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Journal of Materials Chemistry B · 2021 ·Vol. 9 ·期 29 ·5861-5868 · IF 6.331

The shrinking behavior, mechanism and anti-shrinkage resolution of an electrospun PLGA membrane

Chen Yuan,Shue Jin,Jiawei Wei,Jinhui Huang,Chang Liu,Xiaoyu Lei,Yi Zuo,Jidong Li,Yubao Li

The deformation shrinkage of a poly(lactide-co-glycolide) (PLGA) fibrous material seriously affects its biomedical application. To demonstrate the underlying shrinking mechanism and to find a method to prevent the shrinkage of an electrospun PLGA membrane, we investigated the shrinking behavior of PLGA electrospun membranes under various test conditions and discussed the underlying shrinking mechanism. The results indicated that the shrinkage of the electrospun PLGA membrane was mainly regulated by the glass transition of its polymer fiber; the temperature and liquid environment were found to be the two main factors leading to the shrinkage of the electrospun PLGA membrane through affecting its glass transition. Then a heat stretching (HS) technique was proposed by us to stabilize the electrospun PLGA membrane. After HS treatment, the glass transition temperature (Tg) of the electrospun PLGA membrane could increase from 48.38 °C to 54.55 °C. Our results indicated that the HS-treated membranes could maintain a high area percentage of 90.89 ± 2.27% and 84.78 ± 3.36% after immersion respectively in PBS and blood at 37 °C for 2 hours. Further experiments confirmed that the HS technique could also stabilize the dimensional structure of the electrospun PDLLA membrane in PBS and blood at 37 °C. This study provides an effective strategy for preventing the shrinkage of electrospun polyester biomaterials in a physiological environment that may benefit both the material structural stability and the in vivo biological performance.

CAS / MDL: 920-66-1
研究领域: 材料科学 · 生物医学工程
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Drug Design Development and Therapy · 2017 · IF 2.822

Rifapentine-linezolid-loaded PLGA microspheres for interventional therapy of cavitary pulmonary tuberculosis: preparation and in vitro characterization

Jieyun Huang,Zhi Chen,Ying Li,Li Li,Guangyu Zhang

In this study, we aimed to design controlled-release microspheres for the treatment of cavitary pulmonary tuberculosis (TB) for solving the issues of poor drug delivery and short duration maintained at effective drug concentration during bronchoscopic interventional therapy. We fabricated rifapentine-linezolid-loaded poly(lactic acid-co-glycolic acid) microspheres (RLPMs) using the oil-in-water emulsion solvent evaporation method and assessed their in vitro release as well as the bronchial mucosal retention characteristics. The microspheres are spherical in shape with a circular concave on the surface. The particle size of RLPMs was 27.38±1.28 μm. The drug loading of rifapentine and linezolid was 18.51±0.26 and 8.42%±0.24%, respectively, while the encapsulation efficiencies were 55.53±0.78 and 16.87%±0.47%, respectively (n=3). During the burst release phase of the in vitro release test, 21.37%±0.68% rifapentine was released in 3 days and 43.56%±2.54% linezolid was released in 1 day. Then, both the drugs entered the sustained release phase. Finally, the cumulative percentage release of rifapentine and linezolid in 14 days was 27.61±1.52 and 51.01%±3.31%, respectively (n=3). Bronchoscopic observation revealed that the controlled-release microspheres could slowly release the drugs and retain them on the surface of bronchial mucosa of canines for 20 days. These results indicated that the fabricated microspheres exhibited a significant sustained release effect and could effectively retain the drugs on the surface of bronchial mucosa. Therefore, this study provides a theoretical and practical foundation for the development of fabricated microspheres loaded with multiple anti-TB drugs in the bronchoscopic interventional therapy of cavity pulmonary TB.

