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controlled release
EUROPEAN POLYMER JOURNAL · 2015 · IF 3.005

Thermo-sensitive drug controlled release PLA core/PNIPAM shell fibers fabricated using a combination of electrospinning and UV photo-polymerization

Hongwei Zhang,Qijian Niu,Ning Wang,Jun Nie,Guiping Ma

In this research a thermo-sensitive drug loaded core–shell fibers were prepared by UV photo-polymerization combined with electrospinning technology. The biodegradable polymer polylactic acid (PLA) was used as the core with electrospinning and the N-isopropylacrylamide (NIPAM) was selected to be shell of the fibers via UV photo-polymerization, respectively. Combretastatin A4 (CA4) was used as the model drug loaded in PLA (core structure) to test the thermo-sensitivity of the core–shell fibers. SEM was performed to observe the morphology of the fibers. TEM was carried out to confirm the core–shell structure of the fibers. Furthermore, XPS and FTIR results demonstrated that the core–shell structure had been fabricated as designed. Water contact angle (WCA) test indicated that the fibers show different wettability when the temperature was below or above the lower critical solution temperature (LCST). Moreover, in vitro drug release test was conducted to explore the difference of the drug release when the temperature was at 25   °C and 40   °C. The cell culture studies showed that the prepared core–shell structure nanofibers have a potential application in the biomedical fields as tissue engineering.

研究领域: 生物材料 · 药物递送 · 组织工程 · 高分子科学 · 纳米医学
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JOURNAL OF BIOACTIVE AND COMPATIBLE POLYMERS · 2015 · IF 2.352

Synthesis and characterization of β-cyclodextrin-conjugated alginate hydrogel for controlled release of hydrocortisone acetate in response to mechanical stimulation

Li Tan,Jingjing Li,Yang Liu,Huan Zhou,Zhiguo Zhang,Linhong Deng

Alginate hydrogels are a class of biomaterials that can be used as local release depots for therapeutic agents. A particular drug that can take advantage of alginate hydrogel for controlled release is hydrocortisone acetate. Hydrocortisone acetate is a widely used anti-inflammatory agent, but is limited in application due to poor solubility and lack of controlled delivery. To overcome this limitation, a mechanically responsive β-cyclodextrin-conjugated alginate (Alg-β-CD) hydrogel was synthesized and characterized for enhanced aqueous solubility and controlled release of hydrocortisone acetate. We demonstrated that mono-6-deoxy-6-ethylenediamine-β-cyclodextrin and hydrocortisone acetate formed a 1:1 inclusion complex, thus resulting in marked increase in hydrocortisone acetate solubility, while causing no significant inhibition to the growth of cultured mouse fibroblasts (L929). More importantly, the release of hydrocortisone acetate from the hydrogel system was increasingly sensitive to mechanical compression, and the mechanical responsiveness of hydrocortisone acetate release increased dramatically as the concentration of mono-6-deoxy-6-ethylenediamine-β-cyclodextrin increased from 0% to 46%, whereas the swelling rate and stiffness of the hydrogel decreased as the concentration of mono-6-deoxy-6-ethylenediamine-β-cyclodextrin increased. The mechanical responsiveness of hydrocortisone acetate release was attributable to conformational distortion of mono-6-deoxy-6-ethylenediamine-β-cyclodextrin moieties and deformation of the polymer network. Moreover, we demonstrated that the hydrogel continuously released and accumulated hydrocortisone acetate in the medium when compressed for up to 72 h, which led to increasing suppression of nitric oxide production in the lipopolysaccharide-stimulated mouse macrophages (RAW264.7), indicating desirable anti-inflammatory effect at the cell level. Hence, this hydrogel system may provide a useful platform for drug delivery, such as hydrocortisone acetate release to wound site, by intentionally generated mechanical force.

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VETERINARY JOURNAL · 2026 · IF 2.7

Overcoming Mirtazapine's Therapeutic Limitations in Veterinary Practice: Development of a Taste-masked Orally Disintegrating Tablet with Microsphere-based Controlled Release

