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COLLOIDS AND SURFACES B-BIOINTERFACES · 2017 · IF 3.887

Surface-modified PLGA nanoparticles with chitosan for oral delivery of tolbutamide

Yongli Shi,Jintao xue,Liyun Jia,Qian Du,Jie Niu,Dongyang Zhang

The main purpose of present study was to develop novel chitosan-modified polylactic-co-glycolicacid nanoparticles (CS@PLGA NPs) for improving the bio-availability of tolbutamide (TOL). The TOL-loaded CS@PLGA NPs (TOL-CS@PLGA NPs) were fabricated with the solvent evaporation method. The cargo-free CS@PLGA NPs showed a diameter of 228.3   ±   2.5   nm monitored with a laser light particlesizer, and the transmission electron microscope (TEM) photographs revealed their “core-shell” structures. The Zeta potential of the original PLGA NPs and the cargo-free CS@PLGA NPs was measured to be −20.2   ±   3.21   mV and 24.2   ±   1.1   mV, respectively. The changes in Zeta potential indicated the CS chains were coated on the surfaces of the original PLGA NPs. The thermal gravity analysis (TGA) curves suggested that the CS chains improved the thermostability of the original PLGA NPs. The results of cells viability indicated the cargo-free CS@PLGA NPs were nontoxicity. The in vitro release profiles suggested that TOL-CS@PLGA NPs could release TOL in pH 7.4 phosphate buffer solution (PBS) at a sustained manner. Streptozotocin (STZ) was employed to build the diabetic rat models. The physiological changes in the islet β cells confirmed the obtaining of diabetic rats. After treatment by gavage, the TOL-CS@PLGA NPs showed an excellent hypoglycemic effect. Therefore, the TOL-CS@PLGA NPs had a potential application in oral delivery of TOL.

研究领域: 药剂学 · 生物医学工程
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Journal of Macromolecular Science Part B-Physics · 2021 · IF 1.504

In-vitro Degradation Behaviors of Poly(L-lactide-co-glycolide-co-ε-caprolactone) Microspheres

Meiling Yi,Zhihua Zhou,Wenjuan Liu,Tianlong Huang,Yanmin Zhao,Ping Chen,Ziwei Zhou,Dan Wang,Chao Zhang,Jianjun Fang

Among drug delivery systems, polymer microspheres have been proved to be the most promising carriers during the past several years. In this paper we describe the preparation of poly(L-lactide-co-glycolide-co-ε-caprolactone) (PLLGC) random terpolymer microspheres; their in-vitro degradation behaviors, including the changes of pH value, mass loss, molecular mass and surface morphology, were investigated during various degradation periods and compared with poly(lactic-co-glycolic acid) (PLGA) microspheres. The results showed that the introduction of the ε-caprolactone (ε-CL) unit reduced the degradation rate of the PLGA polymers. Therefore, we suggest the PLLGC microspheres with controllable degradation rate could supply a wider application future in drug delivery field than pure PLGA microspheres.

研究领域: 生物医学工程 · 药剂学 · 高分子科学 · 材料科学
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2019 · IF 2.606

Novel triptorelin acetate-loaded microspheres prepared by a liquid/oil/oil method with high encapsulation efficiency and low initial burst release

Liqing Chen,Atef Mohammed Qasem Ahmed,Yibin Deng,Dingyun Cao,Huanhuan Du,Jinghao Cui,Beom-Jin Lee,Qingri Cao

Low encapsulation efficiency (EE) and high initial burst release are key issues for the development of microspheres loading highly water-soluble peptide drugs. In this study, novel triptorelin acetate-loaded microspheres with high EE and low initial burst release were prepared by a liquid/oil/oil (L/O/O) phase separation method using poly(lactic- co -glycolic acid) (PLGA) as the sustained-release carrier. The formulation of the microspheres and the preparation process were optimized in terms of particle size, surface morphology, EE, and in vitro drug release. Importantly, PLGA concentration, solvent and non-solvent ratio, solidification solvent volume, and solidification speed were found to significantly affect the properties of the obtained microspheres. The optimal microspheres present 50–100 μm spherical-shaped particles with remarkably high drug loading and EE. The in vitro drug release of these microspheres exhibit a delayed-release manner, starting to release drug at the third week and displaying approximately 20% drug release at day 28. Fourier transform infrared spectroscopy and differential scanning calorimetry results show that triptorelin acetate slightly interacted with PLGA, indicating that the drug was successfully encapsulated into PLGA microspheres. The drug content in the microspheres had no significant change after the 12-month storage at 4 °C, suggesting their excellent long-term stability. In conclusion, novel triptorelin acetate-loaded PLGA microspheres have been achieved via the L/O/O phase separation method to effectively improve the EE and reduce the initial burst release.

