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
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
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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
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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
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2025
·
IF 4.9
Limo Wang,Danfeng Jian,Bingjie Xu,Zhiye Qiu,Yujie Gao,Jindan Wu
The vicious cycle of reactive oxygen species (ROS) overload and bacterial infection critically impedes diabetic wound healing. While nanozyme-antibiotic dressings offer therapeutic potential, their uncontrolled agent release remains a key challenge. In this study, a functional nanofiber membrane (EIPR) based on the pH-sensitive polymer Eudragit S100 was fabricated via coaxial electrospinning to load iridium nanozymes (Ir NPs-PVP) and roxithromycin (Rox), enabling on-demand release of therapeutic agents for combined antibacterial and antioxidant wound therapy. The obtained dressing displays highly precise and controllable therapeutic agent release characteristics. Rox shows approximately 90 % cumulative release at pH 7.4, while release is suppressed to <8 % at pH 6.0 and 4.5. Notably, the release trend of Ir NPs-PVP mirrors that of Rox, with significantly higher release under alkaline conditions. The results exhibit >97 % eradication of both Staphylococcus aureus ( S. aureus ) and Escherichia coli ( E. coli ) coupled with >75 % ROS clearance at pH 7.4. This study presents a novel dual-function system, highlighting the simplicity and efficiency of electrospinning technology, which are key advantages enhancing its scalability for large-scale manufacturing and suitability for clinical wound care translation.
研究领域:
生物医学工程
·
伤口护理
·
纳米医学
·
抗菌材料
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2014
·
IF 3.785
Meixia Xu,Minjie Sun,Hongzhi Qiao,Qineng Ping,Eltayeb Suliman Elamin
Oral modified-release delivery systems, such as bio-adhesive one, enable drug delivery to affected regions and minimize the side effects by reducing the systemic absorption. Our aim was to develop colon adhesive pellets of 5-aminosalicylic acid (5-ASA) for the treatment of ulcerative colitis . The core of the pellet was formulated from bioadhesive agents, Carbomer 940 and hydroxypropyl cellulose (HPC), by extrusion/spheronization method and coated with Surelease ® as inner layer for waterproof and with Eudragit ® S100 as outer layer for pH control. The rat model of ulcerative colitis was used to evaluate the efficiency of our loaded pellets as a drug carrier. Microcrystalline cellulose 101 (PH 301) was found to be the best agent for pellet core. The ratio of CP940 to HPC should be kept as (1:1) to achieve high bioadhesion. When the amount of Surelease ® was from 16% to 20% and of Eudragit ® S100 was 28%, the dissolution profiles of coated pellets revealed no drug release in the artificial gastric fluid (pH 1.0) within 2 h and less than 10% was released in phosphate buffer (pH 6.0) within 2 h whereas complete dissolution was observed in colonic fluid of pH 7.4 for 20 h. The animal experiment showed that 5-ASA loaded colon adhesive pellets had optimal therapeutic effect. We showed a novel approach to prepare effective bioadhesive pellets as colon targeted drug delivery system .
研究领域:
药剂学
·
消化病学
✓ 已验证
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
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2020
·
IF 4.545
Zhenhua Chen,Teng Zhao,Liangliang Zhou,Jinjin Kang,Yongmei Guan,Ming Yang,Shilin Yang,Hongning Liu
Based on the anti-ulcerative colitis (UC) effect of total saponins of Pulsatilla (PTS), a pH dependent colonic targeting particle design powder of PTS was prepared. The core-shell composite particle design powder of PTS was prepared with pH sensitive polymer material Eudragit S100 superfine powder as shell and the drug as core. The release of PTS composite particle design powder was increased in the artificial colon fluid and decreased in the artificial stomach and small intestine fluid. In this paper, the release performance of Pulsatilla saponin D in PTS and the ulcerative colitis model induced by TNBS in rats were used to evaluate the targeting of PTS composite particle design powder in colon. The results showed that the content of Pulsatilla saponin D in colon tissue was significantly higher than that of the original drug group after oral administration of PTS composite particle design powder. The solubility of Pulsatilla saponin D in colon tissue was also higher than that in the stomach and small intestine. The peak time and retention time in vivo were prolonged, and the maximum blood concentration was decreased (C max ). The effect of colonic targeting powder of PTS (50 mg/kg)on anti-ulcerative colitis induced by TNBS in SD rats was better than the original drug (200 mg/kg). Therefore, it is a great significance to make the PTS into colon targeted preparation for improving bioavailability, efficacy and reducing gastrointestinal stimulation.
