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Drug Delivery and Translational Research · 2022 ·Vol. 13 ·期 1 ·9-17 · IF 5.671

Development and characterization of gastro-floating sustained-release capsule with improved bioavailability of levodopa

Yuan Hao,Zhang Zhengyu,Hu Liandong

In this study, a new gastro-floating sustained-release capsule (GFC) with levodopa (LD) and benserazide hydrochloride (BH) was successfully developed. GFCs were prepared by filling the LD and BH granules into hard capsules and coated with cellulose acetate (CA) solution as a controlled-release layer. The effects of formulation factors on the release of GFCs were conducted. The AUC 0~24 (µg h/mL) of LD were 69.31 ± 3.61 (μg h/mL) and 28.87 ± 2.58 (μg h/mL) and the C max were 7.84 ± 0.34 (μg/mL) and 9.21 ± 1.04 (μg/mL) in the GFCs and commercial tablets respectively. The relative bioavailability of LD was 267.55 ± 34.54%. Compared with commercial tablets, the pharmacokinetic study indicated that the developed GFCs provided a better sustained-release effect and higher bioavailability than commercial tablets. Graphical abstract

CAS / MDL: 77-94-1
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ChemistrySelect · 2022 ·Vol. 7 ·期 30 ·e202200670 · IF 2.307

Preparation of Nanostructured Graphene Oxide and Its Application in Drug Loading and Sustained Release

Dongsheng Fu,Jinhui You,Ruijie Guo,Jie Zhang,Qiang Li,Jing Wen,Huifang Wang,Hong Yan

Graphical Nanostructured graphene oxide (GO) with long-range ordered lamellar or hexagonal structure were prepared by lyotropic liquid crystals (LLCs) templating strategy and used as anticancer drug carriers. Graphene oxide (GO) and its derivatives are considered as a promising drug carrier in tumor therapy due to their excellent biocompatibility. Here, a series of nanostructured GO with long-range ordered lamellar or hexagonal structure were prepared by lyotropic liquid crystals (LLCs) templating strategy and used as drug carriers. The nanostructure was verified via polarized-light optical microscopy (POM), low angle X-ray diffraction (XRD) and transmission electron microscopy (TEM), which showed that the interlayer spacing or pore size was determined by the carbon chain length of templating molecular. 5-fluorouracil (5-Fu), doxorubicin (DOX) and docetaxel (DOC) which had gradually increased molecular size were chosen as model drugs, and the highly ordered nanochannels can be used as space for adsorption and diffusion of drug molecules. Ultraviolet spectrometer and simulated release test in vitro were used to determine drug loading capacity and drug release performance. The results showed that larger pore diameter/layer spacing was beneficial to the adsorption and diffusion of drug molecules, especially those with shorter molecule size. Besides, the water-solvable DOX exhibited fast release rate than the hydrophobic 5-Fu and DOC. The in vitro cytotoxicity assay demonstrated the good biocompatibility of both the pristine GO and the nanostructured GO.

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CHEMICAL ENGINEERING JOURNAL · 2022 · IF 16.744

Butyryl chitosan: Synthesis, characterization and evaluation of the sustained release performance as tacrolimus carrier

Bo Zhu,Jie Shi,Huanchao Sun,Lixin Xia,Weisen Fang,Hongjian Li,Wanshun Liu,Baoqin Han

Chitosan and its water-soluble derivatives have been widely used in biomaterials, but their disadvantages have hindered their widespread application. In this study, butyryl chitosan, a liposoluble chitosan derivative, was prepared by introducing butyryl groups into chitosan molecules through an acylation reaction. The synthesis conditions were optimised, the reaction was more efficient and simpler than previously reported strategies. Two butyryl chitosan with degrees of substitution greater than two were synthesised. Chemical characterisations confirmed that the hydroxyl and primary amine groups in the backbone of chitosan were converted into amide and ester groups, respectively. The butyryl chitosan films have advantages such as high mechanical properties, long biodegradation time, proper surface charge, good cytocompatibility, and histocompatibility. Butyryl chitosan was used as carrier to prepare an implantable tacrolimus sustained release film. Characterization results showed that tacrolimus existed in an amorphous state in the release film. This work embodies an innovative formulation using tacrolimus-loaded carboxymethyl chitosan amorphous solid dispersions embedded butyryl chitosan film with added advantage of sustained release, an effective blood concentration in vivo for 11 days and a systemic exposure but lower intrapatient variability in tacrolimus trough levels. This work merits sustainable tacrolimus release use by providing application-based proofs and qualifies as a potential formulation for sustainable tacrolimus release system. We expect an improvement in terms of therapeutic compliance with positive effects on allograft outcomes.