CAS / MDL: 142-82-5
研究领域: 药剂学 · 生物医学工程
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Biodegradable cellulose scaffolds embedding kartogenin-loaded microspheres for cartilage regeneration

Xinding Yu,Jian Wang,Shenglai Zhou,Peng Pan,Tiantian Chen,Xi Wang,Wentao Liu

Due to the extreme difficulty of cartilage, we endeavored to fabricate a novel biodegradable scaffold using natural polysaccharide cellulose and poly(lactic- co -glycolic acid) (PLGA) microspheres incorporating controllably released the cartilage inducer kartogenin (KGN) for enhancing regenerative healing in cartilage tissue. Initially, to facilitate the loading of KGN, PLGA/KGN microspheres were fabricated using the solvent volatilization method. These microspheres exhibited high sphericity, with particle sizes diminishing from 12.11 to 3.27 μm as the emulsification rate increased. Demonstrating adequate encapsulation efficiency, the microspheres enabled controlled drug release, positively influencing cell migration and recruitment. Subsequently, a biodegradable cellulose composite scaffold loaded with PLGA/KGN microspheres was prepared using the freeze-drying method. Compared with pure MCC scaffolds, composite scaffolds had a lower degradation rate, and the incorporation of microspheres promoted cell proliferation and significantly elevated expression of cartilage-related specific genes. In a rat cartilage defect model, it was further demonstrated that the composite scaffold combined with stem cell implantation achieved an optimal repair effect, characterized by vigorous extracellular matrix secretion and increased maturity of the regenerated cartilage tissues, suggesting potential clinical application value as a novel articular cartilage repair product in the future.

CAS / MDL: 9002-89-5
研究领域: 组织工程学 · 再生医学 · 材料科学
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Advanced Composites and Hybrid Materials · 2025 ·Vol. 8 ·期 2 ·1-17 · IF 21.8

Glutamic acid-loaded separable microneedle composite for long-acting hair regeneration treatment

Mbituyimana Bricard,Fu Lina,Wang Hao,Qi Fuyu,Jiang Yuchi,Meng Fanbo,Wu Min,Shi Zhijun,Yang Guang

Androgenetic alopecia (AGA) is the most common type of hair loss frequently observed in clinics. Right now, there are no effective treatments for AGA. Here, we developed a biodegradable microneedle (MN) patch made of polylactic-co-glycolic acid (PLGA) loaded with glutamic acid (GA) that improves sustainable drug release and effective hair regeneration treatment. Once the patch has penetrated the skin, the GA-loaded MNs (GA-MNs) are quickly separated from their base and enter the skin. These MNs then serve as drug storage tanks inside the skin, releasing the therapeutics gradually for over 4 weeks. The sustained release of GA from long-acting biodegradable needles could lead to endocytosis by dermal papilla cells (DPCs), promoting the proliferation of cells. Compared with topical minoxidil, which requires daily treatment, animal studies have shown that GA-MNs can increase hair regeneration more effectively with lower dose frequency; the number of hair follicles in the GA-MNs group reached 83.68 ± 4.52%, which was significantly higher than that of the minoxidil group (56.93 ± 3.21%). This transdermal technology of biodegradable MNs shows considerable promise in clinical applications and offers a straightforward, safe, and effective therapy approach for clinical hair regeneration treatment.

