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PLGA-PEG
Journal of Materials Research and Technology-JMR&T · 2021 · IF 5.039

Porous PLGA-PEG nerve conduit decorated with oriented electrospun chitosan-RGD nanofibre

Yuzhe Chen,Wenxuan Zhao,Honglian Dai

Chitosan (CS) is a type of natural polysaccharide, widely used as a biomaterial on account of its great biocompatibility and the multitudes of functional groups on the long chitosan chain, making it easy for property augmentations. Nevertheless, the lack of workability and mechanical capacity limits the applications. Herein, electrospinning was chosen to fabricate oriented chitosan/polyethylene oxide (PEO) nanofibres decorated by integrin-targeting polypeptides (RGD, Arg-Gly-Asp), which is essential for cell adhesion. At the same time, porous PLGA-PEG membranes were taken as a shell of the composite film, which can provide mechanical support for the scaffold. Adequate topological anisotropic information from oriented nanofibres helps the scaffold simulate the natural axon structure, which can induce accelerated regeneration of neurotmesis. Moreover, β-Tricalcium Phosphate (β-TCP) nanoparticles were brought into nanofibers to neutralize the acidic environment produced by the degeneration of PLGA-PEG. Cell viability tests at the in vitro level and dorsal root ganglion (DRG, 1-day sucking SD rat) co-culture detection proved that the scaffold possesses excellent biocompatibility while guiding oriented regeneration of damaged nerves. In this study, a CS-RGD/PEO/β-TCP/PLGA-PEG porous composite scaffold with low cytotoxicity was fabricated. The scaffold can not only lead to the oriented growth of nerves but also has selectivity, which can help nutrient exchange while inhibiting the invasion of fibrous tissue.

研究领域: 生物医学工程 · 材料科学 · 神经再生
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JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION · 2020 · IF 2.69

Synthesis and characterization of PLGA-PEG-PLGA based thermosensitive polyurethane micelles for potential drug delivery

Min Wang,Jianghao Zhan,Laijun Xu,Yanjun Wang,Dan Lu,Zhen Li,Jiehua Li,Feng Luo,Hong Tan

Polyurethane nanomicelle is a promising functional drug delivery system. In this work, the polyurethane (P3-PU) was synthesized from PLGA1200-PEG1450-PLGA1200 (P3, a thermosensitive and biodegradable triblock copolymer) and L-lysine ester diisocyanate (LDI). Then, reactive benzaldehyde was further imported to terminate P3-PU to obtain benzaldehyde modified polyurethane (P3-PUDA). The micelles, temperature-sensitive P3-PU nanomicelle and P3-PUDA nanomicelle, were systematically investigated, including the size, stability, temperature sensitivity, drug loading and release behavior, cytotoxic on human hepatocytes (L02), and inhibitory effect on human hepatocellular carcinoma cells (HepG2). The results show the thermosensitive behavior of the micelles can be adjusted by the terminal group. The polyurethane micelles with a uniform size between 20 nm and 30 nm showed excellent stability and good biocompatibility to L02 cells. Besides, in vitro experiments showed that Dox-loaded P3-PUDA micelles exhibited faster and higher release rate at 37 °C and better inhibitory effect on HepG2 than the Dox-loaded P3-PU micelles. Moreover, the achieved benzaldehyde modified polyurethanes also provides various possibilities to adjust further to enlarge its applications. Therefore, the polyurethane micelles will have great potential in the field of drug carriers.

研究领域: 生物材料学 · 药剂学 · 肿瘤学
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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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Expert Opinion on Drug Delivery · 2014 · IF 4.116

Andrographolide-loaded PLGA-PEG-PLGA micelles to improve its bioavailability and anticancer efficacy

Jinming Zhang,Yingbo Li,Wei Gao,Michael A Repka,Yitao Wang,Meiwan Chen

Background: Andrographolide (ADG) isolated from Andrographis paniculata exhibits anti-inflammatory and anticancer activities, but high hydrophobicity and poor bioavailability greatly restricts its clinical application.Objectives: In this study, ADG was encapsulated in a micelle formulation based on poly (D,L-lactide-co-glycolide)-b-poly (ethylene glycol)-b-poly (D,L-lactide-co-glycolide) (PLGA-PEG-PLGA) amphiphilic triblock copolymers, in order to enhance the anticancer efficacy and bioavailability in vivo.Methods: The physicochemical properties of the ADG-loaded PLGA-PEG-PLGA micelles were investigated for encapsulation efficiency, particle size, zeta potential and critical micelle concentration. These micelles were further evaluated for in vitro cytotoxicity, including proliferation inhibition, cell cycle arrest and pro-apoptosis effects against human breast cancer MAD-MB-231 cells, cellular uptake and pharmacokinetics study in rat.Results: ADG-loaded PLGA-PEG-PLGA micelles had a high encapsulation and loading efficiency of about 92 and 8.4% (w/w), respectively, and a stable particle size of 124.3 ± 6.4 nm. In vitro cytotoxicity testing demonstrated that ADG-loaded PLGA-PEG-PLGA micelles exhibited higher proliferation inhibition, cell cycle arrest at the G2/M phase and pro-apoptosis effects in MAD-MB-231 cells, which would be contributed to higher efficiency of cellular uptake and intracellular transport. Further, the plasma AUC(0 – ∞) and mean resident time of ADG-loaded PLGA-PEG-PLGA micelles were increased by 2.7- and 2.5-fold, respectively, when compared to the raw suspension.Conclusion: All of these investigations suggest that PLGA-PEG-PLGA micelles may be a potential drug delivery strategy for improving ADG bioavailability and efficacy in cancer therapy.

