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Materials Science & Engineering C-Materials for Biological Applications · 2017 · IF 4.164

Heparin modified graphene oxide for pH-sensitive sustained release of doxorubicin hydrochloride

Baomei Zhang,Xiaoye Yang,Yang Wang,Guangxi Zhai

A novel nanocarrier of heparin (Hep) modified graphene oxide (GO) was fabricated via a linker (adipic dihydrazide) and used as a pH-sensitive drug delivery system for controlling the release of anticancer drug doxorubicin (DOX) for anti-tumor therapy. The finally obtained nanocarrier was GO-ADH-Hep with better stability, blood compatibility and biocompatibility confirmed by the hemolytic test and in vitro cytotoxicity study. Its safety issue was greatly improved via Hep modification. The amount of DOX loaded onto GO-ADH-Hep was significantly high and dependent on pH value. The release rate of DOX from GO-   ADH-Hep/DOX was pH-sensitive and much-slower than that of free DOX solution suggesting the sustained drug-release capacity of this prepared nanocomplexes. In addition, the results of cytotoxicity study illustrated that this fabricated nanocomplexes displayed effective cytotoxicity to MCF-7 and HepG2 cells. What's more, the results of the in vivo pharmacokinetic study was also indicated that the GO-ADH-Hep/DOX nanocomplexes could significantly prolong the retention time of DOX in vivo and this was consistent with the in vitro drug release performance. And finally, according to the biodistribution study, DOX delivered by GO-ADH-Hep could reduce cardiotoxicity deriving from DOX solution and also decrease the pulmonary toxicity deriving from unmodified GO. Based on the in vitro and in vivo investigations, the fabricated GO-ADH-Hep could be a promising candidate as an ideal nano-carrier for drug delivery and anti-cancer therapy.

CAS / MDL: 7782-42-5
研究领域: 纳米技术 · 药学 · 生物医学工程 · 癌症研究
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AAPS PHARMSCITECH · 2023 ·Vol. 24 ·期 6 ·1-10 · IF 3.3

Transdermal Delivery of Estradiol Simultaneously Possessing Rapid Release and Sustained Release Effect

Tang XiaoFei,Qin Huaiying,Yang Jianhua,Zhang XiaoYun

Dissolving microneedle (DMN) has been researched as a drug delivery technology that improves drug molecule transportation through the skin with little discomfort. However, the sluggish drug absorption, poor skin dissolution, and lengthy time lags of DMN have limited its potential uses. The aim of this study was to design a novel DMN system for the administration of the poorly water-soluble drug, estradiol (E2), with fast skin penetration and a stable release rate for a long time. DMN containing E2 emulsion (E2-EM-DMN) and traditional DMN (T-DMN) were prepared. Rat skin was used for penetration test and guinea pig skin was used for skin irritation experiment. The drug release profiles and stability properties of these two kinds of DMNs were also investigated. High performance liquid chromatography was employed to determine the E2 content in DMN. The E2 concentration in rat plasma was achieved by a newly developed liquid chromatography-mass spectrometry method that was fast, reproducible, and specific. The height of E2-EM-DMN and T-DMN was 600 μm. The drug loading of the E2-EM-DMN and T-DMN was 667.30 ± 7.21 μg/patch and 672.56 ± 6.98 μg/patch. E2-EM-DMN possessed enough mechanical strength to penetrate the skin and caused no irritation to the skin. E2-EM-DMN could release the drug more rapidly and more continuously than T-DMN. E2-EM-DMN had good pharmaceutical stability. In summary, the E2-EM-DMN showed reliable quality and superior release performance. Emulsion-embedded DMN is an ideal transdermal delivery system for drugs. Graphical Abstract

CAS / MDL: 25322-68-3
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JOURNAL OF APPLIED POLYMER SCIENCE · 2023 ·Vol. 140 ·期 15 ·e53716 · IF 3

A pesticide sustained-release microcapsule from cellulose nanocrystal stabilized Pickering emulsion template

