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FIBERS AND POLYMERS · 2022 ·Vol. 23 ·期 5 ·1225-1234 · IF 2.347

Batch Fabrication and Characterization of ZnO/PLGA/PCL Nanofiber Membranes for Antibacterial Materials

Li Siqi,Yin Jing,Xu Lan

As biomaterials with excellent biocompatibility, biodegradation and low toxicity, poly(ε-caprolactone) (PCL) and poly(lactic-co-glycolic acid) (PLGA) are extensively applied as wound dressing and surgical suture in biomedical field. In this paper, an oblique section free surface electrospinning (OSFSE) apparatus was utilized to prepare high-quality and high-output ZnO/PLGA/PCL nanofiber membranes (NFMs) for antibacterial materials, which could significantly increase the production of ZnO/PLGA/PCL NFMs from 0.01–0.1 g/h of traditional electrospinning to 30.84 g/h of OSFSE. The influences of the weight proportion of PLGA and PCL on the viscosity and conductivity of electrospinning solutions along with the yield, morphology and wettability of PLGA/PCL NFMs were researched, and the optimum weight ratio of 6:4 was determined. Then the effects of ZnO contents on the electrospinning solution properties as well as the yield, morphology, structure, wettability, mechanical property and antibacterial performance of ZnO/PLGA/PCL NFMs with the optimal ratio of PLGA and PCL were studied. The results illustrated that additive nano-ZnO could improve markedly the antibacterial effect of NFMs, and the NFMs with 3 wt% nano-ZnO had excellent antibacterial effect on Escherichia coli (95.3 %) and Staphylococcus aureus (95.7 %).

CAS / MDL: 920-66-1
研究领域: 生物医学工程 · 材料科学 · 微生物学
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Journal of Anesthesia · 2024 ·Vol. 38 ·期 2 ·232-243 · IF 2.8

Targeted local anesthesia: a novel slow-release Fe3O4–lidocaine–PLGA microsphere endowed with a magnetic targeting function

Zheng Ling-xi,Yu Qian,Li Qiang,Zheng Chuan-dong

Purpose Lidocaine microspheres can prolong the analgesic time to 24–48 h, which still cannot meet the need of postoperative analgesia lasting more than 3 days. Therefore, we added Fe 3 O 4 to the lidocaine microspheres and used an applied magnetic field to attract Fe 3 O 4 to fix the microspheres around the target nerves, reducing the diffusion of magnetic lidocaine microspheres to the surrounding tissues and prolonging the analgesic time. Methods Fe 3 O 4 –lidocaine–PLGA microspheres were prepared by the complex-emulsion volatilization method to characterize and study the release properties in vitro. The neural anchoring properties and in vivo morphology of the drug were obtained by magnetic resonance imaging. The nerve blocking effect and analgesic effect of magnetic lidocaine microspheres were evaluated by animal experiments. Results The mean diameter of magnetically responsive lidocaine microspheres: 9.04 ± 3.23 μm. The encapsulation and drug loading of the microspheres were 46.18 ± 3.26% and 6.02 ± 1.87%, respectively. Magnetic resonance imaging showed good imaging of Fe 3 O 4 –Lidocain–PLGA microspheres, a drug-carrying model that slowed down the diffusion of the microspheres in the presence of an applied magnetic field. Animal experiments demonstrated that this preparation had a significantly prolonged nerve block, analgesic effect, and a nerve anchoring function. Conclusion Magnetically responsive lidocaine microspheres can prolong analgesia by slowly releasing lidocaine, which can be immobilized around the nerve by a magnetic field on the body surface, avoiding premature diffusion of the microspheres to surrounding tissues and improving drug targeting.

研究领域: 药剂学 · 神经科学 · 医学影像学
✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2015 · IF 3.65

Comparative studies on the properties of glycyrrhetinic acid-loaded PLGA microparticles prepared by emulsion and template methods

