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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2023 · IF 6.1

Mucoadhesive Hydrogel with Anti-gastric Acid and Sustained-Release Functions for Amelioration of DSS-Induced Ulcerative Colitis

Hai-Bo Huang,Wei Gong,Yi-Yang Hou,Wan-Ying He,Ran Wang,Xin-Chuang Wang,Jiang-Ning Hu

Mucoadhesive hydrogels with multifunctional properties such as gastric acid resistance and sustained drug release in the intestinal tract are highly desirable for the oral treatment of inflammatory bowel diseases (IBDs). Polyphenols are proven to have great efficacies compared with the first-line drugs for IBD treatments. We recently reported that gallic acid (GA) was capable of forming a hydrogel. However, this hydrogel is prone to easy degradation and poor adhesion in vivo. To tackle this problem, the current study introduced sodium alginate (SA) to form a gallic acid/sodium alginate hybrid hydrogel (GAS). As expected, the GAS hydrogel showed excellent antiacid, mucoadhesive, and sustained degradation properties in the intestinal tract. In vitro studies demonstrated that the GAS hydrogel significantly alleviated ulcerative colitis (UC) in mice. The colonic length of the GAS group (7.75 ± 0.38 cm) was significantly longer than that of the UC group (6.12 ± 0.25 cm). The disease activity index (DAI) value of the UC group was (5.5 ± 0.57), which was markedly higher than that of the GAS group (2.5 ± 0.65). The GAS hydrogel also could inhibit the expression of inflammatory cytokines, regulating macrophage polarization and improving the intestinal mucosal barrier functions. All these results indicated that the GAS hydrogel was an ideal candidate for oral treatment of UC.

CAS / MDL: 149-91-7
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JOURNAL OF BIOMEDICAL MATERIALS RESEARCH PART A · 2018 ·Vol. 107 ·期 2 ·319-329 · IF 3.231

Preparation and characterization of folic acid functionalized bioactive glass for targeted delivery and sustained release of methotrexate

Jianhui Chen,Xiaofeng Chen,Zhengyu Yang,Xiaojun Tan,Jiachen Wang,Yao Chen

We have successfully prepared a novel targeted drug delivery system, composed of folic acid (FA) as targeting molecule, methotrexate (MTX) as anticancer drug, and bioactive glass (BG) as carrier. The BG nanoparticles were synthesized by sol-gel method with the dodecylamine as template. The surface of BG nanoparticles was grafted with amino groups by (3-aminopropyl) triethoxysilane, then, FA and MTX were covalently conjugated to the surface of modified BG through amidation reaction, so FA functionalized BG (BG-FA) and targeted drug delivery system (MTX-BG-FA) were prepared. The physicochemical properties of BG, BG-NH 2 , and BG-FA were characterized by various methods, such as X-ray diffraction, scanning electron microscopy, transmission electron microscopy, Fourier transform infrared spectroscopy, ultraviolet–visible, and so on. Moreover, the drug release results showed that the MTX-BG-FA had sustained release property because of the peptide bond between MTX and BG-FA. And the cytocompatibility evaluation demonstrated that the BG and BG-FA were biocompatible and BG-FA even could promote cell proliferation, while the MTX-BG-FA had high cytotoxicity owning to the sustained release of anticancer drug. From the above, it could be concluded that MTX-BG-FA could kill tumor cells targetedly and sustainedly, which made it a good cancer targeted therapy material. © 2018 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 107A: 319–329, 2019.

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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2019 · IF 2.606

Berberine-loaded solid proliposomes prepared using solution enhanced dispersion by supercritical CO2: Sustained release and bioavailability enhancement

