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JOURNAL OF CEREAL SCIENCE · 2022 · IF 4.075

Development of a pluronic-zein-curcumin drug delivery system with effective improvement of hydrophilicity, stability and sustained-release

Liping Ye,Wenquan Huang,Yuehua Deng,Zhiqiang Li,Yanbin Jiang,Qiuling Xie

Curcumin (Cur) has been widely studied for its chemo-preventive and chemotherapeutic effects against various types of human cancers, but the clinical application of curcumin is limited due to multiple delivery challenges, including poor water solubility, poor membrane permeability and easy degradation under alkaline conditions. Zein is an excellent carrier for pharmaceutical preparations because of its non-toxicity and biodegradability, but the plant protein source and hydrophobicity limit the application of zein in biomedical applications. The aim of this study is to overcome the limitations of Cur and zein in clinical therapy. To improve the hydrophilicity of zein and obtain a highly stable drug delivery system (DDS), zein was modified with carboxylated pluronic to prepare pluronic-zein (ZSP). The results indicated that the ZSP prepared not only has good hydrophilic and dispersibility properties, where the surface contact angle of the ZSP prepared is reduced by 33.1%–62.8%, but also its stability is not affected by pH and salinity compared with zein particles. After loading Cur into ZSP particles, Cur-ZSP DDS with good dispersibility and drug loading was prepared. Cur-ZSP DDS exhibited sustained release in the simulated in vitro environment. Cell experiments showed that ZSP presented as non-toxic. After loading with Cur, the cytotoxicity of Cur-ZSP DDS was significantly higher than that of raw Cur. The results provide new insight into the construction of zein-based oral drug delivery systems.

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FOOD HYDROCOLLOIDS · 2021 · IF 9.147

Structurally stable sustained-release microcapsules stabilized by self-assembly of pectin-chitosan-collagen in aqueous two-phase system

Zhenyang Jiang,Shaojie Zhao,Minke Yang,Mingyue Song,Juan Li,Jinkai Zheng

Microcapsule colloidal systems have been widely used as delivery vehicles. Natural biopolymers are highly biocompatible shell materials for the fabrication of microcapsules, but no single substance can fulfill the requirements of aqueous two-phase interfacial assembly. In this study, we fabricated pectin-chitosan-collagen composite microcapsules (PCCMs) in an aqueous two-phase system to improve the robustness and sustained-release capacity of resultant microcapsules. Fourier transform infrared spectra and isothermal titration calorimetry thermodynamics analysis indicated that the PCCM interface can be stabilized by pectin, chitosan, and collagen via intermolecular electrostatic interactions and hydrogen bonds. The swelling experiment and atomic force microscopy nanoindentation measurements demonstrated that the PCCMs had excellent anti-swelling performance and enhanced mechanical strength of the composite interfacial membrane. Contraction-recovery measurements and scanning electron microscopy indicated that the PCCMs exhibited prominent anti-shrinkage capacity and restorable surface smoothness. The release kinetics of encapsulated substances under conditions of different osmotic pressure and salt concentrations revealed that the PCCMs had superior sustained-release capacity. This study yielded natural, biocompatible, and robust aqueous two-phase microcapsules for encapsulation and delivery of active biomacromolecules.

CAS / MDL: 3326-32-7
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Biomaterials Science · 2021 ·Vol. 9 ·期 10 ·3821-3829 · IF 6.843

Polyvinyl alcohol/chitosan composite hydrogels with sustained release of traditional Tibetan medicine for promoting chronic diabetic wound healing

Zuxin Wang,Shan Gao,Wanlin Zhang,Hanwen Gong,Kai Xu,Chao Luo,Wei Zhi,Xingyu Chen,Jianshu Li,Jie Weng

