Publications by authors named "Jinsong Tao"

18 Publications

  • Page 1 of 1

Disintegrable, transparent and mechanically robust high-performance antimony tin oxide/nanocellulose/polyvinyl alcohol thermal insulation films.

Carbohydr Polym 2021 Aug 7;266:118175. Epub 2021 May 7.

State Key Lab of Pulp and Paper Engineering, South China University of Technology, Guangzhou 510640, China. Electronic address:

Polymer-based thermal insulation films are widely utilized to reduce the influence of solar radiation. However, current thermal insulation films face several challenges from poor thermal insulation performance and severe environmental pollution, which are caused by the non-disintegratability of polymer substrates. Here, cellulose nanofiber (CNF)/antimony tin oxide (ATO) hybrid films with and without polyvinyl alcohol (PVA) are presented and they can be used as window thermal barrier films and personal thermal management textiles. The hybrid films exhibit prominent thermal insulation performance, blocking 91.07% ultraviolet(UV) light, reflecting 95.19% near-infrared(NIR) light, and transmitting 44.89% visible(VIS) light. Meanwhile, the hybrid films demonstrate high thermal stability, high anti-UV aging stability, and robust mechanical properties. Moreover, the used-up hybrid films based on natural cellulose are of high disintegratability and recyclability. Our present work is anticipated to open up a new avenue for the fabrication of next-generation high-performance thermal insulation films with sustainable and environmentally friendly processes.
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http://dx.doi.org/10.1016/j.carbpol.2021.118175DOI Listing
August 2021

Uptake and trafficking of different sized PLGA nanoparticles by dendritic cells in imiquimod-induced psoriasis-like mice model.

Acta Pharm Sin B 2021 Apr 20;11(4):1047-1055. Epub 2020 Nov 20.

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao 999078, China.

Psoriasis is an autoimmune inflammatory disease, where dendritic cells (DCs) play an important role in its pathogenesis. In our previous work, we have demonstrated that topical delivery of curcumin-loaded poly (lactic--glycolic acid) (PLGA) nanoparticles (NPs) could treat Imiquimod (IMQ)-induced psoriasis-like mice. The objective of this study is to further elucidate biofate of PLGA NPs after intradermal delivery including DCs uptake, and their further trafficking in psoriasis-like mice model by using fluorescence probes. Two-sized DiO/DiI-loaded PLGA NPs of 50 ± 4.9 nm (S-NPs) and 226 ± 7.8 nm (L-NPs) were fabricated, respectively. cellular uptake results showed that NPs could be internalized into DCs with intact form, and DCs preferred to uptake larger NPs. Consistently, study showed that L-NPs were more captured by DCs and NPs were firstly transported to skin-draining lymph nodes (SDLN), then to spleens after 8 h injection, whereas more S-NPs were transported into SDLN and spleens. Moreover, FRET imaging showed more structurally intact L-NPs distributed in skins and lymph nodes. In conclusion, particle size can affect the uptake and trafficking of NPs by DCs in skin and lymphoid system, which needs to be considered in NPs tailing to treat inflammatory skin disease like psoriasis.
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http://dx.doi.org/10.1016/j.apsb.2020.11.008DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8105876PMC
April 2021

Correlations and Prognostic Roles of the Nutritional Status and Neutrophil-to-lymphocyte Ratio in Elderly Patients with Acute Myocardial Infarction Undergoing Primary Coronary Intervention.

Int Heart J 2020 Nov 28;61(6):1114-1120. Epub 2020 Oct 28.

Department of Cardiology, Jiangyin Hospital Affiliated to Medical College of Southeast University.