Jingfu Jia,Kerong Zhang,Xue Zhou,Jinfang Ma,Xiaojing Liu,Anya Xiang,Fahuan Ge

In present study, berberine proliposomes (ber-PL) of powder state that can form liposomal structure via self-assemble in water was prepared using solution enhanced dispersion by supercritical CO 2 (SEDS) to improve the oral bioavailability of berberine. Several important parameters were optimized using Box-Behnken design to get ber-PL with high entrapment efficacy ( EE ) of 90.3% ± 4.9%. Physicochemical characterization showed the optimum ber-PL was amorphous spherical nanoparticles and could form uniform liposomes around 80 nm easily via hydration. EE was closely related to the particle morphology of ber-PL. In vitro drug release study displayed a sustained release profile, and the drug released faster in neutral condition than acid medium. The oral bioavailability for ber-PL was 22.47 times greater than raw berberine, and the mean residence time of berberine in plasma was extended from 6.82 ± 2.99 to 10.83 ± 2.01 h as well. The proliposome formulated using SEDS is a favorable strategy to improve the bioavailability of berberine.

CAS / MDL: 57-88-5 633-65-8
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CHEMOSPHERE · 2018 · IF 4.427

Inhibitory effect and mechanism of linoleic acid sustained-release microspheres on Microcystis aeruginosa at different growth phases

Lixiao Ni,Shiyi Rong,Guoxiu Gu,Lingling Hu,Peifang Wang,Danye Li,Feifei Yue,Na Wang,Hanqi Wu,Shiyin Li

Environment-friendly algaecides based on allelopathy have been extensively studied to control harmful algal blooms (HABs). The inhibitory effects of linoleic acid (LA) sustained-release microspheres on different cell densities of Microcystis aeruginosa ( M. aeruginosa ) at different growth phases were studied. The results showed that the growth of M. aeruginosa could be inhibited within 4 days and the constant inhibitory rate with initial algal density of 8 × 10 5  cells∙mL −1 (exponential phase) was up to 96% compared with control. The chlorophyll-a content in the treatment group had the same change trend with the algal density and declined significantly at day 20th, which suggested that the microspheres could promote the degradation of chlorophyll-a. The activities of superoxide dismutase (SOD) and catalase (CAT) increased gradually within 5 days but then declined sharply, which indicated that LA microspheres could cause oxidative damage to M. aeruginosa during the process of inhibition and reduce the activities of antioxidant enzymes. In addition, the concentration of oxygen free radical (O 2 − ) increased at day 10th and rose constantly, and the content of malodialdehyde (MDA) increased to 2.7 times as much as control at day 20th. Furthermore, the content of protein, nucleic acid and the conductivity in culture solution showed a significant rise. These results showed that algal cell membrane lipid peroxidation occurred and the membrane permeability increased, accompanied by the damage of cell membrane. To sum up, the destruction of algal cell membrane is the main mechanism of LA microspheres inhibiting algal growth.

CAS / MDL: 7439-91-0
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2019 · IF 6.361

Development of a polysaccharide based multi-unit nanofiber mat for colon-targeted sustained release of salmon calcitonin

Kun Feng,Chen Li,Yun-Shan Wei,Min-Hua Zong,Hong Wu,Shuang-Yan Han

Advances in pharmaceutical technology have promoted the development of colon-targeted delivery system for oral administration of bioactive peptides or proteins to enhance their bioavailability. In this study, a multi-unit nanofiber mat was fabricated by coaxial electrospinning and its feasibility as the colon-targeted delivery system for a bioactive peptide, salmon calcitonin (sCT), was investigated. Sodium alginate and sCT-loaded liposome coated with pectin served as the shell layer and core layer, respectively. An in vitro study demonstrated that the encapsulated sCT was released in a sustained and colon-targeted way. Analysis using different mathematical models showed that release followed a complex mechanism. In addition, greater amounts of sCT were released from the core-shell nanofiber mat into simulated colon fluid (SCF) than was released from a uniaxial nanofiber mat (65.2% vs. 47.8%). The use of a core-shell nanofiber mat further alleviated the burst release of sCT into simulated gastric and intestinal fluid (SGF and SIF), demonstrating the superiority of a multi-unit vehicle for colon-targeted delivery of sCT. Furthermore, 88% of the bioactivity of encapsulated sCT was retained. This multi-unit vehicle offers a better-designed vehicle for the colon-targeted sustained release of bioactive peptides or proteins and, thus, should improve oral bioavailability.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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LWT-FOOD SCIENCE AND TECHNOLOGY · 2021 · IF 4.952