The Tibetan eighteen flavor dangshen pills (TEP) are composed of 18 traditional Tibetan medicines, which are commonly used in the treatment of skin diseases in the Tibetan medical system. They have anti-inflammatory and analgesic effects, and healing properties. However, TEP contain large doses and have strong side effects and low bioavailability. To improve the utilization rate of TEP in skin treatment, we prepared TEP powder and then introduced it into polyvinyl alcohol/chitosan (PVA/CS) hydrogels to treat diabetic wounds by slowly releasing the active ingredients of TEP. In vitro studies showed that TEP-loaded hydrogels can effectively and continuously release the active ingredients of TEP and have antibacterial and antioxidant properties. In addition, the hydrogel system was not cytotoxic to L929 cells, and significantly promoted the proliferation of HUVECs. Moreover, when the TEP-loaded hydrogel was applied to diabetic wounds in rats, it reduced the inflammatory response and improved collagen deposition, which in turn promoted skin healing. Our results indicate that TEP-loaded hydrogels may be a new formulation for the application of traditional Tibetan medicines for the treatment of chronic wounds.

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Journal of Materials Chemistry B · 2021 ·Vol. 9 ·期 43 ·8980-8993 · IF 6.331

Superparamagnetic core–shell electrospun scaffolds with sustained release of IONPs facilitating in vitro and in vivo bone regeneration

Shuying Hu,Hanbang Chen,Fang Zhou,Jun Liu,Yunzhu Qian,Ke Hu,Jia Yan,Zhuxiao Gu,Zhaobin Guo,Feimin Zhang,Ning Gu

Bone tissue engineering (BTE) is a promising approach to recover insufficient bone in dental implantations. However, the clinical application of BTE scaffolds is limited by their low mechanical strength and lack of osteoinduction. In an attempt to circumvent these limitations and improve osteogenesis, we introduced magnetic iron oxide nanoparticles (IONPs) into a core–shell porous electrospun scaffold and evaluated their impact on the physical, mechanical, and biological properties of the scaffold. We used poly(lactic-co-glycolic acid)/polycaprolactone/beta-tricalcium phosphate (PPT) scaffolds with and without γ-Fe2O3 encapsulation, namely PPT–Fe scaffolds and PPT scaffolds, respectively. The γ-Fe2O3 used in the PPT–Fe scaffolds was coated with polyglucose sorbitol carboxymethylether and was biocompatible. Structurally, PPT–Fe scaffolds showed uniform iron distribution encapsulated within the resorbable PPT scaffolds, and these scaffolds supported sustainable iron release. Furthermore, compared with PPT scaffolds, PPT–Fe scaffolds showed significantly better physical and mechanical properties, including wettability, superparamagnetism, hardness, tensile strength, and elasticity modulus. In vitro tests of rat adipose-derived mesenchymal stem cells (rADSCs) seeded onto the scaffolds showed increased expression of integrin β1, alkaline phosphatase, and osteogenesis-related genes. In addition, enhanced in vivo bone regeneration was observed after implanting PPT–Fe scaffolds in rat calvarial bone defects. Thus, we can conclude that the incorporation of IONPs into porous scaffolds for long-term release can provide a new strategy for BTE scaffold optimization and is a promising approach that can offer enhanced osteogenic capacity in clinical applications.

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JOURNAL OF SOL-GEL SCIENCE AND TECHNOLOGY · 2019 ·Vol. 92 ·期 3 ·723-735 · IF 1.986

One-step synthesis of methyl eugenol/Schiff base mesoporous silica nanoparticles sustained-release performance with high lure efficiency

