INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Congyi Nie,Qian Liang,Qunyu Gao
Cyclodextrin-based electrospun nanofibers are promising for encapsulating and preserving unstable compounds, but quick dissolution of certain nanofibers hinders their delivery application. In this study, hydroxypropyl-β-cyclodextrin (HPβCD) was used as an effective carrier of resveratrol (RSV) to obtain the RSV/HPβCD inclusion complex (HPIC), which was then incorporated into pullulan nanofibers. For enhancement of RSV release toward colon target, multilayer structure with a pullulan/HPIC film sandwiched between two layers of hydrophobic Eudragit S100 (ES100) nanofibers was employed. The relationship between the superiority of the ES100-pullulan/HPIC-ES100 film and its multilayer structure was verified. The intimate interactions of hydrogen bonds between two adjacent layers enhanced thermal stability , and the hydrophobic outer layers improved water contact resistance. According to release results, multilayer films also showed excellent colon-targeted delivery property and approximately 78.58 % of RSV was observed to release in colon stage. In terms of release mechanism, complex mechanism best described RSV colonic release. Additionally, ES100-pullulan/HPIC-ES100 multilayer films performed higher encapsulation efficiency when compared to the structures without HPIC, which further increased the antioxidant activity and total release amount of RSV. These results suggest a promising strategy for designing safe colonic delivery systems based on multilayer and HPIC structures with superior preservation for RSV.
研究领域:
药学
·
材料科学
·
药物递送系统
·
纳米技术
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2016
·
IF 3.994
Juntao Yin,Cuiyu Xiang,Xiaoyong Song
Psoralidin (PL) has recently been attracting more attention as a new anticancer agent candidate. Nevertheless, peroral administration of PL is largely challenged by its insoluble nature and intestinal efflux. This article aimed to develop a nanoencapsulation formulation of PL using water-soluble chitosan and Eudragit S100 and to evaluate its potential for bioavailability enhancement. PL-loaded nanocapsules (PL-NCs) were prepared by a solvent diffusion and high-pressure homogenization technique with Poloxamer 188 as a stabilizer. The resultant PL-NCs were approximately 132.5 nm in particle size and possessed a high entrapment efficiency (98.1%). In vitro release showed that PL was released less from the nanocapsules due to electrostatic complexation. A lipolytic experiment demonstrated that our prepared PL-NCs were not degraded by lipase , in contrast with the most commonly used lipid nanoparticles. Furthermore, PL-NCs appeared to have less affinity for intestinal mucins. Following oral administration, the bioavailability of PL was significantly enhanced via the PL-NCs, with a value of 339.02% relative to the reference (suspensions). Excellent intestinal adhesion and transepithelial permeability accounted for the enhancement of oral bioavailability. Taken together, these results indicate that nanoencapsulation of PL with chitosan and Eudragit S100 is a promising strategy for improved PL oral delivery.
研究领域:
药剂学
·
肿瘤学
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2015
·
IF 3.65
U. Eranka Illangakoon,Deng-Guang Yu,Bilal S. Ahmad,Nicholas P. Chatterton,Gareth R. Williams
A series of 5-fluorouracil (5-FU) loaded core/shell electrospun fibers is reported. The fibers have shells made of Eudragit S100 (ES-100), and drug-loaded cores comprising poly(vinylpyrrolidone), ethyl cellulose , ES-100, or drug alone. Monolithic 5-FU loaded ES-100 fibers were also prepared for comparison. Electron microscopy showed all the fibers to have smooth cylindrical shapes, and clear core–shell structures were visible for all samples except the monolithic fibers. 5-FU was present in the amorphous physical form in all the materials prepared. Dissolution studies showed that the ES-100 shell was not able to prevent drug release at pH 1.0, even though the polymer is completely insoluble at this pH: around 30–80% of the maximum drug release was reached after 2 h immersion at pH 1.0. These observations are ascribed to the low molecular weight of 5-FU permitting it to diffuse through pores in the ES-100 coating, and the relatively high acid solubility of the drug providing a thermodynamic impetus for this to happen. In addition, the fibers were observed to be broken or merged following 2 h at pH 1.0, giving additional escape routes for the 5-FU.
