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CHEMICAL ENGINEERING JOURNAL · 2024 · IF 13.3

Preparation of NIR responsive resveratrol@Au nanocages using for regulating oxidative stress microenvironment of periodontitis

Mofei Han,Kaiqi Tang,Zhenhua Chen

Periodontitis, as a chronic inflammatory oral disease, is the primary cause of tooth loss. The oxidative stress microenvironment of periodontitis causes damage of both osteoblasts’ mitochondrion and periodontal tissue. Natural extracts with antioxidant properties, including resveratrol (RSV), have been reported in regulating oxidative stress microenvironment, however, the controlled release of them in periodontal tissue is still a challenge. Herein, a smart photothermal-responsive gold nanocages hydrogel (RSV-Au@H) was constructed for the treatment of periodontitis by controlling the release of resveratrol. Under the near-infrared (NIR) light irradiation for 5 min, RSV-Au@H could be heated to 45.8 ℃ due to the good photothermal effect of Au nanocages encapsulated in the hydrogel. This NIR stimulated photothermal effect of RSV-Au@H could control the release of RSV. Molecular biology indicated that RSV-Au@H could scavenge ROS with 42 % efficiency. Transmission electron microscopy (TEM) showed a significant improvement in osteoblasts mitochondrial morphology. Micro-CT scanning revealed that RSV-Au@H reduced the distance between cemento-enamel junction and alveolar bone crest (CEJ-ABC) by up to 55 % and increased bone volume fraction by about 48 %. These results suggested that this multifunctional nanoplatform with NIR controlled release of RSV might be a new therapeutic strategy for periodontitis.

研究领域: 牙科学 · 纳米技术 · 药学 · 生物医学工程
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INTERNATIONAL JOURNAL OF OBESITY · 2024 · IF 4.2

PPARα suppresses low-intensity-noise-induced body weight gain in mice: the activated HPA axis plays an critical role

Yan Zheng,Luo Jia,Wang Ying,Yang Jie,Su Mingli,Jiang Lei,Yang Julin,Dai Manyun,Liu Aiming

Background As the second most risky environmental pollution, noise imposes threats to human health. Exposure to high-intensity noise causes hearing impairment, psychotic disorders, endocrine modifications. The relationship among low-intensity noise, obesity and lipid-regulating nuclear factor PPARα is not yet clear. Methods In this study, male wild-type (WT) and Pparα -null (KO) mice on a high-fat diet (HFD) were exposed to 75 dB noise for 12 weeks to explore the effect of low-intensity noise on obesity development and the role of PPARα. 3T3-L1 cells were treated with dexamethasone (DEX) and sodium oleate (OA) to verify the down-stream effect of hypothalamic-pituitary-adrenal (HPA) axis activation on the adipose tissues. Results The average body weight gain (BWG) of WT mice on HFD exposed to noise was inhibited, which was not observed in KO mice. The mass and adipocyte size of adipose tissues accounted for the above difference of BWG tendency. In WT mice on HFD, the adrenocorticotropic hormone level was increased by the noise challenge. The aggravation of fatty liver by noise exposure occurred in both mouse lines, and the transport of hepatic redundant lipid to adipose tissues were similar. The lipid metabolism in adipose tissue driven by HPA axis accorded with the BWG inhibition in vivo, validated in 3T3-L1 adipogenic stem cells. Conclusion Chronic exposure to low-intensity noise aggravated fatty liver in both WT and KO mice. BWG inhibition was observed only in WT mice, which covered up the aggravation of fatty liver by noise exposure. PPARα mediates the activation of HPA axis by noise exposure in mice on HFD. Elevated adrenocorticotropic hormone (ACTH) promoted lipid metabolism in adipocytes, which contributed to the disassociation of BWG and fatty liver development in male WT mice. Summary of PPARα suppresses noise-induced body weight gain in mice on high-fat-diet. Chronic exposure to low-intensity noise exposure inhibited BWG by PPARα-dependent activation of the HPA axis.