The prognostic capacities of nutritional status and inflammation in patients with acute myocardial infarction (AMI) have attracted increasing interest. However, the combined usefulness of the Controlling Nutritional Status (CONUT) score and neutrophil-to-lymphocyte ratio (NLR) in predicting adverse outcomes has not been investigated. The aim of our study was to investigate the relationship between the CONUT score and the NLR in patients with AMI and assessing the potential of these factors as prognostic markers.In this retrospective study, we reviewed the medical records of consecutive patients aged 65 years or older who were diagnosed with AMI and who underwent primary coronary intervention. We assessed the nutritional and inflammatory statuses using the CONUT score and the NLR, respectively. The NLR and CONUT score in the major adverse cardiovascular event (MACE) (+) patients were significantly higher than those in the MACE (-) patients. The areas under the receiver operating characteristic curves of the NLR and CONUT score were 0.71 and 0.77, respectively. The Kaplan-Meier analysis showed that patients with a high NLR (≥6.07) and CONUT score (≥3.5) had the worst prognoses. The multivariate Cox proportional hazards analyses suggested that the CONUT score was an independent predictor.The CONUT score was proven to be a significant prognostic factor of clinical outcomes in patients with AMI. However, further research in this area is needed to more fully understand the relationship among nutritional status, inflammation, and cardiovascular diseases, which might help reduce MACEs in patients with AMI.
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http://dx.doi.org/10.1536/ihj.20-138DOI Listing
November 2020

Highly Thermally Stable, Green Solvent Disintegrable, and Recyclable Polymer Substrates for Flexible Electronics.

Macromol Rapid Commun 2020 Oct 24;41(19):e2000292. Epub 2020 Aug 24.

State Key Lab of Pulp and Paper Engineering, South China University of Technology, Guangzhou, 510640, China.

Flexible electronics require its substrate to have adequate thermal stability, but current thermally stable polymer substrates are difficult to be disintegrated and recycled; hence, generate enormous electronic solid waste. Here, a thermally stable and green solvent-disintegrable polymer substrate is developed for flexible electronics to promote their recyclability and reduce solid waste generation. Thanks to the proper design of rigid backbones and rational adjustments of polar and bulky side groups, the polymer substrate exhibits excellent thermal and mechanical properties with thermal decomposition temperature (T ) of 430 °C, upper operating temperature of over 300 °C, coefficient of thermal expansion of 48 ppm K , tensile strength of 103 MPa, and elastic modulus of 2.49 GPa. Furthermore, the substrate illustrates outstanding optical and dielectric properties with high transmittance of 91% and a low dielectric constant of 2.30. Additionally, it demonstrates remarkable chemical and flame resistance. A proof-of-concept flexible printed circuit device is fabricated with this substrate, which demonstrates outstanding mechanical-electrical stability. Most importantly, the substrate can be quickly disintegrated and recycled with alcohol. With outstanding thermally stable properties, accompanied by excellent recyclability, the substrate is particularly attractive for a wide range of electronics to reduce solid waste generation, and head toward flexible and "green" electronics.
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http://dx.doi.org/10.1002/marc.202000292DOI Listing
October 2020

Toward understanding the prolonged circulation and elimination mechanism of crosslinked polymeric micelles in zebrafish model.

Biomaterials 2020 10 25;256:120180. Epub 2020 Jun 25.

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, China. Electronic address:

Understanding the behaviors of nanomedicines in vivo is one of the most important prerequisites for the design and optimization of nanomedicines. However, the in vivo tracking of nanomedicines in rodents is severely limited by the restricted imaging possibilities within these animals. To meet these needs, the FRET (fluorescence or Förster resonance energy transfer) imaging combined with visual zebrafish larvae model (7 dpf) was used to study the behaviors of polymeric micelles in vivo at high spatiotemporal resolution. Firstly, the FRET ordinary Pluronic micelles (OPMs) and disulfide bond crosslinked Pluronic micelles (CPMs) were synthesized to quantify their integrity in vitro and in vivo by FRET ratio. The behaviors and integrity of OPMs and CPMs in vivo were visually investigated in zebrafish larvae across the entire living organism and at cellular molecular level after intravenous microinjection. Results showed that OPMs were rapidly disassociated in circulation, then largely sequestrated by the endothelial cells (ECs) of caudal vein (CV) and liver in zebrafish larvae, which resulted in quick elimination from blood circulation. While the CPMs were more stable and escaped the sequestration by ECs of CV and liver, which prolonged their circulation in blood. Moreover, we pioneered to use the zebrafish model to reveal that polymeric micelles were eliminated through hepatobiliary pathway after disassociation. While the intact micelles were relatively difficult to eliminate. We further verified that the scavenger receptors of ECs but not the macrophages mainly mediated the elimination of polymeric micelles in CV and liver of zebrafish larvae. These finding on behaviors and elimination mechanisms of polymeric micelles in zebrafish model could contribute to the rational design and optimization of nanomedicines, further guide their studies in rodents.
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http://dx.doi.org/10.1016/j.biomaterials.2020.120180DOI Listing
October 2020

MiR-216a accelerates proliferation and fibrogenesis via targeting PTEN and SMAD7 in human cardiac fibroblasts.