Chen Huayao,Li Juncai,Shen Zhichuan,Zhou Hongjun,Hao Li,Xu Hua,Zhou Xinhua

The mesoporous silica nanoparticles (MSN) was modified by salicylaldimine, furfuralimine, and benzaldehyde imine, respectively, denoted as Sal-MSN, Fur-MSN, and Ben-MSN for methyl eugenol (Me) delivery by one-step method. The results confirmed that Me was successfully adsorbed by Schiff base mesoporous silica, which maintained regular hexagonal pore structure. Me is distributed in amorphous state in the pores of the mesoporous silica indicated by differential scanning calorimeter (DSC) curves. Schiff base modification strengthened the interaction between Me and mesoporous silica, leading to its higher sustained-release performance and the disappearance of sudden release in sustained-release performance comparing with Me-MSN before Schiff base modification. Me and Me-MSN were most consistent with the First-order kinetic and logistic equation, respectively. After Schiff base modification, Me-Sal-MSN, Me-Fur-MSN, and Me-Ben-MSN were most consistent with Korsmeryer–Peppas kinetic equation. Therefore, the difference of Me concentration was no longer the main control factor of sustained-release system after Schiff base modification. In the attraction of Bactrocera dorsalis test, the lure efficiency for per unit Me for Me-MSN, Me-Sal-MSN, Me-Fur-MSN, and Me-Ben-MSN equal to 2.83, 3.31, 3.32, 4.24 times of pure Me. After Schiff base modification, the samples showed higher lure efficiency due to their ideal sustained-release performance without sudden release. In short, the lure efficiency of Me was improved by the Schiff base mesoporous silica sustained-release system, in the meanwhile its service life was also prolonged.

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International Journal of Nanomedicine · 2018 · IF 4.37

Protein delivery nanosystem of six-arm copolymer poly(ε-caprolactone)–poly(ethylene glycol) for long-term sustained release

Jianwei Duan,Chao Liu,Xiaoyu Liang,Xuanling Li,Youlu Chen,Zuoguan Chen,Xiaoli Wang,Deling Kong,Yongjun Li,Jing Yang

Background To address the issue of delivery of proteins, a six-arm copolymer, six-arm poly (ε-caprolactone)–poly(ethylene glycol) (6S-PCL-PEG), was synthesized by a simple two-step reaction. Thereafter, the application of 6S-PCL-PEG as a protein carrier was evaluated. Materials and methods A six-arm copolymer, six-arm poly(ε-caprolactone) (6S-PCL), was synthesized by ring-opening polymerization, with stannous octoate as a catalyst and inositol as an initiator. Then, poly(ethylene glycol) (PEG) was linked with 6S-PCL by oxalyl chloride to obtain 6S-PCL-PEG. Hydrogen-1 nuclear magnetic resonance spectrum, Fourier-transform infrared spectroscopy, and gel-permeation chromatography were conducted to identify the structure of 6S-PCL-PEG. The biocompatibility of the 6S-PCL-PEG was evaluated by a cell counting kit-8 assay. Polymeric nanoparticles (NPs) were prepared by a water-in-oil-in-water double emulsion (W 1 /O/W 2 ) solvent evaporation method. The size distribution and zeta potential of NPs were determined by dynamic light scattering. Transmission electron microscopy was used to observe the morphology of NPs. Drug-loading capacity, encapsulation efficiency, and the release behavior of ovalbumin (OVA)-loading NPs were tested by the bicinchoninic acid assay kit. The stability and activity of OVA released from NPs were detected and the uptake of NPs was evaluated by NIH-3T3 cells. Results All results indicated the successful synthesis of amphiphilic copolymer 6S-PCL-PEG, which possessed excellent biocompatibility and could formulate NPs easily. High drug-loading capacity and encapsulation efficiency of protein NPs were observed. In vitro, OVA was released slowly and the bioactivity of OVA was maintained for over 28 days. Conclusion 6S-PCL-PEG NPs prepared in this study show promising potential for use as a protein carrier.

CAS / MDL: 87-89-8
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ChemPlusChem · 2014 ·Vol. 79 ·期 5 ·725-731 · IF 3.242

Self-Assembly of Nanocellulose and Indomethacin into Hierarchically Ordered Structures with High Encapsulation Efficiency for Sustained Release Applications

