BIOCONJUGATE CHEMISTRY
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2017
·
IF 4.818
Zhu Jiang,Qixian Chen,Xi Yang,Xiyi Chen,Zhen Li,De-E Liu,Wei Li,Yingjie Lei,Hui Gao
Tetraphenylene (TPE), characterized as a lipophilic and aggregation-induced-emissive fluorophore, was used to incorporate into an electrostatic self-assembled polyethylenimine-poly(ethylene glycol) (PEI–PEG)/plasmid DNA (pDNA) complexed micelle. The hydrophobic character of TPE appeared to drive a higher degree of condensation of the pDNA payload, which consequently resulted in not only strengthened colloidal stability of the constructed polyplex micelle but also improved biocompatibility by virtue of the elevated PEG crowdedness owing to the TPE-induced collapse of pDNA. These beneficial consequences potentially permitted a larger number of polyplex micelles to be internalized into the cells. PEG segments were designed to enable selective detachment from polyplex micelles in acidic milieu, e.g., the tumor microenvironment, and intracellular endosome compartment, based on the strategic arrangement of acid-responsive cleavable linkage between PEG and PEI. Upon PEG detachment, the exposure of cationic PEI/TPE polyplex was allowed to directly interact with the cell membrane, endosome membrane, and charged intracellular species, thus promoting cell internalization, endosome escape, and the release of the pDNA payload. Of note, this association of cationic PEI/TPE polyplex with the endosomal membrane could be further facilitated with the aid of lipophilic TPE, thereby eliciting pronounced destabilization potency to the endosome membrane and exerting an endosomal escape function. Eventually, the proposed system of these facile strategies, including responsive PEG detachment and functional TPE incorporation, was proven to provide efficient gene expression in the targeted tumors with an appreciable safety profile via systemic administration.
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Journal of Physical Chemistry C
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2017
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IF 4.536
Shi Gang Liu,Ting Liu,Na Li,Shuo Geng,Jing Lei Lei,Nian Bing Li,Hong Qun Luo
A kind of nonconjugated polymer dot possessing autofluorescence was synthesized by hyperbranched polyethylenimine and salicylaldehyde via environmentally friendly imine cross-linking and self-assembly in the aqueous phase. Both fluorescence and ultraviolet–visible (UV–vis) absorption of the polymer dots showed a sensitive and reversible response to pH. The mechanism of pH-dependent optical properties was investigated. The existence of two proton-responsive functional groups (phenolic hydroxyl groups and amine groups) on the polymer dot surface is crucial. The pH-dependent fluorescence is ascribed to electron transfer, which is controlled by the protonation degree of amine groups, while the pH-dependent UV–vis absorption is induced by ionization of phenolic hydroxyl groups. Based on the pH-mediated optical properties, a colorimetric and fluorescent dual-signal pH sensor and multiple logic gates were developed. The fluorescent nonconjugated polymer dots with easy preparation and sensitive response to pH are very promising for applications in biological, pharmaceutical, and material science fields.
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ACTA PHARMACOLOGICA SINICA
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2017
·Vol. 38
·期 12
·1655-1662
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IF 3.223
Dong Xin-yue,Lang Tian-qun,Yin Qi,Zhang Peng-cheng,Li Ya-ping
Breast cancer is the most vicious killer for women, and tumor metastasis is one of the leading causes of breast cancer therapy failure. In this study, a new pH-sensitive polymer (polyethylene glycol-block-poly[(1,4-butanediol)-diacrylate-β-N,N-diisopropylethylenediamine], BDP) was synthesized. Based on BDP, docetaxel/silibinin co-delivery micelles (DSMs) was constructed. DSM had a well-defined spherical shape under the transmission electron microscope with average hydrodynamic diameter of 85.3±0.4 nm, and were stable in the bloodstream but could dissociate to release the chemotherapeutic agents in the low pH environment of the endo/lysosomes in the tumor cells. Compared with free drugs, DSM displayed greatly enhanced cellular uptake, higher cytotoxicity and a stronger anti-metastasis effect against mouse breast cancer cell line 4T1. In 4T1 tumor-bearing mice treated with DSM (twice a week for 3 weeks), the inhibition rate on tumor growth and metastasis reached 71.9% and 80.1%, respectively. These results reveal that DSM might be a promising drug delivery system for metastatic breast cancer therapy.
