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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
研究领域: 药剂学 · 生物医学工程
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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
研究领域: 材料科学 · 生物医学工程 · 药物递送系统 · 组织工程
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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
研究领域: 材料科学 · 药学
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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
研究领域: 生物材料 · 药学 · 药物递送系统 · 聚合物化学
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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
研究领域: 药剂学 · 药物代谢动力学
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JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY · 2023 · IF 2.2

Essential oil-loaded chitosan/zinc (II) montmorillonite synergistic sustained-release system as antibacterial material

Jinghui Zhan,Huayao Chen,Hongjun Zhou,Li Hao,Hua Xu,Xinhua Zhou

Tea tree oil (TTO) is a broad-spectrum natural antimicrobial agent. Its application is limited due to its volatile property. To reduce its volatility and improve its sustained-release performance, a synergistic sustained-release system was prepared. Montmorillonite (Mt) was ion-exchanged with sodium ions (Na+) and zinc ions (Zn2+), then organically modified with cetyl trimethyl ammonium bromide (CTAB) and chitosan (CS) to improve its sustained release performance. The results indicated that Mt was exfoliated, but still maintained its ordered layer structure. The surface of CS-Zn-OMt was rough, because some pores and surfaces were filled. The addition of Zn2+ increased the loading of CS (37.8 − 40.8%) and induced more uniform distribution of CS on Mt. Also, CS-Zn-OMt achieved a high loading capacity for TTO and the loading value was 222.0 mg*g−1. Furthermore, the release studies showed that CS-Zn-OMt exhibited sustained-release behavior due to the release from the outer layer of CS and the Mt channel simultaneously. The results of antibacterial test showed that the addition of CS inhibited the drift of Mt and showed good antibacterial performance because of strong effective drug-carrier interaction. The developed system can be potentially applied for the delivery of volatile essential oils for antibacterial infection.

研究领域: 材料科学 · 微生物学 · 药物递送
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MOLECULES · 2022 ·Vol. 27 ·期 21 ·7158 · IF 4.927

Preparation and Characterization of Simvastatin-Loaded PCL/PEG Nanofiber Membranes for Drug Sustained Release

Lu Pan,Jiahao Yang,Lan Xu

Simvastatin (SIM) particles are liposoluble drugs with large particle sizes, resulting in poor compatibility with electrospun polycaprolactone (PCL)/polyethylene glycol (PEG) nanofibers, so that part of them will be exposed to the electrospun nanofiber surface, which is easy to cause the burst release of drugs. Therefore, in this paper, stearic acid (SA) with good biocompatibility was innovatively added to increase the dispersion uniformity of SIM in the spinning solution, thus improving the performances of SIM-loaded PCL/PEG nanofiber membranes (NFMs). Accordingly, the effects of SA addition on the morphologies, mechanical properties, wettability, and drug release properties of the SIM-loaded NFMs were studied. The results showed that after SIM was dissolved in SA solution, the particle size of SIM was significantly reduced and could be evenly dispersed in the polymer spinning solution, thus obtaining the SIM-loaded composite NFMs with the best morphology and performance.Keywords:electrospinning;simvastatin;composite nanofiber membranes;drug release

CAS / MDL: 2386-53-0 57-11-4
研究领域: 药学 · 材料科学 · 纳米技术
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JOURNAL OF HAZARDOUS MATERIALS · 2022 · IF 14.224

Integrated transcriptomic and metabolomic analysis of Microcystis aeruginosa exposed to artemisinin sustained-release microspheres

Cunhao Du,Wenlu Sang,Chu Xu,Zhiyun Jiang,Jiajia Wang,Yuanyi Fang,Chengjie Zhu,Jakpa Wizi,Muhammad Asif Akram,Lixiao Ni,Shiyin Li