Yitong Lu,Yajing Guo,Wanjin Ma,Yifan Li,Shun Wang,Zhiyong Wu

Anorexia is a clinically significant condition in companion animals, particularly cats, that disrupts metabolic homeostasis and impedes recovery from underlying diseases. Mirtazapine (MRZ), a commonly prescribed appetite stimulant in veterinary medicine, has limited clinical utility due to its intense bitterness and suboptimal bioavailability in conventional dosage forms. To address these limitations, we developed a novel drug delivery system integrating microencapsulation technology with an orally disintegrating tablet (ODT) formulation. Using an optimized emulsification-solvent diffusion method, we produced ethyl cellulose-based microspheres exhibiting high encapsulation efficiency (93.19 ± 0.71%), uniform particle size distribution (106.12 ± 1.49 μm), and pH-responsive drug release characteristics. Comprehensive physicochemical characterization confirmed the structural integrity of the microspheres and the absence of detrimental drug-polymer interactions. Furthermore, the ODT formulation exhibited excellent pharmaceutical properties, including rapid disintegration and complete drug release under gastric conditions, and effective masking of MRZ's bitter taste in the oral cavity. In vivo evaluations revealed significantly improved palatability (p < 0.05) and preliminary evidence of appetite stimulation (p < 0.05) compared with conventional formulations, supporting further clinical development. Stability studies indicated robustness under standard storage conditions. This advanced delivery system successfully overcomes the major limitations of current MRZ therapies, offering a promising solution for enhancing treatment compliance and therapeutic outcomes in veterinary practice. Moreover, the developed technology platform provides valuable insights for formulating other challenging active pharmaceutical ingredients requiring taste masking and controlled release.

✓ 已验证 DOI PubMed 高影响因子
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Current Research in Food Science · 2026 · IF 7.7

A Universal "Divide-and-Conquer, Precise Reconstruction" Strategy: Multiscale Simulation-Guided High-Fidelity Restoration and Controlled Release of Rose Aroma

Chenyu Liu,Qingzhao Shi,Yixuan Liu,Xiujuan Xu,Shan Wang,Wu Fan,Weihong Qiao,Guobi Chai,Qidong Zhang

The high-fidelity encapsulation and controlled release of natural aromas remain significant challenges in flavor science due to the compositional complexity of essential oils and heterogeneous host–guest interactions in conventional co-inclusion systems. Using rose aroma as a representative model, this study presents a "divide-and-conquer, precise reconstruction" strategy that integrates multiscale simulation with experimental validation. Seven key aroma-active compounds were screened through GC–MS combined with odor activity value (OAV) analysis. Their host–guest interactions with β-cyclodextrin (β-CD) were subsequently investigated using molecular docking, molecular dynamics simulations, and MM/PBSA free-energy calculations. The results suggest that hydrophobic interactions dominate the complexation process, and the calculated binding free energies (ΔG_bind: −1.67 to −7.34 kcal/mol) show semi-quantitative consistency with experimentally observed encapsulation behavior and release trends. Individual inclusion complexes (ICs) exhibited markedly improved thermal stability, with decomposition onset temperatures increasing by more than 150 °C compared with free compounds. Successful complex formation was confirmed through FTIR, XRD, and 1 H NMR characterization. Release kinetics analysis revealed compound-specific release behaviors governed by interaction strength and molecular compatibility with β-CD. Based on these differentiated release profiles, physical blending of individually prepared ICs enabled reconstruction of a headspace aroma composition highly consistent with that of the original rose extract, outperforming conventional co-inclusion under identical conditions. Beyond demonstrating a successful case for rose aroma, this work establishes a simulation-guided design framework integrating key component screening, interaction prediction, precise preparation, and release-controlled reconstruction. The proposed methodology provides a rational strategy that can potentially be extended to other complex natural aroma systems for the development of advanced flavor delivery system.

CAS / MDL: 60-12-8
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Current Research in Food Science · 2026 · IF 7.7

A novel strategy for controlled release of sialic acid based on W1/O/W2 emulsion microencapsulation for gut microbiota modulation

Donglei Zheng,Mengle Li,Ying Qian,Xiangsong Chen,Jianglin Chen,Long Jin,Lili Cao,Min Pang,Jiaying Huo