Hong Wang,Guangxing Zhang,Hong Sui,Yanhua Liu,Kinam Park,Wenping Wang

The O/W emulsion method has been widely used for the production of poly (lactide- co -glycolide) (PLGA) microparticles . Recently, a template method has been used to make homogeneous microparticles with predefined size and shape, and shown to be useful in encapsulating different types of active compounds. However, differences between the template method and emulsion method have not been examined. In the current study, PLGA microparticles were prepared by the two methods using glycyrrhetinic acid (GA) as a model drug. The properties of obtained microparticles were characterized and compared on drug distribution, in vitro release, and degradation. An encapsulation efficiency of over 70% and a mean particle size of about 40   μm were found for both methods. DSC thermograms and XRPD diffractograms indicated that GA was highly dispersed or in the amorphous state in the matrix of microparticles. The emulsion method produced microparticles of a broad size distribution with a core–shell type structure and many drug-rich domains inside each microparticle. Its drug release and matrix degradation was slow before Day 50 and then accelerated. In contrast, the template method formed microparticles with narrow size distribution and drug distribution without apparent drug-rich domains. The template microparticles with a loading efficiency of 85% exhibited a zero-order release profile for 3 months after the initial burst release of 26.7%, and a steady surface erosion process as well. The same microparticles made by two different methods showed two distinguished drug release profiles. The two different methods can be supplementary with each other in optimization of drug formulation for achieving predetermined drug release patterns.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 生物材料学
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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2017 · IF 4.159

Enhanced encapsulation and bioavailability of breviscapine in PLGA microparticles by nanocrystal and water-soluble polymer template techniques

Hong Wang,Guangxing Zhang,Xueqin Ma,Yanhua Liu,Jun Feng,Kinam Park,Wenping Wang

Poly (lactide-co-glycolide) (PLGA) microparticles are widely used for controlled drug delivery. Emulsion methods have been commonly used for preparation of PLGA microparticles, but they usually result in low loading capacity, especially for drugs with poor solubility in organic solvents . In the present study, the nanocrystal technology and a water-soluble polymer template method were used to fabricate nanocrystal-loaded microparticles with improved drug loading and encapsulation efficiency for prolonged delivery of breviscapine . Breviscapine nanocrystals were prepared using a precipitation-ultrasonication method and further loaded into PLGA microparticles by casting in a mold from a water-soluble polymer. The obtained disc-like particles were then characterized and compared with the spherical particles prepared by an emulsion-solvent evaporation method. X-ray powder diffraction (XRPD) and confocal laser scanning microscopy (CLSM) analysis confirmed a highly-dispersed state of breviscapine inside the microparticles. The drug form, loading percentage and fabrication techniques significantly affected the loading capacity and efficiency of breviscapine in PLGA microparticles, and their release performance as well. Drug loading was increased from 2.4% up to 15.3% when both nanocrystal and template methods were applied, and encapsulation efficiency increased from 48.5% to 91.9%. But loading efficiency was reduced as the drug loading was increased. All microparticles showed an initial burst release, and then a slow release period of 28   days followed by an erosion-accelerated release phase, which provides a sustained delivery of breviscapine over a month. A relatively stable serum drug level for more than 30   days was observed after intramuscular injection of microparticles in rats. Therefore, PLGA microparticles loaded with nanocrystals of poorly soluble drugs provided a promising approach for long-term therapeutic products characterized with preferable in vitro and in vivo performance.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 生物医学工程
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Frontiers in Bioengineering and Biotechnology · 2022 · IF 6.064

Synthesis of Ce/Gd@HA/PLGA Scaffolds Contributing to Bone Repair and MRI Enhancement

Song Xianji,Liu Xilin,Ma Yihang,Zhu Qingsan,Bi Mingchao

It is important for future clinical applications to design and synthesize multipurpose scaffolding materials for bone tissue engineering with high osteogenic induction and MRI capability. In the present study, we synthesized Ce/Gd@HA by co-doping Ce3+ and Gd3+ into hydroxyapatite (HA) using a hydrothermal synthesis method, and then Ce/Gd@HA composites were synthesized by combining Ce/Gd@HA nanoparticles with polylactic-co-glycolic acid (PLGA) to investigate whether implanted Ce/Gd@HA/PLGA composites could promote osteoblast viability, leading to tibia repair of the rats and enhance MRI. The measurement results contain X-ray diffraction (XRD), Fourier-transform infrared (FTIR) spectroscopy, and environmental scanning electron microscopy (ESEM) showing that HA doped with Ce3+ and Gd3+ was still a hexagonal crystal with high crystallinity. The synthesized Ce/Gd@HA/PLGA composites have a structure and obvious magnetic resonance imaging (MRI) capability. The in vitro experimental results indicated that Ce/Gd@HA/PLGA composites significantly promoted the performance of MC3T3-E1 cells, containing proliferation, adhesion, and osteogenic differentiation capacities. These include the improvement of alkaline phosphatase activity, enhancement of mineral deposition, and upregulation of OCN and COL-1 gene expression. The in vivo experimental results demonstrated that the Ce/Gd@HA/PLGA composites significantly improved the healing rate of rat bone defects. The MRI images indicated that the Ga-doped composites were observed in the MRI T1 sequence in rats. The aforementioned results suggested that Ce/Gd@HA/PLGA composites not only effectively promoted bone formation but also enhanced MRI capability. The composites synthesized in this study have great potential in bone regeneration with an extensive application in bone tissue engineering.