CAS / MDL: 38304-91-5
研究领域: 生物医学工程 · 皮肤病学 · 药物递送系统
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Journal of the Mechanical Behavior of Biomedical Materials · 2026 · IF 4.1

Biomimetic PLGA nanofiber scaffolds: Crystallization-driven mechanical reinforcement and degradation kinetics analysis

Jinlong Zhu,Shuqiang Liu,Mengjiao Ji,Rui Sun,Yanan Yao,Lei Shao,Man Zhang,Gaihong Wu,Pengyu Yan,Lu Jia,Yujing Zhang

Balancing mechanical fatigue resistance with precise degradation kinetics remains a pivotal challenge in the engineering of biodegradable polymeric scaffolds. Herein, we fabricated biomimetic tubular scaffolds via sequential electrospinning, systematically modulating the physicochemical properties of poly(lactic-co-glycolic acid) (PLGA) by tailoring the lactide/glycolide monomer ratios. By optimizing the sacrificial layer protocol and collector rotation speed, a defect-free nanofibrous network mimicking the natural extracellular matrix (ECM) was constructed. Structural characterization using XRD and DSC revealed that optimizing the lactide content to a 7:3 ratio triggered a critical phase transition from an amorphous to a semi-crystalline state. This crystallization-driven microstructural evolution endowed the scaffold with superior radial compression resilience and effectively recapitulated the “fiber-bridging" toughening mechanism of natural lotus stems. Degradation kinetics analysis in artificial urine demonstrated that the semi-crystalline scaffold exhibited a diffusion-limited bulk erosion profile with mitigated autocatalysis, maintaining mechanical integrity for over four weeks. Furthermore, the optimized surface wettability and topological cues significantly fostered fibroblast adhesion and proliferation. Collectively, this study elucidates the structure-property relationships of electrospun PLGA nanofibers, offering a robust strategy for designing mechanically durable and degradation-tunable biomaterials.

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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2026 · IF 6

Enzyme-powered PLGA micromotors for biofilm eradication and long-term regrowth inhibition

Jiawei Hou,Zihao Huang,Xiao Jia,Jiamin Wang,Kaihui Xu,Xingyuan Fang,Yingling Zheng,Mai Qiao,Hao Yuan,Tao Meng

Pickering emulsion-templated method fabricates enzyme-powered, drug-loaded asymmetric PLGA micromotors. • Clear-and-inhibit dual action: enzymatic propulsion disrupts biofilm; PLGA degradation releases drug for sustained inhibition. • Biocompatible micromotors provide long-term antibacterial activity and suppress biofilm regrowth for days. • Integrated platform offers a new strategy for eradication and prevention of recurrent biofilm infections. Bacterial biofilms are dense structures composed of microbial communities and their extracellular polymeric substances (EPS), posing severe challenges in the field of biomedical engineering. These EPS matrices form a “mucus protective barrier”, endowing biofilms with robust resistance to antibiotics, biocides and immune responses. Conventional eradication strategies such as disinfectants and enzymatic cleaners have inherent limitations including easy induction of microbial drug resistance, failure to penetrate the EPS barrier, and inability to prevent the rapid regeneration of biofilms. In this study, a fully biodegradable enzyme-driven PLGA micromotors (PLGA MMs) system was developed via a hydroxyapatite (HAP)-stabilized oil-in-water Pickering emulsion templating method, with azithromycin (AZM) and catalase (CAT) encapsulated within the PLGA matrix. The micromotors achieve deep biofilm penetration by virtue of catalase-driven propulsive force, while the biodegradable PLGA matrix enables the sustained release of AZM for several weeks, effectively eliminating residual bacteria and inhibiting biofilm regeneration. Experimental results demonstrated that the PLGA MMs could efficiently eradicate Staphylococcus aureus biofilms (with only 3.2% residual biofilm biomass remaining), kill residual bacteria within the biofilms (with a bacterial survival rate of merely 2.3%), and completely inhibit biofilm regrowth for up to 14 days. Furthermore, the PLGA MMs exhibited favorable biocompatibility (with a CAT activity retention rate of > 88.98% and a hemolysis rate of < 5%). This synergistic “disruption-sustained inhibition” strategy provides a novel and translationally promising platform for combating recalcitrant biofilm infections. Schematic diagrams of the preparation of PLGA micromotors (a), disruption of Staphylococcus aureus biofilms (b), and inhibition of biofilm reconstitution (c) Download: Download high-res image (165KB) Download: Download full-size image