Cai-xia Yang,Jun Li,Yu-qing Zhang,Chao Wu,De-qiang Li

Efficient utilization of pesticides has presented various advantages in the ecological environment, food safety, and agricultural sustainability. Pesticide microcapsule could significantly improve the pesticide utilization ratio, and thus, we prepared a sustained-release microcapsule from cellulose nanocrystal (CNCs) stabilized Pickering emulsion template. The NaCl was added to overcome the strong electrostatic repulsion among CNCs for forming a stable oil-in-water (O/W) CNCs-based Pickering emulsion template, followed by crosslinking with hexamethylene diisocyanate on the interface. UV–vis and zeta-potential were used to characterize the as-prepared Pickering emulsion, and the stability and emulsion fraction were calculated. Results indicated that NaCl contributed to the stability of Pickering emulsion, even at a low concentration. The obtained CNCs-based microcapsule was characterized by FT-IR, XRD, SEM, TG-DTG, and three-phase contact angles. The microcapsule presented an encapsulation efficiency of 96.76% and sustained release of the imidacloprid for more than 82 h. Results indicated the potential for loading and sustained release of imidacloprid, which is beneficial to the environment, food, and agriculture.

CAS / MDL: 822-06-0 138261-41-3
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Materials Today Communications · 2022 · IF 3.662

Solid particles surface-modified with beta-cyclodextrin for sustained release of flavor

Yipeng Zhang,Jianping Zhang,Zechun Liu,Yanjun Huang,Xiaopeng Xiong

Beta-cyclodextrin (β-CD) has promising applications in many fields based on its hydrophobic cavity at the central of the cyclic molecule, which can form inclusion complex with specific molecule via a host-guest interaction. However, the water solubility of β-CD limits its application. Herein, attempts have been made to graft β-CD onto two kinds of solid particles while retaining the function of β-CD, so as to expand its application. First, SiO 2 nanoparticles were modified with silane coupling agent KH-560 to offer epoxy groups. Then, the epoxy groups of the modified SiO 2 and the hydroxyl groups of β-CD were simultaneously esterified by a dicarboxylic acid of succinic acid in a non-toxic solvent medium to obtain the β-CD modified SiO 2 (SiO 2 @β-CD). On the other hand, microcrystalline cellulose (MCC) particles were also modified with β-CD (MCC@β-CD) through co-esterification of their hydroxyl groups with succinic acid. The syntheses were monitored by Fourier transform infrared (FT-IR) spectroscopy, and the obtained materials were characterized by X-ray diffraction (XRD), thermogravimetric analysis (TGA) and scanning electron microscopy (SEM). The degrees of β-CD modification for the particles have been measured and analyzed to optimize the synthesis conditions. The results indicate that the degree of β-CD modification for the SiO 2 @β-CD is relatively low, but the material exhibits over 60 ºC elevation of the thermal stability. In comparison, the degree of β-CD modification for MCC@β-CD reached as high as 422 mg/g. Due to the much higher content of β-CD, the synthesized MCC@β-CD was employed to load a flavor compound of D -limonene, and its sustained release was investigated to suggest the potential of the β-CD modified particles.

CAS / MDL: 2530-83-8 77-09-8
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Journal of Advanced Research · 2020 · IF 6.992

Preparation of biological sustained-release nanocapsules and explore on algae-killing properties

Jinyun Li,Ming Guo,Yiping Wang,Bihuan Ye,Youwu Chen,Xuejuan Yang

Introduction Green algae seriously affect the quality and yield of Torreya grandis, it is important to explore new, environmentally friendly ways to control it. Objectives The present study aimed at preparing sustained-release algae-killing nanocapsules without pollution to the environment. Methods In this work, sodium carboxymethylcellulose (CMC), sodium alginate (SA), and chitosan (CTS) were used as raw materials in acylation reaction with the photosensitive catalytic material iron octaaminophthalocyanine (T) to generate the photoactive bio-based materials T-CMC, T-SA, and T-CMCS. Cinnamaldehyde and 2-aminobenzimidazole were combined using chemical grafting to produce a new algicide, and then formed nanocapsules by phase separation. The molecular structure of products was characterized by UV–Vis, FTIR, and NMR ( 1 H NMR, 13 C NMR). The particle size of the nanocapsules was determined by Zeta particle size analysis and TEM; DSC was used to investigate the thermal stability; The encapsulation efficiency and sustained-release performance were determined by HPLC. Then the phytotoxic of the new algicide was measured. Results The bio-based nanocapsules was successfully synthesized, which had a particle size of 10–30 nm and was stable at 40 °C. The encapsulation efficiency of the nanocapsules was 48.77%, the cumulative release rate was 83%, and the new algicide killed the green algae in a dose-dependent way. Conclusions The bio-based nano capsule is a new and valuable Sustained-release capsule, which is the method of green algae.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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RSC Advances · 2022 ·Vol. 12 ·期 26 ·16444-16453 · IF 4.036

