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FIBERS AND POLYMERS · 2018 ·Vol. 19 ·期 3 ·477-488 · IF 1.353

Porous Laponite/Poly(L-lactic acid) Membrane with Controlled Release of TCH and Efficient Antibacterial Performance

Peng Qingyan,Xu Pengjun,Xiao Shili

Fabrication of porous polymer membrane with controlled drug release and efficient antibacterial performances is of great interest in biomedical fields. In this study, Laponite (LAP) nanodisks were first used to encapsulate a model antibiotic drug, tetracycline hydrochloride (TCH). Then, drug-loaded LAP nanodisks with an optimized loading efficiency (85.3 %) were mixed with poly(L-lactic acid) (PLLA) polymer to form drug-loaded composite porous membrane via solvent coasting. The structure, morphology and swelling property of the porous membranes formed with varied solvent ratio of methylene dichloride (DCM) and dimethyl formamide (DMF) in the mixture solvent were characterized using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy and swelling test. In vitro drug release behavior, the cytotoxicity and the antibacterial activity of drug-loaded composite membranes were evaluated. Results showed that the TCH release was dependent on the physical structure of PLLA membrane and the presence of LAP nanodisks effectively weakened the initial burst release of TCH, and improved the sustained release property of porous PLLA membrane. The released TCH of TCH/LAP/PLLA 3:1 and TCH/LAP/PLLA 4:1 was 10.0 % and 5.3 % within initial 1 h, respectively. More importantly, the porous TCH/LAP/PLLA membrane was cytocompatible and displayed considerable antibacterial activity, solely associated with the loaded TCH drug, confirming its potential utility in wound dressings and tissue engineering.

CAS / MDL: 64-75-5
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Royal Society Open Science · 2018 ·Vol. 5 ·期 1 · IF 2.504

Mesoporous silica nanoparticle-based intelligent drug delivery system for bienzyme-responsive tumour targeting and controlled release

Yang Zhang,Juan Xu

This paper proposes a novel type of multifunctional envelope-type mesoporous silica nanoparticle (MSN) to achieve cancer cell targeting and drug-controlled release. In this system, MSNs were first modified by active targeting moiety hyaluronic acid (HA) for breast cancer cell targeting and hyaluronidases (Hyal)-induced intracellular drug release. Then gelatin, a proteinaceous biopolymer, was grafted onto the MSNs to form a capping layer via glutaraldehyde-mediated cross-linking. To shield against unspecific uptake of cells and prolong circulation time, the nanoparticles were further decorated with poly(ethylene glycol) polymers (PEG) to obtain MSN@HA-gelatin-PEG (MHGP). Doxorubicin (DOX), as a model drug, was loaded into PEMSN to assess the breast cancer cell targeting and drug release behaviours. In vitro study revealed that PEG chains protect the targeting ligand and shield against normal cells. After reaching the breast cancer cells, MMP-2 overpressed by cells hydrolyses gelatin layer to deshield PEG and switch on the function of HA. As a result, DOX-loaded MHGP was selectively trapped by cancer cells through HA receptor-mediated endocytosis and subsequently release DOX due to Hyal-catalysed degradation of HA. This system presents successful bienzyme-responsive targeting drug delivery in an optimal fashion and provides potential applications for targeted cancer therapy.

CAS / MDL: 25316-40-9 9067-32-7
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2017 · IF 4.233

Tunable adhesion of superoleophilic/superhydrophobic poly (lactic acid) membrane for controlled-release of oil soluble drugs

Ailin Gao,Fu Liu,Zhu Xiong,Qing Yang

Superhydrophobic membranes with tunable adhesion have attracted intense interests for various engineering applications. In this work, superhydrophobic sustainable poly (lactic acid) (PLA) porous membrane with tunable adhesive force from 101   μN to 29   μN was successfully fabricated via one-step phase separation method. The incorporation of Perfluoro-1-decene (PFD) into the PLLA/PDLA membrane via the in situ polymerization can facilely tune the PLLA/PDLA stereocomplex crystallization during phase inversion, which consequently caused the unique morphology blooming evolution from bud to full-blown state. The resulted membrane showed tunable pore size, porosity, surface area, surface roughness and superhydrophobicity, which enabled the membrane with controlled-release of oil soluble drugs.