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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2020 · IF 2.365

Odorranalectin modified PEG–PLGA/PEG–PBLG curcumin-loaded nanoparticle for intranasal administration

Xinrui Li,Jing Su,Zul Kamal,Pengcheng Guo,Xinyi Wu,Lina Lu,Hongbing Wu,Mingfeng Qiu

Curcumin (Cur) is a promising drug for neurological diseases. Nevertheless, the application of Cur has been limited due to its difficulty in penetrating blood-brain barrier (BBB). Intranasal drug delivery, a noninvasive alternative delivery of Cur, can effectively help Cur cross BBB and inert into central nervous system directly. Odorranalectin (OL) which is the smallest lectin can prolong the residence time of Cur in the nasal mucosa and promote cellular uptake. In this work, a nasal delivery system incorporating OL modified Cur-loaded nanoparticles (Cur–OL–NPs) was developed and expected to bypass BBB and promote the absorption of Cur. We conjugated OL to polyethylene glycol-poly (lactic-co-glycolic acid) (PEG–PLGA), and combined polyethylene glycol-poly (γ-benzyl-L-glutamate) (PEG–PBLG) and OL–PEG–PLGA to prepare nanoparticles to improve the stability, bioavailability and targeting of Cur. Compared with unmodified NPs, increased efficiency of Cur–OL–NPs cellular uptake by Calu-3 cells had been obtained with no severe toxicity. Furthermore, in vivo pharmacokinetic studies also showed that Cur–OL–NPs had higher relative bioavailability. Thus, it is concluded that the results indicated that OL–NPs as carriers of Cur had a promising future in nasal drug delivery system.

CAS / MDL: 302-95-4
研究领域: 药剂学 · 神经科学 · 生物材料学
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MATERIALS & DESIGN · 2019 · IF 5.77

Three-dimensional printed electrospun fiber-based scaffold for cartilage regeneration

Weiming Chen,Yong Xu,Yanqun Liu,Zongxin Wang,Yaqiang Li,Gening Jiang,Xiumei Mo,Guangdong Zhou

The fabrication of three-dimensional (3D) electrospun fibrous scaffolds with customizable shapes and large pores is a challenging task. In this study, for the first time, one-dimensional (1D) gelatin/poly (lactic- co -glycolic acid) (PLGA) electrospun fibers were processed into inks suitable for 3D printing. By combining 3D printing and freeze drying, electrospun fiber-based inks were successfully fabricated into 3D-printed scaffolds (3DP) with precisely controlled shapes and large pores, in addition to fibrous surface morphologies similar to that of a native extracellular matrix (ECM). The 3DP exhibited good elasticity and water-induced shape memory, and was found to be superior to 3D-printed scaffolds fabricated using pure gelatin fibers and freeze-shaped scaffolds fabricated using non-fibrous gelatin/PLGA powder. Moreover, 3DP combined with chondrocytes achieved satisfactory cartilage regeneration in vivo . The novel strategy of 3D printing electrospun fibers established in this study provides a research model for the design and fabrication of multiple scaffolds for various tissue regeneration applications.

研究领域: 生物材料学 · 组织工程学
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POLYMER INTERNATIONAL · 2021 ·Vol. 70 ·期 9 ·1396-1403 · IF 2.99

Release behaviors and kinetics of coated bead-on-string nanofibrous multilayer membranes loaded with drug particles