CAS / MDL: 9002-89-5
研究领域: 药剂学 · 呼吸病学 · 感染病学
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PARASITOLOGY RESEARCH · 2022 ·Vol. 121 ·期 2 ·675-689 · IF 2.383

Em14-3-3 delivered by PLGA and chitosan nanoparticles conferred improved protection in chicken against Eimeria maxima

Haseeb Muhammad,Huang Jianmei,Lakho Shakeel Ahmed,Yang Zhang,Hasan Muhammad Waqqas,Ehsan Muhammad,Aleem Muhammad Tahir,Memon Muhammad Ali,Ali Haider,Song Xiaokai,Yan Ruofeng,Xu Lixin,Li Xiangrui

Eimeria maxima (E. maxima) are an intracellular apicomplexan protozoan that causes intestinal coccidiosis in chickens. The purpose of this research was to develop a novel delivery approach for recombinant E. maxima (rEm) 14-3-3 antigen to elicit enhanced immunogenic protection using poly (D, L-lactide-co-glycolide) (PLGA) and chitosan (CS) nanoparticles (NPs) against E. maxima challenge. The morphologies of prepared antigen-loaded NPs (PLGA/CS-rEm14-3-3 NPs) were visualized by a scanning electron microscope. The rEm14-3-3 and PLGA/CS-rEm14-3-3 NPs–immunized chicken-induced changes of serum cytokines, IgY-antibody level, and T-lymphocyte subsets and protective efficacies against E. maxima challenge were evaluated. The results revealed that encapsulated rEm14-3-3 in PLGA and CS NPs presented spherical morphology with a smooth surface. The chickens immunized with only rEm14-3-3 and PLGA/CS-rEm14-3-3 NPs elicited a significant ( p <0.05) higher level of IFN-γ cytokine, stimulated the proportions of CD4 + /CD3 + , CD8 + /CD3 + T-cells, and provoked sera IgY-antibody immune response compared to control groups (PBS, pET-32a, PLGA, and CS). Whereas, PLGA-rEm14-3-3 NP–immunized chicken provoked a higher level of IFN- γ production and IgY-antibody response rather than CS-rEm14-3-3 and bare antigen, relatively. The animal experiment results ratified that PLGA-rEm14-3-3 NP–immunized chicken significantly alleviated the relative body weight gain (%), decreased lesion score, and enhanced oocyst decrease ratio compared to CS-rEm14-3-3 NPs and only rEm14-3-3. The anti-coccidial index of the chicken vaccinated with the PLGA-rEm14-3-3 NPs was (180.1) higher than that of the Cs-rEm14-3-3 NPs (167.4) and bare antigen (165.9). Collectively, our statistics approved that PLGA NPs might be an efficient antigen carrier system (Em14-3-3) to act as a nanosubunit vaccine that can improve protective efficacies in chicken against E. maxima challenge.

CAS / MDL: 7758-29-4
研究领域: 兽医学 · 免疫学 · 纳米技术
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JOURNAL OF APPLIED POLYMER SCIENCE · 2022 ·Vol. 139 ·期 23 ·52287 · IF 3.057

Controllable fabrication of multi-modal porous PLGA scaffolds with different sizes of SPIONs using supercritical CO2 foaming

Jinjing Wang,Yi Zhang,Jianfei Sun,Zhen Jiao

Multi-modal porous scaffolds can promote bone regeneration. In the present study, they were successfully fabricated from poly (lactic-co-glycolic acid) (PLGA)/superparamagnetic iron oxide nanoparticles (SPIONs) by supercritical CO 2 foaming, where SPIONs was employed as heterogeneous nucleation agent. The effects of SPION size on pore nucleation in PLGA/SPIONs nanocomposites were investigated. It was found that the addition of smaller SPIONs size caused the reduction of pore size. Multi-modal porous scaffolds could be available by controlling the SPIONs content, soaking temperature, pressure, and depressurization rate. The porosity of the PLGA/SPIONs scaffolds ranged from (58.68 ± 0.62)% to (94.97 ± 0.14)% could be obtained via adjusting the supercritical CO 2 foaming conditions. Moreover, it was found that the compressive modulus and porosity of the scaffolds were strongly associated with the porous structure. This study provided a new green preparation method for magnetic scaffolds to realize the controllable adjustment of the multi-mode porous scaffolds.

