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JOURNAL OF APPLIED POLYMER SCIENCE · 2015 ·Vol. 133 ·期 15 · IF 1.768

A facile preparation of pH-temperature dual stimuli-responsive supramolecular hydrogel and its controllable drug release

Mi Zhou,Kaiyue Liu,Xin Qian

A series of pH-temperature dual stimuli-responsive random copolymers poly[ N,N -dimethylaminoethyl methacrylate- co -poly(poly(ethylene glycol) methyl ether methacrylate][poly(DMAEMA- co -MPEGMA)] were synthesized by free radical polymerization. The supramolecular hydrogel was formed by pseudopolyrotaxane, which was prepared with the host-guest interactions between α-cyclodextrin (α-CD) and poly(ethylene glycol) (PEG) side chains. Fourier transform infrared (FT-IR), nuclear magnetic resonance ( 1 H NMR), and X-ray diffraction (XRD) confirmed the structures of the hydrogels. The pH-temperature dual stimuli responsive properties of the hydrogels were characterized by rheometer. Finally, the controllable drug release behavior of the hydrogel, which was used 5-fluorouracil (5-Fu) as the model drug, was investigated at different temperatures and different pH values. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133 , 43279.

研究领域: 高分子材料科学 · 药物递送系统 · 生物医学工程 · 智能响应材料 · 药剂学
✓ 已验证 DOI 高影响因子
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MACROMOLECULAR CHEMISTRY AND PHYSICS · 2012 ·Vol. 213 ·期 20 ·2192-2200 · IF 2.361

pH-Responsive Double-Hydrophilic Block Copolymers: Synthesis and Drug Delivery Application

Xiao-Hui Dai,Chun-Yan Hong,Cai-Yuan Pan

A novel double-hydrophilic block copolymer P(MEO 2 MA- co -OEGMA)- b -PAMA has been successfully synthesized by two-step RAFT polymerization. Then, the amino groups of PAMA blocks in the copolymers react with 1-pyrenecarboxaldehyde via a “Schiff-base” reaction, and the resulting copolymers are self-assembled to form spherical micelles in aqueous solution. Because the “Schiff-base” linkage is pH sensitive, the release rate of pyrene depends upon the pH of solution. Complete release is achieved at pH 1, and the control release is much faster at pH 5.5 than that at pH 7.4. With progress of pyrene release, the micelles are disassembled gradually and disappeared completely at last. This double-hydrophilic copolymer is a promising candidate of drug carrier for the aldehyde- containing hydrophobic drugs.

研究领域: 高分子化学 · 药剂学 · 纳米医学 · 生物材料 · 药物递送系统
✓ 已验证 DOI 高影响因子
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POLYMERS FOR ADVANCED TECHNOLOGIES · 2020 ·Vol. 31 ·期 11 ·2480-2491 · IF 2.578

Effects of chicken feather keratin on smoke suppression characteristics and flame retardancy of epoxy resin

Po Hu,Xinyu Zheng,Jiwei Zhu,Baolin Wu

Chicken feather keratin (CK), a biomaterial that contains a large amount of nitrogen is extracted from chicken feathers and has significant potential for use as a flame retardant. In this study, CK and 9,10-dihydro-9-oxa-10-phosphenanthrene-10-oxide (DOPO) were added in different amounts to an epoxy resin (EP), and their flame retardancy and smoke suppression effects were studied. The results showed that CK exhibits a good flame-retardancy effect and better smoke suppression characteristics than those of DOPO when added to EP. Furthermore, it greatly reduces the CO yield in smoke. While the EP samples with DOPO showed better flame-retardancy properties than those of the samples with CK, they also produced more smoke, which had a higher CO content. Furthermore, when CK and DOPO were added to EP together, the flame-retardancy characteristics of the samples varied with the CK/DOPO ratio. Then the pyrolysis of all samples was divided into two stages based on thermokinetics analysis and the activation energies of these samples in the two stages were investigated. Finally, the flame-retardancy mechanism was discussed. When samples burn, the PO· free radicals derived from DOPO combine with H· and OH· to induce a quenching effect. In addition, the phosphate resulting from the decomposition of DOPO promotes the formation of the char layer. At the same time, the noncombustible gases generated during the pyrolysis of CK cause the char layer to expand and remove some of the heat. Thus, CK and DOPO synergistically improved the flame retardancy of EP.

