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Polymers · 2019 ·Vol. 11 ·期 3 ·511 · IF 3.164

pH-Responsive Micelles Assembled by Three-Armed Degradable Block Copolymers with a Cholic Acid Core for Drug Controlled-Release

Jingjie Feng,Weiqiu Wen,Yong-Guang Jia,Sa Liu,Jianwei Guo

One of the most famous anticancer drugs, paclitaxel (PTX), has often been used in drug controlled-release studies. The polymers derived from bio-compound bile acids and degradable poly(ε-caprolactone) (PCL) form a reservoir and have been used as a drug delivery system with great advantages. Herein, we grafted poly(N,N-diethylaminoethyl methacrylate) and poly(poly(ethylene glycol) methyl ether methacrylate) into the bile acid-derived three-armed macroinitiator CA-(PCL)3, resulting in the amphiphilic block copolymers CA-(PCL-b-PDEAEMA-b-PPEGMA)3. These pH-responsive three-armed block copolymers self-assembled into micelles in aqueous solution and PTX was encapsulated into the micellar core to form PTX-loaded micelles with a drug loading of 29.92 wt %. The micelles were stable in PBS at pH 7.4 and showed a pH-triggered release behavior of PTX under acidic environments, in which 55% of PTX was released at pH 5.0 in 80 h. These cholic acid-based functionalized three-armed block polymers present good biocompatibility, showing great potential for drug controlled-release.Keywords:cholic acid;pH-sensitive;PTX;drug delivery

研究领域: 生物材料学 · 药剂学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ALLOYS AND COMPOUNDS · 2018 · IF 3.779

Carbon nanodots with intense emission from green to red and their multifunctional applications

Sai Lin,Yinzi Cheng,Chun Lin,Jiali Fang,Weidong Xiang,Xiaojuan Liang

In this report, carbon nanodots (CDs) with tunable full-color emission were successfully synthesized by a solvothermal method. By changing the carbon source (p-phenylenediamine or o-phenylenediamine) and the concentration, green, yellow, orange and red CDs (GCDs, YCDs, OCDs and RCDs) were successfully fabricated. As the concentration of the starting materials was increased, the emission peak was red-shifted. The shifted peaks showed strong intensity and an obvious color change. This concentration-dependent effect was attributed to the reabsorption phenomenon. Carbon source was critical in determining the fluorescence properties and the quantum yield (QY) of full-color CDs was high. The CDs also presented a distinct pH sensitivity. The PL intensity of RCDs showed linear decreases over decreasing pH from 11 to 4 and from 4 to 2. Fluorescent oil carrying CDs was successfully applied for various purposes such as anti-counterfeiting, information encryption and storage purposes. An RCD film was successfully fabricated that could improve the correlated color temperature and color rendering index of white light-emitting diodes.

研究领域: 材料科学 · 光学 · 化学
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DALTON TRANSACTIONS · 2013 ·Vol. 42 ·期 27 ·9852-9861 · IF 3.806

Core–shell structured luminescent and mesoporous β-NaYF4:Ce3+/Tb3+@mSiO2-PEG nanospheres for anti-cancer drug delivery

Yuan Wu,Dongmei Yang,Xiaojiao Kang,Ping'an Ma,Shanshan Huang,Yang Zhang,Chunxia Li,Jun Lin

Multifunctional nanocomposites integrating mesoporous and luminescence properties into a single entity are synthesized via a facile and effective approach. Oleic acid capped β-NaYF4:Ce3+/Tb3+ nanoparticles (NPs) are transferred into aqueous solution by cetyltrimethylammonium bromide (CTAB) surfactants, and further encapsulated with uniform mesoporous silica shell followed by the surface modification with poly(ethylene glycol) (PEG), leading to the formation of water-dispersible and biocompatible core–shell structured β-NaYF4:Ce3+/Tb3+@mSiO2-PEG (denoted as NPs@mSiO2-PEG) nanospheres. The as-synthesized nanospheres show a typical mesoporous structure and a green emission under UV irradiation. Doxorubicin hydrochloride (DOX), a widely used anti-cancer drug, is used as a model drug to evaluate the loading and controlled release behaviors of the NPs@mSiO2-PEG in phosphoric acidic buffer solutions (PBS) at different pH values (pH = 7.4 and 5.0). The composite carriers provide a pH-sensitive drug release pattern and the drug releases faster under lower pH value. The endocytosis process of fluorescein isothiocyanate (FITC)-labelled nanospheres is characterized using flow cytometry and confocal laser scanning microscopy (CLSM) against A549 cells. The in vitro cytotoxic effect against A549 cells of the DOX-loaded carriers is investigated in detail. In addition, the extent of drug release can be monitored by the variation of photoluminescence (PL) intensity of β-NaYF4:Ce3+/Tb3+. Considering the good biocompatibility and pH-dependent drug release pattern, such core–shell structured luminescent NPs@mSiO2-PEG nanospheres have potential applications in controlled drug delivery.