Cardiovasc Diagn Ther 2019 Dec;9(6):535-544

Emergency Center, Kizilsu Kirghiz Autonomous Prefecture People's Hospital, Artux 845350, China.

Background: Heart failure (HF) is a progressive disease with relatively poor prognosis and lacks effective therapy, and the discovery of dysregulated microRNAs (miRNAs) and their role in cardiac fibroblasts have provided a new avenue for elucidating the mechanism involved in HF.

Methods: Two datasets of GSE53080 and GSE57338 were used to screen the miRNAs profiling and analysis the differentially expressed genes (DEGs) in HF. QRT-PCR was used to detect miR-216a between HF and healthy controls (HC). Cell counting kit-8 (CCK-8) assay and clonogenic assay were used to analyze the effect of proliferation and fibrogenesis. Then dual-luciferase activity assay and western blotting were used to confirm the key mechanism.

Results: In this study, the results showed that miR-216a was significantly up-regulated in HF and over-expression of miR-216a promoted proliferation and enhanced the fibrogenesis in the human cardiac fibroblasts (HCF) cells. Phosphatase and tensin homolog (PTEN) and mothers against decapentaplegic homolog 7 (SMAD7) were both validated as the direct target genes of miR-216a, which were confirmed by the dual-luciferase reporter assay. MiR-216a decreased the expression of PTEN and SMAD7 leading to the activation of Akt/mTOR and TGF-βRI/Smad2 in the HCF cells, which might act as a promoter of cardiac fibrosis.

Conclusions: Our study might provide a promising approach for the treatment of HF in the future.
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http://dx.doi.org/10.21037/cdt.2019.11.06DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6987511PMC
December 2019

Highly Transparent, Highly Thermally Stable Nanocellulose/Polymer Hybrid Substrates for Flexible OLED Devices.

ACS Appl Mater Interfaces 2020 Feb 14;12(8):9701-9709. Epub 2020 Feb 14.

CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, CAS Center for Excellence in Nanoscience , National Center for Nanoscience and Technology , Beijing 100190 , China.

Flexible organic light-emitting diode (OLED) devices based on polymer substrates have attracted worldwide attention. However, the current OLED polymer substrates are limited due to weak thermal stability, which is not compatible with the high temperature in OLED fabrication. Here, we developed a novel nanocellulose/polyarylate (PAR) hybrid polymer substrate with both high transparency and excellent thermal properties. Benefiting from the nanometer scale of the cellulose nanofibrils (CNFs) and the efficient interfacial interaction with PAR, the substrate exhibited greatly improved thermal stability, with a glass transition temperature of 192 °C, the thermal decomposition temperature of 501 °C, and upper operating temperature up to over 220 °C. Meanwhile, the hybrid substrate exhibits outstanding mechanical properties. Notably, no apparent transparency loss was observed after the CNF addition, and the hybrid substrate maintains a high transmittance of 85% and a low haze of 1.75%@600 nm. Moreover, OLED devices fabricated on the hybrid substrates exhibit a much improved optoelectrical performance than that of the devices fabricated on the conventional poly(ethylene terephthalate) (PET) substrates. We anticipate this research will open up a new route for fabricating flexible high-performance OLEDs.
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http://dx.doi.org/10.1021/acsami.0c01048DOI Listing
February 2020

Binding Conductive Ink Initiatively and Strongly: Transparent and Thermally Stable Cellulose Nanopaper as a Promising Substrate for Flexible Electronics.

ACS Appl Mater Interfaces 2019 Jun 24;11(22):20281-20290. Epub 2019 May 24.

