INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Yingjie Geng,Yuan Li,Haolong Qi,Jianguo Gao,Yanqing Wu,Xiaoqing Cai
Mesalazine (MSZ), a first-line treatment for ulcerative colitis (UC), was formulated into acid-resistant, colon-targeted gel microspheres to reduce upper gastrointestinal tract (GIT) exposure and extend drug retention in the colon. In this study, we used MSZ/hydroxypropyl-β-cyclodextrin (MSZ/HP-β-CD) as the model drug, dopamine-modified sodium alginate (DA-SA) and konjac glucomannan (KGM) as the carrier matrix, and chitosan (CS) as the coating material. The colon-targeted gel microspheres (MSZ/HP-β-CD/DA-SA/KGM/CS) were prepared using the drop method. These microspheres had a drug loading capacity of 7.9 ± 0.01 % and an encapsulation efficiency of 72.5 ± 0.03 %. The drug primarily released in the colon environment, showing pH and β-mannanase sensitivity. The dried microspheres measured approximately 0.6 mm, suitable for oral administration. In the rat UC model, after oral administration of gel microspheres, the colon length increased, while the DAI score, spleen index, and the expression levels of IL-6, IL-1β, TNF-α, TLR4, MyD88 and NF-κB p65 all decreased. Histopathological examination showed that treated UC rats' colon tissues closely resembled those of healthy controls. These findings indicate that pH-enzyme-responsive coated gel microspheres can effectively target the colon and show potential for UC treatment.
研究领域:
药剂学
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消化病学
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生物医学工程
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DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2021
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IF 4.539
Mengna Zhang,Shujing Zhang,Kun Zhang,Zongyuan Zhu,Yalei Miao,Yudian Qiu,Panke Zhang,Xubo Zhao
Functionality of polymers is crucially fundamental to polymers. However, the application of polymers faces great challenges due to the insufficient function of hydrophobic chain, especially in drug delivery. One novel approach to solve this dilemma involves the use of medicated hydrophobic chains. Herein, the polymer-doxorubicin conjugates are synthesized from hydrophilic copolymer and hydrophobic chain composed of doxorubicin (DOX). DOX, a common hydrophobic anticancer drug , is used to serve as a hydrophobic pendant for inducing self-assembly of polymer-doxorubicin conjugates. The self-assembly of polymer-drug conjugates is employed to encapsulate the unreacted drug for the first time and form drug-loaded polyprodrug micelles that possess a low critical micelle concentration (CMC), which improves the use efficiency of expensive drug. The detachment of DOX moieties from polymer-doxorubicin conjugates caused by amidase facilitates the disintegration of DOX-loaded polyprodrug micelles to trigger the enhanced release of DOX in a slightly acidic medium. It is demonstrated that the DOX-loaded polyprodrug micelles have a higher suppression against cancer cells in in vitro investigations. This work thus proposes a strategy to modify the poor functionality of polymer-based nanostructures , through designing the medicated hydrophobic chains. This strategy facilitates the potential application of polymer-drug conjugates and provides profound insights into the effect of medicated polymer on drug delivery system.
研究领域:
生物材料学
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药剂学
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肿瘤学
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产品关联
DOI
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2024
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IF 13.3
Tiantian Min,Jin Yue,Chuanxiang Cheng,Xiaoyun Ma,Shihan Weng,Yuwan Luo,Yujie Lei,Yangyang Long
Developing stimuli-responsive on-demand release systems is very important to effectively suppress microbial infections and excessive food decomposition. However, the commonly designed controlled release systems with a single responsiveness cannot accurately response to environmental changes in food packaging scenarios. Herein, a pH/enzyme dual-responsive active packaging was fabricated based on in situ growth of ZIF-8 nanoparticles (ZIF-8 NPs) on TEMPO-oxidized cellulose (TOCNF) film and loading with carvacrol (CAR), after that electrostatic adsorbing pectin as “gatekeeper” for fruit preservation. The developed CAR@ZIF-8/TOCNF/Pec film was able to respond to acidic condition and pectinase produced by microorganisms in the case of fungal infections during food storage, thus possessing a dual-responsive controlled-release function. The release rate of CAR reached approximately 86.83 ± 1.82 % at pH = 5.0 and reached 88.65 ± 1.86 % in the presence of pectinase (1.0 mg/mL) after 168 h. In addition, the CAR@ZIF-8/TOCNF/Pec film performed superior inhibition efficacy against Escherichia coli, Staphylococcus aureus , and Aspergillus niger . The CAR@ZIF-8/TOCNF/Pec film were highly effective in preserving the freshness of fungus-inoculated raspberries and mangoes, and inhibited the spread of fungal spores during storage for 5 and 7 days, respectively. Therefore, this work provided a promising, smart and eco-friendly strategy for on-demand and precise release of bioactive ingredients during food storage and preservation.