研究领域: 生物材料 · 纳米医学 · 肿瘤学
✓ 已验证 DOI PubMed 高影响因子
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Polymers · 2018 ·Vol. 10 ·期 10 ·1127 · IF 2.935

Design, Synthesis, and Characterization of Schiff Base Bond-Linked pH-Responsive Doxorubicin Prodrug Based on Functionalized mPEG-PCL for Targeted Cancer Therapy

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
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BIOMACROMOLECULES · 2022 · IF 6.978

Tumor Targeting and pH-Sensitive Inclusion Complex Based on HP-β-CD as a Potential Carrier for Paclitaxel: Fabrication, Molecular Docking, and Characterization

Zixue Li,Wei Zhao,Na Liang,Pengfei Yan,Shaoping Sun

In this study, a tumor-targeting and pH-sensitive inclusion complex based on the host–guest recognition between the chitosan and folic acid grafted HP-β-CD (FA–CS–CD) and stearic acid modified 2-benzimidazolemethanol (BM-SA) was designed and fabricated for the controlled delivery of paclitaxel (PTX). Through the combination of computational simulations and experiments, the interaction between FA–CS–CD, BM-SA, and PTX was investigated, and the optimized preparation method was obtained. For the optimized PTX-loaded FA–CS–CD/BM-SA inclusion complex, the particle size and zeta potential were 146 nm and +15.4 mV, respectively. In vitro drug release study revealed the pH-triggered drug release behavior of the inclusion complex. Both in vitro and in vivo evaluations demonstrated that the PTX-loaded FA–CS–CD/BM-SA inclusion complex exhibited enhanced antitumor efficiency and minimized systemic toxicity. This system might be a promising carrier for PTX.

研究领域: 药剂学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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Polymers · 2017 ·Vol. 9 ·期 12 ·698 · IF 3.364

Acetal-Linked Paclitaxel Polymeric Prodrug Based on Functionalized mPEG-PCL Diblock Polymer for pH-Triggered Drug Delivery

Yinglei Zhai,Xing Zhou,Lina Jia,Chao Ma,Ronghua Song,Yanhao Deng,Xueyao Hu,Wei Sun

The differences in micro-environment between cancer cells and the normal ones offer the possibility to develop stimuli-responsive drug-delivery systems for overcoming the drawbacks in the clinical use of anticancer drugs, such as paclitaxel, doxorubicin, and etc. Hence, we developed a novel endosomal pH-sensitive paclitaxel (PTX) prodrug micelles based on functionalized poly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL) diblock polymer with an acid-cleavable acetal (Ace) linkage (mPEG-PCL-Ace-PTX). The mPEG-PCL-Ace-PTX5with a high drug content of 23.5 wt % was self-assembled in phosphate buffer (pH 7.4, 10 mM) into nanosized micelles with an average diameter of 68.5 nm. The in vitro release studies demonstrated that mPEG-PCL-Ace-PTX5micelles was highly pH-sensitive, in which 16.8%, 32.8%, and 48.2% of parent free PTX was released from mPEG-PCL-Ace-PTX5micelles in 48 h at pH 7.4, 6.0, and 5.0, respectively. Thiazolyl Blue Tetrazolium Bromide (MTT) assays suggested that the pH-sensitive PTX prodrug micelles displayed higher therapeutic efficacy against MCF-7 cells compared with free PTX. Therefore, the PTX prodrug micelles with acetal bond may offer a promising strategy for cancer therapy.Keywords:prodrug;polymer micelles;pH-sensitive;acetal;paclitaxel

研究领域: 药学 · 肿瘤学
✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2016 · IF 3.138

Manipulation of pH-Sensitive interactions between podophyllotoxin-chitosan for enhanced controlled drug release

Chao Chen,Yong Yu,Xiaoli Wang,Ping Shi,Yibing Wang,Ping Wang

Podophyllotoxin (PPT) offers a broad-spectrum of anticancer activities, but little has been reported for its controlled release. This work shows that by manipulating molecular interactions between PPT and Chitosan, efficient nanoscale capsulation of PPT can be realized. The drug encapsulation efficiency is as high as 52%, with a final particle drug loading in the order of 10% (wt/wt). It further demonstrates that changes in pH can also significantly affect the rate of drug release from the Chitosan nanoparticles. Upon contact with cancer cells, chitosan nanoparticles enable efficient internalization and drug release. In vitro evaluations with HepG-2 and MCF-7 cells indicate that the chitosan nanoparticle carriers can improve drug efficacy in comparison to free PPT, most likely by regulating the intrinsic apoptotic signaling pathway to induce apoptosis. Overall, PPT chitosan nanoparticles promise a safe and efficient drug delivery system for PPT.