State Key Lab of Pulp and Paper Engineering , South China University of Technology , Guangzhou 510640 , China.

For flexible electronics, the substrates play key roles in ensuring their performance. However, most substrates suffer from weak bonding with the conductive ink and need additional aids. Here, inspired by the Ag-S bond theory, a novel cellulose nanopaper substrate is presented to improve the bond strength with the Ag nanoparticle ink through a facile printing method. The substrate is fabricated using thiol-modified nanofibrillated cellulose and exhibits excellent optical properties (∼85%@550 nm), ultra-small surface roughness (3.47 nm), and high thermal dimensional stability (up to at least 90 °C). Most importantly, it can attract Ag nanoparticles initiatively and bind them firmly, which enable the conductive ink to be printed without using the ink binder and form a strong substrate-ink bonding and maintain a stable conductivity of 2 × 10 Ω cm even after extensive peeling and bending. This work may lead to exploring new opportunities to fabricate high-performance flexible electronics using the newly developed nanopaper substrate.
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http://dx.doi.org/10.1021/acsami.9b04596DOI Listing
June 2019

NPC1L1-Targeted Cholesterol-Grafted Poly(β-Amino Ester)/pDNA Complexes for Oral Gene Delivery.

Adv Healthc Mater 2019 04 18;8(8):e1800934. Epub 2019 Feb 18.

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, No. 501 Haike Road, Shanghai, 201203, P. R. China.

Gene vectors for oral delivery encounter harsh conditions throughout the gastrointestinal tract, and the continuous peristaltic activity can quickly remove the vectors, leading to inefficient intestinal permeation. Therefore, vectors have demanding property requirements, such as stability under various pH and, more importantly, efficient uptake in different intestinal segments. In this study, a functional polymer, cholesterol-grafted poly(β-amino ester) (poly[hexamethylene diacrylate-β-(5-amino-1-pentanol)] (CH-PHP)), is synthesized and electrostatically interacted with plasmid DNA to form a CH-PHP/DNA complex (CPNC). This complex is designed to target the Niemann-Pick C1-like receptor, a cholesterol receptor, to improve oral gene delivery efficacy. With the presence of cholesterol, CH-PHP shows mitigated cytotoxicity, enhanced enzyme resistance, and improved gene condensing ability. CPNC further contributes to ≈43.1- and 2.3-fold increases in luciferase expression in Caco-2 cells compared with PNC and Lipo 2000/DNA complexes, respectively. In addition, the in vivo transfection efficacy of CPNC is ≈4.1-, 2.1-, and 1.6-fold higher than that of Lipo 2000/DNA complexes in rat duodenum, jejunum, and ileum, respectively. Therefore, CPNC may be a promising delivery vector for gene delivery, and using a cholesterol-specific endocytic pathway can be a novel approach to achieve efficient oral gene transfection.
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http://dx.doi.org/10.1002/adhm.201800934DOI Listing
April 2019

Application of flash nanoprecipitation to fabricate poorly water-soluble drug nanoparticles.

Acta Pharm Sin B 2019 Jan 14;9(1):4-18. Epub 2018 Nov 14.

State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Science, University of Macau, Macau, China.

Nanoparticles are considered to be a powerful approach for the delivery of poorly water-soluble drugs. One of the main challenges is developing an appropriate method for preparation of drug nanoparticles. As a simple, rapid and scalable method, the flash nanoprecipitation (FNP) has been widely used to fabricate these drug nanoparticles, including pure drug nanocrystals, polymeric micelles, polymeric nanoparticles, solid lipid nanoparticles, and polyelectrolyte complexes. This review introduces the application of FNP to produce poorly water-soluble drug nanoparticles by controllable mixing devices, such as confined impinging jets mixer (CIJM), multi-inlet vortex mixer (MIVM) and many other microfluidic mixer systems. The formation mechanisms and processes of drug nanoparticles by FNP are described in detail. Then, the controlling of supersaturation level and mixing rate during the FNP process to tailor the ultrafine drug nanoparticles as well as the influence of drugs, solvent, anti-solvent, stabilizers and temperature on the fabrication are discussed. The ultrafine and uniform nanoparticles of poorly water-soluble drug nanoparticles prepared by CIJM, MIVM and microfluidic mixer systems are reviewed briefly. We believe that the application of microfluidic mixing devices in laboratory with continuous process control and good reproducibility will be benefit for industrial formulation scale-up.
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http://dx.doi.org/10.1016/j.apsb.2018.11.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6361851PMC
January 2019

SnS hollow nanofibers as anode materials for sodium-ion batteries with high capacity and ultra-long cycling stability.

