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JOURNAL OF CONTROLLED RELEASE · 2022 · IF 11.467

Tumor-oriented mathematical models in hydrogel regulation for precise topical administration regimens

Zhen Wang,Bixi Ding,Yuanpei Zhao,Yue Han,Yu Sheng,Ling Tao,Xiangchun Shen,Jianping Zhou,Lei Jiang,Yang Ding

Increasing knowledge of drug delivery properties, tumor profiles and their relationship promotes precise administration regimens, representing a promising pattern to personalized tumor treatment. Herein, we propose a regulatory hydrogel depot toward metastatic cancer by establishing mathematical models between tumor characteristics and administration regimens. Specifically, a thermo-sensitive PLGA-PEG-PLGA polymer is introduced as injectable hydrogel matrix, of which the administration volume and frequency are manipulated elaborately according to tumor size and gel-degradation kinetics. Structurally, doxorubicin (Dox) and arginine-terminated nanoparticles containing KIAA1199 specific shRNA ( shKIAA RPDNs) are incorporated into hydrogels, thereby formulating a topical and sustained drug depot to achieve synergy treatment. For dual-targeting therapy, Dox interdicts DNA replication/transcription, and shKIAA persistently silences KIAA1199 protein to modulate aggressive phenotypes. After individual peritumoral injection, Gel/ shKIAA RPDNs/Dox demonstrates desirable distribution patterns and gel degradation kinetics with enhanced tumor penetration. Moreover, a preferable inhibition of tumor proliferation and metastasis is confirmed after twice treatment in 12 days, indicating better therapeutic efficacy with less dosage and frequency. Consequently, the controllable administration regimen inspired mathematical models of thermosensitive hydrogel provides an intelligent platform for personalized treatment to metastatic cancer.

研究领域: 肿瘤学 · 药学 · 生物医学工程 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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EUROPEAN POLYMER JOURNAL · 2026 · IF 6.8

Highly flexible polyester macroinitiator enabled strength-retaining toughening of PLGA

Qianqian Qi,Mingyu Zhang,Hongshuo Ren,Qingguo Wang

Poly(lactic-co-glycolic acid) (PLGA) is a biodegradable aliphatic polyester with tunable composition and degradation behavior, but its intrinsic brittleness limits its broader use as a structural material. In this work, a highly flexible polyester macroinitiator (FPM) was introduced into PLGA through bulk ring-opening copolymerization of L-lactide and glycolide, followed by chain extension with hexamethylene diisocyanate (HDI), to construct PLGA FPM multiblock copolymers. FPM incorporation weakened the ordered packing of PLGA and progressively changed its tensile behavior from brittle fracture to pronounced ductile deformation. With increasing FPM content, PLGAFPM copolymers showed a gradual transition from brittle fracture to ductile deformation, accompanied by markedly improved elongation at break and tensile toughness. Among the investigated samples, PLGAFPM10 provided the most favorable balance between strength retention and toughness improvement, retaining a tensile strength of 55.6 MPa together with an elongation at break of 182.9 % and a toughness of 45.3 MJ/m 3 . Further increasing FPM content promoted extensibility but reduced tensile strength. Seawater immersion further showed a composition-dependent aqueous degradation response, with mass retention decreasing from 94.5 % for neat PLGA to 74.8 % for PLGA FPM20 after 126 d. This result indicates that FPM incorporation retained the hydrolyzable PLGA-based polyester framework while increasing water-related structural evolution. These results provide a chain-structure design strategy for toughening PLGA while maintaining its degradable polyester framework.

CAS / MDL: 822-06-0
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2021 · IF 6.953

Electrospun PLGA/SF/artemisinin composite nanofibrous membranes for wound dressing

Yan Peng,Yan Ma,Yu Bao,Zulan Liu,Li Chen,Fangyin Dai,Zhi Li

Combining biodegradable materials with natural plant components for wound dressing has been receiving significant attention. ART is a sesquiterpene lactone compound extracted from Artemisia annua L., possessing multiple pharmacological effects including antibacterial activity and anti-inflammatory property. Herein, the blended polylactic acid glycolic acid (PLGA)/silk fibroin (SF) membranes loaded with artemisinin (ART) are fabricated through electrospinning. With aid of SF, the fabricated membranes have a good sustained-release effect, and the accumulated ART release can reach 69% after three weeks. PLGA/SF/ART membranes exhibit favorable anti-inflammatory and cell compatibility in vitro evaluations. The in vivo experiment indicates that PLGA/SF/ART2 membranes can shorten the inflammation period and enhance skin regeneration in a full-thickness wound model through down-regulating the expressions of pro-inflammatory cytokines IL-1β and TNF-α. To sum up, the fabricated PLGA/SF/ART2 composite membranes with anti-inflammatory properties can be a proposal wound dressing for chronic wound healing.