CAS / MDL: 50-02-2 28822-58-4
研究领域: 环境健康 · 内分泌学 · 营养学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2025 · IF 5.6

Platelet membrane-cloaked biomimetic nanoparticles for targeted acute lung injury therapy

Peihong Lin,Rui Gao,Wenjing Yang,Zhengyu Fang,Zhouru Wang,Mengdie Yu,Lihua Xu,Zhen Ma,Jie Fang,Wenying Yu

Acute lung injury (ALI) is a medical condition characterized by significant morbidity and elevated mortality rates; however, to date, there are no clinically approved pharmacological interventions that are both safe and effective for its treatment. In the pathophysiology of ALI, a robust inflammatory response is a critical factor. Dexamethasone (Dex), a potent glucocorticoid, is commonly employed in clinical settings to manage inflammatory conditions. However, the frequent or high-dose administration of corticosteroids can result in significant adverse effects and long-term complications. In this study, we have developed a biomimetic anti-inflammatory nanosystem, designated PM-LPs@Dex, aimed at treating ALI. This system leverages the inherent affinity of platelets for sites of inflammation, alongside the advantageous drug encapsulation properties of liposomes (LPs). By harnessing the suitable physicochemical characteristics of LPs and the distinctive biological functions of platelet membranes (PM), PM-LPs@Dex is capable of stable and sustained drug release in vitro. Experimental results regarding cellular uptake and biodistribution reveal that PM-LPs@Dex is preferentially internalized by inflammatory cells and exhibits enhanced accumulation in inflamed lung tissue compared to LPs@Dex. Pharmacokinetic studies displayed that PM-LPs@Dex showed prolonged circulation time in blood. Additionally, pharmacodynamic assessments demonstrate that PM-LPs@Dex significantly mitigates the severity of ALI, as evidenced by reductions in pulmonary edema, tissue pathology, bronchoalveolar lavage cell counts, protein concentration, and levels of inflammatory cytokines. Notably, PM-LPs@Dex also exhibits favorable biocompatibility. This research is anticipated to contribute novel strategies for the safe and effective targeted management of inflammatory diseases.

CAS / MDL: 50-02-2
研究领域: 药理学 · 纳米医学 · 肺科学 · 炎症研究
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International Journal of Chronic Obstructive Pulmonary Disease · 2024 · IF 2.7

Therapeutic Effects of Lifei Decoction in a Murine Model of COPD Induced by LPS and Cigarette Smoke

Liguo Lu,Chengdong Zhu,Jian Xu,Yulan Hu,Juxiang Dai,Sheng Wang,Tao Wei

Introduction The Lifei Decoction (LD) is a commonly utilized Chinese medicine for the treatment of sepsis and bronchial inflammation. However, its therapeutic potential in chronic obstructive pulmonary disease (COPD) remains unknown. Therefore, the objective of this study was to investigate the therapeutic efficacy and underlying mechanism of LD in a mouse model of COPD induced by cigarette smoke (CS) combined with lipopolysaccharide (LPS).Methods Hematoxylin-eosin (H&E) staining was employed to observe the pathological alterations in lung tissue, while ELISA was utilized for the detection of levels of inflammatory factors in both lung tissue and bronchoalveolar lavage fluid (BALF). Additionally, Western blot analysis was conducted to assess the expression of p-NF-κB, GDF11, ZO-1, and Occludin-1 proteins. The changes in intestinal flora were evaluated using the viable bacteria count method.Results The administration of LD demonstrates significant efficacy in mitigating pulmonary tissue damage in a murine model, while concurrently inhibiting the activation of the inflammatory pathway NF-κB to attenuate the levels of pro-inflammatory factors. Moreover, LD exhibits the capacity to enhance the expression of intestinal functional proteins ZO-1 and Occludin-1, thereby rectifying dysbiosis within the gut microbiota.Conclusion The LD shows great promise as a potential treatment for COPD.

CAS / MDL: 50-02-2
研究领域: 药理学 · 呼吸病学 · 免疫学 · 微生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Materials Today Communications · 2025 · IF 4.5

Synthesis and characterization of photocrosslinked gelatin-silk fibroin composite microspheres for mesenchymal stem cell expansion and osteogenic differentiation