Artemisinin sustained-release microspheres (ASMs) have been shown to inhibit Microcystis aeruginosa ( M. aeruginosa ) blooms. Previous studies have focused on inhibitory mechanism of ASMs on the physiological level of M. aeruginosa , but the algal inhibitory mechanism of ASMs has not been comprehensively and profoundly revealed. The study proposed to reveal the toxicity mechanism of ASMs on M. aeruginosa based on transcriptomics and metabolomics. After exposure to 0.2 g·L −1 ASMs for 7 days, M. aeruginosa biomass was significantly inhibited, with an inhibition rate (IR) of 47 % on day 7. Transcriptomic and metabolomic results showed that: (1) 478 differentially expressed genes (DEGs) and 251 differential metabolites (DMs) were obtained; (2) ASMs inhibited photosynthesis by blocking photosynthetic pigment synthesis, destroying photoreaction centers and photosynthetic carbon reactions; (3) ASMs reduced L -glutamic acid content and blocked glutathione (GSH) synthesis, leading to an imbalance in the antioxidant system; (4) ASM disrupted nitrogen metabolism and the hindered synthesis of various amino acids; (5) ASMs inhibited glyoxylate cycle and TCA cycle. This study provides an important prerequisite for the practical application of ASMs and a new perspective for the management of harmful algal blooms (HABs).

CAS / MDL: 63968-64-9 9012-76-4
研究领域: 环境科学 · 毒理学 · 分子生物学
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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
研究领域: 生物医学工程 · 分子生物学
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PARTICLE & PARTICLE SYSTEMS CHARACTERIZATION · 2023 · IF 2.7

Sustained Release of Hydrogen by PdH-Te Nanozyme for Anti-Inflammatory Therapy Against Atherosclerosis

Min Xu,Xuan Zhang,Baowen Dong,Wenjuan Wang,Zhihuan Zhao

Atherosclerosis is induced by the persistent inflammation of the arterial wall. The regulation of inflammation through active drugs can mitigate atherosclerotic lesions, but the therapeutic outcome is limited due to its insufficient efficacy and stability. Herein, a PdH-Te nanozyme with excellent reactive oxygen species (ROS) scavenging capability is designed for anti-inflammatory therapy, thereby preventing foam cell formation to alleviate atherosclerosis. As expected, the PdH-Te nanozyme shows outstanding multiple antioxidant enzyme activities and sustained hydrogen release properties. Benefiting from decreased ROS levels by enzyme catalysis, PdH-Te nanozyme significantly suppresses the pro-inflammatory cytokines for atherosclerosis treatment. Taken together, the presented results demonstrate that inhibition of inflammation based on PdH-Te nanozyme can effectively treat atherosclerosis, identifying an attractive strategy against cardiovascular diseases.

CAS / MDL: 7446-07-3 7783-00-8
研究领域: 纳米技术 · 心血管疾病 · 炎症 · 材料科学
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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
研究领域: 材料科学 · 食品科学 · 环境科学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Visualization of thermosensitive hydroxypropyl chitin with aggregation-induced emission features for sustained-release drug delivery

Taotao Li,Long Huang,Xulin Jiang

Hydroxypropyl chitin (HPCH) has been studied as a carrier for drug delivery due to its excellent biocompatibility, biodegradability and reversible thermosensitivity. However, the behaviors of the erosion/degradation of HPCH and release of drug for drug-loaded HPCH in vivo are unclear. Visualization of the drug-loaded HPCH could reveal the location and degradation of the carrier, and the release and distribution of the drug in vivo, which is more beneficial for promoting the clinical translation. Herein, we simultaneously tracked HPCH labeled by aggregation-induced emission fluorogens (AnDA-HPCH) and a model drug (indocyanine green, ICG) in vitro and in vivo without mutual interference. The erosion/degradation rate of AnDA-HPCH and the drug release of ICG from the ICG-loaded AnDA-HPCH sponge implanted in the buttock of mice were slower than those of the injected hydrogel containing the same amounts of drug and polymer. Further, the long-acting local anesthetic ropivacaine-loaded HPCH sponge implanted in the back of rats showed an effective analgesic time of approximately 30 h, which was 3-fold longer than that with the injected RPH@HPCH hydrogel (10 h) and much longer (6 times) than that of the xaracoll-like formulation (5 h). This thermosensitive HPCH sponge may be a promising visible biomedical implant for sustained-release drug carrier and tissue repair.

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