Jiali Gao,Qing Li,Wenshuai Chen,Yixing Liu,Haipeng Yu

Graphical Long-lasting effects : A hierarchical structure of cellulose nanofibers and indomethacin has been fabricated through self-assembly and recrystallization under the combined effects of solvent and processing method (see figure). Such hybrid films possess a high loading capacity and encapsulation efficiency, and show a sustained drug release period over 30 days. Cellulose nanofibers (CNFs) were isolated from poplar wood by using a mild chemical pretreatment combined with a high-intensity ultrasonication method. The as-prepared CNFs were used as a template to load indomethacin (IMC). With the nucleation and growth of IMC on the surfaces of CNFs and CNF clusters, CNF/IMC composite fibers were eventually fabricated. The effects of solvent and processing method on the structures of the composite fibers were analyzed in terms of morphology, surface charge, and crystal form. Drug-release characteristics of the composite fibers were evaluated by dissolution tests, in which the drug-releasing curves of the composite fibers were fitted to a mathematical model describing the releasing kinetics. The experimental results demonstrated that the composite fibers possessed an encapsulation efficiency of up to 97 %, and a sustained drug-release period of over 30 days.

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Asian Journal of Pharmaceutical Sciences · 2017 · IF 0

Preparation of 5-fluorouracil-loaded chitosan nanoparticles and study of the sustained release in vitro and in vivo

Li Sun,Yunna Chen,Yali Zhou,Dongdong Guo,Yufan Fan,Fangyan Guo,Yufeng Zheng,Weidong Chen

The sustained-release properties of the biodegradable nano-drug delivery systems were used to improve the residence time of the chemotherapeutic agent in the body. These drug delivery systems were widely used to deliver chemotherapeutic drugs. The 5-fluorouracil loaded chitosan nanoparticles prepared in this paper have the above advantage. Here, we found that when the mass ratio of 5-fluorouracil and chitosan was 1:1, the maximum drug loading of nanoparticles was 20.13 ± 0.007%, the encapsulation efficiency was 44.28 ± 1.69%, the particle size was 283.9 ± 5.25 nm and the zeta potential was 45.3 ± 3.23 mV. The prepared nanoparticles had both burst-release and sustained-release phases in vitro release studies. In addition, the inhibitory effect of the prepared nanoparticles on gastric cancer SGC-7901 cells was similar to that of 5-fluorouracil injection, and the blank vector had no obvious inhibitory effect on SGC-7901 cells. In the pharmacokinetic study of rats in vivo , we found that AUC (0−t) , MRT (0−t) and t 1/2z of nanoparticles were significantly increased in vivo compared with 5-fluorouracil solution, indicating that the prepared nanoparticles can play a role in sustained-release.

CAS / MDL: 51-21-8
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY · 2017 · IF 2.295

Preparation and evaluation of metoprolol tartrate sustained-release pellets using hot melt extrusion combined with hot melt coating

Yan Yang,Lian Shen,Juan Li,Wei-guang Shan

The objective of this study was to prepare and evaluate metoprolol tartrate sustained-release pellets. Cores were prepared by hot melt extrusion and coated pellets were prepared by hot melt coating. Cores were found to exist in a single-phase state and drug in amorphous form. Plasticizers had a significant effect on torque and drug content, while release modifiers and coating level significantly affected the drug-release behavior. The mechanisms of drug release from cores and coated pellets were Fickian diffusion and diffusion–erosion. The coated pellets exhibited sustained-release properties in vitro and in vivo.

CAS / MDL: 109-43-3
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2016 · IF 2.857

Synthesis and Characterization of Chlorpyrifos/Copper(II) Schiff Base Mesoporous Silica with pH Sensitivity for Pesticide Sustained Release

Huayao Chen,Yueshun Lin,Hongjun Zhou,Xinhua Zhou,Sheng Gong,Hua Xu

The salicylaldehyde-modified mesoporous silica (SA–MCM-41) was prepared through a co-condensation method. Through the bridge effect from the copper ion, which also acts as the nutrition of the plant, the model drug chlorpyrifos (CH) was supported on the copper(II) Schiff base mesoporous silica (Cu–MCM-41) to form a highly efficient sustained-release system (CH–Cu–MCM-41) for pesticide delivery. The experimental results showed that the larger the concentration of the copper ion, the more adsorption capacity (AC) of Cu–MCM-41 for chlorpyrifos and the smaller its release rate. The results confirmed the existence of a coordination bond between SA–MCM-41 and copper ions as well as a coordination bond between Cu–MCM-41 and chlorpyrifos. The AC of SA–MCM-41 is 106 mg/g, while that of Cu–MCM-41 is 295 mg/g. The as-synthesized system showed significant pH sensitivity. Under the condition of pH ≤ 7, the release rate of chlorpyrifos decreased with increasing pH, whereas its release rate in weak base conditions was slightly larger than that in weak acid conditions. Meanwhile, the drug release rate of the as-synthesized system was also affected by the temperature. Their sustained-release curves can be described by the Korsmeyer–Peppas equation.