研究领域:
药学
·
材料科学
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
ENGINEERING IN LIFE SCIENCES
·
2012
·Vol. 13
·期 2
·194-200
·
IF 1.925
Yuanyuan Yu,Jiugang Yuan,Qiang Wang,Xuerong Fan,Ping Wang,Xuejiao Sun
Cellulases can penetrate into the fiber, causing tensile strength loss of the cellulosic fibers or fabrics. To minimize the tensile strength loss, we have immobilized cellulases on Eudragit S-100. The characteristics of covalent Eudragit cellulase were evaluated using gel filtration analysis and UV spectra. Gel filtration analysis revealed that the cellulases were covalently bound to the polymer. Covalent Eudragit cellulase was loaded with the enzyme of about 40% and had a relative activity about 80% at a Eudragit S-100 concentration of 15 g/L. When cellulase is bound to the polymer, the solubility profile becomes similar to the one of Eudragit. In addition, the effects of the enzyme on the cotton yarns and fabric using cellulases have been investigated. Native and immobilized cellulases caused improvements in whiteness and wrinkle recovery angle of the fabric in comparison to the control samples. The bending stiffness results show that native and immobilized cellulase treated cotton fabric has an improved softness than the control samples. It was found that using the immobilized cellulase reduced the weight and tensile strength, because the hydrolytic attack is only limited to the surfaces of cotton fibers.
研究领域:
生物化学
·
纺织科学
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DOI
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
·
2015
·Vol. 17
·期 2
·1-11
·
IF 2.184
Zhang Yan,Yang Zhijie,Hu Xi,Zhang Ling,Li Feng,Li Meimei,Tang Xing,Xiao Wei
The objective of this study was to develop pH-sensitive Eudragit L100–cysteine/reduced glutathione (Eul–cys/GSH) nanoparticles (NPs), which provided the mucoadhesion and protection for protein drugs against enzymatic degradation. Insulin was chosen as a model biomolecule for testing this system. The Eul–cys conjugate, which was obtained by grafting cysteine onto the carboxy group of Eudragit L100, was analyzed by HNMR and SEM, and the swelling degree (SD), cation binding, and enzymatic inhibition were also determined. The results obtained showed that the Eul–cys conjugate represent a pH-sensitive delivery system which effectively protected the insulin from being degraded by the proteases, and this is related to the mechanism of Ca 2+ binding. Insulin-loaded Eul–cys/GSH NPs were prepared by a diffusion method involving an electrostatic interaction between the network structure of the polymer and the embedded proteins, including insulin and GSH. TEM images indicated that Eul–cys/GSH existed as smooth and spherical NPs in aqueous solution with particle sizes of 260 ± 20 nm. The X-ray diffraction (XRD) and X-ray photoelectron spectroscopy (XPS) findings showed the presence of amorphous insulin in thiolated NPs and higher free thiol oxidation than the result obtained by Ellman’s reagent method. In addition, thiolated NPs showed excellent binding efficiency to the mucin in rat intestine, indicating that Eul–cys/GSH NPs have great potential to be applied as safe carriers for the oral administration of protein drugs.
研究领域:
药剂学
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生物材料
·
药物传递系统
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纳米医学
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蛋白质递送
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DOI
高影响因子
MACROMOLECULAR BIOSCIENCE
·
2014
·Vol. 14
·期 6
·842-852
·
IF 3.65
Yan Zhang,Xuli Du,Yu Zhang,Guofei Li,Cuifang Cai,Jinghua Xu,Xing Tang
This work deals with the synthesis of insulin loaded nanoparticles (NPs) composed of thiolated Eudragit L100 (Eul-cys) and reduced glutathione (GSH) as potential nanocarriers for oral delivery of insulin. Perfectly spherical NPs with an average particle size of nearly 200–300 nm are prepared. The insulin release from Eul-cys/GSH and Eul-cys NPs in PBS (pH 7.4) shows that GSH can slightly decrease the release rate of insulin. Eul-cys in combination with GSH or sodium caprate (SC) is evaluated for its permeation enhancing effect of FITC-insulin using the Caco-2 monolayer and Caco-2/HT29-MTX co-cultured cells models. SC results in greater permeation enhancement compared to GSH. However, GSH proves to be less toxic. Paracellular transport of insulin represents the main mechanism by which the NPs facilitate insulin permeation through the intestinal epithelium, whereas a number of NPs are also taken up by the cells and release insulin within the cells.