Sialic acid (Neu5Ac) possesses a wide range of bioactivities; however, its instability under acidic conditions prevents it from effectively reaching the intestine. This underscores the urgent need to develop a stable delivery system capable of protecting Neu5Ac from gastric degradation and achieving its controlled release in the intestine. To enhance the stability and achieve controlled release, Neu5Ac was encapsulated within water-in-oil-in-water (W1/O/W2) emulsion-based microcapsules in this work. S2 emulsions featured a “dual-chamber, tri-phase” structure, comprising a Neu5Ac-chitosan fluid gel (inner aqueous phase), maize oil (oil phase), and an external aqueous phase of 13% sodium starch octenyl succinate, 5% β-cyclodextrin, 1.5% sodium caseinate, and 0.5% carboxymethyl cellulose. Microstructural analyses confirmed spherical morphology with core-shell architecture and bimodal droplet distribution (1-10 μm). In addition, S2 emulsions exhibited an encapsulation efficiency (EE) of 92.44%, a zeta potential of −60.80 mV, a Sauter mean diameter (d 3 , 2 ) of 1.337 μm, shear-thinning behavior and weak gel network stability. S2 emulsions were spray-dried to obtain S2 microcapsules. S2 microcapsules exhibited an EE of 89.43% and a d 3 , 2 of 3.839 μm, while FT-IR and XRD verified physical encapsulation without covalent bonding. In vitro digestion, S2 microcapsules exhibited controlled release behavior during simulated intestinal digestion, with a Neu5Ac release rate of 85.61% after 120 min. In mice, microencapsulated Neu5Ac increased the relative abundance of Akkermansia , Lactobacillus , and Bifidobacterium . This system demonstrates promising potential for the co-delivery and controlled release of Neu5Ac, and shows great promise for expanding its applications in the food industry.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS · 2025 · IF 5.4

Palmitic acid modified liposomes as promising nanoplatform for encapsulation of bioactive peptides: Physicochemical, stability, controlled release and intestinal absorption analysis

Ruihan Huang,Hongdong Song,Sen Li,Song Miao,Xiao Guan

Despite the growing identification of food-derived bioactive peptides, their health-promoting effects are often hindered by low oral bioavailability. To address this challenge, we hypothesized that structural modification of liposomes with palmitic acid (PA) could enhance gastrointestinal stability and intestinal permeation to improve peptide bioavailability. Here, we successfully prepared the PA modified liposomes through thin-film hydration technique. The results demonstrated that PA was successfully inserted into the liposome membranes, meanwhile increased liposome size (from 139 nm to 146 nm) and enhanced surface charge (from −15 mV to −18 mV). Fourier transform infrared spectroscopy and fluorescence analysis revealed that PA improved the integrity of the phospholipid bilayer through hydrogen bond and electrostatic repulsion, thereby enhancing controlled release profile of liposomes in simulated digestive fluids. Storage stability tests demonstrated that while the liposomes effectively prevented peptide degradation, PA decreased liposome stability at lower temperatures. Importantly, PA-modified liposomes significantly enhanced intestinal permeation efficiency and promoted Caco-2 cellular uptake without inducing cytotoxicity (>90 % cell viability). Overall, the liposomes with PA modification provide an effective nano platform for improving the bioavailability of bioactive peptides

CAS / MDL: 38215-36-0
研究领域: 食品科学 · 纳米医学 · 药剂学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Dual-functional nanoengineered carrier for controlled release and enhanced intestinal translocation: Modulating lipid transporters to boost fucoxanthin anti-obesity efficacy

Yuanjie Guo,Jiabao Huang,Yu Luo,Yan Wang,Dan Li,Yixiang Liu

Obesity disrupts intestinal transporter function, limiting oral bioavailability and efficacy of anti-obesity bioactives. To overcome this challenge, the fucoidan-bovine serum albumin-palmitic acid (FA-BSA-PA) nanoparticles co-loaded with fucoxanthin (FUC) was engineered, leveraging PA's transporter-modulating function and FA-BSA's controlled release for nutrient-inspired delivery. In high-fat diet (HFD)-induced obese mice, FA-BSA-PA-FUC elicited significantly ( P  < 0.05) greater anti-obesity effects than free FUC at equivalent doses, markedly suppressing weight gain, improving blood lipid profiles, and ameliorating tissue histology. Crucially, these nanoparticles enhanced FUC absorption by upregulating scavenger receptor class B type 1 (SR-B1) and ATP-binding cassette transporter A1 (ABCA1) while suppressing P-glycoprotein (P-gp). This dual-action transporter modulation boosted FUC bioaccumulation 2.56-fold in the liver and 3.85-fold in epididymal adipose tissue. Furthermore, FA-BSA-PA-FUC profoundly ( P  < 0.05) regulated intestinal cholesterol metabolism: it inhibited Niemann-Pick C1-like 1 (NPC1L1)-mediated absorption (reducing jejunal and colonic NPC1L1 expression by 70 % and 45 %, respectively) and activated ATP-binding cassette transporter G5/G8 (ABCG5/G8)-mediated efflux (increasing jejunal ABCG5/G8 mRNA 7.65- and 7.73-fold). Consequently, fecal cholesterol excretion increased 2.26-fold and serum cholesterol clearance improved by 23.13 % versus the obese model group. This study demonstrates that functionalized delivery vehicles simultaneously promoting oral utilization of bioactive substances and inhibiting cholesterol absorption represent an effective strategy for obesity treatment.