CAS / MDL: 518-28-5
研究领域: 药理学 · 生物材料 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION · 2018 · IF 1.911

Synthesis and evaluation of water soluble pH sensitive poly (vinyl alcohol)-doxorubicin conjugates

Nahla Rahoui,Bo Jiang,Nadia Taloub,Mohammad Hegazy,Yu Dong Huang

The accuracy of spatiotemporal control cargo delivery and release are primordial to enhance the therapeutic efficiency and decrease the undesirable effects, in this context a novel prodrug were developed based on biocompatible polyvinyl alcohol (PVA) substrate. PVA was conjugated to doxorubicin (PVA-DOX) via an acid-labile hydrazone linkage. PVA was first functionalized with acidic groups, then reacted with hydrazine hydrate to form an amide bond. The amine group of PVA hydrazide was linked to carbonyl group (C = O) of DOX to form a pH sensitive hydrazone bond. The molecular structure of the PVA-DOX was confirmed by FTIR, XPS, and 1H-NMR analysis methods. The degree of grafting were evaluated by TGA and confirmed by XPS, which reveals the successful bond attachment of DOX to PVA. Our findings confirm pH dependent DOX release from PVA-DOX prodrug with faster release rate in acidic environment (pH 5.0, pH 6.0) and slower release rate in neutral pH environment (pH 7.4). Compared to the primary DOX, our synthesized PVA-DOX conjugates could exhibit a promising therapeutic effect, high biocompatibility and zero premature release. The results prove the successful synthesis of PVA-DOX conjugates with high efficiency.

CAS / MDL: 6066-82-6 7647-01-0
研究领域: 药剂学 · 生物材料学 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF NANOPARTICLE RESEARCH · 2017 ·Vol. 19 ·期 12 ·1-11 · IF 2.02

Design and evaluation of dual CD44 receptor and folate receptor-targeting double-smart pH-response multifunctional nanocarrier

Chen Daquan,Song Xiaoyan,Wang Kaili,Guo Chunjing,Yu Yueming,Fan Huaying,Zhao Feng

In this article, in order to enhance the bioavailiability and tumor targeting of curcumin (Cur), the oligosaccharides of hyaluronan conjugates, folic acid-oligosaccharides of hyaluronan-acetal-menthone 1,2-glycerol ketal (FA-oHA-Ace-MGK) carried oHA as a ligand to CD44 receptor, double-pH-sensitive Ace-MGK as hydrophobic moieties, and FA as the target of folate receptor. The structure characteristics of this smart response multifunctional dual-targeting nano-sized carrier was measured by fourier-transform infrared (FT-IR) and nuclear magnetic resonance ( 1 H–NMR). Cur, an anticancer drug, was successfully loaded in FA-oHA-Ace-MGK micelles by self-assembly. The measurement results of transmission electron microscopy (TEM) presented that the Cur-loaded micelles were spherical in shape with the average size of 166.3 ± 2.12 nm and zeta potential − 30.07 mV. Much more encapsulated Cur could be released at mildly acidic environments than at pH 7.4, from the Cur-FA-oHA-Ace-MGK micelles. Cytotoxicity assay indicated that non-Cur loaded micelles mostly had no cytotoxicity to MCF-7 cells and A549 cells, and Cur-loaded micelles had significantly lower survival rate than Cur suspension in the same concentration, which proved that the drug-loaded micelles can effectively inhibit tumor cell growth. The targeting of CD44 receptors and folate receptors was proved in vitro cellular uptake assay. These results showed the promising potential of FA-oHA-Ace-MGK as an effective nano-sized carrier for anti-tumor drug delivery.

研究领域: 药学 · 肿瘤学 · 生物材料学
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Water · 2022 ·Vol. 14 ·期 8 ·1190 · IF 3.53

pH-Responsive Eco-Friendly Chitosan–Chlorella Hydrogel Beads for Water Retention and Controlled Release of Humic Acid

Hao Li,Jin Wang,Yu Luo,Bo Bai,Fangli Cao

For improving the mechanical strength of controlled release fertilizer (CRF) hydrogels, a novel material ofChlorellawas employed as a bio-based filler to prepare chitosan–chlorella hydrogel beads with physical crosslink method. Here, the synthesis mechanism was investigated, and the chitosan–chlorella hydrogel beads exhibited enhanced mechanical stability under centrifugation and sonication than pure chitosan hydrogel beads.Chlorellabrought more abundant functional groups to original chitosan hydrogel, hence, chitosan–chlorella hydrogel beads represented greater sensitivity and controllable response to external factors including pH, salt solution, temperature. In distilled water, the hydrogel beads with 40 wt%Chlorellareached the largest water absorption ratio of 42.92 g/g. Moreover, the mechanism and kinetics process of swelling behavior of the chitosan–chlorella hydrogel beads were evaluated, and the loading and releasing of humic acid by the hydrogel beads as a carrier material were pH-dependent and adjustable, which exhibit the potential of chitosan–chlorella hydrogel beads in the field of controlled release carrier biomaterials.Keywords:hydrogel;controlled release;swelling;Chlorella;pH sensitivity