Liuxin Yang,Guanhua Jiao,Dandan Wei,Tianzhu Zhang

Microspheres have shown great potential as biomaterial substrates for culturing and expanding stem cells to meet the requirements of cell therapy. Gelatin microspheres have been widely researched in cell culture; however, the size, pore structure, and stability of these microspheres still need to be further optimized. In this study, gelatin methacrylamide (GelMA) and glycidyl-methacrylate-modified silk fibroin (SFMA) composite microspheres (denoted as GSM microspheres) were synthesized using a simple water-oil (W/O) emulsion method followed by photo-crosslinking. The swelling ratio (34 % (w/v) GelMA = 799.8 ± 67.7 %; 34 % (w/v) GSM = 643.1 ± 66.3 %) and degradation ratio (relative weights at 15 d: 34 % (w/v); GelMA = 13.3 ± 3.9 %; 34 % (w/v) GSM = 38.6 ± 6.2 %) of GSM microspheres decreased with the incorporation of SFMA. Moreover, the constructed microspheres demonstrated adjustable size distribution (from 75 to 775 µm for GM0 to 25–275 µm for GSM3), pore structure, and surface curvature. Thus, the initial cell adhesion efficiency of microspheres increased with the content of GelMA (GSM1, GSM2, and GSM3 was 39.5 %, 23.3 %, and 7.7 %, respectively), and the cell amplification achieved by microsphere-microsphere transfer demonstrates the potential for cell expansion in vitro . In addition, On the higher curvature surface of GSM3, the cells were overspread and the shape factor of the nucleus was high (0.88 ± 0.05). Alkaline phosphatase (ALP) activity, osteogenesis-related gene expression, and Alizarin Red S staining showed that the addition of SFMA could promote osteogenic differentiation of BMSCs. Thus, the composite microspheres can serve as an adjustable three-dimensional (3D) culture platform for the amplification and osteogenic differentiation of BMSCs.

研究领域: 生物材料学 · 细胞生物学 · 再生医学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2024 · IF 5.7

Palmatine Attenuated Lipopolysaccharide-Induced Acute Lung Injury by Inhibiting M1 Phenotype Macrophage Polarization via NAMPT/TLR2/CCR1 Signaling

Lei Wang,Jinchun Wang,Lei Han,Tong Chen

The present work was conducted to research the potential mechanism of palmatine (PAL) on lipopolysaccharide (LPS)-caused acute lung injury (ALI). Network pharmacology and bioinformatic analyses were carried out. Mice were intragastrically treated with PAL and intratracheally stimulated with LPS. LPS-induced RAW264.7 cells were employed for the in vitro model. The MPO activity, W/D ratio, neutrophils, total cell number in BALF, and histopathological alteration were examined. The levels of TNF-α, IL-1β, IL-6, IL-18, IL-4, and IL-10 in serum, BALF, and supernatant were examined by ELISA. The mRNA expressions of iNOS, CD68, Arg1, Ym1, and CD206 and protein expressions of NAMPT, TLR2, CCR1, and NLRP3 inflammasome were detected by PCR, WB, and immunofluorescence. The NAMPT inhibitor FK866, TLR2 inhibitor C29, CCR1 inhibitor BX471, NAMPT-overexpression (OE) plasmid, and TLR2-OE plasmid were used for mechanism research. As a result, PAL relieved the symptoms of ALI. PAL inhibited M1 phenotype indices and promoted M2 phenotype indices in both LPS-induced mice and RAW264.7 cells. PAL also inhibited the expressions of NAMPT, TLR2, CCR1, and NLRP3 inflammasome. The treatments with FK866, NAMPT-OE plasmid, C29, TLR2-OE plasmid, and BX471 proved that PAL exerted its effect via NAMPT/TLR2/CCR1. Molecular docking suggested that PAL might combine with NAMPT. In conclusion, PAL ameliorated LPS-induced ALI by inhibiting M1 phenotype macrophage polarization via NAMPT/TLR2/CCR1 signaling.

CAS / MDL: 50-02-2 171869-95-7
研究领域: 药理学 · 免疫学 · 呼吸病学 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Sulfated polysaccharide from Apostichopus japonicus viscera exhibits anti-inflammatory properties in vitro and in vivo

Jing Ye,Linjing Zheng,Weipeng Pan,Yayan Huang,Na Zhang,Dongda Yang,Yucheng Yang,Bingde Zheng,Xueqin Zhang,Meitian Xiao