研究领域: 高分子材料科学 · 阻燃化学 · 热分析 · 环境友好材料 · 生物基添加剂
✓ 已验证 DOI 高影响因子
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JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE · 2017 ·Vol. 28 ·期 5 ·67 · IF 2.325

Self-assembled polyelectrolyte complexes films as efficient compression coating layers for controlled-releasing tablets

Li Wenyan,Huo Mengmeng,Sen Chaudhuri Arka,Yang Chen,Cao Dazhong,Wu Zhenghong,Qi Xiaole

Currently, polysaccharide-based hydrogels are widely studied macromolecular networks to modify drug dissolution from controlled-releasing matrix tablets. Among them, polyelectrolyte complexes (PEC) films consisted of chitosan (CS) and sodium alginate (SA) could be obtained via spontaneously assembling under physiological gastrointestinal environment. Here, we utilized these self-assembled PEC films as an efficient coating materials to develop controlled-released matrix tablets through compression coating process, with paracetamol (APAP) as model drug. The constitutive and morphology characteristic studies on these PEC films illustrated that the mixture of CS and SA with the weight ratio of 1:1 would be an promising outer layer for compression-coating tablets. In addition, the in vitro drug releasing behavior experiments demonstrated that the optimized compression coating tablets displayed satisfied zero-order drug releasing profits. Furthermore, the in vivo pharmacokinetic studies of these APAP loaded compression-coated tablets in New Zealand rabbits gave that the T max (12.32 ± 1.05 h) was significantly prolonged ( p  < 0.01), compared to that (0.89 ± 0.26 h) of common APAP tablets (Jinfuning ® ) after oral administration. These studies suggest that the compression-coated tablets with self-assembled PEC film as coating outer layer may be a promising strategy for peroral controlled release delivery system of water soluble drugs. Graphical

研究领域: 药剂学 · 生物材料 · 药物递送系统 · 药代动力学 · 胃肠药理学
✓ 已验证 DOI 高影响因子
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MACROMOLECULAR CHEMISTRY AND PHYSICS · 2016 ·Vol. 217 ·期 9 ·1047-1056 · IF 2.495

Cross-Linked Nano-Objects Containing Aldehyde Groups: Synthesis via RAFT Dispersion Polymerization and Application

Liang Qiu,Chao-Ran Xu,Feng Zhong,Chun-Yan Hong,Cai-Yuan Pan

Pure cross-linked spherical micelles, nanowires, and vesicles are successfully fabricated from poly(2-hydroxypropyl methacrylate- b - p -(methacryloxyethoxy)benzaldehyde)s (PHPMA– b –PMAEBAs) through reversible addition-fragmentation chain transfer dispersion polymerization of MAEBA in methanol using PHPMA as a macro-CTA and subsequent cross-linking. The cross-linking reaction is conducted by stirring a mixture of 1,4-butanediamine and the resultant nano-objects in methanol at room temperature. For all polymerizations with feed molar ratios of MAEBA/PHPMA ranging from 75/1 to 240/1, the monomer MAEBA conversions are almost complete, and block copolymers with controlled molecular weight are obtained. The transmission electron microscopy, dynamic light scattering, and gel permeation chromatography results reveal that the following three factors significantly influence the morphology of the nano-objects: the feed molar ratio of MAEBA/PHPMA, the copolymer concentration, and the degree of polymerization of PHPMA. The cross-linked nano-objects are very stable in good solvents, the spheres and nanowires slightly decrease in size after cross-linking, whereas the vesicles slightly increase in size. The cross-linked nano-objects are stable in neutral solutions, but they dissociate in weekly acidic solutions. The loading of 1-pyrenemethylamine (PMA) into the vesicles and the unloading of PMA from the vesicles are studied.

研究领域: 高分子化学 · 纳米材料 · 药物递送 · 生物医学工程 · 胶体与界面科学
✓ 已验证 DOI 高影响因子
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Materials Science & Engineering C-Materials for Biological Applications · 2016 · IF 3.42

Molecular imprinting functionalized silica xerogel for selective recognition of levorotatory ofloxacin

Jing Li,Sanming Li,Zhonggui He

In the present work, molecular imprinting silica xerogel (MISX) with selective recognition function aiming to regulate drug therapy was synthesized using biomimetic method with poly(ethyleneimine)s (PEIs) as the polymer template and levorotatory ofloxacin (LOFL) as recognition template. Ultraviolet spectroscopy wavelength scanning was used to test the removal process of LOFL, and characteristics of selective loading ofloxacin (OFL) into MISX were investigated using Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Molecular recognition functionality of MISX was intensively studied, including OFL loading and release. The results suggested that MISX possessed ability to recognize and selectively adsorb LOFL into MISX in OFL aqueous solution. Amorphous phase of adsorbed molecules contributed to molecular recognition because amorphous state increased the stability of LOFL that were selectively adsorbed into MISX, which induced stronger hydrogen bonding formed between LOFL and MISX so as to improve LOFL recognition ability. In vitro release revealed that OFL-MISX tablet initially released LOFL and later gradually OFL into dissolution medium. Thus conversion of drug release with different pharmacological activity had special value in delivering systems.