CAS / MDL: 919-30-2 90-02-8
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2024 · IF 7.7

Coaxial nanofibrous aerogel featuring porous network-structured channels for ovarian cancer treatment by sustained release of chitosan oligosaccharide

Zhimin Deng,Hua Liu,Gantao Chen,Hongbing Deng,Xiangyang Dong,Linlin Wang,Fenghua Tao,Fangfang Dai,Yanxiang Cheng

Ovarian cancer , the deadliest gynecological malignancy, primarily treated with chemotherapy. However, systemic chemotherapy often leads to severe toxic side effects and chemoresistance. Drug-loaded aerogels have emerged as a promising method for drug delivery, as they can improve drug solubility and bioavailability, control drug release, and reduce drug distribution in non-targeted tissues, thereby minimizing side effects. In this research, chitosan oligosaccharide (COS)-loaded nanofibers composite chitosan (CS) aerogels (COS-NFs/CS) with a porous network structure were created using nanofiber recombination and freeze-drying techniques. The core layer of the aerogel has a COS loading rate of 60 %, enabling the COS-NFs/CS aerogel to significantly inhibit the migration and proliferation of ovarian cancer cells (resulting in a decrease in the survival rate of ovarian cancer cells to 33.70 % after 48 h). The coaxial fiber's unique shell-core structure and the aerogel's porous network structure enable the COS-NFs/CS aerogels to release COS steadily and slowly over 30 days, effectively reducing the initial burst release of COS. Additionally, the COS-NFs/CS aerogels exhibit good biocompatibility , degradability (only retaining 18.52 % of their weight after 6 weeks of implantation), and promote angiogenesis, thus promoting wound healing post-oophorectomy. In conclusion, COS-NFs/CS aerogels show great potential for application in the treatment of ovarian cancer.

CAS / MDL: 81-88-9 148411-57-8
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2025 · IF 4.9

Development and in vitro-in vivo evaluation of a novel sustained-release tablet based on constant-release surface

Lele Wang,Tijie Duan,Yawen Gao,Heqing Liu,Rui Sun,Tong Wu,Jihui Tang

Subject The release rate of hydrophilic gel tablets varies depending on their surface area. In this study, we aimed to develop a sustained-release tablet that maintains a constant release area during drug release. Methods Initially, commercially accessible gliclazide, sinomenine hydrochloride, and trimetazidine hydrochloride tablets were side coated with ethylcellulose to ensure a constant release area. Next, sustained-release gliclazide tablets were prepared by altering their size and thickness to assess the impact of specific surface area on drug release. Then, two types of sustained-release gliclazide tablets were developed and evaluated in vitro. One involved side-coating the tablets with an ethylcellulose solution. The second was a novel three-layer donut-shaped tablet. Finally, these novel sustained-release tablets were evaluated for in vivo drug release and pharmacokinetics in rabbits. Results After lateral coating, commercial tablets altered drug release from first-order to zero-order kinetics. Tablets with the same specific surface area, but different diameters and thicknesses, can have similar release profiles. If the drug release area is unchanged, the tablet typically exhibits zero-order release behavior. Thus, we developed two types of gliclazide sustained-release tablets with a constant release area that achieved zero-order drug release. In vivo, they showed smoother plasma concentration profiles with lower C max , extended T max , and reduced fluctuation, and were bioequivalent to commercial tablets in pharmacokinetic studies. Conclusions Stable drug release can be achieved by maintaining a constant release area. In this study, the novel tablet preparations exhibited consistent drug release both in vivo and in vitro.

CAS / MDL: 64-19-7 21187-98-4
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