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FOOD HYDROCOLLOIDS
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2017
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IF 4.747
Meng Wang,Mei-qin Feng,Kun Jia,Jian Sun,Xing-lian Xu,Guang-hong Zhou
This study investigated the effects of flaxseed gum (FG) concentrations (0.1–0.5%, w/w) and pH values (5.0, 6.0 and 7.0) on the stability of 10% (w/w) liquid lard emulsions. The emulsions were analyzed for particle size, rheological properties, creaming stability, optical microscopy and nuclear magnetic resonance (NMR) measurement. With the increase of FG concentration, there was an improved packing of polysaccharide onto the droplet surface, which caused a significant reduction in particle size, with the smallest oil droplets being formed in 0.5% (w/w) FG emulsions. Rheological and creaming stability measurements showed that FG solutions had thickening and gelling properties. When FG concentration increased to greater than 0.3% (w/w), the samples no longer exhibited creaming behavior, and pH values no longer had significant effect on the emulsion stability. Shorter spin-spin relaxation time (T 2 , by low-field 1 H NMR) were observed for emulsions containing 0.1% (w/w) and 0.2% (w/w) FG, suggesting more restriction of mobility of oil droplets. The increased line-width in high-field 1 H, 13 C NMR spectra with increasing FG concentration indicated an increased interaction between FG and oil molecules. These results showed that FG had the potential to substitute for protein emulsifiers which is sensitive to pH to stabilize the emulsion-type products.
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LANGMUIR
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2016
·
IF 3.993
Shi Gang Liu,Na Li,Yu Ling,Bei Hua Kang,Shuo Geng,Nian Bing Li,Hong Qun Luo
We report that fluorescence properties and morphology of hyperbranched polyethylenimine (hPEI) cross-linked with formaldehyde are highly dependent on the pH values of the cross-linking reaction. Under acidic and neutral conditions, water-soluble fluorescent copolymer particles (CPs) were produced. However, under basic conditions, white gels with weak fluorescence emission would be obtained. The water-soluble hPEI-formaldehyde (hPEI-F) CPs show strong intrinsic fluorescence without the conjugation to any classical fluorescent agents. By the combination of spectroscopy and microscopy techniques, the mechanism of fluorescence emission was discussed. We propose that the intrinsic fluorescence originates from the formation of a Schiff base in the cross-linking process between hPEI and formaldehyde. Schiff base bonds are the fluorescence-emitting moieties, and the compact structure of hPEI-F CPs plays an important role in their strong fluorescence emission. The exploration on fluorescence mechanism may provide a new strategy to prepare fluorescent polymer particles. In addition, the investigation shows that the hPEI-F CPs hold potential as a fluorescent probe for the detection of copper ions in aqueous media.
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ACS Biomaterials Science & Engineering
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2016
·
IF 0
Hongshan Liang,Jing Li,Yun He,Wei Xu,Shilin Liu,Yan Li,Yijie Chen,Bin Li
Here, we reported a designable pH-responsive system on the basis of coordination bonded metal-tannic acid (TA) networks on zein/quaternized chitosan (HTCC) nanoparticles (NPs). Zein/HTCC NPs has been developed as a promising delivery system for natural bioactives in our lab previously. The coordination bonds between either the “NH2-metal” or the “metal-TA” are sensitive to pH variations that would release encapsulated drugs under designated pH conditions. Metal-TA film-coated zein/HTCC NPs had a spherical structure with particle size of 110–120 nm. Doxorubicin (DOX) was used as a model anticancer drug for release study and cell viability. The in vitro release profile of DOX loaded metal-TA films coated zein/HTCC NPs (DOX-zein/HTCC-TA/metal NPs) showed a significant pH-responsiveness when changing the amount or the type of metal ions. In in vitro cell assays, the blank zein/HTCC-TA/metal NPs showed low cytotoxicity, but the DOX-loaded NPs exhibited a high cytotoxic activity against HepG2. To impart enhanced imaging properties of metal-TA films, we used EuIII to chelate with ligand named 2-thenoyltrifluoroacetone (TTA) to intense fluorescence intensities of EuIII-TA films so as to develop pH-responsive zein/HTCC-TA/metal NPs for anticancer drug delivery as well as cell imaging.