CAS / MDL: 141-75-3 106-31-0
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ACS Applied Materials & Interfaces · 2023 · IF 9.5

Biobased Intelligent Food-Packaging Materials with Sustained-Release Antibacterial and Real-Time Monitoring Ability

Changchun Li,Jize Liu,Wanhe Li,Zhenghong Liu,Xin Yang,Bin Liang,Zhuo Huang,Xiaoyan Qiu,Xinkai Li,Kai Huang,Xinxing Zhang

It has been widely accepted that sustainable polymers derived from renewable resources are able to replace the short-turnover petroleum-based materials and reduce environmental impact in the future. However, their hydrophilic chemical structures rich with oxygen groups could lead to easy growth of bacteria, which greatly limit their applications in packaging materials. Here, we present an intelligent food-packaging material with sustained-release antibacterial and real-time monitoring ability based on totally biobased contents. In detail, sodium alginate with Artemisia argyi emission oil (encapsulated in gelatin–Arabic gum microcapsules) and citric acid-sourced pH-responsive carbon quantum dots (CQDs) are coated on bamboo cellulose papers. The obtained biobased composite material (almost 100% biocarbon content) with antibacterial ability is able to extend the shelf life of fresh shrimps and can be biodegraded. Moreover, owing to the introduction of CQDs, the composite can rapidly (within 1 s) detect slight pH variations (response pH ∼5, 10–9 mol/L of OH–) through an obvious color change (hue value from 305 to 355°). The developed strategy may open up new opportunities in the design of multifunctional biobased composites for intelligent applications.

CAS / MDL: 9005-38-3
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ACS Nano · 2023 · IF 17.1

Implantable Epigallocatechin Gallate Sustained-Release Nanofibers for the Prevention of Immobilization-Induced Muscle Atrophy

Renjie Tan,Ke Zhang,Yifan Si,Shuai Zhang,Jieqiong Yang,Jinlian Hu

Long-term immobilization of joints can lead to disuse atrophy of the muscles in the joints. Oral nutrients are used clinically for rehabilitation and therapeutic purposes, but bioavailability and targeting are limited. Here, we report tea polyphenols (dietary polyphenols), sustained-release nanofilms that release tea polyphenols through slow local degradation of core–shell nanofibers in muscles. This dietary polyphenol does not require gastrointestinal consumption and multiple doses and can directly remove inflammatory factors and superoxide generated in muscle tissue during joint fixation. The quality of muscles is increased by 30%, and muscle movement function is effectively improved. Although nanofibers need to be implanted into muscles, they can improve bacterial infections after joint surgery. To investigate the biological mechanism of this core–shell nanomembrane prevention, we conducted further transcriptomic studies on muscle, confirming that in addition to achieving antioxidation and anti-inflammation by inhibiting TNF-α and NF-κB signaling pathways, tea polyphenol core–shell nanofibers can also promote muscle formation by activating the p-Akt signaling pathway.

CAS / MDL: 9000-70-8 920-66-1
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JOURNAL OF POLYMERS AND THE ENVIRONMENT · 2024 · IF 4.7

Long-Acting Sustained-Release Hydrogel for Soil-Borne Pathogen Control in Chinese Herbal Medicine

Wang Xiaoyan,Xiang Shunyu,Wang Jing,Luo Xingyi,Du Changxue,Sun Xianchao

The Chinese herbal medicine industry plays a crucial role globally, providing traditional remedies and significantly contributing to healthcare. Disease prevention and control in Chinese herbal medicine face unique challenges distinct from conventional plant protection methods. The distinctive requirements for disease control add complexity to disease management, necessitating specialized approaches. In this study, we developed a bio-based hydrogel (CSA-gel) using a straightforward procedure designed for the sustained release of azoxystrobin for soil disinfection with the aim of preventing fungal diseases in Chinese herbal medicine. The synthesized hydrogel was characterized using FTIR, zeta potential measurement, cryo-TEM, SEM, and elemental analysis. CSA-gel demonstrated a release duration of azoxystrobin for over 14 days, maintaining high antifungal activity throughout the entire release period. Additionally, CSA-gel exhibited the ability to release a significant quantity of calcium ions during pesticide release, fostering plant growth and enhancing plant disease resistance. The use of CSA-gel is anticipated to decrease both how often and how much pesticide is needed, highlighting the significance of our research in improving sustainable disease control in traditional Chinese herbal medicine farming.