CAS / MDL: 63968-64-9 920-66-1
研究领域: 材料科学 · 药剂学 · 生物医学工程 · 伤口愈合
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY · 2016 ·Vol. 16 ·期 5 ·4718-4726 · IF 1.338

Applying Electrospun Gelatin/Poly(lactic acid-co-glycolic acid) Bilayered Nanofibers to Fabrication of Meniscal Tissue Engineering Scaffold

Li Peng,Zhang Weiguo,Yu Hongquan,Zheng Lianjie,Yang Liang,Liu Gang,Sheng Chenchen,Gui Haoran,Ni Shuo,Li Pengsheng,Shi Feng

The menisci are fibrocartilaginous tissues composed primarily of an interlacing network of collagen fibers with nanoscale diameter. Electrospinning is a suitable process of producing nanoscale fibers that mimic collagen fibers. In this study, a bilayered scaffold (group B), which consists of a gelatin nanofiber mesh and a PLGA nanofiber mesh, has been fabricated through an electrospinning method. At the same time, we electrospun pure PLGA fibrous mesh (group A) and gelatin/PLGA composite fibrous mesh (group C) as control groups. In order to compare all scaffold morphologies, the scaffolds were imaged by SEM and some parameters were measured and analyzed as following: Diameters of fibrils are from the smallest of less than average 0.14 μm for group C to the biggest of nearly average 0.38 μm for group B. The scaffolds pore diameters are from average 4.9 μm for group A to average 11.2 μm for group B. Porosity rates show that the group B has the highest porosity rate at about 91%. The scaffolds’ properties were compared and analyzed, including hydrophilicity property (water contact angle) and mechanical properties (tensile strength). The results of water contact angle showed the group B is the most hydrophil among the groups. The results of tensile strength showed the tensile strength of group C is the weakest among the groups. All the results showed significant differences between the groups. Finally, in vitro, the meniscal cells derived from New Zealand white rabbits menisci were seeded in the scaffolds. We observed the cells proliferation behavior in the scaffolds. All above demonstrates that a bi-layered gelatin/PLGA scaffold reveals not only concurrent effects of mechanics and cytocompatibility in a fibrous context, but also a promising scaffold for future meniscal repair strategies.

研究领域: 生物材料学 · 组织工程学
✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2022 · IF 3.571

Matrix-assisted laser desorption/ionization mass spectrometric imaging the spatial distribution of biodegradable vascular stents using a self-made semi-quantitative target plate

Houwei Lin,Yinlian Yuan,Tian Hang,Peng Wang,Shijiao Lu,Hang Wang

In recent years, the development and optimization of biodegradable coronary stents have become the research focus of many medical device manufacturers and scientific research institutions since they can be completely degraded and absorbed, and they restore vascular function. However, there is a lack of in situ quantification of these stents spatially in tissue in vivo . In this study, matrix-assisted laser desorption/ionization (MALDI) Fourier transform ion cyclotron resonance (FT ICR) and time-of-flight (TOF) mass spectrometric imaging (MSI) were used to analyze the time-dependent distributions of a biodegradable vascular scaffold, which consisted of copolymers of lactic acid and glycolic acid (PLGA) and its degradation products in cross-sections and longitudinal sections of blood vessels. The MALDI-MSI methods for analyzing the distribution of PLGA and its derivatives in vivo were established by optimizing the conditions of sample pretreatment and mass spectrometry (MS). In order to semi-quantify the contents of PLGA degradation products in blood vessels, self-made stainless-steel and indium tin oxide (ITO) target plates were developed to compare and establish the standard curves for semi-quantitative analysis. The target plate can be placed on the target carrier of MS simultaneously with the conductive slide, which can simultaneously carry out vapor deposition or spray on the substrate, to ensure the parallelism of the pretreatment experiments between the standards and the actual vascular samples. The proposed method provided a powerful tool for evaluating the distributions and degradation process of biological stent materials in the coronary artery, as well as provided technical support for the research and development of degradable biological stents and product optimization.