研究领域: 生物材料学 · 组织工程学 · 医学影像学
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CHEMICAL & PHARMACEUTICAL BULLETIN · 2015 ·Vol. 63 ·期 2 ·68-74 · IF 1.164

Development and Evaluation of a Novel TPGS-Mediated Paclitaxel-Loaded PLGA-mPEG Nanoparticle for the Treatment of Ovarian Cancer

Wen Lv,Lihua Cheng,Baohua Li

One of the major obstacles to successful paclitaxel (PTX) chemotherapy is toxic side effects, which are often due to the conventional surfactants used, such as Cremophor EL. PTX is characterized by its hydrophobicity and insolubility, which limit its application in ovarian cancer therapy. The aim of this study was to develop Cremophor EL-free PTX-loaded methoxy poly(ethylene glycol)-block-(lactic-co-glycolic acid) copolymers (PLGA-mPEG) nanoparticles (NPs) using d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) as a novel emulsifier. The ability of nanoparticles loaded with paclitaxel (NP-PTX) to inhibit tumor growth was assessed in vitro and in vivo. The acute toxicity of NP-PTX was also evaluated in vivo. We found that paclitaxel was efficiently encapsulated into PLGA-mPEG NPs with a low concentration of TPGS as the emulsifier. The synthesized NP-PTX demonstrated the desired diameter of 80 nm as characterized by transmission electron microscopy. The NP-PTX also exhibited a sustained release of loaded PTX over 4 d with the same chemotherapeutic efficiency and reduced side effects. NP-PTX-treated cells showed slightly lower cytotoxic responses compared with those treated with free PTX at the same concentration. In vivo studies confirmed that NP-PTX significantly enhanced the median lethal dose of paclitaxel by 10-fold, and a similar effect on the inhibition of tumor growth was achieved in nude mice.

研究领域: 药剂学 · 肿瘤学
✓ 已验证 DOI PubMed 高影响因子
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RSC Advances · 2018 ·Vol. 8 ·期 32 ·17958-17966 · IF 2.936

Selective ultrasound contrast enhancement in the tumor by nanocapsules with perfluorooctylbromide: effect of PLGA–PEG proportion

Zheng Wang,Jinsong Ding,Xiaoqian Ma,Shengjuan Luo

We used PLGA–COOH and PLGA–PEG–COOH blended polymer material to encapsulate perfluorooctyl bromide to prepare nanocapsules (NCs) as nano-ultrasound contrast agents. The aim of this study was to assess the effect of PLGA–PEG proportion on the physical, biological and acoustic characteristics of the nanocapsules, and to develop optimal nanocapsules for selective ultrasound contrast enhancement in tumors. The weight ratio of PLGA–PEG in the formulation was 0, 25%, 50%, 75%, and 100%, and the corresponding nanocapsules were designated NCsPLGA, NCs25% PLGA–PEG, NCs50% PLGA–PEG, NCs75% PLGA–PEG and NCs100% PLGA–PEG. As the PLGA–PEG proportion increased, the diameter and bulk modulus of the NCs gradually decreased, and the originally smooth surface of NCs was roughened. NCsPLGA, NCs25% PLGA–PEG and NCs50% PLGA–PEG had regular spherical shape and relatively distinct boundaries compared with NCs75% PLGA–PEG and NCs100% PLGA–PEG, which showed heavy agglomeration. The proportion of PLGA–PEG in the formula could also change the uptake rate of NCs by RAW 264.7 cells. NCs50% PLGA–PEG and NCs75% PLGA–PEG had the lowest uptake by RAW 264.7 cells. In vitro, the ultrasonic gray values of NCs50% PLGA–PEG, NCs75% PLGA–PEG and NCs100% PLGA–PEG were obviously higher than those of NCsPLGA and NCs100% PLGA–PEG. NCsPLGA, NCs50% PLGA–PEG and NCs100% PLGA–PEG were injected into mice via the tail vein, but only NCs50% PLGA–PEG could produce persistent gray contrast enhancement in tumors after 24 h. Histological fluorescence of the tumor tissue confirmed that NCs50% PLGA–PEG and NCs100% PLGA–PEG gathered in tumor tissues. Our results indicate that the PLGA–PEG proportion in the formula is an important factor in constructing optimal nano-ultrasound contrast agents with a liquid core, and could change the nanocapsule size, surface morphology, elastic modulus, macrophage cellular uptake, and ultrasonic reflection. An appropriate PLGA–PEG proportion could help nanoparticles to achieve selective gray contrast enhancement in tumors.