CAS / MDL: 8049-47-6 9001-75-6
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF INDUSTRIAL AND ENGINEERING CHEMISTRY · 2022 · IF 6.76

A kind of core cross-linked “semi-amphiphilic” polymer assemblies for controlled release of corrosion inhibitors and autonomous corrosion alarm

Ying Cao,Aoqi Zhu,Jianmin He,Jianhua Wu,Mingjin Xue,Yiting Xu,Birong Zeng,Guorong Chen,Lizong Dai

A novel kind of core cross-linked assemblies formed from a “semi-amphiphilic” block copolymer, poly (syringaldehyde methacrylate)-block-poly (dopamine methacrylate-co-methyl methacrylate-co-styrene) (PSMA-b-P(DMA-co-MMA-co-St)), was designed and served as the carrier for anti-corrosive and corrosion detective molecules. Different from the core cross-linked micelles formed by the amphiphilic polymers in water, the core cross-linked assemblies in this research were formed from the “semi-amphiphilic” block copolymer, which took advantage of the different compatibility between epoxy and the blocks in the polymer, leading to the self-assembly behavior happening in the organic resin, while they shared the advantages of traditional core cross-linked micelles with the properties of being stable, stimuli-responsive and multifunctional. The pH-responsive properties of the assemblies and their complexation with Fe 3+ caused by the corrosion of the steel were confirmed by UV spectrophotometry and XPS analysis of the corrosive products. The controlled release of corrosion inhibitors was fully reflected by the expansion of the capacitor ring and the increase of the coating resistance (R c ) with the extension of the immersion time, which was got via fitting the electrochemical impedance spectroscopy (EIS) data with the equivalent electric circuits. Ultimately, the anti-corrosive mechanism of smart coating with the functional core cross-linked assemblies were also illustrated.

研究领域: 材料科学 · 腐蚀防护 · 高分子化学
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International Journal of Nanomedicine · 2021 · IF 6.4

Tumour-Targeted and Redox-Responsive Mesoporous Silica Nanoparticles for Controlled Release of Doxorubicin and an siRNA Against Metastatic Breast Cancer

Jialang Zhuang,Siqi Chen,Ye Hu,Fan Yang,Qin Huo,Ni Xie

Introduction Metastatic breast cancer seriously harms women’s health and is currently the tumour type with the highest mortality rate in women. Recently, the combinatorial therapeutic approaches that integrate anti-cancer drugs and genetic agents is an attractive and promising strategy for the treatment of metastatic breast cancer. Moreover, such a combination strategy requires better drug carriers that can effectively deliver the cargo to the breast cancer cells and achieve controlled release in the cells to achieve better therapeutic effects. Methods The tumour-targeted and redox-responsive mesoporous silica nanoparticles (MSNs) functionalised with DNA aptamers (AS1411) as a co-delivery system was developed and investigated for the potential against metastatic breast cancer. Doxorubicin (Dox) was loaded onto the MSNs, while AS1411 and a small interfering RNA (siTIE2) were employed as gatekeepers via attachment to the MSNs with redox-sensitive disulfide bonds. Results The controlled release of Dox and siTIE2 was associated with intracellular glutathione. AS1411 mediated the targeted delivery of Dox by increasing its cellular uptake in metastatic breast cancer, ultimately resulting in a lower IC50 in MDA-MB-231 cells (human breast cancer cell line with high metastatic potency), improved biodistribution in tumour-bearing mice, and enhanced in vivo anti-tumour effects. The in vitro cell migration/invasion assay and in vivo anti-metastatic study revealed synergism in the co-delivery system that suppresses cancer cell metastasis. Conclusion The tumour-targeted and redox-responsive MSN prepared in this study are promising for the effective delivery and controlled release of Dox and siTIE2 for improved treatment of metastatic breast cancer.