Encapsulation of curcumin in ZEIN-HTCC complexes: Physicochemical characterization, in vitro sustained release behavior and encapsulation mechanism

Gerui Ren,Ying He,Chengzhi Liu,Fangfang Ni,Xin Luo,Jieyu Shi,Yuling Song,Ting Li,Min Huang,Qing Shen,Hujun Xie

In order to improve the water solubility and stability of curcumin (CUR) and achieve its sustained release, the ZEIN– N -(2-hydroxy) propyl-3-trimethylammonium chitosan chloride (HTCC) complexes were designed to encapsulate CUR using an antisolvent precipitation (ASP) method. The encapsulation efficiency ( EE ) and loading capacity ( LC ) of curcumin in ZEIN-HTCC complexes were 92.2% and 0.6%, respectively. After encapsulation, the resistance of curcumin to thermal, natural light and UV irradiation, as well as the antioxidative activity were improved significantly ( P  < 0.05). ZEIN-HTCC-CUR complexes exhibited good redispersibility and enhanced the water solubility of curcumin. In vitro simulated digestion experiments clarified that the ZEIN-HTCC complexes can control the sustained release behavior of curcumin, and the release kinetics can be fitted by the Higuchi model. Results taken from fluorescence spectra and Fourier transform infrared spectroscopy (FTIR) indicated that hydrophobic interaction, hydrogen bonding and electrostatic interactions were the main driving forces to form the ZEIN-HTCC-CUR complexes. The X-ray diffraction (XRD) results revealed that the encapsulated curcumin was in an amorphous state. The information provided by this study should be of interest to food industry to fabricate robust nanoscale delivery systems with ZEIN-HTCC complexes for CUR and other hydrophobic bioactive compounds.

CAS / MDL: 458-37-7 9001-75-6
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JOURNAL OF HAZARDOUS MATERIALS · 2021 · IF 10.588

Calcium sulfide-organosilicon complex for sustained release of H2S in strongly acidic wastewater: Synthesis, mechanism and efficiency

Feng Zhu,Xingyun Hu,Linghao Kong,Xianjia Peng

Sulfide precipitation is an efficient method to remove Cu(II) and As(III) from strongly acidic wastewater, but the instantaneous release of H 2 S from traditional sulfuration reagents causes serious H 2 S pollution. Moreover, the obtained precipitates are mixtures of CuS and As 2 S 3 , leading to difficulties in resource recovery. In this study, a calcium sulfide-organosilicon complex (CaS-OSCS), in which CaS was coated into a matrix of {[O 1.5 Si(CH 2 ) 3 NH]CS} n (OSCS) via the coordination bonding, was developed. OSCS, as a matrix of CaS-OSCS, can ensure the sustained and stable release of H 2 S under strongly acidic conditions owing to its low swelling (1.75% swelling ratio) and excellent acid resistance. The release longevity of H 2 S from CaS-OSCS extended from 5 min up to 50 min compared with that from CaS because the hydrophobic OSCS prevented solution diffusing to the pores of CaS-OSCS and thus slowed down the hydrolysis of CaS in pores. 99% of Cu(II)/As(III) was precipitated without H 2 S escape, and the dosage of sulfuration reagents was reduced by 30%. In addition, CaS-OSCS improved the selective separation of copper from wastewater, and a separation factor between Cu(II) and As(III) reached 2376. This study provides a potential approach for the elimination of H 2 S pollution and selective recovery of copper.

