Polymers
·
2018
·Vol. 10
·期 10
·1127
·
IF 2.935
Yinglei Zhai,Xing Zhou,Zhiqiang Zhang,Lei Zhang,Dianyu Wang,Xinhui Wang,Wei Sun
The side effects of doxorubicin (DOX) extremely limit its application in the treatment of malignant tumors. Nano-sized polymeric drugs based on the acidic microenvironment of tissular- or intra- tumor have attracted ample attention because of their potential in reducing side effects. In this research, an amphiphilic diblock copolymer based on poly (ethylene glycol) (PEG) and functionalized polycaprolactone (PCL) was synthesized and utilized as the drug carrier. DOX was chemically conjugated with the polymer via acid-cleavable imine bonds to obtain a novel pH-sensitive DOX prodrug (mPEG-PCL-Imi-DOX). mPEG-PCL-Imi-DOX (24.2 wt % DOX content) formed micelles with an average diameter of 125 nm through a simple solvent evaporation method. The in vitro release profile demonstrated that DOX release of the prodrug micelles was pH-responsive and able to be accelerated with the decrease of pH. In vitro cytotoxicity assay tests revealed that the pH-sensitive DOX prodrug micelles exhibited relatively lower toxicity and similar antitumor efficacy towards MCF-7 cells compared with free DOX. Hence, the DOX prodrug micelles with imine bonds can offer a carrier with great potential for chemo-therapeutics.Keywords:doxorubicin;pH-sensitive;prodrug;micelles;imine
研究领域:
药学
·
肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF LUMINESCENCE
·
2013
·
IF 2.144
Weiguang Kong,Huizhen Wu,Zhenyu Ye,Ruifeng Li,Tianning Xu,Bingpo Zhang
Carbon dots with unique characters of chemical inertness, low cytotoxicity and good biocompatibility, demonstrate important applications in biology and optoelectronics . In this paper we report the optical properties of pH-sensitive carbon dots with different surface modifications. The as-prepared carbon dots can be well dispersed in water by modifying with acid, alkali or metal ions though they tend to form a suspension when being directly dispersed in water. We find that the carbon dots dispersed in water show a new emission and absorption character which is tunable due to the pH-sensitive nature. It is firstly proved that the addition of bivalent copper ions offers a high color contrast for visual colorimetric assays for pH measurement. The effect of surface defects with different modification on the performances of the carbon dots is also explored with a core–shell model. The hydro-dispersed carbon dots can be potentially utilized for cellular imaging or metal ion probes in biochemistry.
研究领域:
生物技术
·
材料科学
·
光学
✓ 已验证
DOI
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2018
·
IF 5.08
Tingsheng Yan,Jinju Cheng,Zongjun Liu,Feng Cheng,Xinjing Wei,Yudong Huang,Jinmei He
Liver cancer is one of the top death causing cancers, traditional treatments have not settled for the requirement of patients. In this work, a smart acid-responsive micelle based on glycyrrhetinic acid modified chitosan-polyethyleneimine-4-Hydrazinobenzoic acid-doxorubicin (GA-CS-PEI-HBA-DOX) was synthesized for targeted delivery of DOX to liver cancer. A dual pH-sensitive and receptor-mediated strategy has been exploited to enhance the delivery efficiency. The micelle possesses positive charges under pH 6.8 and can be turned into negative charges above pH 7.0, which help to be accumulated in tumor tissues (pH 6.0–7.0). In the intracellular environment (pH 4.5–6.5) of tumor cells, the pH-sensitive hydrazone bonds between DOX and GA-CS-PEI-HBA would break and release as much as 90.3% of the encapsulated payloads in 48 h. In addition, GA was modified to improve the targeting abilities. The micelles exhibited high lethality to HepG2 cells while showed much lower cytotoxicity to HUVEC cells. With high drug-loading capacity and the targeted release ability, the GA-CS-PEI-HBA-DOX micelle might be employed as a promising candidate for targeted cancer treatment.