研究领域: 医学影像学 · 材料科学 · 生物医学工程
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Materials Science & Engineering C-Materials for Biological Applications · 2016 · IF 3.42

Preparation, physicochemical properties and biocompatibility of PBLG/PLGA/bioglass composite scaffolds

Ning Cui,Junmin Qian,Jinlei Wang,Chuanlei Ji,Weijun Xu,Hongjie Wang

In this study, novel poly(γ-benzyl l -glutamate)/poly(lactic- co -glycolic acid)/bioglass (PBLG/PLGA/BG) composite scaffolds with different weight ratios were fabricated using a negative NaCl-templating method. The morphology, compression modulus and degradation kinetics of the scaffolds were characterized. The results showed that the PBLG/PLGA/BG composite scaffolds with a weight ratio of 5:5:1, namely PBLG5PLGA5BG composite scaffolds, displayed a pore size range of 50–500   μm, high compressive modulus (566.6   ±   8.8   kPa), suitable glass transition temperature (46.8   ±   0.2   °C) and low degradation rate (>   8   weeks). The in vitro biocompatibility of the scaffolds was evaluated with MC3T3-E1 cells by live-dead staining, MTT and ALP activity assays. The obtained results indicated that the PBLG5PLGA5BG composite scaffolds were more conducive to the adhesion, proliferation and osteoblastic differentiation of MC3T3-E1 cells than PBLG and PBLG/PLGA composite scaffolds. The in vivo biocompatibility of the scaffolds was evaluated in both SD rat subcutaneous model and rabbit tibia defect model. The results of H&E, Masson's trichrome and CD34 staining assays demonstrated that the PBLG5PLGA5BG composite scaffolds allowed the ingrowth of tissue and microvessels more effectively than PBLG/PLGA composite scaffolds. The results of digital radiography confirmed that the PBLG5PLGA5BG composite scaffolds significantly improved in vivo osteogenesis. Collectively, the PBLG5PLGA5BG composite scaffolds could be a promising candidate for tissue engineering applications.

研究领域: 生物材料 · 组织工程 · 生物医学工程 · 材料科学
✓ 已验证 DOI PubMed 高影响因子
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Biomaterials Advances · 2022 · IF 0

Chitosan-modified Phellinus igniarius polysaccharide PLGA nanoparticles ameliorated inflammatory bowel disease

Xinxin Bai,Zian Feng,Song Peng,Tianyu Zhu,Lina Jiao,Ningning Mao,Pengfei Gu,Zhenguang Liu,Yang Yang,Deyun Wang

In many clinical studies, prebiotics have been used as adjuvant therapy for inflammatory bowel disease (IBD). Phellinus igniarius polysaccharide (PIP) possesses great anti-inflammatory and prebiotic activities. Herein, we developed an orally deliverable PIP-loaded chitosan-modified PLGA nanomedicine (CS-PIPP) to investigate its anti-inflammatory effect in vitro and in vivo. Dextran sodium sulfate (DSS)-induced colitis model was established to evaluate the preventive effect of CS-PIPP on IBD. This study characterized that CS-PIPP had a size of 288.7 ± 5.49 nm, positive zeta potential, and showed good stability over four weeks. The in-vitro study suggested that CS-PIPP had enhanced phagocytosis by macrophages, which could further significantly inhibit M1-like macrophages phenotype and regulate lipopolysaccharide (LPS)-induced inflammatory cytokines. The in-vivo study revealed that CS-PIPP prominently prevented intestinal inflammatory damage and protected the integrity of the intestinal barrier. Moreover, CS-PIPP increased the contents of short-chain fatty acids (SCFAs) and positively regulated the gut microbiota. Specifically, CS-PIPP reduced enteropathogenic microorganisms while increasing the beneficial microbiota, including Lactobacillus and Akkermansia , which revealed the potential of CS-PIPP as prebiotics. Generally, CS-PIPP promoted the anti-inflammatory effect of PIP, so it could be regarded as a novel and potent nanoformulation to treat IBD.