CAS / MDL: 872-50-4 123-77-3
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JOURNAL OF APPLIED POLYMER SCIENCE · 2016 ·Vol. 133 ·期 18 · IF 1.866

Synthesis, characterization, and cytotoxicity of star-shaped polyester-based elastomers as controlled release systems for proteins

Fangyuan Guo,Wei Zhang,Xiaohong Pei,Xia Shen,Qinying Yan,Weiyong Hong,Gensheng Yang

With the growing number of therapeutic proteins on the market, effective delivery systems are receiving particular attention. In this study, biodegradable elastomers, intended for protein drug delivery and based on methacrylic tripoly(ε-caprolactone- co - d , l -lactide) cyclic ester with different ratios of ɛ-caprolactone to d , l -lactide and methacrylic bipoly[ɛ-caprolactone- b -poly(ethylene glycol)- b -ɛ-caprolactone], were synthesized and characterized. The degradation behavior, bovine serum albumin (BSA)-releasing kinetics, and cytotoxicity of the elastomers in vitro were investigated. The elastomers were degraded by the hydrolysis of the ester bond; this resulted in pH changes, which further affected the degradation rate. The BSA-releasing behavior was strongly dependent on the diffusion mechanism. In the diffusion-controlled period, nearly sustained and stable BSA release was achieved. Furthermore, the elastomers displayed good biocompatibility, as demonstrated by a 3-(4,5-dimethyl thiazol-2-yl)−2,5-diphenyl tetrazolium bromide assay and inflammation–induction experiments, and are considered promising candidates for the controllable delivery of protein drugs. © 2016 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016 , 133 , 43393.

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Polymer Chemistry · 2015 ·Vol. 7 ·期 4 ·899-904 · IF 5.52

Synthesis of photoresponsive polymeric propesticide micelles based on PEG for the controlled release of a herbicide

Kaikai Ding,Liyan Shi,Ling Zhang,Tian Zeng,Yihua Yin,Ying Yi

A novel amphiphilic polymer–pesticide conjugate was synthesized by conjugation of PEG with the photolabile o-nitrobenzyl group followed by grafting dichlorophenoxyacetic acid (2,4-D), which can self-assemble into photoresponsive micelles in aqueous solutions for a controlled release of the herbicide. 1H NMR and FT-IR confirmed the structure of the synthesized conjugate. TEM observations showed that the micelles had a core–shell configuration. DLS and TEM measurements showed that the average diameters of the micelles decreased by about 40 nm after 365 nm UV irradiation. 1H NMR and UV-Vis studies confirmed that the photoresponse may be ascribed to the photolytic cleavage of o-nitrobenzyl as the connecting arm in the polymeric chain. No release of the micelles was detected without light, while the cumulative release rate from the micelles increased gradually upon solar-simulating radiation, reaching 99.6% in 8 h.

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Polymer Chemistry · 2014 ·Vol. 6 ·期 10 ·1817-1829 · IF 5.368

Self-assembly and disassembly of a redox-responsive ferrocene-containing amphiphilic block copolymer for controlled release

Lichao Liu,Leilei Rui,Yun Gao,Weian Zhang

Stimuli-responsive block copolymer micelles have recently emerged as promising drug delivery systems with controllable drug release. Herein, we report well-defined redox-responsive ferrocene-containing amphiphilic block copolymers PEG-b-PMAEFc, which were synthesized by the atom transfer radical polymerization (ATRP) of 2-(methacryloyloxy) ethyl ferrocene-carboxylate (MAEFc) using a PEG-based macro-ATRP agent. These block copolymers can self-assemble into various interesting nanostructures in aqueous solution. The self-assembled morphology of amphiphilic block copolymers is influenced by the nature of the common solvents used, the polymer composition and concentration, and the addition of β-cyclodextrin (β-CD) and redox agents (H2O2 and KMnO4), the effects of which were investigated by transmission electron microscopy (TEM) and dynamic light scattering (DLS). Furthermore, the redox agent H2O2 can be used to trigger the release of encapsulated cargo (Rhodamine B) in the polymeric nanocarriers. This redox behavior of the amphiphiles could open up an approach for redox-controlled drug delivery systems.