CAS / MDL: 75-09-2
研究领域: 生物材料学 · 组织工程学
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INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH · 2021 · IF 3.764

Toward Understanding the Effect of Solvent Evaporation on the Morphology of PLGA Microspheres by Double Emulsion Method

Wei Si,Qingqing Yang,Yuan Zong,Guobin Ren,Ling Zhao,Minghuang Hong,Zhong Xin

During the fabrication of poly(lactide-co-glycolic acid) (PLGA) microspheres by the water/oil/water (W1/O/W2) emulsion solvent evaporation method, water permeation coupled with dichloromethane (DCM) volatilization represents a critical process affecting the microsphere morphology. In this work, the mechanism of pore formation in PLGA through water permeation has been verified. By molecular simulations, the diffusion coefficients of water with different DCM contents were determined. The results showed that the diffusion coefficient decreased rapidly from 53.33 × 10–6 to 6.73 × 10–6 cm2/s after decreasing the DCM mass fraction from 94 to 63%. Furthermore, the higher stirring speed and lower volume of the external aqueous phase promoted the DCM volatilization. Two different mass transfer stages were identified for water permeation, and the first stage could be considered the main mass transfer window because of its high diffusion coefficient. The morphology of PLGA microspheres confirmed the existence of a relationship between water permeation and DCM volatilization.

CAS / MDL: 9002-89-5
研究领域: 材料科学 · 制药工程
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BIOMEDICINE & PHARMACOTHERAPY · 2024 · IF 6.9

Preparation and evaluation of Puerarin-loaded PLGA nanoparticles for improving oral bioavailability in SD rats

Lili Zhang,Chengcheng Duan,Shiquan Feng,Beicheng Zhao,Hailong Li,Xi Zhang,Yan Zhou,Zhenmiao Qin

Background Puerarin (Pue) is an isoflavone compound with significant therapeutic effect on cardiovascular diseases, but its poor water solubility and low oral bioavailability limit clinical application. Methods In this study, Pue was prepared into PLGA nanoparticles (Pue-PLGA NPs) by emulsion solvent volatilization method. The morphology, particle size, Zeta potential, X-ray diffraction (XRD), and fourier transform infrared (FTIR) of the NPs were characterized. Additionally, their stability and in vitro release were evaluated. SD rats were orally administered wtih Pue and Pue-PLGA NPs, and a high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was established to determine the concentration of blood samples and to investigate the pharmacokinetic behaviour of Pue and Pue-PLGA NPs in rats. Results The NPs were observed by transmission electron microscopy (TEM) as regular spheroids and uniformly dispersed. The average particle size of the NPs was (167.1±5.26)nm, the Zeta potential was (-29.88±2.46)mV, the encapsulation rate was (83.12 %±4.73 %) and the drug loading capacity was (7.75 %±1.81 %). The results of in vitro release showed that the drug was released slowly and continuously from the NPs, reaching the release platform in 24 h, and the cumulative release amount was (88.55±2.86) %. The pharmacokinetic results showed that the AUC 0–24 , AUC 0-∞ , C max , T max , t 1/2 , MRT 0–24 and MRT 0-∞ of Pue-PLGA NPs were 2.196, 1.978, 1.327, 1.5, 1.385, 3.915 and 3.140 times of Pue, respectively. The relative bioavailability was (197.82±25.28) %. Conclusion These results indicated that the prepared nanoparticles had small particle size, high encapsulation rate, drug loading capacity and good slow-release effect, and could significantly improve the oral bioavailability of Pue in rats.

CAS / MDL: 128446-35-5 9002-89-5
研究领域: 药剂学 · 药物递送系统 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF MICROENCAPSULATION · 2019 · IF 2.04

Influence of drying processes on the structures, morphology and in vitro release profiles of risperidone-loaded PLGA microspheres

Zhaoying Wu,Mengqing Zhao,Wei Zhang,Zhao Yang,Shuxin Xu,Qing Shang

The purpose of this study was to investigate the influences of drying methods on the risperidone (RIS) release profiles of RIS-loaded PLGA microspheres. These microspheres were fabricated with an O/W emulsion solvent evaporation method. The wet microspheres were dried with freeze drying and vacuum drying methods. The microspheres were mono-dispersed spheres with an average diameter of 100 μm. Studies found that drying methods had great influence on the porosity, morphology, and release profiles of RIS-loaded PLGA microspheres. Specifically, the freeze-dried microspheres had higher porosity (78.46 ± 1.64%) than those vacuum-dried ones (52.45 ± 2.68%), and they showed higher RIS release rates (p < 0.05). In the accelerated release tests (45 °C), these microspheres dried under the pressures of 700 mmHg and 200 mmHg gave faster release rates than those ones dried under the pressure of 450 mmHg. Importantly, the accelerated release test (45 °C) had a high correlation with the real-time test (37 °C) (R2 > 0.99). These studies exhibited a significance in the precise preparation of RIS-loaded PLGA microspheres.