CAS / MDL: 423-55-2
研究领域: 医学影像学 · 生物材料学 · 肿瘤学
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Soft Matter · 2020 ·Vol. 16 ·期 46 ·10528-10536 · IF 3.14

PLGA nanoparticle-reinforced supramolecular peptide hydrogels for local delivery of multiple drugs with enhanced synergism

Can Wu,Chunlu Wang,Lu Sun,Keming Xu,Wenying Zhong

Localized drug delivery offers great therapeutic efficacy at local tissues while avoiding the systemic toxicity of drugs. Yet it demands the development of structurally-stable drug carrier systems with excellent injectability, as well as the capability to facilitate controlled release of multiple drugs. Herein, we describe the design and synthesis of a supramolecular hydrogel (Cis/Peptide@NP/Irino) for the combined delivery of cisplatin (Cis) and irinotecan (Irino). The self-assembled hydrogel consisted of an inner phase of irinotecan-loaded PLGA nanoparticles (NP/Irino) and an outer phase of cisplatin-loaded peptide nanofibers (Cis/Peptide). Through the structural reinforcement of PLGA nanoparticles, the Cis/Peptide@NP/Irino hydrogel exhibited better mechanical properties than Cis/Peptide or Peptide hydrogels. With excellent shear-thinning properties, it facilitated the development of a localized drug delivery system with an improved retention time in vivo. The hydrogel incorporated two anticancer drugs, Cis and Irino, at the Peptide and PLGA domains, respectively, and exhibited a faster release of Cis prior to the continuous release of Irino in vitro. Furthermore, the Cis/Peptide@NP/Irino formulation showed a better inhibition efficacy against the proliferation of cancerous A549 cells, with the synergism of Cis and Irino exceeding that of the simple solution mixtures, which was plausibly due to the enhanced cellular uptake of drugs through endocytosis. We believe that structurally-stable supramolecular hydrogels show great promise in the local delivery of various drug combinations for cancer therapy.

研究领域: 药剂学 · 肿瘤学 · 生物材料科学
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JOURNAL OF THE ELECTROCHEMICAL SOCIETY · 2025 ·Vol. 172 ·期 4 ·047501 · IF 3.3

Sensitive Electrochemical Detection of DR1 Based on Electrodeposit AuNPs-Poly(thiophene-3-acetic acid) and Copolymer PLGA

Yaping Zhang,Gao Si,Yilong Wang,Zhendong Wang,Zutian Li,Haiyan Wei,Huaixia Yang,Fuchun Si,Xiaofei Li

The sensitive detection of down-regulator of transcription 1 (DR1) provides important information for early noninvasive diagnosis and treatment of Hashimoto thyroiditis (HT). In this study, a label-free electrochemical biosensor for DR1 detection was constructed based on electrodeposited gold nanoparticles (AuNPs) and poly(lactic-co-glycolic acid) (PLGA). The AuNPs were first modified to the electrode surface by electrodeposition to increase the specific surface area of the electrode, thus loading more target molecules to increase the sensitivity of the sensor. Then, a sandwich structure was formed on the electrode surface based on the specific recognition of antigen and antibody. PLGA was fixed on the electrode surface by binding with antibody 2 (Ab2) through amide bond to further improve the sensitivity of the sensor. Induced by the dual signal amplification, the sensor has a linear detection range of 50 fg·ml−1 to 50 ng·ml−1, with a detection limit as low as 19.4 fg·ml−1. Moreover, the sensor has good selectivity, specificity, and anti-interference capability, which holds great potential for the early diagnosis of HT and analysis of other disease markers.

CAS / MDL: 6964-21-2 9048-46-8
研究领域: 生物医学工程 · 分析化学 · 免疫学
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Polymers · 2025 ·Vol. 17 ·期 5 ·574 · IF 4.9

Formation of PEG-PLGA Microspheres for Controlled Release of Simvastatin and Carvacrol: Enhanced Lipid-Lowering Efficacy and Improved Patient Compliance in Hyperlipidemia Therapy