研究领域:
药剂学
·
肿瘤学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF BIOMATERIALS APPLICATIONS
·
2016
·
IF 1.988
Feng Xu,Jing-Wen Xu,Yan-Ling Luo
pH-Sensitive poly(methacrylic acid)-block-hydroxyl-terminated polybutadiene-block-poly(methacrylic acid) (PMAA-b-HTPB-b-PMAA) was synthesized and then hydrogenated in this work. The chain structure, phase behavior and thermal properties were characterized by 1H NMR, FTIR, XRD, DSC, TGA, etc., and the physicochemical and biomedical properties were investigated via fluorescence spectroscopy, TEM, DLS, loading and release of drug and MTT, and so on. The experimental results indicated that the hydrogenation led to the change in the chain aggregate structure of hydrophobic HTPB blocks and the formation of more stable spherical core-shell micelle aggregates, and the critical micelle concentration decreased from 41.8 mg L−1 before hydrogenation to 4.4 mg L−1 after hydrogenation. The hydrogenated block copolymer micelle aggregates exhibited pH-triggered response, and could entrap twice as much hydrophobic drug as the unhydrided counterparts and the encapsulation efficiency was significantly improved, which makes them fine to meet the requirements for drug carriers. Therefore, the hydrogenated PMAA-b-HTPB-b-PMAA copolymer micelles as drug target release carriers can be well used in the field of prevention and treatment of cancers.
研究领域:
材料科学
·
生物医学工程
·
药学
✓ 已验证
DOI
PubMed
高影响因子
RSC Advances
·
2015
·Vol. 5
·期 95
·77986-77995
·
IF 3.84
Nuannuan Li,Pei Zhang,Chunzhi Huang,Yunmei Song,Sanjay Garg,Yuxia Luan
In this paper, we synthesized the pH-sensitive and biodegradable amphiphilic polypeptide-based block copolymer methoxy-poly(ethylene glycol)2K-poly(ε-caprolactone)4K-poly(glutamic acid)1K (mPEG2K-PCL4K-PGA1K). mPEG2K-PCL4K-PGA1K had low critical aggregation concentration and could self-assemble into polymersomes in aqueous solution revealed by transmission electron microscopy. Therefore, two hydrophilic drug doxorubicin hydrochloride (DOX) and verapamil hydrochloride (VER) were encapsulated into the mPEG2K-PCL4K-PGA1K polymersomes to form poly(DOX + VER) co-delivery system to reverse the multidrug resistance by inhibiting the expression of P-glycoprotein and improve the anti-cancer effect of DOX. The in vitro cytotoxicity experiments indicated the obviously higher inhibition ratio to MCF-7/ADR resistant cells of poly(DOX + VER) compared with that of free DOX solution and polyDOX. The release rate of the two drugs from poly(DOX + VER) were much slower than that from the free drug solutions, and their release behaviors exhibited high pH-sensitive character. Furthermore, the low hemolysis ratio of mPEG2K-PCL4K-PGA1K confirmed that the copolymer could be applied for intravenous injection safely. Therefore, all these findings indicated that the co-delivery of DOX and VER by mPEG2K-PCL4K-PGA1K polymersomes is very promising for cancer therapy.
研究领域:
药学
·
肿瘤学
✓ 已验证
DOI
高影响因子
FIBERS AND POLYMERS
·
2016
·Vol. 17
·期 10
·1531-1539
·
IF 1.022
Mao Yanli,Cui Jiuyun,Zhao Juan,Wu Yilin,Wang Chen,Lu Jian,Lin Xinyu,Yan Yongsheng
Via Pickering emulsion polymerization, pH-sensitive magnetic molecularly imprinted polymers (HM-MIPs) were synthesized using bifenthrin (BF) as the template molecule, and pH-sensitive monomer methacrylic acid as the functional monomer. Characterizations of HM-MIPs were achieved by FTIR, TGA, TEM, SEM, and VSM, and the results indicated that HM-MIPs exhibited magnetic property (Ms=1.06 emu/g). HM-MIPs were acted as the adsorbent for a series of adsorption performance testing of BF. Equilibrium data were described by the Langmuir and Freundlich isotherm models. Kinetic properties were successfully investigated by pseudo-first-order model, pseudo-second-order model. The selective recognition experiments exhibited outstanding selectively adsorption effect of the HM-MIPs for target BF over diethyl phthalate and fenvalerate. In water, the HM-MIPs could achieve the adsorption and release of BF by controlling the pH value of the aqueous solution. The results indicated that the molecularly imprinted polymers exhibited good adsorption, selectivity and pH-sensitive performance for BF.