Chem Commun (Camb) 2019 Jan;55(4):505-508

Key Laboratory of Textile Science and Technology, Ministry of Education, College of Textiles, Donghua University, Shanghai, 201620, China.

In this study, a novel anode material of SnS hollow nanofibers (SnS HNFs) was rationally synthesized by a facile process and demonstrated to be a promising anode candidate for sodium-ion batteries. The synergetic effect of unique hollow and porous microstructures of SnS HNFs led to high capacity and ultra-long cycling stability.
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http://dx.doi.org/10.1039/c8cc07332eDOI Listing
January 2019

Electrospun Kraft Lignin/Cellulose Acetate-Derived Nanocarbon Network as an Anode for High-Performance Sodium-Ion Batteries.

ACS Appl Mater Interfaces 2018 Dec 14;10(51):44368-44375. Epub 2018 Dec 14.

Fiber and Polymer Science Program, Department of Textile Engineering, Chemistry and Science , North Carolina State University , Raleigh , North Carolina 27695-8301 , United States.

An innovative nanocarbon network material was synthesized from electrospun kraft lignin and cellulose acetate blend nanofibers after carbonization at 1000 °C in a nitrogen atmosphere, and its electrochemical performance was evaluated as an anode material in sodium-ion batteries. Apart from its unique network architecture, introduced carbon material possesses high oxygen content of 13.26%, wide interplanar spacing of 0.384 nm, and large specific surface area of 540.95 m·g. The electrochemical test results demonstrate that this new nanocarbon network structure delivers a reversible capacity of 340 mA h·g at a current density of 50 mA·g after 200 cycles and exhibits a high rate capacity by delivering a capacity of 103 mA h·g at an increased current density of 400 mA·g. The present work rendered an innovative approach for preparing nanocarbon materials for energy-storage applications and could open up new avenues for novel nanocarbon fabrication from green and environmentally friendly raw materials.
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http://dx.doi.org/10.1021/acsami.8b13033DOI Listing
December 2018

A panel of seven-miRNA signature in plasma as potential biomarker for colorectal cancer diagnosis.

Gene 2019 Mar 17;687:246-254. Epub 2018 Nov 17.

Department of Oncology, First Affiliated Hospital of Nanjing Medical University, Nanjing 210029, PR China; Department of Oncology, The Affiliated Jiangsu Shengze Hospital of Nanjing Medical University, Suzhou 215000, PR China. Electronic address:

Colorectal cancer (CRC) has been one of the most commonly diagnosed cancers in global. The differential expression profiles of microRNAs (miRNAs) in CRC plasma of patients have the potential to serve as a diagnostic biomarker. We conducted a four-stage study to identify the potential plasma miRNAs for CRC detection. In the initial screening phase, Exiqon panel (miRCURY-Ready-to-Use-PCR-Human-panel-I + II-V1.M) including 3 CRC pools and 1 normal controls (NCs) pool were applied to acquire miRNA profiles. In the training stage (30 CRC VS. 30 NCs) and testing stage (79 CRC VS. 76 NCs), quantitative real-time polymerase chain reaction (qRT-PCR) was utilized to conduct candidate miRNA profiles. Then the identified miRNAs were verified in external validation stage (30 CRC VS. 26 NCs). Expression levels of identified miRNAs were assessed in tissue samples (24 pairs) and plasma exosomes (18 CRC VS. 18 NCs). Receiver operating characteristic (ROC) curves were constructed to evaluate the diagnostic accuracy. Seven miRNAs (miR-103a-3p, miR-127-3p, miR-151a-5p, miR-17-5p, miR-181a-5p, miR-18a-5p and miR-18b-5p) were significantly overexpressed in CRC compared with NCs. Area under the ROC curve of the seven-miRNA signature was 0.762, 0.824 and 0.895 for the training, testing and the external validation stages, respectively. Additionally, miR-103a-3p, miR-127-3p, miR-17-5p and miR-18a-5p were discovered significantly up-regulated in CRC tissues; while miR-17-5p, miR-181a-5p, miR-18a-5p and miR-18b-5p were significantly elevated in CRC plasma exosomes. In conclusion, we established a seven-miRNA signature in the peripheral plasma for CRC detection.
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http://dx.doi.org/10.1016/j.gene.2018.11.055DOI Listing
March 2019