研究领域: 肿瘤学 · 药学 · 纳米技术 · 癌症治疗
✓ 已验证 DOI PubMed 高影响因子
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ACS Applied Materials & Interfaces · 2017 · IF 7.504

NIR Light-, Temperature-, pH-, and Redox-Responsive Polymer-Modified Reduced Graphene Oxide/Mesoporous Silica Sandwich-Like Nanocomposites for Controlled Release

Panjun Wang,Shuo Chen,Ziquan Cao,Guojie Wang

Here a novel quadruple-responsive nanocarrier based on reduced graphene oxide/mesoporous silica sandwich-like nanocomposites (rGO@MS) modified by pH- and temperature-responsive poly(N,N-dimethylaminoethyl methacrylate) (PDMAEMA) with a linker of disulfide was constructed via surface-initiated atom transfer radical polymerization. The polymer chains would be used as gatekeepers to control the release of the loaded cargo molecules under pH, temperature, NIR light and redox stimuli. The cargo molecules (rhodamine B) were demonstrated to release from the polymer-modified nanocomposites triggered by the quadruple-stimuli. It is noted that the release of the loaded rhodamine B from the nanocarriers could be enhanced greatly under the synergistic effect of multiple stimuli. The prepared quadruple-responsive polymer-modified nanocomposites show a bright prospect in the field of smart nanocarriers for controlled release.

研究领域: 材料科学 · 药物递送系统 · 生物医学工程
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Advanced Healthcare Materials · 2026 · IF 11

Silk Fibroin-Modified Metal Organic Framework Acid-Controlled Release Nanocarrier for Polyetheretherketone to Combat Implant-Associated Infections and Promote Angiogenesis

Yadi Su,Junqi Wang,Heyi Gong,Xiao Han,Yu Wang,Yue Liu,Wanqiu Chen,Sihan Ma,Jinghui Zhao

Polyetheretherketone (PEEK) has been regarded as a prospective alternative orthopedic implant, because of its elastic modulus approximately equal to human cortical bone. However, the poor antibacterial and angiogenic properties of bioinert PEEK have become a limitation to its clinical application. Therefore, a biomimetic metal organic framework acid-controlled release nanocarrier consisting of Zeolitic Imidazolate Framework-8 (ZIF-8) nanoparticles loaded with gentamicin and modified with silk fibroin nanospheres for PEEK implants is prepared. In this study, acidity-responsive PEEK implant can efficiently capture bacteria and eradicate bacterial biofilms, achieving antibacterial rates up to 99.9% against Staphylococcus aureus ( S. aureus ) and Escherichia coli ( E. coli ). Furthermore, acidity-responsive PEEK implant is expected to promote angiogenesis by assisting proliferation and migration of endothelial cells, thereby accelerating peri-implant tissue regeneration. By constructing subcutaneous infection models, it is further indicated that acidity-responsive implant can resist bacterial proliferation and facilitate peri-implant angiogenesis. In summary, this study provided an effective approach for the improvement of orthopedic implants that realized antibacterial and angiogenic effects, offering a potential solution for preventing infection and promoting angiogenesis during the early phase after implantation.

CAS / MDL: 62-31-7
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COLLOID AND POLYMER SCIENCE · 2026 · IF 2.9

ZIF@polymer monolith as small-caliber vascular prosthesis prototype based on controlled release of heparin and its application in sterilization

Zhou Lu,Yu Xiaozhou,Lyu Shuxiang,Liao Xiaoyuan,Li Zhen,Yao Yue,Zhang Haoling

A novel small-caliber vascular prosthesis prototype (SCVPs) with antibacterial application is proposed based on the controlled delivery of heparin from ZIF@polymer monolith. The traditional powdery small-caliber vascular prosthesis material has the disadvantages of difficult separation and easy agglomeration, which limits its applications. Heparin (HP)-loaded porous ZIF-8/Polymer (PEG, PVA, and PVP) monoliths were fabricated using a freeze-casting method in liquid nitrogen (− 196 ℃) for controlled heparin release and sterilization. The incorporation of ZIF-8/Polymer significantly improved the antibacterial performance of the samples, prolonged the slow-release time of heparin sodium, and also resulted in better mechanical properties. The samples synthesized at a heparin sodium concentration of 0.36 mg·mL −1 exhibited good sustained release of heparin sodium when used as artificial antigenic matrix. Among these materials, the cured HP@ZIF-8 sample had a retarded release time of up to 15 h, with a cumulative release of 223.56 μg at 24 h. With PVA as the optimal polymer, heavy metal ions from the cured HP@ZIF-8 material can cause severe toxic damage to the internal structure of bacteria, interfere with bacterial metabolism, and thus show obvious antibacterial effects.

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