研究领域:
材料科学
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食品科学
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生物技术
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产品关联
DOI
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
·
2023
·Vol. 21
·期 1
·1-20
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IF 10.2
Dong Lanlan,Huang Can,Zhao Baohua,Hu Guangyun,Huang Yong,Zhang Xiaorong,Hu Xiaohong,Wang Ying,XiaoyanSun,Qian Wei,Luo Gaoxing
Suppressing persistent multidrug-resistant (MDR) bacterial infections and excessive inflammation is the key for treating chronic wounds. Therefore, developing a microenvironment-responsive material with good biodegradability, drug-loading, anti-infection, and anti-inflammatory properties is desired to boost the chronic wounds healing process; however, using ordinary assembly remains a defect. Herein, we propose a pH/enzyme dual-responsive polymyxin B (PMB) spatiotemporal-release hydrogel (GelMA/OSSA/PMB), namely, the amount of OSSA and PMB released from GelMA/OSSA/PMB was closely related the wound pH and the enzyme concentration changing. The GelMA/OSSA/PMB showed better biosafety than equivalent free PMB, owing to the controlled release of PMB, which helped kill planktonic bacteria and inhibit biofilm activity in vitro. In addition, the GelMA/OSSA/PMB exhibited excellent antibacterial and anti-inflammatory properties. A MDR Pseudomonas aeruginosa caused infection was effectively resolved by the GelMA/OSSA/PMB hydrogel in vivo, thereby significantly boosting wound closure during the inflammatory phase. Furthermore, GelMA/OSSA/PMB accelerated the sequential phases of wound repair.
研究领域:
生物医学工程
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材料科学
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药物学
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伤口愈合
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传染病
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产品关联
DOI
PubMed
高影响因子
EUROPEAN POLYMER JOURNAL
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2019
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IF 3.621
Jie Wu,Ximing Tian,Yihua Yin,Meng He,Weiquan Cai,Guanghua He,Wenjin Xu,Yue Dai,Jiahao Mai,Mengqi Gan,Fengxinjia Zhang
To improve hydrolytic stability and biological half-life and anticancer efficacy of the anti-cancer drug melphalan (Mel), a novel esterification strategy was developed to fabricate a pH/enzyme dual-responsive polymer prodrug (mPEG-Mel) via the formation of an ion bond between the carboxyl group in Mel and diazotized p-aminobenzoate-terminated poly(ethylene glycol) monomethyl ether (mPEG-N 2 + ) followed by light-induced conversion of the ionic bond to an ester bond. The prodrug could self-assemble into nanoparticles. Under physiological conditions (pH 7.4), the nanoparticles exhibited a regular core-shell structure with about 100 nm, which could effectively inhibit the hydrolysis of pharmacophores in Mel structure and showed the long-circulation ability. While pH dropped to 5.0, an obvious increase in the nanoparticle size was observed and enhanced by different concentrations of cathepsin B (CTB), reaching a diameter of 675 nm or more in the presence of 2.0 µg/mL CTB. The nanoparticles showed minimal drug release at pH 7.4 (less than 10% in 24 h); however, drug release could be significantly accelerated in a CTB-containing medium at pH 5.0. Cell experiments showed that the half-inhibitory concentration (IC50) of nanoparticles was 1.00 µg/mL, which was about 5 times lower than that of free Mel (5.00 µg/mL), and indicating that the nanoparticles were more cytotoxic to cancer cells (4T1 cells). However, significantly reduced cytostatic effects were observed for normal cells (3T3 cells). In addition, cell uptake observation further supported the above experimental results, a stronger red fluorescence in 4T1 cells was observed for NR-loaded nanoparticles, which meant that the nanoparticles could release drug in response to pH/enzyme stimulation. Thus, mPEG-Mel based pH/enzyme double-response polymer prodrug nanoparticles could effectively enhance drug stability and anticancer efficacy.
研究领域:
药学
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纳米技术
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癌症研究
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药物递送系统
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）