Self-Assembled Core-Shell-Type Lipid-Polymer Hybrid Nanoparticles: Intracellular Trafficking and Relevance for Oral Absorption.

J Pharm Sci 2017 10 27;106(10):3120-3130. Epub 2017 May 27.

Department of Pharmaceutics, School of Pharmacy, Chongqing Medical University, Chongqing 400016, China. Electronic address:

Lipid-polymer hybrid nanoparticles (NPs) are advantageous for drug delivery. However, their intracellular trafficking mechanism and relevance for oral drug absorption are poorly understood. In this study, self-assembled core-shell lipid-polymer hybrid NPs made of poly(lactic-co-glycolic acid) (PLGA) and various lipids were developed to study their differing intracellular trafficking in intestinal epithelial cells and their relevance for oral absorption of a model drug saquinavir (SQV). Our results demonstrated that the endocytosis and exocytosis of hybrid NPs could be changed by varying the kind of lipid. A glyceride mixture (hybrid NPs-1) decreased endocytosis but increased exocytosis in Caco-2 cells, whereas the phospholipid (E200) (hybrid NPs-2) decreased endocytosis but exocytosis was unaffected as compared with PLGA nanoparticles. The transport of hybrid NPs-1 in cells involved various pathways, including caveolae/lipid raft-dependent endocytosis, and clathrin-mediated endocytosis and macropinocytosis, which was different from the other groups of NPs that involved only caveolae/lipid raft-dependent endocytosis. Compared with that of the reference formulation (nanoemulsion), the oral absorption of SQV-loaded hybrid NPs in rats was poor, probably due to the limited drug release and transcytosis of NPs across the intestinal epithelium. In conclusion, the intracellular processing of hybrid NPs in intestinal epithelia can be altered by adding lipids to the NP. However, it appears unfavorable to use PLGA-based NPs to improve oral absorption of SQV compared with nanoemulsion. Our findings will be essential in the development of polymer-based NPs for the oral delivery of drugs with the purpose of improving their oral absorption.
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http://dx.doi.org/10.1016/j.xphs.2017.05.029DOI Listing
October 2017

A Decision-Based Modified Total Variation Diffusion Method for Impulse Noise Removal.

Comput Intell Neurosci 2017 27;2017:2024396. Epub 2017 Apr 27.

School of Electrical Engineering, Wuhan University, Wuhan 430072, China.

Impulsive noise removal usually employs median filtering, switching median filtering, the total variation method, and variants. These approaches however often introduce excessive smoothing and can result in extensive visual feature blurring and thus are suitable only for images with low density noise. A new method to remove noise is proposed in this paper to overcome this limitation, which divides pixels into different categories based on different noise characteristics. If an image is corrupted by salt-and-pepper noise, the pixels are divided into corrupted and noise-free; if the image is corrupted by random valued impulses, the pixels are divided into corrupted, noise-free, and possibly corrupted. Pixels falling into different categories are processed differently. If a pixel is corrupted, modified total variation diffusion is applied; if the pixel is possibly corrupted, weighted total variation diffusion is applied; otherwise, the pixel is left unchanged. Experimental results show that the proposed method is robust to different noise strengths and suitable for different images, with strong noise removal capability as shown by PSNR/SSIM results as well as the visual quality of restored images.
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http://dx.doi.org/10.1155/2017/2024396DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5426081PMC
March 2018

Wheat germ agglutinin nanocage stabilized drug nanocrystals cross intestinal epithelium barrier via goblet cells.

J Control Release 2015 Sep 19;213:e25-6. Epub 2015 Aug 19.