研究领域: 药剂学 · 肿瘤学 · 纳米医学
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LAB ON A CHIP · 2024 · IF 6.1

Microfluidic preparation of monodisperse PLGA-PEG/PLGA microspheres with controllable morphology for drug release

Wenwen Chen,Hao Li,Xinyue Zhang,Yutao Sang,Zhihong Nie

Monodisperse biodegradable polymer microspheres show broad applications in drug delivery and other fields. In this study, we developed an effective method that combines microfluidics with interfacial instability to prepare monodispersed poly(lactic-co-glycolic acid)-b-polyethylene glycol (PLGA-PEG)/poly(lactic-co-glycolic acid) (PLGA) microspheres with tailored surface morphology. By adjusting the mass ratio of PLGA-PEG to PLGA, the concentration of stabilizers and the type of PLGA, we generated microspheres with various unique folded morphologies, such as “fishtail-like”, “lace-like” and “sponge-like” porous structures. Additionally, we demonstrated that risperidone-loaded PLGA-PEG/PLGA microspheres with these folded morphologies significantly enhanced drug release, particularly in the initial stage, by exhibiting a logarithmic release profile. This feature could potentially address the issue of delayed release commonly observed in sustained-release formulations. This study presents a straightforward yet effective approach to construct precisely engineered microspheres offering enhanced control over drug release dynamics.

研究领域: 药剂学 · 材料科学 · 药物递送系统
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ACS Biomaterials Science & Engineering · 2021 · IF 4.749

Fabrication of Porous Crystalline PLGA-PEG Induced by Swelling during the Recrystallization Annealing Process

Jidong Dai,Xin Tan,Min Liang,Dandan Wei,Yinhua Tao,Pengfei Ren,Tianzhu Zhang

Poly(lactide-co-glycolide) (PLGA) has been widely used as a scaffold material for tissue engineering owing to its biocompatibility, biodegradability, and biosafety. However, lactic acid (LA) produced during PLGA degradation is prone to inflammation, which is a shortcoming that must be avoided. To this end, crystalline PLGA-PEG was synthesized here for the first time. To make the crystalline PLGA-PEG more suitable for tissue engineering, porous crystalline PLGA-PEG was prepared via the swelling behavior during recrystallization annealing. The structure and properties of the porous crystalline PLGA-PEG were confirmed by SEM, POM, and XRD. Furthermore, the swelling behavior of different PEG molecular weights was studied, and the cell viability test and alkaline phosphatase activity test showed that PLGA-PEG has good biocompatibility. Such a porous crystalline PLGA-PEG will make PLGA have a broader application prospect in bone repair.

研究领域: 材料科学 · 生物医学工程 · 组织工程
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES · 2012 · IF 3.212

Folic acid and cell-penetrating peptide conjugated PLGA–PEG bifunctional nanoparticles for vincristine sulfate delivery

Jianian Chen,Shaoshun Li,Qi Shen

Dual- and multi-functional drug delivery systems , especially ligand-modified nanoparticles (NPs) loaded with chemotherapeutic agents are paid much attention to due to their excellent behavior in vitro and in vivo . Bifunctional NPs (BF-NPs), which were based on PLGA–PEG and modified with folic acid and cell penetrating peptide R 7 simultaneously, were developed. BF-NPs loaded with vincristine sulfate (VCR) were prepared via the water–oil–water emulsion solvent evaporation method. BF-NPs showed favorable particle size and zeta potentials , promising drug loading and entrapment efficiency. The release of VCR from BF-NPs exhibited a biphase release manner. Cellular uptake of BF-NPs was found to be higher than that of the NPs merely modified by folic acid or R 7 . In vitro cytotoxicity, cell apoptosis and cell cycle arrest studies also revealed that BF-NPs were more potent than those of the NPs merely modified by folic acid or R 7 . Therefore, the results demonstrated that BF-NPs developed in this study could be a potential vehicle for delivering chemotherapeutic agents such as VCR and breast cancer therapy.