研究领域:
药剂学
·
药物递送
·
药理学
·
结直肠疾病
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2024
·
IF 4.8
Dandan Zhang,Hao Wan,Ran Zhao,Yu Zhang,Hong Chen
The therapeutic effect of 5-amino salicylic acid (5-ASA), a first-line therapeutic agent for the treatment of ulcerative colitis (UC), is limited by the modest bioavailability afforded by its oral administration. In this study, a 5-ASA oral delivery system was developed using Eudragit S100-coated iron oxide-chitosan nanocomposites (ES-IOCS/5-ASA) to address this issue. According to drug release studies in vitro, ES-IOCS/5-ASA only released a small amount of drug in simulated gastric fluid with a pH of 1.2. However, in a medium with a pH of 7.5, a relatively rapid and complete release was noted. 5-ASA-loaded iron oxide-chitosan nanocomposites (IOCS/5-ASA) could be effectively taken up by NCM460 cells and performed better anti-inflammatory effects than free 5-ASA. At the same time, IOCS/5-ASA improved barrier damage in DSS-induced NCM460 cells. In vivo models of dextran sulphate sodium (DSS)-induced colitis were used to assess the therapeutic efficacy of oral administration of ES-IOCS/5-ASA. ES-IOCS/5-ASA significantly relieved DSS-induced colitis and enhanced the integrity of the intestinal epithelial barrier. ES-IOCS/5-ASA also reduced the expression of NLRP3, ASC and IL-1β. Additionally, iron oxide nanoparticles used as nanozymes could alleviate inflammation. In summary, this study indicates that ES-IOCS/5-ASA exert anti-inflammatory effects on DSS-induced colitis by improving intestinal barrier function and inhibiting NLRP3 inflammasome expression, presenting a viable therapeutic choice for the treatment of UC.
研究领域:
药学
·
纳米技术
·
炎症性肠病
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
International Journal of Pharmaceutics-X
·
2025
·
IF 6.4
Jie-Zhou,Tian-Le Li,Bo-Wei,Yue-Feng Ruan,Ye-Qin Wang,Jiao-Yan Liu,Meng-Meng Song,Yu-Xian Shen
Midbrain astrocyte-derived neurotrophic factor (MANF) is a secreted protein induced by endoplasmic reticulum stress. Previous studies have indicated that intravenous administration of 1 mg/kg/day recombinant human MANF protein with His tag (His-MANF) for 3 days can ameliorate acute ulcerative colitis in mice. However, long-term intravenous therapy has many disadvantages. In this paper, His-MANF protein was successfully encapsulated into alginate and hyaluronic acid hybrid hydrogel microcapsules in one step using the gas shear method and then coated by Eudragit S100 to construct an oral colon-targeted delivery system (MSH@E). The MSH@E microcapsules exhibited controlled and sustained release behavior and colon-targeting properties. Both fluorescent imaging and immunohistochemistry staining results showed that His-MANF protein could accumulate in the colitis colon for a longer residence time after oral delivery. In vivo studies demonstrated that oral administration of MSH@E microcapsules could alleviate DSS-induced colitis in mice without systemic toxicity. Importantly, even if the oral His-MANF dose was half of the intravenous His-MANF dose, oral delivery was still much more effective than intravenous injection, suggesting the development of the oral colon-targeted delivery system (MSH@E) has great significance and makes a breakthrough from intravenous to oral administration for His-MANF treatment of ulcerative colitis (UC).
研究领域:
药剂学
·
胃肠病学
·
药物递送系统
·
生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2023
·
IF 10.8
Hongbing Liu,Muse Ji,Yuti Bi,Peifu Xiao,Jiansong Zhao,Jingxin Gou,Tian Yin,Haibing He,Huaiwei Ding,Xing Tang,Yu Zhang
Excessive reactive oxygen species (ROS) and stressed inflammatory response are major characteristics of ulcerative colitis , which cause disease progression and aggravation. Herein, a novel mesoporous cerium oxide nanozymes (MCN) was designed and then loaded with Myeloid differentiation factor-88 (MyD88) inhibitor for synergistic treatment of colitis by scavenging ROS and regulating inflammation. This innovative MCN with average particle size of 200.7 nm , specific surface area of 119.78 m 2 /g and mesopores of 4.47 nm not only exhibited excellent SOD-like and CAT-like activities to scavenge ROS but also could act as a carrier to load MyD88 inhibitor, TJ-M2010–5, (abbreviated as TJ-5) into their mesopores, achieving the effect of ‘two birds with one stone’. Besides, the modification of dextran sulfate sodium (TJ-5/MCN/DSS) increased the internalization of nanozymes into activated macrophages and enhanced in vitro anti-inflammatory ability. To enhance colon targeting, we coated TJ-5/MCN/DSS with the enteric material Eudragit S100 , preventing premature release or absorption of the drug in the gastrointestinal tract after oral administration. The results demonstrated that TJ-5/MCN/DSS/Eudragit not only achieved delayed drug release and improved colon targeting but also exhibited optimal therapeutic efficacy in colitis mice. Mechanistically, the MCN-mediated ROS scavenging and TJ-5-mediated MyD88 blockade synergistically inhibited the NF-κB signaling pathway, thereby reducing the inflammatory response. Importantly, TJ-5/MCN/DSS/Eudragit did not induce systemic toxicity. In conclusion, our work not only presents a novel carrier capable of scavenging ROS but also provides proof of concept for the synergistic treatment of colitis using this carrier in combination with MyD88 inhibitors. This study proposes a safe and efficient strategy for targeting ROS-associated inflammation.
研究领域:
药学
·
纳米技术
·
炎症性肠病
·
药物递送系统
·
生物医学工程
✓ 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）