A sustained-release Trametinib bio-multifunction hydrogel inhibits orthodontically induced inflammatory root resorption

Hang Yu,Zhina Wu,Xingfu Bao,Xiaoduo Tang,Junhu Zhang,Yi Zhang,Min Hu

Orthodontic tooth movement (OTM) is a bone reconstruction process. In most cases, OTM could induce root resorption as a common side effect, called orthodontically induced inflammatory root resorption (OIIRR). OIIRR affects tooth health and interferes with the stability of orthodontic treatment. Osteoclasts, which perform bone resorption in OTM, attack cementum, causing OIIRR. Many signaling pathways are involved in the maturation and differentiation of osteoclasts, among which the ERK1/2 is one of the important pathways. In this experiment, we added Trametinib (Tra), a specific inhibitor of ERK1/2, to catechol-modified chitosan (CHI-C) and oxidized dextran (ODex) to form a CCOD–Trametinib composite hydrogel (CCOD–Tra) to prevent OIIRR. CCOD–Tra exhibited good biocompatibility, injectability, strong adhesion, good hemostatic function and sustained release of Tra. We performed local injection of CCOD–Tra into the periodontal tissues of rats. CCOD–Tra firmly adhered to the periodontal tissues and then released Tra to establish a good biological environment and maintain a drug concentration at a high level around the roots for a long time. H&E, TRAP, immunochemistry staining and micro-CT indicated that CCOD–Tra had a good effect in terms of preventing OIIRR. Cell experiments showed that CCOD–Tra reduced the expression of TRAP, MMP-9 and C-FOS in osteoclast cells through the ERK1/2 signaling pathway to inhibit the differentiation and maturation of osteoclasts. Based on the above results, we concluded that CCOD–Tra had the ability to prevent OIIRR, the high adhesion and injectability of CCOD may provide better therapeutic ideas for clinical prevention of OIIRR.

研究领域: 牙科学 · 药学 · 生物材料 · 组织工程
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2026 · IF 2.6

Microfluidic-based intra-articular sustained release of triamcinolone acetonide microsphere-gel composite system

Yuan Zhu,Yongqi Lv,Jiaqi Xu,Yingshu Feng,Caleb Kesse Firempong,Runfeng Wang,Haibing He,Guoqing Zhang,Hongfei Liu

Objective This study presents a novel injectable microsphere-gel system for sustained intra-articular delivery of triamcinolone acetonide (TA) to treat osteoarthritis.Significance This system aims to overcome the shortcomings of conventional TA suspensions, such as short joint residence time and significant systemic exposure, thereby improving therapeutic efficacy and safety for osteoarthritis treatment.Methods TA-loaded polycaprolactone (PCL) microspheres (TA@PCL) were prepared using microfluidic technology under optimized conditions. The TA@PCL microspheres were incorporated into the cross-linked hyaluronic acid (CLHA) gel matrix to form an injectable composite (TA@PCL@CLHA), which was evaluated by in vitro studies (rheological property, stability, and drug release) and in vivo studies (plasma pharmacokinetics and drug retention in knee joints).Results TA@PCL microspheres with uniform size (D50 value of 61.4 ± 1.9 µm, span value of 0.075) and high encapsulation efficiency (87.2 ± 4.1%) were successfully prepared. The TA@PCL@CLHA composite exhibited excellent injectability (extrusion force of 12.1 ± 0.4 N) and physical stability over 90 days. In vitro, the CLHA gel effectively mitigated the initial burst release and provided a more sustained TA release profile over one month. In vivo evaluation in rabbits demonstrated that TA@PCL@CLHA significantly reduced the peak plasma concentration (Cmax reduced by approximately 65%) and decreased systemic exposure (AUC0-∞ reduced by about 49%), while maintaining detectable drug levels in the synovial fluid for at least 30 days.Conclusion The TA@PCL@CLHA microsphere-gel composite provides an effective local drug delivery system with minimized systemic exposure, offering a promising strategy for OA treatment.