Polysaccharides from sea cucumbers are known for their biological activities, but little is known about those from sea cucumber viscera. The present study isolated a sulfated polysaccharide (SCVP-2) from the viscera of Apostichopus japonicas , which had a molecular weight of 209.1 kDa. SCVP-2 comprised 66.3 % total sugars, 2.1 % uronic acid, 4.5 % proteins, and 25.5 % sulfate groups, containing glucosamine, galactosamine, glucose, galactose, and fucose. FT-IR and NMR analyses identified SCVP-2 as a fucoidan sulfate with sulfation patterns of the fucose branches as Fuc2S, Fuc4S, and Fuc0S. SEM and AFM analyses showed irregular clusters and linear conformations. SCVP-2 demonstrated strong anti-inflammatory properties both in vitro and in vivo . In lipopolysaccharide (LPS)-induced inflammation in macrophage RAW264.7 cells, SCVP-2 significantly reduced nitric oxide (NO) and cytokine secretion (IL-1β, IL-6, TNF-α). Additionally, it downregulated the expression of these cytokine genes. Furthermore, the anti-inflammatory mechanism of SCVP-2 was related to the inhibition of the MAPKs and NF-κB pathways. SCVP-2's anti-inflammatory capacity was confirmed in acute inflammation models, including xylene-induced ear swelling and acetic acid-induced peritoneal capillary permeability, and in high-fat diet-induced systemic low-grade chronic inflammation. In conclusion, SCVP-2 exhibits significant anti-inflammatory activity, suggesting its potential for development as a functional food ingredient or therapeutic agent for inflammation-related diseases.

研究领域: 海洋生物学 · 药理学 · 免疫学
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Bioactive Materials · 2024 · IF 18

Protocol for engineering bone organoids from mesenchymal stem cells

Jian Wang,Dongyang Zhou,Ruiyang Li,Shihao Sheng,Guangfeng Li,Yue Sun,Peng Wang,Yulin Mo,Han Liu,Xiao Chen,Zhen Geng,Qin Zhang,Yingying Jing,Long Bai,Ke Xu,Jiacan Su

Bone organoids are emerging as powerful tools for studying bone development and related diseases. However, the simplified design of current methods somewhat limits their application potential, as these methods produce single-tissue organoids that fail to replicate the bone microarchitecture or achieve effective mineralization. To address this issue, we propose a three-dimensional (3D) construction strategy for generating mineralized bone structures using bone marrow-derived mesenchymal stem cells (BMSCs). By mixing BMSCs with hydrogel to create a bone matrix-mimicking bioink and employing projection-based light-curing 3D printing technology, we constructed 3D-printed structures, which were then implanted subcutaneously into nude mice, away from the native bone microenvironment. Even without external stimulation, these implants spontaneously formed mineralized bone domains. With long-term culture, these structures gradually matured into fully differentiated bone tissue, completing both mineralization and vascularization. This in vivo bone organoid model offers a novel platform for studying bone development, exploring congenital diseases, testing drugs, and developing therapeutic applications.

研究领域: 组织工程 · 再生医学 · 干细胞生物学 · 骨骼发育 · 药物测试
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CHEMICAL ENGINEERING JOURNAL · 2025 · IF 13.2

Extracellular matrix-mimetic hydrogel encapsulating myoblast exosomes attenuates muscle atrophy by targeting Nrf2-mitochondrial axis

Xuehui Deng,Xuchen Wang,Wenlong Xiao,Li Song,Qiaofeng Guo,Kai Huang,Nani Wang

The pathogenesis of sarcopenia, a geriatric syndrome associated with chronic glucocorticoid exposure, involves redox homeostasis dysregulation of skeletal muscle. There is an urgent need for targeted therapeutic strategies. In this study, we developed a thermosensitive hydrogel composed of skeletal muscle-derived decellularized extracellular matrix, chitosan, and β-glycerophosphate. This multifunctional platform was co-encapsulated with a nuclear factor erythroid 2-related factor 2 (Nrf2) agonist (bardoxolone) and myoblast-derived exosomes to synergistically enhance muscle regeneration. The injectable hydrogel exhibited rapid sol-gel transition at 37 °C and sustained bardoxolone release kinetics. In dexamethasone (Dex)-induced C2C12 myoblasts, the hydrogel effectively normalized atrophic markers (muscle-specific RING finger protein 1, muscle atrophy F-box protein), while upregulating myogenic factors (myoblast determination protein 1, myosin heavy chain, myosin heavy chain 7, and myogenin). Intramuscular administration of the hydrogel in Dex-treated mice ameliorated sarcopenic manifestations through enhanced skeletal muscle mass, grip strength, weight-loaded swimming time, rotating rod time, and myofiber cross-sectional area. Mechanistically, the hydrogel restored mitochondrial impairment in Dex-treated myoblasts through Nrf2 pathway activation, evidenced by upregulated nuclear Nrf2, translocase of outer mitochondrial membrane 20, voltage dependent anion channel 1, and recovered oxygen consumption rate. Crucially, complete therapeutic efficacy ablation in both in vitro and in vivo Nrf2-knockout models confirmed Nrf2 as the central regulatory hub. This hydrogel integrates extracellular matrix-mimetic architecture, controlled molecular release kinetics, and exosome-mediated cytoprotection, establishing a therapeutic strategy for sarcopenia management.