研究领域:
材料科学
·
环境科学
·
分析化学
✓ 已验证
DOI
高影响因子
Scientific Reports
·
2014
·Vol. 4
·期 1
·1-5
·
IF 5.078
Xiang Tao,Wang Ling-Ren,Ma Lang,Han Zhi-Yuan,Wang Rui,Cheng Chong,Xia Yi,Qin Hui,Zhao Chang-Sheng
Functional polymers bear specified chemical groups and have specified physical, chemical, biological, pharmacological, or other uses. To adjust the properties while keeping material usage low, a method for direct synthesis of functional polymers is indispensable. Here we show that various functional polymers can be synthesized by in situ cross-linked polymerization/copolymerization. We demonstrate that the polymers synthesized by the facile method using different functional monomers own outstanding pH-sensitivity and pH-reversibility, antifouling property, antibacterial and anticoagulant property. Our study opens a route for the functionalization of commodity polymers, which lead to important advances in polymeric materials applications.
研究领域:
材料科学
·
生物学
·
医学
✓ 已验证
DOI
PubMed
高影响因子
Journal of Materials Chemistry B
·
2015
·Vol. 3
·期 43
·8499-8507
·
IF 4.726
Di-Wei Zheng,Qi Lei,Si Chen,Wen-Xiu Qiu,Meng-Yi Liu,Xian Chen,Yu-Xue Ding,Peng-Hui Li,Quan-Yuan Zhang,Zu-Shun Xu,Xian-Zheng Zhang,Paul K. Chu
Magnetite (Fe3O4) microcapsules prepared by layer-by-layer self-assembly are investigated as multi-functional magnetic resonance imaging contrast agents and drug carriers. They are produced by host–guest interactions and Coulombic force from different supramolecular polymers. Drug molecules are released controllably from the microcapsules by non-invasive ultra-violet light induced photo-isomerization of the azobenzene molecule and pH sensitive Schiff's base. In addition, by encapsulation of the superparamagnetic iron oxide nanoparticles (SPION) in the nearby layers, magnetic field targeting and MRI contrast are achieved. Under tumor-like acidic conditions (pH = 5.6), the r2 relaxivity of the microcapsules is 126 mM−1 s−1 which is 37% higher than that in a neutral environment (92 mM−1 s−1). As a result of the low pH enhanced MRI contrast agent, the tumor structure can be observed clearly in vivo confirming the high efficacy as a negative MRI agent in T2-weighted imaging. The materials as combined carriers have great potential in clinical applications as drug delivery agents and contrast agents in MRI.
研究领域:
医学影像学
·
药剂学
·
生物材料学
✓ 已验证
DOI
高影响因子
JOURNAL OF MATERIALS SCIENCE
·
2019
·Vol. 54
·期 7
·5695-5711
·
IF 3.442
Qin Jiejie,Huang Yan,Yan Guoqing,Wang Jun,Hu Liefeng,Zhang Panpan,Tang Rupei
In this work, the tumor-targeted ultra-pH-responsive conjugates (PBA/Dex-g-OE) and nontargeted conjugates (Dex-g-OE) were successfully prepared and could easily self-assemble into stable micelles with lower CMC values in neutral aqueous solution. Transmission electron microscopy and dynamic light scattering measurement indicated that the resulting micelles have desirable size distribution and regular spherical shape. The PBA/Dex-g-OE micelles possessed high stability in physiological condition and were pH sensitive to both extracellular and intracellular acidic conditions. Doxorubicin (DOX) was efficiently loaded to give the DOX-loaded micelles (PBA/Dex-g-OE-DOX and Dex-g-OE-DOX) with the desirable drug loading contents. In vitro cellular uptake and growth inhibition assays suggested that PBA/Dex-g-OE-DOX micelles were more efficiently internalized by monolayer tumor cells and three-dimensional multicellular tumor spheroids (MCTS) than nontargeted micelles (Dex-g-OE-DOX), leading to the fast and complete destruction of MCTS in vitro.