CAS / MDL: 2425-79-8
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FOOD CHEMISTRY · 2026 · IF 9.8

Anthocyanins-quercetin copigmentation enhances liposomal encapsulation: Mechanisms, bilayer interactions, and sustained release performance

Bowen Luo,Xiang Li,Xiuyu Jiang,Jianwei Liu,Huiji Zhou,Bo Wang,Benu Adhikari,Xianwu Peng,Wanping Zhang,Zijia Zhang

Conventional liposome preparation techniques often show poor encapsulation efficiency (EE) for hydrophilic compounds. In this study, copigmentation was employed as a hydrophobic modification strategy to improve the liposomal delivery of anthocyanins (ACNs). ACNs formed stable copigmentation complexes with quercetin (QTI), primarily through π–π stacking and hydrophobic interactions. These interactions enhanced the hydrophobicity of ACNs and promoted their redistribution from the aqueous phase toward the bilayer interfacial region. Liposomes prepared by the polyol dilution method encapsulated ACNs@QTI complexes more efficiently than free ACNs, achieving an EE of 81.5 ± 0.6% and a particle size of 166.4 ± 7.9 nm. FTIR, DSC, and fluorescence analyses confirmed stronger interactions between ACNs@QTI complexes and phospholipid membranes, while in-vitro release experiments demonstrated its superior sustained-release performance. These findings highlight copigmentation as a practical non-covalent strategy to enhance liposomal encapsulation of hydrophilic bioactives, offering a basis for enhancing the stability and delivery of ACNs and other water-soluble compounds in food and pharmaceutical applications.

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Drug Delivery and Translational Research · 2021 ·Vol. 12 ·期 3 ·589-602 · IF 4.617

Preparation of olmesartan medoxomil solid dispersion with sustained release performance by mechanochemical technology

Zhang Qihong,Feng Zongmiao,Ren Wei,Zhao Yunchun,Dushkin Alexandr V.,Su Weike

Hypertension is a common disease for human with high morbidity and mortality, and olmesartan medoxomil (OM) is widely used in the therapy of hypertension. However, poor water solubility and low bioavailability limit its widespread use. To improve the effect of OM, a ternary OM solid dispersion consisting of hydroxypropyl- β -cyclodextrin (HP- β- CD) and hydroxypropyl methylcellulose (HPMC) was prepared by mechanochemical method. The best preparation parameters were OM/HP- β -CD/HPMC-E5 with mass ratio of 1:2.6:1 and milling time of 4 h. Under the optimal preparation conditions, the solubility of the ternary solid dispersion could be increased by 12 times as compared with pure OM. Due to the addition of HPMC-E5, the solid dispersion had sustained release performance with prolonged release time of 12 h. Furthermore, in vivo study demonstrated that the prepared solid dispersion could afford significantly improved bioavailability of ~ 3-fold in comparison with pure drug. Hence, the prepared ternary solid dispersion of OM may be a promise delivery system for clinical application. Graphical abstract

研究领域: 药剂学 · 高血压治疗 · 药物递送系统
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JOURNAL OF CLUSTER SCIENCE · 2023 ·Vol. 35 ·期 2 ·419-428 · IF 2.8

Preparation and Characterization of Titanium Oxide Nanocapsules Containing Retinoic Acid for Sustained Release

Yu Xuecheng,Zhao Yunhe,Chen Gang,Yu Jing,Wang Ruolan,Deng Yuhao,Wang Xiaoying,Yuan Xinru,Yu Xue-Feng,He Rui