研究领域:
药剂学
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生物医学工程
·
药物递送系统
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DOI
PubMed
高影响因子
Pharmaceutics
·
2023
·Vol. 15
·期 7
·2007
·
IF 5.4
Mengzhen Xing,Yuning Ma,Xiaocen Wei,Chen Chen,Xueli Peng,Yuxia Ma,Bingwen Liang,Yunhua Gao,Jibiao Wu
Poor transdermal permeability limits the possibility of most drug delivery through the skin. Auxiliary permeable microneedles (AP-MNs) with a three-dimensional network structure can effectively break the skin stratum corneum barrier and assist in the transdermal delivery of active ingredients. Herein, we propose a simple method for preparing AP-MNs using polyvinyl alcohol and Eudragit NM30D for the first time. To optimize the formulation of microneedles, the characteristics of swelling properties, skin insertion, solution viscosity, and needle integrity were systematically examined. Additionally, the morphology, mechanical strength, formation mechanism, skin permeability, swelling performance, biocompatibility, and in vitro transdermal drug delivery of AP-MNs were evaluated. The results indicated that the microneedles exhibited excellent mechanical-strength and hydrogel-forming properties after swelling. Further, it proved that a continuous and unblockable network channel was created based on physical entanglement and encapsulation of two materials. The 24 h cumulative permeation of acidic and alkaline model drugs, azelaic acid and matrine, were 51.73 ± 2.61% and 54.02 ± 2.85%, respectively, significantly enhancing the transdermal permeability of the two drugs. In summary, the novel auxiliary permeable microneedles prepared through a simple blending route of two materials was a promising and valuable way to improve drug permeation efficiency.Keywords:auxiliary permeation microneedles;polyvinyl alcohol;Eudragit NM30D;skin permeability;transdermal drug delivery
研究领域:
药剂学
·
药物递送系统
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2018
·
IF 3.909
Bohui Xu,Wenjing Zhang,Yulin Chen,Yan Xu,Bo Wang,Li Zong
The aim of this study was to develop a novel biodegradable polymeric carrier for the delivery of protein vaccine orally in order to target the antigen presenting cells (APCs) in the region of Peyer's patches (PPs). Here, bovine serum albumin (BSA) was chosen as a model protein vaccine and was loaded into the mannosylated chitosan nanoparticles (MCS NPs) by ionic gelation method with tripolyphosphate (TPP), followed by coating MCS NPs with Eudragit® L100 (Eud) by electrostatic interaction. The spherical NPs were successfully prepared with appropriate particle size around 558.2 ± 35.6 nm, high entrapment efficiency about 90.38 ± 9.12%, good stability and reasonable release behavior in the simulated gastrointestinal fluid, meanwhile high resistance of enzymatic and acid degradations were verified. The targeting ability of the NPs to PPs in rat was investigated by a closed ileal loop assay, where fluorescence visualization was performed. MCS NPs were accumulated more specifically into PPs after Eudragit® L100 dissolved in intestinal juices. Oral immunization using BSA-loaded Eudragit® L100-coated MCS NPs was found to elicit strong systemic IgG antibody and mucosal IgA responses. These results suggested that enteric-coated MCS NPs could serve as a promising carrier for oral protein vaccine delivery.
研究领域:
药剂学
·
免疫学
·
纳米技术
·
药物递送系统
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF LIPOSOME RESEARCH
·
2021
·
IF 3.648
Gang Wang,Yu Yang,Du Yi,Lu Yuan,Pei-Hao Yin,Xu Ke,Wang Jun-Jie,Min-Fang Tao
This study aimed to develop polymer Eudragit S100 for preparing pH-responsive liposomes-loaded betulinic acid (pH-BA-LP) to improve the therapeutic index of chemotherapy for colorectal cancer. BA-loaded liposomes were coated with Eudragit S100 by a thin film dispersion and easily scalable pH-driven method. The prepared liposomes were evaluated for size, surface morphology, entrapment efficiency, stability, in vitro drug release, and antitumor activity. In particular, pH-BA-LP showed advantages such as lower size (<100 nm), encapsulation efficiency of 90%, high stability, and stably cumulative release. By detecting the antitumor effects of pH-BA-LP in vivo, it showed that the tumor proliferation and cell migration were significantly inhibited in colorectal cancer. The pH-BA-LP also inhibited tumor growth via the regulation of Akt/TLR-mediated signalling and significantly down-regulated the expression of NFAT1 and NFAT4 proteins. It was found that pH-BA-LP can increase NK cells and CD3+ cells in tumor tissues, and the proportion of CD8+ cells in CD3+ cells was also increased, which proved that pH-BA-LP can play an antitumor effect by enhancing the autoimmunity level in tumor-bearing mice. The positive infiltration rates of CD8 and CD68 were increased and CD163 was relatively decreased by using pH-BA-LP, which proved that pH-BA-LP can regulate the immune infiltration levels in tumor-bearing mice. Therefore, the present work provides an effective method to prepare pH-responsive polymer-coated liposomes for colonic delivery with biologically active compounds.