Tingxiao Li,Yifan Huang,Lei Wang,Binjie Xin

A bead-on-string structure with special beads at the microscale level could act as an effective carrier for solid drug particles as well as giving a continuous and sustained release profile. Tetracycline hydrochloride (TCH), used as solid model drug particles, was ground to obtain nanoscale and well-distributed size. Electrospun poly[lactic- co -(glycolic acid)] (PLGA) bead-on-string nanofibers loaded with TCH of different particle sizes were fabricated for controlled drug delivery. The morphology of TCH particles and bead-on-string nanofibers were observed using a particle sizer and scanning electron microscopy. The effects of drug particle size on the release behaviors of nanofibers were further investigated and analyzed using UV–visible spectrophotometry. In vitro release results suggested that bead-on-string nanofibers encapsulating ground TCH particles had higher total drug release quantity compared with unground particle-loaded nanofibers. Coating of the surface of PLGA/TCH nanofibers was investigated for controlled-release effects and the release mechanism to understand the drug–polymer carrier interaction. The results indicated that coating on both sides of nanofibrous membranes could effectively decrease the initial burst release. Bead-on-string nanofibers proved to be promising mats for drug delivery applications. © 2021 Society of Industrial Chemistry.

研究领域: 生物材料学 · 药剂学
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Science Advances · 2024 ·Vol. 10 ·期 10 · IF 11.7

Engineered MgO nanoparticles for cartilage-bone synergistic therapy

Liming Zheng,Sheng Zhao,Yixuan Li,Jiankun Xu,Wenjin Yan,Baosheng Guo,Jianbin Xu,Lifeng Jiang,Yifeng Zhang,Hui Wei,Qing Jiang

The emerging therapeutic strategies for osteoarthritis (OA) are shifting toward comprehensive approaches that target periarticular tissues, involving both cartilage and subchondral bone. This shift drives the development of single-component therapeutics capable of acting on multiple tissues and cells. Magnesium, an element essential for maintaining skeletal health, shows promise in treating OA. However, the precise effects of magnesium on cartilage and subchondral bone are not yet clear. Here, we investigated the therapeutic effect of Mg2+ on OA, unveiling its protective effects on both cartilage and bone at the cellular and animal levels. The beneficial effect on the cartilage-bone interaction is primarily mediated by the PI3K/AKT pathway. In addition, we developed poly(lactic-co-glycolic acid) (PLGA) microspheres loaded with nano-magnesium oxide modified with stearic acid (SA), MgO&SA@PLGA, for intra-articular injection. These microspheres demonstrated remarkable efficacy in alleviating OA in rat models, highlighting their translational potential in clinical applications.

研究领域: 医学 · 生物材料学 · 骨科
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Preparation and evaluation of oral insulin nanocapsule delivery systems

Meng Zhang,Chunxin Wang,Junqian Pan,Mengjie Wang,Haixin Cui,Xiang Zhao

Insulin therapy is essential for regulating blood sugar levels. Conventional subcutaneous injection is prone to psychological stress, local tissue damage and severe blood glucose fluctuations, and thus the development of oral insulin technology has become an alternative therapy. However, oral insulin faces challenges such as difficult absorption, poor adhesion, low bioavailability, and short duration of action, due to the large molecular weight, low permeability, and easily degradable by enzymes and gastric acids. In this study, oral insulin nanocapsule delivery systems (Orl-Ins-NPs) were developed by using polylactic acid- co -glycolic acid (PLGA) as the encapsulation material for insulin loading. After preparation, optimization and characterization, the mean size of Orl-Ins-NPs was 140.08 nm, the encapsulation efficiency of the system was 54.3 %, and the loading capacity of insulin was 2.2 %. In addition, cationic modification with chitosan/ polyethyleneimine promoted adhesion and permeation of the intestinal mucus layer, and surface coating with pH-responsive methyl methacrylate trimethylamine ethyl chloride copolymer achieved 100 % gastric protection. The results of rat blood glucose test showed that, subcutaneous injection of the control group reduced blood glucose concentrations within 1 h and returned to initial levels within 4 h, while Orl-Ins-NPs slowly reduced blood glucose concentration to 51.3 % of the initial level and maintains stability within 10 h. Orl-Ins-NPs exhibited good physicochemical stabilities, sustained release property, improved in vitro acid resistance, as well as long-term in vivo hypoglycemic effect. This system demonstrates its potential clinical application in oral insulin and other protein drugs delivery.

CAS / MDL: 865-49-6
研究领域: 药剂学 · 生物医学工程 · 糖尿病研究
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