (AR) remains a major health problem worldwide. Compared with traditional oral drugs, nasal administration avoids first-pass metabolism and achieve faster and more effective efficacy. In this study, we used the ion crosslinking method to prepare quercetin–chitosan nasal adaptive nanomedicine (QCS) delivery system and evaluated in the treatment of allergic rhinitis mice models. The obtained positively charged nanoparticles with a particle size of 229.2 ± 0.2 nm have excellent characteristics in encapsulation efficiency (79.604%), drug loading rate (14.068%), drug release (673.068 μg) and stability(> 7 days). Excitingly, QCS treatment significantly reduced the number of sneezing and nasal rubbing events in AR mice, while reducing the levels of inflammatory factors such as immunoglobulin E (IgE), interleukin (IL)-17, tumor necrosis factor (TNF)-α, and (IL)-6 to alleviate AR symptoms. Hematoxylin–eosin (HE) staining also showed the damaged nasal mucosa was improved. These experimental results suggest that QCS can effectively suppress allergic inflammation in a mouse model and hold promise as a therapeutic option for allergic rhinitis.
研究领域:
药剂学
·
免疫学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2020
·
IF 5.162
Yuanhao Qiu,Dan Xu,Guoqing Sui,Dongdong Wang,Ming Wu,Lipeng Han,Haibo Mu,Jinyou Duan
Biofilms and intracellular bacteria often cause a series of overwhelming public health issues due to their strong drug resistance. Hence, chitosan nanoparticles (CS NPs), phosphatidylcholine and gentamicin were used to synthesize a novel nanodrug delivery system (GPC NPs). Dynamic light scattering (DLS) demonstrated that the surface zeta-potential of GPC NPs was −19.5 mV. The morphology of GPC NPs was observed by scanning electron microscopy (SEM). The gentamicin adsorption and release behaviors of GPC NPs were also investigated. The GPC NPs could effectively damage and remove the biofilm formed by pathogens through permeation of the antibiotic into the biofilm. In addition, the nanoparticles were readily engulfed by macrophages which facilitated the killing of intracellular bacteria and had neglectable cytotoxicity. Our study indicated that GPC NPs could be used as a promising nanoantibacterial agent against biofilms and intracellular bacteria.
研究领域:
药学
·
纳米技术
·
微生物学
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Polymers
·
2015
·Vol. 7
·期 9
·1850-1870
·
IF 3.681
Jiaojiao Xu,Beihua Xu,Dan Shou,Xiaojing Xia,Ying Hu
Chronic intracellular infections caused by drug-resistant pathogens pose a challenge to the treatment of chronic osteomyelitis. Such treatment requires an intracellular delivery system for the sustained release of antibiotics such as vancomycin (VCM), which is an antibiotic of last resort used against many clinically resistant bacteria. In this work, we report VCM-loadedN-trimethyl chitosan (TMC) nanoparticles and their potential application for drug delivery. The results showed that the prepared nanoparticles were predominantly spherical in shape with an average particle diameter of 220 nm, a positive zeta potential, and a loading efficiency of 73.65% ± 1.83%. Furthermore, their drug release profile followed the Higuchi model for sustained release, with non-Fickian diffusion. Over a 24-h period, 6.51% ± 0.58% of the drug within the optimized nanoparticles was released.In vitrocytology showed that osteoblasts (OBs) exhibited higher alkaline phosphatase activity (ALP) after exposure to TMC nanoparticle material. Furthermore, TMC nanoparticles increased the uptake of water-soluble quantum dots (QDs) by OBs, and both nanoparticles and VCM/TMC mixtures improved OB proliferative activity. We also investigated the minimum inhibitory concentration (MIC, 60 μg/mL), half maximal inhibitory concentration (IC50, 48.47 μg/mL), diameter of inhibition zone (DIZ, 1.050 cm), and turbidimetric (TB) assay of nanoparticles. All data demonstrated that VCM/TMC nanoparticles had excellent antibacterial activity against the Gram-positive bacteriumStaphylococcus aureus. These findings suggest that VCM-loaded TMC nanoparticles have good potential for the sustained delivery of antibiotics to bone infections.Keywords:vancomycin (VCM);N-trimethyl chitosan (TMC);intracellular infections;nanoparticles
研究领域:
药学
·
生物医学工程
·
微生物学
✓ 已验证
产品关联
DOI
高影响因子
CARBOHYDRATE POLYMERS
·
2022
·
IF 10.723
Lumin Yang,Haofei Huang,Huajing Zeng,Xiaoduo Zhao,Rui Wang,Zhengfeng Ma,Zengjie Fan,Yong-min Liang,Shuanhong Ma,Feng Zhou
Rheumatoid arthritis (RA) is a chronic inflammatory immune and lubrication dysfunction disease that causes great damage to the joints. Herein, inspired by the unique biochemistry structure and excellent hydration of chondroitin sulfate (CHI) existing in joint system, one kind of novel polysaccharide nanoparticle lubricant, that is chitosan nanoparticles (CS NPs) grafting CHI (CS-CHI), is synthesized by one-step surface chemistry reaction. CHI with negative charges can form hydration layers on the surface of CS NPs, thus improving the lubricity of nanoparticles. Simultaneously, CS-CHI NPs have effective loading and sustained drug release ability for anti-inflammatory drug diclofenac sodium (DS), along with good biocompatibility. Finally, based on a collagen-induced rat RA model, in vitro animals experimental results indicate that the as-synthesized CS-CHI@DS NPs has obvious inhibitory effects on inflammatory factors and can effectively prevent the damaged cartilage from further destruction.