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JOURNAL OF HAZARDOUS MATERIALS · 2024 · IF 12.2

Carbon fate and potential carbon metabolism effects during in-situ cyanobacterial inhibition by artemisinin sustained-release algaecides

Yushen Ma,Xiaoming Zhu,Lixiao Ni,Cunhao Du,Wenlu Sang,Chu Xu,Jiahui Shi,Yiping Li,Shiyin Li,Linyun Zhang

Carbon pools and microbial carbon metabolism can be significantly altered due to the diverse organic matter properties and low pH characteristics of artemisinin sustained-release algaecides (ASAs). These effects have still not been systematically studied, leading to uncertainty in the application of ASAs for cyanobacterial management in natural waters. This study assessed the effects of ASAs on carbon fate, carbon metabolism and potential ecological impacts during in-situ cyanobacterial inhibition. In the initial phase of ASAs-induced cyanobacterial inhibition (2–10 days), the carbon pool underwent significant changes due to the increased proportion of C4 plant-derived organic matter (97 %), humification level (FI =0.9–1.5), and inorganic carbon concentration (TIC = 80–110 mg/L). The cyanobacterial apoptosis triggered by ASAs produced particulate organic carbon, which provided a bioavailable carbon source for bacterial metabolism. ASAs enhanced the connection between bacteria and the carbon pool, as well as their carbon metabolism capabilities, by increasing the relative abundance of Proteobacteria (33.1 %−37.3 %), bacterial diversity, the proportion of Alphaproteobacteria and Betaproteobacteria (19.3 %−29.5 %) involved in carbon metabolism, and the complexity of the environment-bacteria co-occurrence network. These effects contributed to maintaining long-term ecosystem stability and resistance to cyanobacterial proliferation. Our findings elucidate the influence of bacterial carbon metabolism by ASAs as one of an important mechanism for achieving cyanobacterial inhibition in natural water, and emphasize the important role of bacteria in maintaining ecological stability during in situ cyanobacterial management.

CAS / MDL: 9012-76-4
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2024 · IF 5.3

Construction of injectable micron-sized polymorphic vesicles for prolonged local anesthesia with weekly sustained release of ropivacaine

Xin Tan,Peng Ke,Ziying Chen,Yi Zhou,Linjie Wu,Xiaoyan Bao,Yaxin Qin,Ruolin Jiang,Min Han

Currently, to overcome the short half-life of the local anesthetic ropivacaine, drug delivery systems such as nanoparticles and liposomes have been used to prolong the analgesic effect, but they are prone to abrupt release from the site of administration or have poor slow-release effects, which increases the risk of cardiotoxicity. In this study, injectable lipid suspensions based on ropivacaine-docusate sodium hydrophobic ion pairing (HIP) were designed to significantly prolong the duration of analgesia. The resulting ion-paired lipid suspension (HIP/LIPO) had a micrometer scale and a high zeta potential, which facilitates stable in situ retention. The strong interaction between docusate sodium and ropivacaine was verified using thermal and spectroscopic analyses, and the formation of micron-sized polymorphic vesicles was attributed to the mutual stabilizing interactions between ropivacaine-docusate sodium HIP, docusate sodium and lecithin. The HIP/LIPO delivery system could maintain drug release for more than 5 days in vitro and achieve high analgesic efficacy for more than 10 days in vivo , reducing the side effects associated with high drug doses. The stable HIP/LIPO delivery system is a promising strategy that offers a clinically beneficial alternative for postoperative pain management and other diseases.

CAS / MDL: 577-11-7 9004-32-4
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POLYMERS FOR ADVANCED TECHNOLOGIES · 2017 ·Vol. 29 ·期 1 ·384-393 · IF 1.907

In vitro evaluation of sustained release of risperidone-loaded microspheres fabricated from different viscosity of PLGA polymers