Retinoic acid (RA) is widely used in cosmetics and medicine. However, high concentrations of RA may cause adverse effects, and carcinogenic substances can be generated by light degradation. Herein, a convenient and eco-friendly method was developed to achieve the sustained release of RA by TiO 2 nanocapsules. The surface morphologies, crystalline properties, and chemical structures were studied by SEM, XRD, FT-IR, NMR. The particle size is ~ 200 nm. The synthesis conditions, photostability and biological properties were also investigated. The XRD results indicated that the low crystallinity of anatase TiO 2 shell contributed to the sustained release of inner RA. The sustained release properties were investigated by the elution process. It confirmed that the RA was encapsulated in the TiO 2 shell with loose structures. Light irradiation experiments showed that the irradiation time was extended from ~ 30 s to ~ 120 s when the concentration of residual RA was reduced to half under the same conditions. This showed that inner RA was well protected and continuously released. The RA-TiO 2 nanocapsules showed good dispersion in water and oil phases, sustained release properties, extended effect time, long-acting antibacterial properties and photostability.

研究领域: 纳米技术 · 药学 · 材料科学 · 生物医学工程
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COLLOID AND POLYMER SCIENCE · 2024 ·Vol. 302 ·期 5 ·819-828 · IF 2.2

Molecularly imprinted polymers based on attapulgite and sustained-release properties for 5-FU

Ji Xinyuan,Yang Zhe,Fang Jiahui,Hu Sheng

In this study, a novel molecularly imprinted polymer (MIP) was synthesized with attapulgite (ATP) and acrylamide (AM) and ethyl methacrylate (MMA) for controlled release carrier of 5-fluorouracil (5-FU). The MIPs (PAM-PMMA) were characterized by XRD, FESEM, HRTEM, and FTIR. The drug loading and in vitro controlled release ability of MIP on 5-FU was investigated by adsorption property analysis and in vitro release analysis. MIPs (PAM-PMMA) reached a maximum drug loading of 12 mg/g and a maximum release of 80% at an ATP dosage of 0.2 g (0.4%), an initial concentration of 5-FU of 100 mg/L, and an adsorption time of 240 min. Cytotoxicity analysis showed that the maximum inhibition of cells could reach 25% at 72 h of cell culture time under the above conditions. The results showed that MIPs synthesized with ATP as the substrate and AM and MMA as the functional monomers were successfully synthesized and could be used as a drug delivery system for 5-FU. Graphical

研究领域: 材料科学 · 高分子科学 · 药剂学 · 纳米技术
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ChemistrySelect · 2026 ·Vol. 11 ·期 11 ·e05338 · IF 2.3

Study on Magadiite/Carvedilol Composite as Well as Its Sustained Release of Carvedilol

Fang Guo,Xuling Weng,Wanyun Feng,Yu Zhong,Xiaoqiang shang,Yufeng Chen

To mitigate the side effects of carvedilol (CV) caused by excessive dosage in cardiovascular disease treatment, a sustained-release of drug from delivery system is required. Magadiite is recognized as a promising carrier for CV due to its advantages. For this reason, a drug delivery system based on magadiite for CV (labeled Mag-CV) has been constructed by protonation of Na-magadiite (Na-Mag), Tetrabutylammonium ion (TBA+)-intercalation, and multi-step ion exchanges. Compositional and structural analyses revealed that Na-magadiite was protonated to be H-magadiite (labeled as H-Mag), and TBA+ was successfully intercalated into the interlayers of H-Mag to obtain the intercalated Mag-TBA. After multiple-step ion exchanges, TBA+ in the Mag-TBA was fully replaced by the positively charged CV, resulting in Mag-CV. The loading capacity of Mag-CV for CV was about 30.9%. Drug release experiments revealed that the Mag-CV exhibited sustained release of drug either in phosphate buffer solution (PBS, pH = 7.40) or in HCl solution (pH = 1.35). Moreover, the drug release followed the Allometric model. These results imply that the magadiite may be a feasible carrier for control the dosage of CV by sustained release of drug. Graphical

CAS / MDL: 2052-49-5
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