CAS / MDL: 100-51-6 141-78-6
研究领域: 药学 · 生物材料学
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MATERIALS & DESIGN · 2020 · IF 6.289

Electrospun PLGA nanomembrane: A novel formulation of extended-release bupivacaine delivery reducing postoperative pain

Yumiao He,Linan Qin,Yehong Fang,Zhenkang Dan,Yang Shen,Gang Tan,Yuguang Huang,Chao Ma

Efficacy and safety are fundamental qualities to uphold and improve when developing an extended-release carrier system for local anesthetics (LAs). This is especially true as diverse analgesics are applied in multimodal analgesia regimens and interactions between drugs may lead to adverse events. Here we propose a new formulation of LA carrier delivery: a PLGA nanomembrane produced by electrospinning technique that allows improved analgesia and better compatibility with combination analgesia regimen. In vitro release profile of this nanomembrane exhibited prolonged release profile (~35 days) compared to other extended-release systems of LAs studied so far. In vivo bupivacaine delivered through nanomembrane showed superior and prolonged analgesia compared to lidocaine infiltration in rat model of postoperative pain. Furthermore, in vivo safety profile of nanomembrane in single or combined use was confirmed by symptomatic, histological and pharmacokinetic analysis. These results indicate a novel formula of extended-release system that may potentiate better safety and analgesia of LAs compared to available extended-release products of LAs.

CAS / MDL: 920-66-1
研究领域: 药学 · 生物医学工程 · 疼痛管理
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2016 · IF 3.902

Sequential delivery of chlorhexidine acetate and bFGF from PLGA-glycol chitosan core-shell microspheres

Ming-Mao Chen,Huan Cao,Yuan-Yuan Liu,Yan Liu,Fei-Fei Song,Jing-Di Chen,Qi-Qing Zhang,Wen-Zhi Yang

Wound treatment should meet the challenge both of preventing infection and promoting wound healing. To design a sequential delivery system for wound healing, PLGA-glycol chitosan (GC) core-shell microspheres containing chlorhexidine acetate (CHA) at the GC shell and bFGF in the core of PLGA microspheres were fabricated using emulsion-solvent evaporation method. SEM showed that the microspheres were all spherical in shape with a smooth surface. The average size of PLGA-GC microspheres increased due to the GC coating on the surface. The results of release profiles and fluorescence images indicated that PLGA-GC microspheres had an ability to deliver drugs in sequence. The CHA was rapidly released, whereas the proteins presented a sustained release. The release behavior could be modulated by changing the GC amount. Antibacterial assay and cell proliferation tests suggested that the released CHA and bFGF retained their antimicrobial activity and bioactivity during preparation. The microspheres exhibited non-cytotoxicity against 3T3 cells and had a good biocompatibility. These results demonstrated that PLGA-GC core-shell microspheres could be a promising controlled release system of delivering drugs and proteins in sequence for wound healing.

研究领域: 药剂学 · 生物医学工程 · 材料科学
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RSC Advances · 2014 ·Vol. 4 ·期 95 ·53344-53351 · IF 3.708

Antitumor efficacy of a PLGA composite nanofiber embedded with doxorubicin@MSNs and hydroxycamptothecin@HANPs