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Materials · 2015 ·Vol. 8 ·期 2 ·379-391 · IF 2.651

Preparation of pH Sensitive Pluronic-Docetaxel Conjugate Micelles to Balance the Stability and Controlled Release Issues

Yanchao Liang,Zhihui Su,Yao Yao,Na Zhang

A novel polymer-drug conjugate was prepared by the chemical reaction between the copolymer Pluronic P123 and the docetaxel via a pH sensitive hydrazone bond. These pluronic P123-docetaxel (DTX) conjugates (P123-DTX) could form the stable drug-loaded materials that can self-assemble into the defined nano-micelles in aqueous solution because of their obvious amphiphilic property and low critical micelle concentration. The spherical morphology and particle size of the prepared nano-micelles were characterized by transmission electron microscopy and dynamic light scattering, respectively. Moreover, after the introduction of pH sensitive hydrazone bond, P123-DTX micelle showed a pH dependent drug release behavior. At pH 5.0 (in 48 h), the cumulative release amount of DTX were ~84.9%, which is about six times higher than that at pH 7.4. The prepared novel p123-DTX conjugates may offer a great benefit for drug delivery and controlling the drug release.Keywords:docetaxel;conjugates;nano-micelles;stability;pH controlled release

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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION · 2015 · IF 1.648

Synthesis of poly(glutamic acid)-tyramine hydrogel by enzyme-mediated gelation for controlled release of proteins

Zhiping Peng,Yingqi She,Lei Chen

An in situ-formed hydrogel was synthesized by enzymatic cross-linking of poly(γ-glutamic acid)–tyramine conjugates (PGA–Tyr) using horseradish peroxidase (HRP) and hydrogen peroxide (H2O2). The gelation time ranged from 25 s to 5 min was accomplished by tuning the concentration of HRP, H2O2/Tyr molar ratio and the degree of substitution (DS) of Tyr groups. The storage modulus (G′), cross-link density, and mesh size can be tailored by controlling the H2O2/Tyr ratio and DS. The rheological analysis indicated that the storage modulus (G′) can be tailored from approximately 40 to over 1100 Pa with the increasing H2O2/Tyr ratio and DS. The bovine serum albumin (BSA) was used as model protein and encapsulated into the hydrogel during the enzyme-mediated cross-linking reaction. Controlled release of BSA in vitro from the PGA–Tyr hydrogel was obtained. The release rate and cumulative release amount of encapsulated BSA were manipulated by controlling the H2O2/Tyr ratio and DS. More than 90% of encapsulated BSA was released from the hydrogel with low cross-link density and lager mesh size in 60 h, while only 68% of BSA was released from the hydrogel with high cross-link density and small mesh size. The results indicated that the PGA–Tyr hydrogel is a promising material for the controlled release of therapeutic protein or peptides.

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PLoS One · 2014 ·Vol. 9 ·期 12 ·e113797 · IF 3.534

A Novel Controlled-Release System for Antibacterial Enzyme Lysostaphin Delivery Using Hydroxyapatite/Chitosan Composite Bone Cement

Bai Xue,Cheng Zhang,Yihan Wang,Jincheng Wang,Jien Zhang,Min Lu,Guodong Li,Zhizhong Cao,Qingshan Huang

In this work, a lysostaphin-loaded, control-released, self-setting and injectable porous bone cement with efficient protein delivery was prepared by a novel setting method using hydroxyapatite/chitosan (HA/CS) composite scaffold. The cement samples were made through cementitious reactions by mixing solid powder, a mixture of HA/CS composite particles, lysostaphin, Ca(OH) 2 , CaCO 3 and NaHCO 3 , with setting liquid containing citric acid, acetic acid, NaH 2 PO 4 , CaCl 2 and poloxamer. The setting parameters of the cement samples were determined. The results showed that the final setting time was 96.6±5.2 min and the pH value increased from approximately 6.2 to nearly 10 during the setting process and the porosity was 34% at the end. And the microstructure and composition were detected by scanning electron microscopy (SEM), x-ray diffraction and Fourier transform-infrared spectroscopy. For the release behavior of lysostaphin loaded in the cement sample, the in vitro cement extract experiment indicated that about 94.2±10.9% of the loaded protein was released before day 8 and the in vivo Qdot 625 fluorescence tracking experiment showed that the loaded protein released slower than the free one. Then the biocompatibility of the cement samples was evaluated using the methylthiazol tetrazolium assay, SEM and hematoxylin-eosin staining, which suggested good biocompatibility of cement samples with MC 3T3-E1 cells and subcutaneous tissues of mice. Finally the antibacterial activity assay indicated that the loaded lysostaphin had good release ability and strong antibacterial enzymatic activity against methicillin-resistant Staphylococcus aureus . Collectively, all the results suggested that the lysostaphin-loaded self-setting injectable porous bone cement released the protein in a controlled and effective way and the protein activity was well retained during the setting and releasing process. Thus this bone cement can be potentially applied as a combination of artificial bone substitute and controlled-release system for delivery of lysostaphin to treat bone defects and infections.