研究领域:
药学
·
肿瘤学
·
药理学
·
免疫学
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产品关联
DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2022
·Vol. 23
·期 4
·1-10
·
IF 4.026
Liu Xia,Zhang Mengying,Tian Yuxin,Liu Ruijia,Wang Yunfei,Guo Feifei,Gong Yanling,Yan Meixing
Luteolin (Lu) is a kind of flavonoid that has been proved to treat non-alcoholic fatty liver disease by alleviating intestinal microbiota disorder. In this study, luteolin was coated with methoxy poly(ethylene glycol)–poly(dl-lactide-co-glycolic acid) (mPEG-PLGA) using an emulsion solvent evaporation method, and the optimum preparation process was determined by a single-factor experiment combined with response surface methodology (RSM). Methacrylic acid-methyl methacrylate (1:2) copolymer (Eudragit S100) was then used to coat the surface of Lu/mPEG-PLGA nanoparticles. The physical parameters of Eudragit S100-coated Lu/mPEG-PLGA nanoparticles (Lu-NPs), such as appearance, particle size, potential, particle size distribution and drug release, and stability in vitro, were evaluated. In addition, its cytotoxicity in vitro , pharmacokinetics, tissue distribution, and toxicity in vivo were also studied. The results showed that the prepared Lu-NPs had uniform particle size distribution, high encapsulation efficiency, and good stability. Normal colonic epithelial cells showed good tolerance to Lu-NPs. After oral administration, the blood concentration of luteolin peaked at 8 h, and the main tissue distribution was within the colon, confirming its colon-targeted profile. Safety assessments also indicated that no significant changes were observed in main organs after administration of Lu-NPs. The use of Eudragit S100-coated Lu/mPEG-PLGA nanoparticles is a new strategy for colon-targeted delivery of luteolin that encourages luteolin to fulfill its role in the colon. Graphical abstract
研究领域:
药学
·
纳米技术
·
药物递送系统
·
药理学
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2024
·
IF 4.5
Haigang Li,Jiaxuan Liu,Lei Zhang,Xinru Zhu,Jing Jiang,Zhaohui Ge,Yifei Zuo,Xiangzhu Chen,Chun Zhang
This study aims to achieve co-delivery of paeoniflorin (PF) and butyric acid (BA) to the colon through Eudragit S100 (EUS100)-coated halloysite nanotube/o-butyryl chitosan microspheres (EUS100-HNT-BUCHNPs). O-butyrylated chitosan (BUCH) was prepared by the acylation reaction of chitosan (CH) and butyric anhydride with methane sulfonic acid as a catalyst. PF-loaded halloysite nanotube/o-butyrylated chitosan microspheres (HNT-BUCHNPs) were prepared by emulsion crosslinking with glutaraldehyde as the crosslinking agent and then coated with EUS100 using the emulsion solvent evaporation method. X-ray photoelectron spectroscopy (XPS) and scanning electron microscopy results indicated the presence of EUS100 coating on the surface of HNT-BUCHNPs. In vitro release studies demonstrated that the EUS100 coating effectively prevented the release of PF and BA at pH 1.2, while the halloysite nanotube slowed down PF release at pH 6.8. Sequential release experiments in different pH media showed lower release of PF and BA at pH 1.2 and pH 6.8, and higher release at pH 7.4, reaching approximately 80 % and 85 %, respectively. Gastrointestinal tract retention studies in mice confirmed that EUS100-HNT-BUCHNPs reduced the release of PF and BA in the upper digestive tract, facilitating delivery to the colon. In vivo and in vitro results indicated efficient transport of PF and BA to the colon, suggesting the potential of EUS100-HNT-BUCHNPs as colon-targeted carriers for PF and BA.
研究领域:
药剂学
·
生物医学工程
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产品关联
DOI
高影响因子
APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY
·
2012
·Vol. 166
·期 6
·1433-1441
·
IF 1.943
Yu Yuanyuan,Yuan Jiugang,Wang Qiang,Fan Xuerong,Wang Ping
The covalent immobilization of a commercial preparation of cellulase on a reversibly soluble–insoluble enteric polymer Eudragit S-100 by carbodiimide coupling was carried out. The characteristics of covalent Eudragit cellulase were evaluated using Fourier transform infrared (FTIR) spectra, circular dichroism (CD) spectra, and fluorescence spectra. FTIR, CD, and fluorescence measurements also revealed that the cellulases were covalently bonded to the supports. Covalent Eudragit cellulase had binding efficiency of 81.08% which was higher than the noncovalent Eudragit cellulase 56.83%. The relative activity of the native cellulase and covalent Eudragit cellulase increased and reached the maximum (at pH 5.0, 50°C) and then decreased with further increases in pH and temperature. The covalent Eudragit cellulase shows higher stability especially at higher pH and temperature. The K
m value of covalent Eudragit cellulase (4.78 g·L −1 ) was decreased compared to that of the native cellulase (2.89 g·L −1 ). The affinity of the cellulase to its substrate was increased when it was immobilized on Eudragit S-100.
研究领域:
生物化学
·
酶工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）