研究领域: 药理学 · 纳米技术 · 免疫学 · 胃肠病学 · 微生物学
✓ 已验证 DOI PubMed
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MATERIALS AND MANUFACTURING PROCESSES · 2016 · IF 1.419

Manufacture, Characterization, and Release Profiles of Insulin-Loaded Mesoporous PLGA Microspheres

Yongli Shi,Suying Ma,Ruiqiong Tian,Yingge Zhao,Fangyu Cai,Ranran Li,Qing Shang

This paper reports the fabrication of insulin-loaded mesoporous microspheres by a double emulsion-solvent evaporation technique using poly(lactic acid-co-glycolic acid) (PLGA) as carrier materials. PLGA solutions with two different concentrations (4% and 5%) were used as the oil phases to fabricate the mesoporous microspheres. The morphology and the particle size distribution of final microspheres were studied by optical microscope, scanning electronic microscope (SEM), and Malvern 2600 sizer, respectively. The mesoporous microspheres were monodisperse with an average diameter of 7 ± 3.5 µm. Insulin, as a model drug, was encapsulated into the final microspheres. In vitro release studies suggested that insulin was continuously released from the medicated microspheres. Furthermore, the final microspheres obtained from 4% PLGA solution showed a small “burst release” effect for their dense structures, which shortened the lag time to the effective plasma concentration. To summarize, the insulin-loaded PLGA microsphere are very promising for use in pharmaceutical applications.

研究领域: 药学 · 材料科学 · 药物递送系统
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BIOMACROMOLECULES · 2026 · IF 5.9

Degradation-Function Coupling in Eugenol-Functionalized PLGA Polyurethanes for Antifouling Interfaces

Chunying Si,Yunbiao Qi,Haoyi Wang,Quanxing Zhang,Wei Jiang

The development of biodegradable antifouling coatings represents a promising route to environmentally compatible marine protection. However, most polyester-based systems exhibit limited interfacial evolution and a poor long-term biofouling resistance. Here, we report poly(lactic-co-glycolic acid) (PLGA)-based polyurethane (PU) coatings that bear covalently tethered eugenol (EU) side groups (PLGA–PU-EUx), designed to couple hydrolytic degradation with interfacial bioactivity. Compared with PLA-based analogues, the PLGA–PU-EUx coatings show greater mass loss, lower water contact angles during seawater immersion, more evident chemical and morphological evolution, and markedly enhanced inhibition of marine bacteria (Micrococcus luteus) and diatoms (Navicula incerta). At 15 wt % EU, diatom inhibition exceeds 95%. Leachate analysis indicates that freely dissolved EU-related species are highly limited under the tested conditions, while zebrafish embryo assays show no obvious acute developmental toxicity. These findings establish degradation-function coupling as a general strategy for designing durable and environmentally benign antifouling interfaces.

✓ 已验证 DOI PubMed 高影响因子
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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS · 2025 · IF 2.2

Folic acid-functionalized PLGA nanomedicines encapsulating echinacoside for liver cancer therapy

Yang Han,Junyong Fan,Wei Xia,Xiao Dong,Ying Ye

Primary liver cancer remains a major contributor to global cancer-related mortality. Echinacoside, a bioactive phenylethanoid glycoside isolated from traditional Chinese medicinal herbs, has shown potent anti-tumor effects. In this study, poly (lactic-co-glycolic acid) (PLGA) nanoparticles encapsulating echinacoside (E@PLGA and E@PLGA-FA) were synthesized via the double emulsification method. Their physicochemical properties, drug release kinetics, and anti-cancer efficacy were systematically evaluated through in vitro and in vivo models. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) analyses revealed that the particle sizes of E@PLGA and E@PLGA-FA were approximately 91 nm and 100 nm, respectively, with zeta potentials of -22.50 mV and -31.89 mV. The polydispersity index (PDI) of E@PLGA and E@PLGA-FA was determined to be 0.16±0.01 and 0.19±0.01, respectively. The encapsulation efficiency and drug-loading capacity of echinacoside in E@PLGA-FA were 28.78% and 12.05%, respectively, slightly lower than those in E@PLGA nanoparticles (40.34% and 16.12%), likely due to folic acid modification altering PLGA solubility during formulation. In vitro release profiles demonstrated pH-dependent drug release: 22% at physiological pH (7.4) versus 67% under acidic conditions (pH 5.5) over 12 h, indicating tumor microenvironment-responsive behavior. Furthermore, E@PLGA-FA significantly inhibited the proliferation of HepG2 cells, induced apoptosis, caused cell cycle arrest at the G0/G1 phase, and suppressed cell mobility. Meanwhile, the protein levels of MMP2, MMP9 and Bax were increased after exposure to E@PLGA and E@PLGA-FA, whereas the protein levels of COL-Ⅰ, COL-Ⅱ, Bcl-2, Cyclin D1, and PCNA were decreased. In vivo, E@PLGA-FA effectively inhibited tumor growth, induced tumor cell apoptosis, and exhibited tumor-specific accumulation confirmed by fluorescence imaging. In addition, The E@PLGA-FA nanoparticle intervention did not induce pathological damage or inflammatory responses in murine liver and kidney tissues, suggesting a favorable safety profile for this compound. In conclusion, we engineered a novel tumor-targeted PLGA-based nanoparticle system for echinacoside delivery, which synergizes pH-responsive drug release, multi-mechanistic anti-cancer effects, and biosafety, offering a promising therapeutic platform for hepatocellular carcinoma.