研究领域: 药剂学 · 药物化学 · 纳米医学 · 生物材料 · 分子识别 · 药物递送系统
✓ 已验证 DOI 高影响因子
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2020 · IF 4.845

Multifunctional composite nanoparticles based on hyaluronic acid-paclitaxel conjugates for enhanced cancer therapy

Kaipei Luo,Shaoping Yin,Ruixia Zhang,Hua Yu,Guangji Wang,Juan Li

The efficient delivery of chemotherapeutic drugs to the tumor tissues unavoidably encounters numerous obstacles, such as poor tumor targeting capability, slow intracellular drug release and massive accumulation in the liver. In this study, by self-assembling methoxy poly (ethylene glycol)-poly (lactide) block copolymer (mPEG-PLA) and hyaluronic acid-paclitaxel conjugate (HA-PTX), the composite nanoparticles (mPPHP NPs) were fabricated for efficient therapy of cancer. mPPHP NPs formed self-assembled nanoparticles (116 nm in diameter) with a narrow size distribution; and showed a rapid release of PTX in the presence of hyaluronidase and esterase . mPPHP NPs exhibited enhanced internalization by cells via CD44 receptors and selected cytotoxicity against A549 cells in vitro . More importantly, compared with other PTX formulations, mPPHP NPs were demonstrated to present the reduced liver accumulation, excellent tumor-targeting ability and superior antitumor efficacy in vivo , with a TIR of 75.9%. The multifunctional composite nanoparticles could be developed as a promising nano-carrier for improved therapeutic efficacy.

研究领域: 肿瘤学 · 纳米医学 · 药剂学 · 分子靶向治疗 · 药物递送系统 · 转化医学
✓ 已验证 DOI 高影响因子
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RSC Advances · 2016 ·Vol. 6 ·期 112 ·111217-111225 · IF 3.289

pH-sensitive drug release of star-shaped micelles with OEG brush corona

Sijie Zhao,Huiru Yang,Cai Zuo,Lu Sun,Liwei Ma,Hua Wei

Star-shaped polymers are attractive as drug carriers due to the integration of relatively easy synthesis compared to the preparation of hyper-branched dendrimers and their potential ability to form unimolecular nanoparticles with enhanced stability to survive the high dilution-associated deformation and subsequently premature drug release in the body fluids and blood during circulation. Clearly, the star structure exerts a significant effect on their bioproperties and potential applications. In this study, three star-shaped amphiphilic copolymers with the same polymer compositions but different star structures were synthesized to investigate the effect of star architecture on their properties as well as potential applications as drug carriers. Three different branched alcohols, 2-(hydroxymethyl) propane-1,3-diol, pentaerythritol and dipentaerythritol with 3, 4, and 6 respective hydroxyl groups were chosen as the starting core to generate the target star-shaped amphiphilic block copolymers composed of hydrophobic poly(ε-caprolactone) (PCL) and hydrophilic poly(oligoethyleneglycol methacrylate) (POEGMA) with 3, 4, and 6 corresponding star arms by a combination of ring-opening polymerization (ROP) and atom transfer radical polymerization (ATRP). Dynamic light scattering (DLS) measurements and pyrene fluorescence probe technique confirmed the capability of the resultant star-shaped amphiphilic copolymers to form unimolecular micelles with average diameters smaller than 50 nm in an aqueous phase. A comparison of the drug loading capacity revealed that the micelles of 4-star-PCL–POEGMA (4s-PCL–POEGMA) exhibited the highest drug loading content (DLC) of all the three formulations. More importantly, in vitro doxorubicin (DOX) release study showed unique pH-mediated drug release behaviors, i.e., dramatically accelerated release at pH 6.0 but a much slower profile at pH 7.4, from these generally recognized “pH-insensitive” 4-arm star-shaped micelles. An acid-triggered degradation and an acid–base titration were performed to further reveal that such interesting pH-responsive drug release behaviors were attributed primarily to the hydrophilic corona of OEG brushes. This study is believed to provide a new insight into the structure–bioproperties relationship of star-shaped polymers, thus should be useful for the future design and development of novel star-shaped polymers for controlled drug delivery.

研究领域: 高分子药剂学 · 纳米医学 · 药物控释 · 生物材料 · 药剂学 · 肿瘤治疗 · 纳米载体
✓ 已验证 DOI 高影响因子
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2013 · IF 3.458

A novel pulsatile drug delivery system based on the physiochemical reaction between acrylic copolymer and organic acid: In vitro and in vivo evaluation