CAS / MDL: 25389-94-0 3810-74-0
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FOOD CHEMISTRY · 2024 · IF 8.5

Controlled release characteristics of alkyl gallates and gallic acid from β-cyclodextrin inclusion complexes of alkyl gallates

Dong Cai,Xinmiao Wang,Qian Wang,Peiyong Tong,Weiyuan Niu,Xu Guo,Jinghan Yu,Xuan Chen,Xiaoyang Liu,Dayong Zhou,Fawen Yin

The freeze-drying approach was used to create inclusion complexes utilizing alkyl gallates and β-cyclodextrin, namely dodecyl gallate, octyl gallate, butyl gallate, and ethyl gallate, which are exemplary examples of phenolic esters. The everted-rat-gut-sac model demonstrated that the inclusion complexes released alkyl gallates, which were subsequently hydrolyzed to generate free gallic acid, as evidenced by HPLC-UV analysis. Both gallic acid and short-chain alkyl gallates were capable of permeating the small intestinal membrane. The transport rate of gallic acid (or alkyl gallates) exhibited an initial rise followed by a drop when the carbon-chain lengths varied. The inclusion complex groups exhibited a superior sustained-release effect compared to the comparable alkyl gallates groups, thus possibly leading to higher bioavailability and stronger bioactivity. Moreover, altering the length of the carbon chain will allow for the effortless achievement of regulated release of phenolic compounds and short-chain phenolic esters from such β-cyclodextrin inclusion complexes.

研究领域: 药剂学 · 生物化学
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FOOD RESEARCH INTERNATIONAL · 2025 · IF 8

Colonic delivery and controlled release of curcumin encapsulated within plant-based extracellular vesicles loaded into hydrogel beads

Hang Liu,Yikun Liu,Shengfeng Peng,Lei Zhou,David Julian McClements,Suqiong Fang,Wei Liu

In this study, the application of banana-derived extracellular vesicles (EVs) as natural carriers for hydrophobic nutraceuticals was investigated for the first time. Curcumin was solubilized in an amorphous state within the hydrophobic domains of the EVs in banana juice. The bioaccessibility of the curcumin was considerably higher in the curcumin-loaded EVs (CEVs) than for pure curcumin crystals. The retention/release behavior of the curcumin in the CEVs was regulated by incorporating the curcumin-loaded banana juice into hydrogel beads, which were assembled from sodium alginate and banana pectin. The pectin and D-galacturonic acid contents of the banana juice were 0.87 % ± 0.11 % and 0.58 % ± 0.08 %, respectively. With the introduction of sodium alginate, the sphericity, hardness, chewiness, water holding capacity, surface smoothness and other physiochemical properties of the hydrogel beads were improved. Fourier Transform infrared analysis showed that hydrogen bonding played an important role in the formation of the hydrogel beads. The hydrogel beads had a higher swelling ratio under neutral conditions than under acidic conditions. Encapsulation of the curcumin-loaded banana juice within the hydrogel beads retarded curcumin release and enhanced the therapy potential of ulcerative colitis, which indicated that these delivery systems could be designed to regulate the release profile of the CEVs. Encapsulation of the curcumin also improved its resistance to heating, exposure and storage. In summary, we have shown that encapsulation of curcumin within plant-based EVs loaded into hydrogel beads can improve its functional performance.

CAS / MDL: 9005-38-3
研究领域: 食品科学 · 药理学 · 生物技术
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Biomimetic design of platelet-rich plasma controlled release bacterial cellulose/hydroxyapatite composite hydrogel for bone tissue engineering

Xiangmei Wang,Xiaoli Yang,Xin Xiao,Xueqian Li,Chuntao Chen,Dongping Sun

Bacterial cellulose (BC) hydrogel is renowned in the field of tissue engineering for its high biocompatibility, excellent mechanical strength, and eco-friendliness. Herein, we present a biomimetic mineralization method for preparing BC/hydroxyapatite (HAP) composite hydrogel scaffolds with different mineralization time and ion concentration of the mineralized solution. Spherical HAP reinforcement enhanced bone mineralization, thereby imparting increased bioactivity to BC matrix materials. Subsequently, platelet-rich plasma (PRP) was introduced into the scaffold. The PRP-loaded hydrogel enhanced the release of growth factors, which promoted cell adhesion, growth, and bone healing. After 3 weeks of MC3T3-E1 cell-induced osteogenesis, PRP positively affected cell differentiation in BC/HAP@PRP scaffolds. Overall, these scaffolds exhibited excellent biocompatibility, mineralized nodule formation, and controlled release in vitro , demonstrating great potential for application in bone tissue repair.

研究领域: 组织工程 · 生物材料 · 生物医学工程 · 材料科学
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