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RSC Advances
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2016
·Vol. 6
·期 18
·15192-15200
·
IF 3.289
Huan Yuan,Jie Yu,Suling Feng,Yijun Gong
Nitrogen-doped carbon quantum dots (N-CDs) have become a current focus of chemical research due to their superior photoluminescence (PL) properties and high fluorescence quantum yield (QY). In this paper, we reported a facile, simple and low-cost approach for the synthesis of highly fluorescent and stable N-CDs by hydrothermal treatment of maleic acid and ethylenediamine. The as-prepared N-CDs emitted strong blue fluorescence with an absolute QY of up to 45%, and exhibited pH-independent behavior in a wide pH range from 1 to 13 and good water solubility. In addition, the fluorescence of the N-CDs can be significantly quenched by p-nitrophenol (4-NP) through an electron-transfer-induced dynamic quenching mechanism, leading to 4-NP being sensed optically. The sensor presented a good linearity with 4-NP concentration in the range of 0.10–11 μg mL−1. The detection limit of 22 ng mL−1 4-NP could be obtained, which is lower than the 60 ng mL−1 limit allowed in drinking water by the U. S. Environmental Protection Agency. The sensor exhibited rapid recognition and distinguished selectivity to 4-NP over other structural analogues of phenols. Moreover, the sensing system was successfully applied for the determination of 4-NP in environmental water samples.
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Journal of Materials Chemistry B
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2016
·Vol. 4
·期 8
·1480-1488
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IF 4.872
Yu-Bo Long,Wen-Xing Gu,Chengcai Pang,Jianbiao Ma,Hui Gao
It is still a major challenge for targeted cancer chemotherapy to design a stable biocompatible micellar drug delivery system. To address this dilemma, novel responsive cross-linked micelles (x-micelles) based on polyurethane with photo-responsive coumarin derivatives and pH-responsive hydrazone groups were synthesized. The polymers could be self-assembled into micelles using a typical and facile way. The x-micelles were stable at physiological conditions after UV light induced cross-linking, and can be disassociated under acidic condition. The drug loading content (DLC) and the encapsulation efficiency (EE) of the obtained x-micelles (15.2% and 60.8% respectively) were higher than those of micelles (9.8% and 39.2% respectively), and the DOX release rate of x-micelles was also improved. For targeted therapy, folic acid (FA) was then conjugated to x-micelles, resulting in x-micelles–FA. Cellular viability experiments show that both x-micelles and micelles had a low cytotoxicity and good biocompatibility of up to 1000 μg mL−1, and DOX-loaded x-micelles–FA and x-micelles exhibited half-maximal inhibitory concentration (IC50) values of 1.17 and 2.40 μg mL−1, respectively, to HeLa cells, but have lower cytotoxicity to L929 cells. The pH-responsive x-micelles–FA exhibited superior extracellular stability but activated intracellular drug release. We have demonstrated that the polyurethane with UV- and pH-responsive properties as a novel platform for tumor-targeting drug delivery.
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BIOMATERIALS
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2016
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IF 8.387
Zi-Wei Jing,Yi-Yang Jia,Ning Wan,Min Luo,Meng-Lei Huan,Tai-Bin Kang,Si-Yuan Zhou,Bang-Le Zhang
The covalently modified ureido-conjugated chitosan/TPP multifunctional nanoparticles have been developed as targeted nanomedicine delivery system for eradication of Helicobacter pylori . H. pylori can specifically express the urea transport protein on its membrane to transport urea into cytoplasm for urease to produce ammonia, which protects the bacterium in the acid milieu of stomach. The clinical applicability of topical antimicrobial agent is needed to eradicate H. pylori in the infected fundal area. In this study, we designed and synthesized two ureido-conjugated chitosan derivatives UCCs-1 and UCCs-2 for preparation of multifunctional nanoparticles. The process was optimized in order to prepare UCCs/TPP nanoparticles for encapsulation of amoxicillin. The results showed that the amoxicillin-UCCs/TPP nanoparticles exhibited favorable pH-sensitive characteristics, which could procrastinate the release of amoxicillin at gastric acids and enable the drug to deliver and target to H. pylori at its survival region effectively. Compared with unmodified amoxicillin-chitosan/TPP nanoparticles, a more specific and effective H. pylori growth inhibition was observed for amoxicillin-UCCs/TPP nanoparticles. Drug uptake analysis tested by flow cytometry and confocal laser scanning microscopy verified that the uptake of FITC-UCCs-2/TPP nanoparticles was associated with urea transport protein on the membrane of H. pylori and reduced with the addition of urea as competitive transport substrate. These findings suggest that the multifunctional amoxicillin-loaded nanoparticles have great potential for effective therapy of H. pylori infection. They may also serve as pharmacologically effective nanocarriers for oral targeted delivery of other therapeutic drugs to treat H. pylori .