CAS / MDL: 9012-76-4 9005-38-3
研究领域: 植物病理学 · 农业科学 · 药用植物学
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ACS Biomaterials Science & Engineering · 2020 · IF 4.152

Tuning Microcapsule Shell Thickness and Structure with Silk Fibroin and Nanoparticles for Sustained Release

Yongfeng Wang,Qingqing Cheng,Jian Liu,Zeeshan Tariq,Zhaozhu Zheng,Gang Li,David L. Kaplan,Xiaoqin Wang

Microcapsules have attracted widespread interest for their unique properties in encapsulation, protection, and separation of active ingredients from the surrounding environment. However, microcapsule carriers with controllable shell thickness, permeability, good mechanical properties, and thermostability are challenging to obtain. Herein, robust and versatile composite microcapsules were fabricated using SiO2 nanoparticle-stabilized (Pickering) oil emulsions as core templates, while silk fibroin (SF) was assembled at the oil/water interface. This process resulted in the formation of physically and chemically stable microcapsules with a thick (∼800 nm) shell that protected the encapsulated ingredient from high shear forces and high temperatures during spray-drying. SiO2 nanoparticles were randomly distributed in the shell matrix after preparation, making the microcapsules mechanically robust (4.48 times higher than control samples prepared using surfactant Tween 80 instead of the SiO2 nanoparticles), as well as thermostable (retained shape to 900 °C). The microcapsules displayed tunable drug release by adjusting the SF content in the shell. Under optimal conditions (weight ratio of SiO2/SF = 7:10, corn oil content about 55 wt %), a model drug (curcumin) was encapsulated in the SF microcapsules with an encapsulation efficiency up to 95%. The in vitro drug release from these SF microcapsules lasted longer than control microcapsules, demonstrating the capability of these novel microcapsules in sustaining drug release.

CAS / MDL: 8001-30-7 115-95-7
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FUEL · 2021 · IF 6.609

Preparation and characteristics of sustained-release microcapsule-based inhibitory foam with high foaming ratio

Jian Qiao,Duan Zhao,Yan-Yun Zhao,Wei Lu,Miao-Miao Li,Xiang-Ming Hu,Yun-Tao Liang,Fu-Chao Tian,Shuang Ju,Bing-Rui Yan

To reduce the effect of conventional halogen salt inhibitors on the performance of foaming solutions and extend the fire prevention and suppression time of water-based foams, herein, microencapsulation technology has been used in the preparation of inhibitors. Calcium chloride sustained-release microcapsule with ethyl cellulose as wall material was successfully prepared by solvent evaporation method. The microcapsule complied with Higuchi release kinetics equation. The experiment showed that the foaming solution added with 20 g microcapsules had almost the same foaming capacity as the pure foaming solution, and the foaming multiple could reach 14 times, and the half-life of the foam could reach 123 min. The foaming multiple was much higher than the foaming multiple of calcium chloride foam (0 times). Compared with calcium chloride foam, the new type of foam prepared in this paper has better inhibition ability, and the inhibition rate is as high as 83.8%. Ethyl cellulose used as wall material in microcapsules can soften covered coal in the process of heating up, isolate coal and oxygen, and thus inhibit coal and oxygen binding. The experimental results show that the temperature of T1 (84.6℃), T3 (338.2℃) and the cross-point temperatures of the coal sample treated with the new type of foam are higher than that of the coal sample treated with the calcium chloride foam. At the same time, the new type of foam can significantly inhibit the oxidation rate of methyl and methylene. It can be seen that the microencapsulation technology can improve the ability of the inhibitor foam.

CAS / MDL: 9004-57-3
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JOURNAL OF BIOMATERIALS APPLICATIONS · 2018 · IF 2.082

3D printing mesoporous bioactive glass/sodium alginate/gelatin sustained release scaffolds for bone repair

Jingwen Wu,Guohou Miao,Zhichao Zheng,Zhengmao Li,Wen Ren,Caijuan Wu,Yuanjing Li,Zhu Huang,Lan Yang,Lvhua Guo

Drug delivery and release are a major challenge fabricating bone tissue engineering. In this study, we fabricated new sustained release hydrogel scaffolds composited of mesoporous bioactive glass, sodium alginate and gelatin by a three-dimensional printing technique. Naringin and calcitonin gene-related peptide were used as drugs to prepare drug-loaded scaffolds by direct printing or surface absorption. The physicochemical properties of the scaffolds and the drug release profiles of the two drug-loading models were investigated. We also examined the biocompatibility of the scaffolds, as well as the effect of the released medium on the proliferation and osteogenic differentiation of human osteoblast-like MG-63 cell. The results showed that the scaffolds had a high porosity (approximately 80%) with an interconnected cubic pore structure, rough surface morphology, bioactivity and strong biocompatibility. Furthermore, the naringin or calcitonin gene-related peptide co-printed into the scaffold displayed a steady sustained release behaviour for up to 21 days without an initial burst release, while both naringin and calcitonin gene-related peptide absorbed onto the surface of the scaffold were completely released within two days. MG-63 cells cultured with the extraction containing released drugs displayed promoted cell proliferation and the expression of osteogenesis-related genes more effectively compared with the drug-free extractions. Therefore, these results demonstrate that the developed mesoporous bioactive glass/sodium alginate/gelatin sustained release scaffolds provide a potential application for bone tissue engineering.