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FOOD RESEARCH INTERNATIONAL · 2025 · IF 8

Antioxidant and anti-inflammatory properties of Xianju wheat paste: A traditional condiment with functional food potential

Jinsong Che,Yi Zhang,Shida Li,Xiujuan Li

The antioxidant and anti-inflammatory properties of Xianju wheat paste (XJWP), a traditional condiment originating from Hubei Province, China, were evaluated for the first time. XJWP is an essential appetizer and condiment for local residents. It is also utilized for its anti-inflammatory properties in treating minor wounds in daily life, which suggests that it possesses bioactive properties, notably anti-inflammatory effects. In this study, five extracts of XJWP were obtained using different polar solvents, and all of them exhibited antioxidant activity through DPPH, •OH, ABTS free radical scavenging tests and ferric reducing antioxidant power. Subsequently, a lipopolysaccharide-induced RAW264.7 cell model was established to evaluate their anti-inflammatory effects. All of the XJWP extracts significantly inhibited NO secretion in the cells ( p  < 0.05), and ethyl acetate extract (XJ-EA) exhibited the most potent effect characterized by an EC 50 value of 61.92 μg/mL. At a concentration of 40 μg/mL, XJ-EA suppressed the overproduction of TNF-α, IL-6, and IL-1β to normal levels. The in vivo anti-inflammatory activity of XJ-EA was evaluated using a mouse model of ear edema induced by xylene exposure. The result revealed that high-dose XJ-EA reduced the ear edema rate in mice by 56 %, mitigated oxidative damage, inhibited the activity of COX-2 and iNOS, decreased the levels of prostaglandin E2 and NO, and achieved significant anti-inflammatory effects ( p  < 0.05). Qualitative analysis identified 21 potential anti-inflammatory components in XJ-EA, and molecular docking studies showed favorable interactions with iNOS and COX-2. These findings provide a theoretical foundation for the development of XJWP as a functional condiment, and even as a natural antioxidant and anti-inflammatory drug resource to improve public health and increase the economic value of this product.

CAS / MDL: 1330-20-7 50-02-2
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PHYTOMEDICINE · 2024 · IF 6.7

Gleditsiae Sinensis Fructus Ingredients and Mechanism in Anti-Asthmatic Bronchitis Research

Hongwei Li,Le Kang,Shirong Dou,Yiming Zhang,Yumei Zhang,Ning Li,Yangang Cao,Mengyun Liu,Deen Han,Kai Li,Weisheng Feng