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2017
·
IF 3.671
Min Zhang,Jia Liu,Ying Kuang,Qilin Li,Di-Wei Zheng,Qiongfang Song,Hui Chen,Xueqin Chen,Yanglin Xu,Cao Li,Bingbing Jiang
In this work, dextran, a polysaccharide with excellent biocompatibility, is applied as the “gatekeeper” to fabricate the pH-sensitive dextran/mesoporous silica nanoparticles (MSNs) based drug delivery systems for controlled intracellular drug release. Dextran encapsulating on the surface of MSNs is oxidized by NaIO 4 to obtain three kinds of dextran dialdehydes (PADs), which are then coupled with MSNs via pH-sensitive hydrazone bond to fabricate three kinds of drug carriers. At pH 7.4, PADs block the pores to prevent premature release of anti-cancer drug doxorubicin hydrochloride (DOX). However, in the weakly acidic intracellular environment (pH ∼ 5.5) the hydrazone can be ruptured; and the drug can be released from the carriers. The drug loading capacity, entrapment efficiency and release rates of the drug carriers can be adjusted by the amount of NaIO 4 applied in the oxidation reaction. And from which DOX@MSN-NH-N=C-PAD 10 is chosen as the most satisfactory one for the further in vitro cytotoxicity studies and cellular uptake studies. The results demonstrate that DOX@MSN-NH-N=C-PAD 10 with an excellent pH-sensitivity can enter HeLa cells to release DOX intracellular due to the weakly acidic pH intracellular and kill the cells. In our opinion, the ingenious pH-sensitive drug delivery systems have application potentials for cancer therapy.
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Scientific Reports
·
2016
·Vol. 6
·期 1
·1-9
·
IF 5.228
Lv Yongjiu,Hao Lan,Hu Wenjing,Ran Ya,Bai Yan,Zhang Liangke
This study fabricated novel multifunctional pH-sensitive nanoparticles loaded into microbubbles (PNP-MB) with the combined advantages of two excellent drug delivery vehicles, namely, pH-sensitive nanoparticles and microbubbles. As an antitumor drug, resveratrol (RES) was loaded into acetylated β-cyclodextrin nanoparticles (RES-PNP). The drug-loaded nanoparticles were then encapsulated into the internal space of the microbubbles. The characterization and morphology of this vehicle were investigated through dynamic light scattering and confocal laser scanning microscopy, respectively. In vitro drug release was performed to investigate the pH sensitivity of RES-PNP. The antitumor property of RES-loaded PNP-MB (RES-PNP-MB) was also analyzed in vivo to evaluate the antitumor effect of RES-PNP-MB. Results suggested that PNP exhibited pH sensitivity, and was successfully encapsulated into the microbubbles. RES-PNP-MB exhibit effective tumor growth suppressing in vivo . Therefore, such drug delivery vehicle should be of great attention in tumor therapy.
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ELECTROCHIMICA ACTA
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2016
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IF 4.803
Yonghai Song,Yuan Shen,Jingyi Chen,Yonggui Song,Coucong Gong,Li Wang
A novel pH-dependent immunosensor to detect tumor biomarker, carcinoembryonic antigen (CEA), was developed by using the pH-dependent AuNPs-Ab 2 -glucose oxidase-Concanavalin A as tracing tag and the albumin bovine V-Ab 1 /chitosan-AuNPs/three-dimensional kenaf stem-derived macroporous carbon (3D-KSCs) integrated electrode as signal collector based on a sandwich-type assay mode. The integrated 3D-KSCs electrode provided a large specific surface area to load a large number of Ab 1 effectively and the tracing tag with a lots of pH-dependent surface negative charges repulsed the negatively charged probe of Fe(CN) 6 3− in a pH 9.0 solution. Accordingly, after a sandwich immunoreaction, the quantitative capture of tracing tag on the signal collector greatly hindered the electron transfer of Fe(CN) 6 3−/4− due to the electrostatic repulsion, which improved the sensitivity and selectivity of the immunosensors significantly. It was verified by electrochemical impedance spectroscopy. The resistance to charge transfer of Fe(CN) 6 3−/4− changed proportionally toward CEA concentration from 4 pg mL −1 to 50 ng mL −1 with a low detection limit of 1.3 pg mL −1 ( S / N = 3) and a high sensitivity of 57.57 Ω ng −1 mL. Based on human serum experiments, the sensing platform was proved to be suitable to assay CEA in a practical biosystem. This work not only gives a sensitive way to detect CEA but also provides a potential strategy for immunosensors based on 3D-KSC electrode and pH-dependent behavior.
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