Mengxia Chen,Wei Feng,Si Lin,Chuanglong He,Yu Gao,Hongsheng Wang

A co-delivery system with two or more anticancer drugs has been proposed to minimize the dosage of drug and to achieve the synergistic therapeutic effect in cancer therapy. In this study, we present a dual drug delivery system for the co-release of two anticancer drugs doxorubicin hydrochloride (DOX) and hydroxycamptothecin (CPT). To achieve this goal, DOX and CPT were first separately loaded into mesoporous silica and hydroxyapatite nanocarriers, thus, the two prepared drug loaded nanocarriers were then simultaneously incorporated into poly(lactic-co-glycolic acid) (PLGA) nanofibers by electrospinning. The as-prepared medicated nanofibers were well-characterized by different assays, and the results demonstrated that both of the two drug loaded nanocarriers were successfully incorporated into PLGA nanofibers. The in vitro release study indicated that the loaded DOX and CPT exhibited a sustained and controlled release behavior from the dual drug loaded nanofibers. Furthermore, the dual drug loaded nanofibers displayed a superior capacity of inhibiting HeLa cells in vitro to the single drug loaded PLGA nanofibers. Thus, the synthesized dual drug loaded composite nanofibers may find a promising application for cancer therapy.

CAS / MDL: 1306-06-5 12167-74-7
研究领域: 生物医学工程 · 药剂学 · 肿瘤学
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2023 · IF 5

MAG-encapsulated PLGA microspheres for Lipopolysaccharide-induced acute lung injury

Jiajia Jin,Jun chen,Xin Shou,Keqing Shi,Xingjie Zan,Yan Zu,Xiaoying Huang

Monoammoniuma Glycyrrhizinate is a great substitute for antibiotics in treating acute lung injury and can reduce the range of problems caused by antibiotic resistance. However, Monoammoniuma Glycyrrhizinate is not widely used in clinical practice due to its poor water solubility and the frequent use of large doses of drugs can cause adverse reactions in other organs. To solve this problem, we use electrostatic spray technology to produce microspheres which can be inhaled directly into the lungs and allow for slow release of the drug in the lungs, and they have smooth surface and good biocompatibility. In animal models, we find out that the MAG-encapsulated microspheres group show the best treatment effect compared to other treatment groups and may attenuate the activity of the LPS-activated Nuclear Factor signaling pathway. Therefore, this therapeutic strategy could potentially deliver the drug precisely to the lung, avoid these side effects, and provide a more scientifically effective way to treat pulmonary diseases with potential medicine.

研究领域: 药学 · 肺医学 · 生物技术 · 药理学
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International Journal of Nanomedicine · 2022 · IF 7.033

Superhydrophilic PLGA-Graft-PVP/PC Nanofiber Membranes for the Prevention of Epidural Adhesion

Qingxin Fan,Hao Wu,Qingquan Kong

Background The frequent occurrence of failed back surgery syndrome (FBSS) seriously affects the quality of life of postoperative lumbar patients. Epidural adhesion is the major factor in FBSS.Purpose A safe and effective antiadhesion material is urgently needed.Methods A superhydrophilic PLGA-g-PVP/PC nanofiber membrane (NFm) was prepared by electrospinning. FTIR was performed to identify its successful synthesis. Scanning electron microscopy, thermogravimetric analysis, differential scanning calorimetry, and water contact angle measurement were performed. CCK-8 assays were performed in primary rabbit fibroblasts (PRFs) and RAW264.7 cells to explore the cytotoxicity of PLGA-g-PVP/PC NFm. Calcein-AM/PI staining was used to measure the adhesion status in PRFs. ELISA was performed to measure the concentrations of TNF-α and IL-10 in RAW264.7 cells. In addition, the anti-epidural adhesion efficacy of the PLGA-g-PVP/PC NFm was determined in a rabbit model of lumbar laminectomy.Results The PLGA-g-PVP/PC NFm exhibited ultrastrong hydrophilicity and an appropriate degradation rate. Based on the results of the CCK-8 assays, PLGA-g-PVP/PC NFm had no cytotoxicity to PRFs and RAW264.7 cells. Calcein-AM/PI staining showed that PLGA-g-PVP/PC NFm could inhibit PRF adhesion. ELISAs showed that PLGA-g-PVP/PC NFm could attenuate lipopolysaccharide-induced macrophage activation. In vivo experiments further confirmed the favorable anti-epidural adhesion effect of PLGA-g-PVP/PC NFm and the lack of a strong inflammatory response.Conclusion In this study, PLGA-g-PVP/PC NFm was developed successfully to provide a safe and effective physical barrier for preventing epidural adhesion. PLGA-g-PVP/PC NFm provides a promising strategy for preventing postoperative adhesion and has potential for clinical translation.

研究领域: 生物医学工程 · 材料科学 · 神经外科
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