研究领域:
药剂学
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
·
2013
·Vol. 13
·期 6
·3832-3840
·
IF 1.149
Cui Qinmin,Dai Lijun,Yang Liu,Ziener Ulrich,Cao Zhihai
Cross-linked chitosan (CS) nanohydrogels were successfully prepared via cross-linking CS nanodroplets in inverse miniemulsions. The cross-linker was transferred to the CS nanodroplets via the evaporation from its aqueous solution and diffusion through the continuous phase. The formation
of cross-linked CS nanohydrogels was confirmed by the morphological investigation during the reaction and the successful preparation of acidic aqueous dispersion of CS nanohydrogels. The size and size distribution of the CS nanodroplets and nanohydrogels were characterized by dynamic light
scattering (DLS). The particle morphology of CS nanohydrogels was observed by transmission electron microscopy (TEM). The influence of the synthetic parameters on the particle properties and colloidal stability was investigated with respect to sonication time, surfactant type and amount, type
of low polarity solvent, and concentration of CS solution. The cross-linked CS nanohydrogels could be easily re-dispersed in water, and showed a pH sensitivity.
研究领域:
材料科学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
POLYMER SCIENCE SERIES A
·
2021
·Vol. 63
·期 2
·143-153
·
IF 1.206
Qiuyue Guo,Chen Yuying,Li Xin,Liu Jun,Gu Qintian,Hu Jian,Jiang Yan,Zhang Hongwen,Liu Hongbo
Abstract In this paper, partly esterified β-cyclodextrin derivative had been synthesized by esterification of β-cyclodextrin and maleic anhydride. Then, it is amidated by diethanolamine. β-Cyclodextrin copolymer had been prepared from amidated β-cyclodextrin derivative, cholic acid and epichlorohydrin in sodium hydroxide aqueous solution. β-Cyclodextrin hydrogel had been prepared through radical polymerization of β-cyclodextrin copolymer, N -isopropylacrylamide and acrylic acid. The structures, compositions and morphology of the hydrogel were characterized by infrared spectroscopy, nuclear magnetic resonance, differential scanning calorimetry and field-emission scanning electron microscope. Its properties were tested and analyzed by ultraviolet spectroscopy, thermogravimetric analysis and swelling experiments. The results show that the β-cyclodextrin hydrogel owns sustained release performance, temperature and pH sensitivities.
研究领域:
材料科学
·
化学工程
·
生物医药
✓ 已验证
DOI
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2019
·
IF 3.743
Gang Zheng,Meizhu Zheng,Ben Yang,Hui Fu,Yongqing Li
Breast cancer is the leading cause of cancer mortality in women worldwide. To overcome the toxic side effects and multidrug resistance (MDR) during doxorubicin (DOX) chemotherapy, an arginine-glycine-aspartic (RGD) tripeptide modified, pH-sensitive solid lipid nanoparticles (SLNs) is employed in this study. In this study, a RGD conjugated, pH sensitive lipid was synthesized using glycerin monostearate (GMS) and adipic acid dihydrazide (HZ) as lipid materials and named RGD-HZ-GMS. RGD-HZ-GMS was applied to encapsulate DOX to construct a RGD modified, DOX loaded SLNs (RGD-DOX-SLNs). To evaluate the anticancer effect of RGD-DOX-SLNs, breast cancer cell line (MCF-7 cells) and DOX resistant cell line (MCF-7/ADR cells) were used. in vivo tumor suspension and toxicity effects were evaluated on mice bearing MCF-7/ADR cells breast cancer model. RGD-DOX-SLNs had a uniformly spherical shape. The mean particle size and zeta potential of the RGD-DOX-SLNs was 96.3 nm and 35.6 mV, respectively. RGD-DOX-SLNs showed 5.58 fold higher area under the plasma concentration – time curve (AUC) compared with DOX solution. Terminal half life (T 1/2 ) and peak concentration (C max ) of RGD-DOX-SLNs was 10.85 h and 39.12 ± 2.71 L/kg/h. in vitro and in vivo antitumor results indicate that RGD-DOX-SLNs might be a promising novel lipid carrier which could improve breast cancer therapy.
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
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