CAS / MDL: 9000-70-8 9005-38-3
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RSC Advances · 2013 ·Vol. 3 ·期 45 ·23423-23431 · IF 2.562

Spray-dried magnetic chitosan/Fe3O4/halloysite nanotubes/ofloxacin microspheres for sustained release of ofloxacin

Qin Wang,Junping Zhang,Aiqin Wang

A series of magnetic chitosan/Fe3O4/halloysite nanotubes/ofloxacin (CTS/Fe3O4/HNTs/OFL) microspheres was prepared by spray-drying for the sustained release of OFL. CTS was in situ crosslinked by glutaraldehyde in the spray-drying process. The magnetic microspheres were characterized by FT-IR, scanning electron microscopy and thermogravimetric analysis. The magnetic properties, encapsulation efficiency, drug loading and in vitro sustained release properties of the magnetic microspheres for OFL were also evaluated. The CTS/Fe3O4/HNTs/OFL microspheres show superparamagnetic properties and fast magnetic response. The Fe3O4 nanoparticles have a remarkable effect on the surface morphology of the microspheres compared with HNTs. The encapsulation efficiency and the cumulative release are closely related to HNTs and Fe3O4 contents, crosslinking density and CTS concentration. OFL is released from the magnetic CTS/Fe3O4/HNTs/OFL microspheres via anomalous transport.

CAS / MDL: 1317-61-9
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RSC Advances · 2017 ·Vol. 7 ·期 36 ·22280-22285 · IF 3.108

Preparation of a colon-specific sustained-release capsule with curcumin-loaded SMEDDS alginate beads

Yuxia Zhang,Yan Bai,Huali Chen,Yuanrui Huang,Pei Yuan,Liangke Zhang

A colon-specific capsule with alginate beads containing a self-microemulsifying drug delivery system (SMEDDS) was developed and evaluated. The SMEDDS technique was used to improve the solubility of curcumin (Cur). After encapsulating the Cur-loaded SMEDDS, the alginate beads were placed inside an impermeable capsule body. A konjac glucomannan/lactose/hydroxypropyl methylcellulose (KG/Lac/HPMC) plug tablet was then prepared and placed in the mouth of the capsule. The capsule demonstrated a pulsatile drug-release profile with a specific lag time and subsequent sustained-release phase. The lag time was modified by changing the type of HPMC and the ratio of KG/Lac/HPMC. In addition, 0.5% β-mannase solution and 5% rat cecal solution were used to simulate the colon fluid, significantly decreasing the lag time of the capsule. The results show that the capsule has potential for use in colon-specific drug delivery and exhibits a sustained-release characteristic.

CAS / MDL: 458-37-7
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ACS Applied Materials & Interfaces · 2025 · IF 8.2

Bimetallic MOF-Based Hybrid Platform with Dual Stimuli-Responsiveness for Sustained Release and Enhanced Retention

Vinayak Hegde,Mahesh P. Bhat,Jae-Ho Lee,Cheol Soo Kim,Kyeong-Hwan Lee

Pesticide delivery carriers provide protection against pathogens but face significant challenges, including limited loading capacity, rapid release rates, and inconsistent performance. To address these issues, this study develops a dual-stimuli-responsive pesticide delivery carrier, featuring an iron–copper bimetal–organic framework (Fe–Cu MOF) supported on diatomaceous earth (DE) and coated with lauric acid (LA). Here, DE serves as a biocompatible scaffold, enhancing the adhesion and retention of MOF particles at target sites, thereby improving the pesticide localization and delivery efficiency. The carrier exhibits a high thiabendazole (Tbz) loading capacity of 38.14% owing to its nanoporous structure. The LA coating functions as a pH- and temperature-responsive barrier, regulating pesticide release to prolong the treatment duration and minimizing the need for repeated applications. The carrier demonstrates controlled release rates of 80.73% at pH 5 and 96.55% at 40 °C, confirming its dual-stimuli responsiveness. In vitro assays reveal 92.26% inhibition of Botrytis cinerea at 1 μg mL–1, while in vivo experiments on tomato plants and fruits show complete inhibition at 200 μg mL–1. Additionally, the developed composites adhere strongly to leaves through electrostatic and hydrogen-bonding interactions, reducing the loss of pesticide due to rain erosion. Overall, DE-MOF-Tbz-LA presents a promising and efficient alternative to conventional pesticide applications.

CAS / MDL: 3326-32-7
研究领域: 农业科学 · 材料科学
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