Ziwei Zhang,Xiaole Qi,Xiangbo Li,Jiayu Xing,Xuehua Zhu,Zhenghong Wu

Multilayer-coating technology is the traditional method to achieve pulsatile drug release with the drawbacks of time consuming, more materials demanding and lack of efficiency. The purpose of this study was to design a novel pulsatile drug delivery system based on the physiochemical interaction between acrylic copolymer and organic acid with relatively simpler formulation and manufacturing process. The Enalapril Maleate (EM) pulsatile release pellets were prepared using extruding granulation, spheronization and fluid-bed coating technology. The ion-exchange experiment, hydration study and determination of glass transition temperature were conducted to explore the related drug release mechanism. Bioavailability experiment was carried out by administering the pulsatile release pellets to rats compared with marketed rapid release tablets Yisu ® . An obvious 4   h lag time period and rapid drug release was observed from in vitro dissolution profiles. The release mechanism was a combination of both disassociated and undisassociated forms of succinic acid physiochemically interacting with Eudragit ® RS. The AUC0-τ of the EM pulsatile pellets and the market tablets was 702.384   ±   96.891   h   ng/mL and 810.817   ±   67.712   h   ng/mL, while the relative bioavailability was 86.62%. These studies demonstrate this novel pulsatile release concept may be a promising strategy for oral pulsatile delivery system.

研究领域: 药剂学 · 药物递送 · 生物药剂学 · 药物代谢 · 制剂工程 · 药动学
✓ 已验证 DOI 高影响因子
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Small · 2017 ·Vol. 14 ·期 7 ·1702288 · IF 8.643

Bioadhesive Polymersome for Localized and Sustained Drug Delivery at Pathological Sites with Harsh Enzymatic and Fluidic Environment via Supramolecular Host–Guest Complexation

Meiling Zhu,Kongchang Wei,Sien Lin,Xiaoyu Chen,Chia-Ching Wu,Gang Li,Liming Bian

Targeted and sustained delivery of drugs to diseased tissues/organs, where body fluid exchange and catabolic activity are substantial, is challenging due to the fast cleansing and degradation of the drugs by these harsh environmental factors. Herein, a multifunctional and bioadhesive polycaprolactone-β-cyclodextrin (PCL-CD) polymersome is developed for localized and sustained co-delivery of hydrophilic and hydrophobic drug molecules. This PCL-CD polymersome affords multivalent crosslinking action via surface CD-mediated host–guest interactions to generate a supramolecular hydrogel that exhibits evident shear thinning and efficient self-healing behavior. The co-delivery of small molecule and proteinaceous agents by the encapsulated PCL-CD polymersomes enhances the differentiation of stem cells seeded in the hydrogel. Furthermore, the PCL-CD polymersomes are capable of in situ grafting to biological tissues via host–guest complexation between surface CD and native guest groups in the tissue matrix both in vitro and in vivo, thereby effectively extending the retention of loaded cargo in the grafted tissue. It is further demonstrated that the co-delivery of small molecule and proteinaceous drugs via PCL-CD polymersomes averts cartilage degeneration in animal osteoarthritic (OA) knee joints, which are known for their biochemically harsh and fluidically dynamic environment.

研究领域: 药物递送 · 生物材料 · 组织工程 · 纳米医学 · 再生医学 · 关节生物学 · 转化医学
✓ 已验证 DOI 高影响因子
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Revista Brasileira de Farmacognosia-Brazilian Journal of Pharmacognosy · 2019 ·Vol. 29 ·期 1 ·46-53 · IF 1.754

Anti-allergic rhinitis effects of caffeoylquinic acids from the fruits of Xanthium strumarium in rodent animals via alleviating allergic and inflammatory reactions

Peng Wei,Han Ping,Yu Luyao,Chen Ying,Ye Bingzhu,Qin Luping,Xin Hailiang,Han Ting

The fruits of Xanthium strumarium L., Asteraceae, have been used for various diseases in Chinese folk medicine, including allergic rhinitis, tympanitis, arthritis, ozena etc. The current study was aimed to investigate the therapeutic effects of caffeoylquinic acids from fruits of X. strumarium on allergic rhinitis in animals. The toxicity test indicated that the caffeoylquinic acids have no obvious toxicity. By using HPLC assays combined with reference standards, ten caffeoylquinic acids were identified as the predominant constituents. Anti-allergic activities of the caffeoylquinic acids were evaluated using passive cutaneous anaphylaxis test and Schultz-Dale test; dimethylbenzene induced ear edema test was performed to evaluate its anti-inflammatory effect. Then, the allergic rhinitis model in rats was established to evaluate the therapeutic effects of the caffeoylquinic acids against allergic rhinitis with the following indexes: allergic rhinitis symptom scores, serum levels of pro-inflammatory cytokines, histopathological examination, and histamine release. Our study revealed that the caffeoylquinic acids showed obvious anti-allergic and anti-inflammatory properties, and its treatments were beneficial for ameliorating the nasal symptoms, decreasing pro-inflammatory cytokines, and inhibiting the releases of histamine. Collectively, the caffeoylquinic acids might be utilized as effective and safe disease therapeutic agents for allergic rhinitis.

CAS / MDL: 79794-75-5
研究领域: 药理学 · 免疫学 · 过敏 · 植物化学
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