研究领域:
生物医学工程
·
材料科学
·
免疫学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2026
·
IF 5.4
Zhixiang Wu,Yanjuan He,Hao Deng,Yue Tan,Wangzi Gao,Jiaxin Yin,Ziqin Zeng,Jing Sun,Lijuan Zhang,Yue Li,Shentang Li
Chronic kidney disease (CKD), whose prevalence is rising substantially, has become a major global health challenge. In this study, we developed linagliptin-loaded chitosan nanoparticles (HCS-LGP NPs) for the treatment of renal fibrosis. The synthesized nanoparticles exhibited a uniform particle size of 178.8 ± 4.4 nm and a zeta potential of −29.9 ± 2.5 mV, along with acid-responsive drug release properties. In vitro , the HCS-LGP NPs showed efficient cellular uptake in TGF-β1-induced HK-2 cells and significantly inhibited cell proliferation by downregulating the expression of TGF-β1 and Collagen I. In vivo studies demonstrated effective renal accumulation of HCS-LGP NPs in rats with renal fibrosis. Treatment with HCS-LGP NPs significantly reduced serum creatinine, blood urea nitrogen, and the protein levels of TGF-β1 and Collagen I. Notably, the administration of HCS-LGP NPs promoted marked recovery from renal injury and markedly reduced collagen fiber deposition in rats with renal fibrosis. Histopathological analysis confirmed excellent biocompatibility, with no observable damage to the heart, liver, spleen, or lungs. These findings indicate that HCS-LGP NPs hold great potential as a targeted therapy for renal fibrosis, offering enhanced efficacy and a favorable safety profile.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
International Journal of Nanomedicine
·
2025
·
IF 6.5
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.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Biomedical Nanotechnology
·
2018
·Vol. 14
·期 8
·1486-1495
·
IF 5.068
Wang Yonghong,Wen Baofang,Yu Hongli,Ding Dejun,Zhang JingJing,Zhang Yunxiang,Zhao Limin,Zhang Weifen
Nasopharyngeal carcinoma (NPC) is a common epithelial malignancy that occurs in the nasopharynx and it is one of the high incidences of malignant tumors in China. As previous reports, berberine hydrochloride (BH) possesses a repressive effect on the proliferation of various cancer types.
But the application of BH was hampered for a long time due to its hydrophobic properties, along with poor stability and bioavailability. In this study, folate acid modified chitosan nanoparticles loaded berberine hydrochloride (BH/FA-CTS NPs) were prepared by the ionic cross-linking technique,
the physicochemical properties and the influence of BH/FA-CTS NPs on proliferation, migration and apoptosis in human nasopharyngeal carcinoma CNE-1 cells were studied in vitro and in vivo. Results of scanning electron microscopy (SEM) images showed that BH/FA-CTS NPs were sphere
and the diameter was 258.2±9.1 nm. The drug loading and encapsulation efficiency were 8.17±1.12% and 87.73±4.21%, respectively. The drug release kinetics exhibited a slower and sustained release over a period of 48 h. Moreover, results of MTT assay and scratch assay displayed
that BH/FA-CTS NPs inhibited proliferation and migration of CNE-1 cells remarkably. BH/FA-CTS NPs promoted apoptosis and necrosis of CNE-1 cells. And BH/FA-CTS NPs displayed distinguished higher tumor inhibition than control group, free BH and BH/CTS NPs in vivo. Therefore, as a nanocomposite,
BH/FA-CTS NPs provide a new method and option for the treatment of nasopharyngeal carcinoma patients.
研究领域:
肿瘤学
·
药剂学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES
·
2015
·Vol. 18
·期 2
·155-170
·
IF 1.856
Ke Z,Guo H,Zhu X,Jin Y,Huang Y.
Purpose We investigated the effect of vitamin B12 (VB12) modification on the insulin absorption from trimethyl chitosan(TMC) nanoparticles (NPs) under the influence of mucus. Methods TMC and TMC-VB12 were synthesized and insulin loaded TMC/TMC-VB12 nanoparticles were prepared and characterized. Modified and unmodified nanoparticles were studied with Caco-2/HT29-MTX cell model and ligated rat ileum loop. Results Compared with unmodified NPs, VB12 modified NPs showed significantly higher drug internalization in Caco-2/HT29-MTX cell model. The internalization mechanism via VB12 mediation included caveolae and clathrin-mediated endocytosis pathway. Meanwhile, an increased transportation of drugs was observed for VB12 modified NPs, possibly due to the ligand-receptor interaction via an intrinsic factor-dependent fashion. Although the uptake and transport of VB12 modified NPs could be partially influenced by mucus, they still showed higher drug permeation through Caco-2/HT29-MTX co-cultured cells than unmodified NPs in the presence or absence of mucus. Moreover, in situ study in ligated rat ileum loop demonstrated that VB12 modified nanoparticles could reduce the residual insulin in intestinal lumen (0.59 times) and increase their absorption in epithelial tissue (4.8 times) compared with the unmodified ones. Conclusion VB12 modified trimethyl chitosan nanoparticle is a promising carrier for peroral delivery of insulin.
研究领域:
药剂学
·
药物递送
·
纳米医学
·
生物药剂学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）