CAS / MDL: 82854-37-3
研究领域: 药剂学 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Biomaterials Science · 2025 · IF 5.7

Development of rapamycin-loaded PLGA nanoparticles for treating retinopathy of prematurity

Hui Shi,Yuqiao Ju,Qing Chang,Lian Cen

With the increasing incidence of retinopathy of prematurity (ROP) and the gradual emergence of side effects associated with existing treatments, the development of novel nano-therapy strategies for ROP has become critically urgent. The aim of the current study was to explore the possibility of developing PLGA nanoparticles loaded with rapamycin (RPM) (RPM-PLGA NPs) for the sustained release of RPM as a nano-therapy for ROP intervention. RPM-PLGA NPs were prepared using a nanoprecipitation method, and their physicochemical properties were characterized. The safety profile and therapeutic efficacy of RPM-PLGA NPs were evaluated in BV2, HUVEC cells and in an oxygen-induced retinopathy (OIR) mouse model. RPM-PLGA NPs of 144.23 ± 3.40 nm, a polydispersity index of 0.05 ± 0.02, an encapsulation efficiency of 81.39%, and a drug loading capacity of 16.28% were successfully prepared. The sustained and gradual release of RPM from these NPs was achieved for over 35 days. It was demonstrated that RPM-PLGA NPs had no significant effect on the viability and migration of BV2 and HUVECs. In the oxygen-induced OIR model, RPM-PLGA NPs significantly reduced the areas of vaso-obliteration and pathological neovascularization in the mouse retina, showing superior therapeutic effects compared to RPM alone. These findings validated the feasibility of RPM-PLGA NPs as an intravitreal injection for the treatment of ROP. It is believed that the current study could provide promising experimental data for nano-therapy as an effective and superior treatment for ROP with few side effects.

CAS / MDL: 9002-89-5
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2026 ·Vol. 27 ·期 7 ·3300 · IF 5.6

Oral Delivery of Liraglutide Formulated with PLGA for Sustained Obesity Management

Nipeng Chen,Zhipeng Zeng,Xiaoyu Ji,Weijia Huang,Zhen Zhang,Yongming Chen

Liraglutide (Lira), a glucagon-like peptide-1 (GLP-1) receptor agonist, has demonstrated substantial efficacy in improving glycemic control and reducing body weight. However, subcutaneous injection is poorly adherent for patients. To improve treatment compliance, we developed a poly(lactic-co-glycolic acid) (PLGA)-based nanovesicle (PLGA-Lira-NV) system for the oral delivery of Lira using a double-emulsion solvent evaporation technique. The optimized formulation yielded a narrow size distribution and high encapsulation efficiency (>95%). In vitro release studies showed that PLGA-Lira-NVs remained relatively stable under acidic conditions (pH 1.2 to 6.8) and exhibited sustained drug release in a neutral environment (pH 7.4), enabling protection of the fragile peptide in the stomach and controlled release after crossing the intestine. Following oral administration to obese mice (10 mg/kg), PLGA-Lira-NVs achieved prolonged glycemic control for up to 72 h. Notably, body weight decreased to 83% of baseline after 12 days, outperforming the subcutaneous injection (free Lira) group (88%). The consistent trend toward weight reduction confirms the sustained-release properties of PLGA nanocarrier for Lira, highlighting its potential to reduce dosing frequency and improve patient compliance. Collectively, these findings underscore the promising potential of PLGA nanovesicles as an oral delivery platform for peptide therapeutics.

✓ 已验证 DOI PubMed 高影响因子
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