研究领域: 药学 · 纳米技术 · 癌症研究
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POLYMER DEGRADATION AND STABILITY · 2019 · IF 3.78

PLGA–PEG terpolymers as a carriers of bioactive agents, influence of PEG blocks content on degradation and release of herbicides into soil

Piotr Rychter,Kamila Lewicka,Małgorzata Pastusiak,Marian Domański,Piotr Dobrzyński

Nowadays, researchers in the field of agrochemicals are trying to find effective methods to limit the excessive usage of pesticides and protect the environment. One of the most popular and promising techniques is the immobilization of pesticides using environment-friendly polymers. In the conducted research, it was demonstrated that the family of lactide/glycolide copolymers are unsuitable for this purpose due to very slow degradation in the soil. We examined influence of relatively small content of PEG blocks in newly synthesized poly( l -lactide-co-glycolide)-poly(ethylene glycol)–poly( l -lactide-co-glycolide) (PLGA–PEG–PLGA) on the degradation in soil, in activated sludge and usefulness of this terpolymers as a biodegraded carrier for the controlled release of two commonly used herbicides (Metazachlor and Pendimethalin). Presence of even small amount of PEG block in the terpolymer chain increases slightly the hydrophilicity of the polymeric chain, thereby increasing its susceptibility to hydrolytic and unexpectedly strongly to enzymatic degradation in soil environment. The amorphism of used as a carriers PLGA-PEG-PLGA terpolymers and the lack of the phenomenon of increasing the degree of crystallinity during degradation allow to achieve uniform progress of degradation, and thus is obtained a relatively constantly release of tested herbicides. In this way, it is possible to determine the optimal profile of degradation of polymer in soil and proper rate of diffusion and leaching of active agents which allows the release of herbicides in optimal and effective doses within 3–4 months of its application.

研究领域: 农业科学 · 高分子化学 · 环境科学
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Journal of Functional Foods · 2022 · IF 5.223

PLGA-PEG-fucoxanthin nanoparticles protect against ischemic stroke in vivo

Qiyao Wang,Difan Zhang,Jiani Lu,Jiaying Zhang,Zhenquan Xuan,Luyun Gong,Mengxiang Yang,Lingli Jin,Jingyang Le,An Zhu,Hongze Liang,C. Benjamin Naman,Jinrong Zhang,Li Zhao,Shan He,Qinwen Wang,Hao Liu,Xiaojun Yan,Lingling Zhao,Wei Cui

Fucoxanthin is the most abundant marine carotenoid derived from edible brown seaweeds and has been used as a functional ingredient for the treatment of obesity. However, poor brain bioavailability of fucoxanthin has limited its application in combating neurological diseases. In this study, we demonstrated that 40 % fucoxanthin was released from polylactic- co -glycolic acid-polyethylene glycol (PLGA-PEG) nanoparticles at one day after incubation. Fucoxanthin nanoparticles (20–40 mg/kg, i.v. ) significantly prevented neurological and behavioral deficits in middle cerebral artery occlusion/reperfusion (MCAO)-treated rats via the reduction of M1 microglial activation, decrease of pro-inflammatory factor production, inactivation of the nuclear factor-κB (NF-κB) pathway, and elevation of the nuclear factor-E2-related factor 2 (Nrf2) pathway in ischemic penumbra. Moreover, fucoxanthin nanoparticles (5–15 μg/mL) inhibited hypoxia-stimulated neurotoxicity in a mouse hippocampal neuron cell line (HT22 cells). These results suggest that fucoxanthin nanoparticles enhanced brain bioavailability and produced neuroprotection against ischemic stroke in vivo with much lower effective concentrations than fucoxanthin itself, providing further support for the development of fucoxanthin as a functional ingredient for the prevention of ischemic stroke with proper nanoparticle formulations.

CAS / MDL: 66085-59-4
研究领域: 神经科学 · 药学 · 生物技术
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JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES · 2011 · IF 2.971

An HPLC method for the pharmacokinetic study of vincristine sulfate-loaded PLGA–PEG nanoparticle formulations after injection to rats