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China. Electronic address:

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http://dx.doi.org/10.1016/j.jconrel.2015.05.039DOI Listing
September 2015

Supersaturated polymeric micelles for oral cyclosporine A delivery: The role of Soluplus-sodium dodecyl sulfate complex.

Colloids Surf B Biointerfaces 2016 May 29;141:301-310. Epub 2016 Jan 29.

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, No. 501, Haike Road, Zhang Jiang Hi-Tech Park, Pudong, Shanghai 201203, China. Electronic address:

Our previous study demonstrated that the retention of drug in the hydrophobic core of Soluplus micelle greatly impeded drug absorption from gastrointestinal tract. Using supersaturated polymeric micelles can improve drug release, however, insufficient maintaining of supersaturation of drug is still unfavorable for drug absorption. Here, we report adding small amount of small molecule, sodium dodecyl sulfate (SDS), to Soluplus solution can form a Soluplus-SDS complex. This complex not only showed a higher solubilization capability for the model drug cyclosporine A (CsA), but also maintained a longer period of and higher supersaturation than was achieved with Soluplus alone. The Soluplus-SDS interactions were characterized by analyzing surface tension, small-angle X-ray scattering (SAXS), fluorescence spectra, and nuclear magnetic resonance spectroscopy. The results demonstrated that the formation of Soluplus-SDS complex via SDS adsorption on hydrophobic segments of Soluplus, which have more hydrophobic domain than that of Soluplus micelle, contributed significantly to the solubilization and stabilization of supersaturated CsA. Using this amphiphilic copolymer-small molecule surfactant system, the cellular uptake and rat in vivo absorption of CsA were more effectively achieved than pure Soluplus. The area under the plasma concentration-time curve (AUC) and the maximal plasma concentration (Cmax) achieved by CsA-loaded Soluplus-SDS complex were 1.58- and 1.8-times higher than the corresponding values for CsA-loaded pure Soluplus, respectively. This study highlighted the benefits of Soluplus-SDS complex for optimizing the solubilization and oral absorption of a drug with low aqueous solubility.
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http://dx.doi.org/10.1016/j.colsurfb.2016.01.047DOI Listing
May 2016

Enhanced transport of nanocage stabilized pure nanodrug across intestinal epithelial barrier mimicking Listeria monocytogenes.

Biomaterials 2015 Jan 25;37:320-32. Epub 2014 Oct 25.

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai 201203, China. Electronic address:

Ligand grafted nanoparticles have been shown to enhance drug transport across epithelium barrier and are expected to improve drug delivery. However, grafting of these ligands to the surface of pure nanodrug, i.e., nanocrystals (NCs), is a critical challenge due to the shedding of ligands along with the stabilizer upon high dilution or dissolving of the drug. Herein, a non-sheddable nanocage-like stabilizer was designed by covalent cross-linking of poly(acrylic acid)-b-poly(methyl acrylate) on drug nanocrystal surface, and a ligand, wheat germ agglutinin (WGA), was successfully anchored to the surface of itraconazole (ITZ) NCs by covalent conjugation to the nanocage (WGA-cage-NCs). The cellular study showed that large amount of WGA-cage-NCs were adhered to Caco-2 cell membrane, and invaded into cells, resulting in a higher drug uptake than that of ordinary NCs (ONCs). After oral administration to rats, WGA-cage-NC were largely accumulated on the apical side of epithelium cells, facilitating drug diffusing across epithelium barrier. Interestingly, WGA-cage-NCs were capable of invading rat intestinal villi and reaching to lamina propria by transcytosis across goblet cells, which behaved like a foodborne pathogen, Listeria monocytogenes. The WGA-cage-NCs showed an improved oral bioavailability, which was 17.5- and 2.41-folds higher than that of coarse crystals and ONCs, respectively. To our best knowledge, this may represent the first report that a functional ligand was successfully anchored to the surface of pure nanodrug by using a cage-like stabilizer, showing unique biological functions in gastrointestinal tract and having an important significance in oral drug delivery.
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http://dx.doi.org/10.1016/j.biomaterials.2014.10.038DOI Listing
January 2015
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