Qing Shang,Aixin Zhang,Zhaoying Wu,Sijin Huang,Ruiqiong Tian

The aim of this study was to fabricate different risperidone (RIS)–loaded poly(lactic-co-glycolic acid) microspheres (PLGA MS) with various viscosity of PLGA polymers and investigate the RIS release profiles. Risperidone-loaded PLGA MS were fabricated via an oil/water–type emulsion solvent evaporation method, using ethyl acetate and benzil alcohol as the dispersed solvents. The PLGA (75:25) with the viscosity of 0.82, 0.93, and 1.10 dL/g was used in the fabrication. The morphology and the degradation of the RIS-PLGA MS were investigated with a scanning electron microscope. The distribution states of RIS in the PLGA MS were studied with differential scanning calorimetry. The residual of ethyl acetate and benzil alcohol in the resulting MS was monitored with gas chromatography. The in vitro release profiles of RIS from PLGA MS were also studied. Scanning electron microscope photographs illustrated that the obtained PLGA MS were monodisperse spheres with an average diameter of 100 μm. Gas chromatography results suggested that no residual ethyl acetate was left in the final RIS-PLGA MS, and the residue amount of benzil alcohol was about 1%. In vitro drug release profiles from the microsphere showed a substantially sigmoidal pattern of negligible initial burst up to 24 hours and minimal release (time lag) for 14 days. After the lag phase, slow release took a place up to 30 days, and then rapid release occurred sharply for about 2 weeks. The RIS release reached equilibrium around day 50. All release profiles showed the similar trend, and no significant difference was observed among these release profiles ( P > .05). This phenomenon indicated that RIS-loaded PLGA MS with the viscosity of 0.82 to 0.93 dL/g showed the optimal release behavior. However, no obvious differences were found among the MS obtained from the viscosity of 0.82 to 1.10 dL/g. These studies provided basis for the quality control in the industrial production of PLGA MS.

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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2014 · IF 3.107

Amphiphilic Chitosan Derivatives-Based Liposomes: Synthesis, Development, and Properties as a Carrier for Sustained Release of Salidroside

Hailong Peng,Wenjian Li,Fangjian Ning,Lihua Yao,Mei Luo,Xuemei Zhu,Qiang Zhao,Hua Xiong

A novel amphiphilic chitosan derivative of N,N-dimethylhexadecyl carboxymethyl chitosan (DCMCs) was synthesized. The structure of DCMCs was confirmed via FT-IR and 1H NMR, and the critical micelle concentration (CMC) was investigated by fluorescence spectroscopy. The results indicated that DCMCs has hydrophilic carboxyl and hydrophobic methylene groups and the CMC value was 23.00 mg·L–1. The polymeric liposomes (DCMCs/cholesterol liposomes, DC-Ls) were developed, and its properties were evaluated. The DC-Ls exhibited multilamellar spheres with positive charge (+73.30 mV), narrow size distribution (PDI = 0.277), and good crystal properties. Salidroside was first to encapsulate into DC-Ls. Compared with traditional liposomes (phosphatidylcholine/cholesterol liposome, PC-Ls), DC-Ls showed higher encapsulation efficiency (82.46%) and slower sustained release rate. The in vitro salidroside release from DC-Ls was governed by two distinct stages (i.e., burst release and sustained release) and was dependent on the pH of the release medium. The case II transport and case I Fichian diffusion were the main release mechanisms for the entire release procedure. These results indicated that DC-Ls may be a potential carrier system for the production of functional foods that contain salidroside or other bioactive food ingredients.

CAS / MDL: 57-88-5 129-00-0
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POLYMERS FOR ADVANCED TECHNOLOGIES · 2015 ·Vol. 27 ·期 5 ·615-622 · IF 1.757

Enhancement of electrostatic charge dissipation properties of polymers by a sustained-release effect of mesoporous silica nanoparticles

Rui Li,JingJing Si,Ping Tang

Small molecular surfactant (SMS), used as antistatic agent of polymers, is prone to the wash-out effects thus reducing its lifetime. To address this issue, the sustained-release antistatic agent is prepared by encapsulating SMS (HDC-102 or HDC-193) into mesoporous silica nanoparticles such as MCM-41 and is used to modify the antistatic properties of polystyrene (PS). The water-resistant test is used to evaluate the sustained-release effect, and the results showed that the HDC-102/MCM-41/PS composite retains favorable antistatic properties with the R s of 6.2 × 10 11 after five times washing, while the HDC-102/PS loses antistatic properties after twice washing. The contact angle measurement demonstrates that the sustained-release effect is affected by the characteristics of SMS. Moreover, the coefficient of thermal expansion of SMS/PS composites is decreased, and the thermal decomposition temperature is increased with incorporation of MCM-41. This approach may be used in polymer systems with the other small molecular additives to prolong their lifetime. Copyright © 2015 John Wiley & Sons, Ltd.

CAS / MDL: 872-50-4
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