Jianian Chen,Huijuan He,Shaoshun Li,Qi Shen

The aim of this study is to develop a simple and applicable HPLC method for the detection of vincristine in rat plasma after administration of poly(lactic- co -glycolic acid)–poly(ethylene glycol) (PLGA–PEG) nanoparticles loaded with vincristine sulfate (VCR). Vincristine was extracted from rat plasma and vinblastine sulfate was chosen as the internal standard (IS). Chromatographic separation of VCR and IS was achieved by a Dikma Dimonsil C 18 column (200   mm   ×   4.6   mm) with the mobile phase consisting of 0.02   M sodium dihydrogen phosphate–methanol (36:64, v/v, pH   =   4.7) at a flow rate of 1.0   mL/min. The ultraviolet detection wavelength was set at 276   nm. The calibration curve was linear over a concentration range of 0.05–5.0   μg/mL. The intra-day and inter-day accuracy for three quality controls (QC) samples was 93.48–107.74% and 92.61–96.58%, respectively; the precision was less than 9%. The average method recoveries for vincristine from spiked plasma at all QC levels were over 83%; and extraction recoveries were between 66 and 70%. Vincristine was stable in rat plasma for one month at −80   °C, for 8   h at room temperature , as well as during three freeze–thaw cycles. This HPLC method was applied successfully to the pharmacokinetic study of vincristine in rats after a single intravenous injection of VCR in physiological saline (F-VCR) solution, VCR-loaded PLGA–mPEG nanoparticles with (NP1) and PLGA–PEG–folate nanoparticles (NP2) suspension, respectively. There were significant differences in main pharmacokinetic parameters between F-VCR and the nanoparticles. Both kinds of VCR-loaded nanoparticles displayed improved pharmacokinetic profiles.

CAS / MDL: 59-30-3 2068-78-2
研究领域: 药理学 · 生物医学工程 · 分析化学
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Artificial Cells Nanomedicine and Biotechnology · 2019 · IF 4.462

Liposomal doxorubicin loaded PLGA-PEG-PLGA based thermogel for sustained local drug delivery for the treatment of breast cancer

Dinglingge Cao,Xingxian Zhang,MD. Akabar,Yuan Luo,Hao Wu,Xue Ke,Tianyuan Ci

The aim of this research is to utilize a hybrid system of liposomal doxorubicin (DOX-Lip) loaded thermogel (DOX-Lip-Gel) to realize the steady sustained delivery of doxorubicin (DOX), a small hydrophilic drug, for the treatment of breast cancer locally. Herein, liposomal doxorubicin was prepared via the traditional film dispersion method with the particle size of 75 nm and drug entrapment efficiency of 86%. And, the triblock copolymer of poly (D, L-lactide-co-glycolide)-b-poly (ethylene glycol)-b-poly (D, L-lactide -co-glycolide) (PLGA-PEG-PLGA) was synthesized via ring-opening polymerization to prepare the thermosensitive hydrogel through dissolving the polymers in DOX-Lip solution. The liposome loaded hydrogel was in a sol state at room temperature and converted into the gel state at body temperature and would degrade gradually during the time in vivo. The drug release of DOX out of DOX-Lip-Gel could be in a steady sustained manner up to 11 days without significant burst release as compared to that of DOX-loaded hydrogel (DOX-Gel). An orthotopic breast cancer model was adopted to evaluate the in vivo antitumor efficacy. And, the results revealed DOX-Lip-Gel had better antitumor efficiency as well as lower side effects.

CAS / MDL: 57-88-5
研究领域: 药剂学 · 肿瘤学 · 药物递送系统
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Artificial Cells Nanomedicine and Biotechnology · 2019 · IF 4.462

Co-encapsulation of magnetic Fe3O4 nanoparticles and doxorubicin into biocompatible PLGA-PEG nanocarriers for early detection and treatment of tumours

Chenghua Liang,Nan Li,Zikai Cai,Rongpu Liang,Xiaoming Zheng,Li Deng,Longbao Feng,Rui Guo,Bo Wei

At present, cancer is the first cause of death for humans, but early detection and treatment can help improve prognoses and reduce mortality. However, further development of carrier-assistant drug delivery systems (DDSs) is retarded by the aspects such as the low drug-carrying capacity, carrier-induced toxicity and immunogenicity, complex synthesis manipulation. The development of nanoscale drug delivery systems (NDDS) have been rapidly developed to address these issues. In this article, we used PLGA-PEG with good biocompatibility to encapsulate Fe3O4 nanoparticles (a magnetic resonance imaging contrast agent) and DOX (an antitumour drug) via the emulsion-solvent evaporation method, aimed at achieving a dual function of the early detection and the treatment of mammary cancer. The results showed that the Fe3O4/DOX/PLGA-PEG nanoparticles had a relatively uniform size, a high carrier rate of Fe3O4 and high encapsulation efficiency of DOX, and a relatively high activity of released DOX within 120 h. In addition, in vitro studies showed that the Fe3O4/DOX/PLGA-PEG nanoparticles were cytocompatibility in NIH 3T3 fibroblast cells culture study while had a special effect on destroying human breast cancer MCF-7 cells compared with pure DOX solution. In vitro studies revealed that the Fe3O4/DOX/PLGA-PEG enabled enhanced T2 contrast magnetic resonance. Overall, our multifunctional Fe3O4/DOX/PLGA-PEG nanoparticles, composed of biocompatible substances and therapeutic/imaging materials, have great potential for the early detection of cancer and accurate drug delivery via the dynamic monitoring using MRI.

研究领域: 生物医学工程 · 纳米医学 · 肿瘤学
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