Lin Fu,Hengxin Ren,Chaoxing Wang,Yaxin Zhao,Bohang Zou,Xiangyu Zhang

Polymer-based drug-controlled release systems offer greater efficacy and potency than conventional therapies. However, prominent drug side effects, lower circulation, and low drug loading capabilities limit their application range. In this work, the combination of Simvastatin (SIV) and Carvacrol (CAV) into PEG-PLGA microspheres (SIV-CAV-PP-MS) was achieved via an emulsification-solvent evaporation technique, resulting in microspheres characterized by high encapsulation efficiency and reduced particle size. In vitro studies demonstrated that the cumulative drug release increased with higher SIV and CAV levels in the release medium, reaching 88.91% and 89.35% at 25 days. Pharmacokinetic analysis revealed that the concentrations of SIV and CAV reached their maximum levels at approximately seven days in the SIV-CAV-PP-MS group, which indicates that using PEG-PLGA as a carrier significantly delays drug release. In vivo, evaluation demonstrated that the SIV-CAV-PP-MS high-dose group and positive drug control group showed reductions in low-density lipoprotein cholesterol levels by 0.39-fold and 0.36-fold compared to the Hyperlipidemia model group, and the addition of CAV significantly enhanced the lipid-lowering effects of SIV. Histological examinations indicated that the SIV-CAV-PP-MS medium-dose group displayed histological features more closely resembling those of normal mice compared to the Simvastatin control group, with a well-organized hepatocyte structure, a significant reduction in lipids, and improved liver health. The prepared polymeric microsphere utilizing SIV and SAV will be a promising dosage form for hyperlipidemia disease patients, with superior lipid-lowering efficacy and improved patient compliance.

研究领域: 药学 · 生物医学工程
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2023 · IF 5.2

Insight into the behavior regulation of drug transfer of nimodipine loaded PLGA microspheres by emulsion evaporation method

Qingqing Yang,Yizhen Bian,Guobin Ren,Minghuang Hong

In the process of preparing microspheres by evaporation of emulsion, drug transfer in the system makes it difficult to control the drug loading and encapsulation efficiency of the product. In this study, Nimodipine loaded microspheres were prepared using poly(lactic-co-glycolic acid) (PLGA) as the matrix materials . The transfer process of drug molecules and solvent molecules in the preparation process were observed by online imaging. Combined with weighing experiments and molecular simulation , three stages of dichloromethane (DCM) diffusion in oil phase were proposed. At 20 °C,15 % and 46 % of DCM content were taken as the critical point, and between the content was slow volatilization stage, which dominated the occurrence of drug reflux and crystallization. The oil phase diffusion and emulsion mass transfer equations of DCM were proposed to judge the influence of each single factor on drug molecular transfer. Low temperature, oil-water ratio and stirring speed could slow down the volatilization of DCM and increase the drug loading and encapsulation efficiency. Low stirring speed could increase the drug loading while avoiding crystallization and reflux, which was the best control factor.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 生物医学工程
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Applied Materials Today · 2022 · IF 8.663

Microfluidic PLGA microcapsules with PD-L1 aptamers and docetaxel encapsulation for enhancing tumor immunity

Ruirui Zhang,Liping Zhong,Xiuli Liu,Xiyu Liu,Qiaoying Chen,Pan Wu,Jian He,Yongmei Li,Yongxiang Zhao,Ziqun Liu,Yan Zu,Yong Huang,Bing Wang

Immunotherapy has made encouraging progress in the field of cancer treatment. Among them, the programmed cell death-ligand 1 (PD-L1) antibody-mediated immunotherapy has stimulated the development of various carrier delivery systems. Inspired by related researchs, in this study, we prepare core-shell structured poly(lactide-co-glycolide) (PLGA) microcapsules as a drug delivery system through microfluidics technology, loaded with PD-L1 aptamers and chemotherapy drug docetaxel. The PD-L1 aptamer loaded in the nuclear layer binds to the PD-L1 molecule produced by tumor cells, blocking the immune checkpoint protein-1/programmed cell death-ligand 1 (PD-1/PD-L1) pathway. As a result, phagocytosis of tumor cells is promoted by using lipopolysaccharide (LPS) induced tumor associated macrophages. Furthermore, docetaxel in the shell is further released, inhibiting tumor cell growth as the PLGA microcapsules degrade. More importantly, the combination of PD-L1 aptamers and the chemotherapy drug docetaxel improved the immune response of the tumor. It showed significant anti-tumor activity and reduced systemic side effects in the melanoma model. At present, more and more nucleic acid aptamers as affinity reagents that can replace antibodies have been used to improve tumor treatment. Therefore, this therapeutic strategy provides more possibilities for tumor treatment by combining aptamer molecules with chemotherapy drugs when exploring more effective combination drugs.

CAS / MDL: 75-09-2
研究领域: 癌症治疗 · 药物递送系统 · 免疫学 · 制药学
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