研究领域: 材料科学 · 环境科学 · 农业
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JOURNAL OF BIOMATERIALS APPLICATIONS · 2017 · IF 2.31

Synthesis and evaluation of pH-sensitive, self-assembled chitosan-based nanoparticles as efficient doxorubicin carriers

Mazhar Ali Raja,Muhammad Arif,Chao Feng,Shah Zeenat,Chen-Guang Liu

A novel pH-responsive polymer based on amphiphilic N-acetyl histidine and arginine-grafted chitosan was synthesized using N-acetyl histidine as hydrophobic segment and arginine as hydrophilic segment by 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide-mediated coupling reactions as anticancer drug delivery system for doxorubicin. The structure of the synthesized polymer was confirmed by Fourier transform infrared and 1H nuclear magnetic resonance analysis. Due to self-association behavior, N-acetyl histidine and arginine-grafted chitosan structured nanoparticles with in size range of 204 nm. N-acetyl histidine and arginine-grafted chitosan with different substitution degree of N-acetyl histidine were initially prepared and characterized. The critical micelle concentration decreased with increasing substitution degree of N-acetyl histidine. Furthermore, N-acetyl histidine and arginine-grafted chitosan nanoparticles exhibited an acidic pH-triggered aggregation and disassembling nature. The doxorubicin-encapsulated nanoparticles based on synthesized conjugate (N-acetyl histidine and arginine-grafted chitosan/doxorubicin nanoparticles) showed a sustained drug release pattern, which could be hastened under acidic pH conditions but delayed with increasing substitution degree of N-acetyl histidine. Anticancer effects demonstrated that N-acetyl histidine and arginine-grafted chitosan/doxorubicin nanoparticles could suppress both sensitive and resistant human breast tumor cell line (MCF-7) efficiently in a dose- and time-dependent pattern. Confocal microscopy results evidenced increased cellular uptake and enhanced retention of the synthesized nanoparticles in drug-resistant cells demonstrating better efficacy of nanoparticles over native doxorubicin. These results suggest that N-acetyl histidine and arginine-grafted chitosan/doxorubicin nanoparticles might be promising carriers for delivery of hydrophobic drug doxorubicin against drug-resistant tumors.

研究领域: 药学 · 生物材料 · 肿瘤学
✓ 已验证 DOI PubMed 高影响因子
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Materials Today Communications · 2025 · IF 4.5

Stretchable and pH-sensitive liquid metal/mxene hydrogels for antibacterial environment creation and photothermal therapy of infected wounds

Wenqiang Zhang,Hongjie Guo,Xiang Zhang,Hongliang Li

Wound infection remains a significant challenge in clinical medicine, impeding the healing process of wounds. Conventional therapeutic approaches, including antibiotics, surgical debridement, and conventional dressings, are often limited by issues such as antibiotic resistance, secondary tissue damage, and insufficient biocompatibility. Existing wound dressings exhibit poor mechanical properties and possess only single therapeutic functions, lacking the ability to effectively monitor wound healing status. To address these limitations, this study have developed a novel hydrogel dressing. This dressing utilizes microfibrillated cellulose (MFC) to stably encapsulate liquid metal (Ga) droplets, which also serve as a photothermal filler for the hydrogel. The addition of MXene stabilizes the colloidal system, and the resulting hydrogel is integrated with a pH-sensitive optical fiber to form a pH-sensitive optical fiber/ PMGa hydrogel. This composite hydrogel exhibits excellent mechanical properties (400 % elongation at break), antimicrobial activity, and pH sensitivity. Moreover, the hydrogel's tissue adhesion and stretchability enable it to conform to various skin surfaces and accommodate skin movement and stretching. The pH-sensitive optical fiber/PMGa hydrogel not only monitors the pH value of the wound through different light transmittance to judge the state of the wound environment, but also effectively inhibits bacterial growth through its photothermal effect. It provides an optimal temperature and humidity environment to promote cell proliferation and granulation tissue formation, thereby facilitating photothermal therapy. In summary, this work presents a novel hydrogel dressing that integrates monitoring and therapeutic functions. This comprehensive solution offers a new platform for the development of wound infection treatment materials.

CAS / MDL: 81-88-9
研究领域: 生物医学工程 · 材料科学 · 伤口护理
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