Background Gleditsiae Sinensis Fructus (GSF) is commonly used in traditional medicine to treat respiratory diseases such as bronchial asthma. However, there is a lack of research on the chemical composition of GSF and the pharmacological substance and mechanism of action for GSF in treating bronchial asthma. Purpose The chemical constituents of GSF were analyzed using ultrahigh-performance liquid chromatography-quadrupole-Orbitrap high-resolution mass spectrometry (UHPLC-Q-Orbitrap HRMS). In this study, we combined network pharmacology, molecular docking techniques, and experimental validation to explore the therapeutic efficacy and underlying mechanism of GSF in the treatment of bronchial asthma. Methods Characterization of the chemical constituents of GSF was conducted using UHPLC-Q-Orbitrap HRMS. The identified chemical components were subjected to screening for active ingredients in the Swiss Absorption, Distribution, Metabolism, and Excretion (ADME) database. Relevant databases were utilized to retrieve target proteins for the active ingredients and targets associated with bronchial asthma disease, and the common targets between the two were selected. Subsequently, the protein-protein interaction (PPI) network was constructed using the String database and Cytoscape software to identify key targets. Gene Ontology (GO) and the Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were performed using the Metascape database. The "component-common target" network was constructed using Cytoscape to identify the primary active ingredients. Molecular docking validation was conducted using AutoDock software. The bronchial asthma mouse model was established using ovalbumin (OVA), and the lung organ index of the mice was measured. Lung tissue pathological changes were observed using hematoxylin and eosin (HE), Periodic Acid-Schiff (PAS), and Masson staining. The respiratory resistance (Penh) of the mice was assessed using a pulmonary function test instrument. An enzyme-linked immunosorbent assay (ELISA) was used to determine the levels of IgE, IL-4, IL-5, and IL-13 in the mouse serum. Immunofluorescence staining was performed to detect the protein expression levels of AKT and PI3K in the lung tissues. An in vitro experiment was performed to observe the effects of echinocystic acid (EA) on IL-4 stimulated Human ASMCs (hASMCs). Cell viability was measured using a CCK-8 assay to calculate the IC50 value of the EA. A wound healing test was conducted to observe the effect of EA on degree of healing. RT-qPCR was performed to detect the influence of EA on the mRNA expression levels of ALB, SRC, TNF-α, AKT1, and IL6 in the cells. Results A total of 95 chemical constituents were identified from the GSF. Of these, 37 were identified as active ingredients. There were 169 overlapping targets between the active ingredients and the disease targets. A topological analysis of the protein-protein interaction (PPI) network identified the core targets as IL6, TNF, ALB, AKT1, and SRC. An enrichment analysis revealed that the treatment of bronchial asthma with GSF primarily involved the AGE-RAGE signaling pathway and the PI3K-Akt signaling pathway, among others. The primary active ingredients included 13(s)-HOTRE, linolenic acid, and acacetin. The molecular docking results demonstrated a favorable binding activity between the critical components of GSF and the core targets. Animal experimental studies indicated that GSF effectively improved symptoms, lung function, and lung tissue pathological changes in the OVA-induced asthmatic mice, while alleviating inflammatory responses. GSF decreased the fluorescent intensity of the AKT and PI3K proteins. The IC50 value of EA was 30.02μg/ml. EA (30) significantly promoted the proliferation of IL4-stimulated hASMCs cells. EA (30) significantly increased the expression of ALB and SRC mRNA and decreased the expressions of TNF-α, AKT, and IL6 mRNA. Conclusion The multiple active ingredients found in GSF exerted their anti-inflammatory effects through multiple targets and pathways. This preliminary study revealed the core target and the mechanism of action underlying its treatment of bronchial asthma. These findings provided valuable insights for further research on the pharmacological substances and quality control of GSF.

CAS / MDL: 50-02-2
研究领域: 药理学 · 中药学 · 呼吸系统疾病 · 分子生物学 · 生物信息学
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JOURNAL OF CONTROLLED RELEASE · 2024 · IF 10.5

FRET-based analysis on the fate of liposome and cyclodextrin@liposome nanocomposites from ocular surface to the posterior segment of the eye

Xiaomeng Zhu,Shihang Li,Jiahui Huang,Chengjing Yin,Yanting Li,Wei Guo,Feng Jiang,Feng Cao

Investigating the structural integrity of nanocarriers in vivo is vital for exploring the fate of nanocarriers from ocular surface to the posterior segment of the eye. Most of the published studies adopted the structural integrity ratio of nanocarriers to determine the fate of them, which lacked scientific support. In this study, two methods were used to explore the factors which affected the structural integrity of liposomes. A new method with the standard curve of FRET fluorescence intensity and carbocyanine 7 (Cy7) content was drawn for the first time. Secondly, we used the traditional method of drawing the standard curve of FRET fluorescence efficiency and structural integrity ratios. The results showed that liposomes with particle size about 120 nm, positively charged, polyethyleneglycol 5000 (PEG 5000 ) and glycine sarcosine (GS) modified had the highest Cy7 content in rabbit tissues. When the dosage of Cy7 was 25 μg, at 60 min, the content of Cy7 in intact liposomes and the structural integrity ratio of liposomes in sclera was 210.5 ± 14.9 ng and 19.8 ± 5.3 %, respectively. Compared with the structural integrity ratio, the Cy7 content in the intact carrier could better estimate the fate of nanocarriers in vivo scientifically. On this basis, the fate of dual-carrier nanocomposites and the inner cyclodextrin complexes in vivo was investigated. The intact cyclodextrin complexes could reach choroid-retina with the protection of outer liposomes. The structural integrity ratios of liposomes were also studied after crossing human conjunctival epithelial cells (HConEpiC) monolayer, but in vitro cellular experiments could not simulate the real situation in vivo . Finally, the tissue distribution of nanocomposites was studied in rabbit eyes. The concentration of dexamethasone (Dex) in choroid-retina was 158 ± 23 ng/g after 3 h, which exhibited better drug delivery ability compared with our previous study. Overall, the present study provides a new scientific method to estimate the structural integrity in vivo , which is beneficial for the rational design of drug delivery systems with more structural integrity in vivo and higher drug delivery efficiency.

研究领域: 药剂学 · 眼科学 · 生物医学工程
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