Brazilian Journal of Pharmaceutical Sciences
·
2019
·
IF 0.512
Guo Jian,Fang Huihui,Gui Shuangying,Huang Yuzhe
The intent of the present investigation is to develop and evaluate colon-specific coated tacrolimus solid dispersion pellet (SDP) that retards drug release in the stomach and small intestine but progressively releases in the colon. Tacrolimus-SDP was prepared by extrusion-spheronization technology and optimized by the micromeritic properties including flowability, friability, yields and dissolution rate. Subsequently, the pH-dependent layer (Eudragit L30D55) and time-dependent layer (Eudragit NE30D and L30D55) were coated on the SDP to form tacrolimus colon-specific pellets (CSP) using a fluidized bed coater. Under in vitro gradient pH environment, tacrolimus only released from CSP after changing pH to 6.8 and then quickly released in the phosphate buffer solution of pH 7.2. The Cmax of CSP was 195.68 ± 3.14 ng/mL at Tmax 4.5 ± 0.24 h where as in case of SDP, the Cmax was 646.16 ± 8.15 ng/mL at Tmax 0.5 ± 0.03 h, indicating the ability of CSP targeted to colon. The highest area under the curve was achieved 2479.58 ± 183.33 ng·h/mL for SDP, which was 2.27-fold higher than tacrolimus suspension. However, the best biodistribution performance was achieved from CSP. In conclusion, SDP combining of pH- and time-dependent approaches was suitable for targeted delivery of tacrolimus to colon.
研究领域:
药剂学
·
药物递送系统
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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,Lin Xia,Du Xuli,Geng Sicong,Li Hongren,Sun Hong,Tang Xing,Xiao Wei
In this work, we designed and developed a delivery system composed of enteric Eudragit L100-cysteine/reduced glutathione nanoparticles (Eul-cys/GSH NPs) for oral delivery of insulin. First, interactions between Eul-cys and mucin glycoproteins, which are believed to be the result of disulfide bonds, were confirmed using rheology experiments. Subsequently, the insulin-loaded Eul-cys/GSH NPs were prepared by the diffusion method using the rich gel network multipore structure at the surface of the Eul-cys when the pH was higher than the p K a of Eul-cys polymer. The Eul-cys/GSH NPs obtained were characterized by dynamic light scattering, transmission electron microscopy, and atomic force microscopy. The results obtained showed that the average particle size ranged from 240 to 280 nm, and the particles were almost spherical in shape. The in vitro drug release results showed that the Eul-cys/GSH NPs retained a large amount of insulin in simulated gastric fluid, while a significant insulin release was found in simulated intestinal fluid. The in situ release study suggested that NPs released a greater amount of FITC-insulin (49.2 %) into the intestinal mucus layer compared with that of FITC-insulin solution (16.4 %), which facilitating insulin delivery through the intestinal mucosa. Eul-cys/GSH NPs exhibited promising mucoadhesive properties demonstrated using an in vitro cell model. Consequently, NPs were introduced into the ileum loop of healthy rats, thus enhancing the intestinal absorption of insulin and providing a prolonged reduction in blood glucose levels. These results suggest that Eul-cys/GSH NPs may be a promising delivery system for the treatment of diabetes.
研究领域:
药剂学
·
生物医学工程
·
糖尿病治疗
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DOI
高影响因子
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
·
2021
·Vol. 37
·期 3
·443-449
·
IF 1.307
Wang Yibin,Tian Liang,Zhu Tianhao,Mei Jing,Chen Zezhong,Yu Deng-Guang
B oth electrospinning apparatus and their commercial products are extending their applications in a wide variety of fields. However, very limited reports can be found about how to implement an energy-saving process and in turn to reduce the production cost. In this paper, a brand-new type of coaxial spinneret with a solid core and its electrospinning methods are developed. A novel sort of medicated Eudragit/lipid hybrid nanofibers are generated for providing a colon-targeted sustained release of aspirin. A series of characterizations demonstrates that the as-prepared hybrid nanofibers have a fine linear morphology with the aspirin/lipid separated from the matrix Eudragit to form many tiny islands. In vitro dissolution tests exhibit that the hybrid nanofibers are able to effectively prevent the release of aspirin under an acid condition (8.7%±3.4% for the first two hours), whereas prolong the drug release time period under a neutral condition(99.7±4.2% at the seventh hour). The energy-saving mechanism is discussed in detail. The prepared aspirin-loaded hybrid nanofibers can be further transferred into an oral dosage form for potential application in countering COVID-19 in the future.
研究领域:
药学
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纳米技术
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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
·
2026
·
IF 7.9
Yu Chen,Bo Liu,Xiaoyu Zhang,Rong Xie,Jiayang Li,Jie Qu,Wei Wei,Yuqi Sun
Diabetic retinopathy, a leading cause of vision impairment, is characterized by pathological retinal neovascularization driven by chronic hyperglycemia. Current treatments, including laser therapy and intravitreal injections, are invasive, limiting patient compliance. To address these challenges, we developed Eudragit RL (EUD)-coated hyaluronic acid (HA)-bovine serum albumin (BSA) nanoparticles (HB㊏EUD) loaded with sorafenib (SFB@(HB㊏EUD)) for targeted ocular drug delivery. The nanoparticles were prepared using an emulsification-evaporation thermal cross-linking method assisted by electrostatic interaction, yielding spherical particles of uniform size, with a particle size of 242.2 ± 1.9 nm (PDI = 0.19). The EUD coating significantly altered the nanoparticles' surface, transitioning the zeta potential from −40.6 ± 0.9 mV to −20.6 ± 0.5 mV. This change indicated a reduction in overall negative charge density and potential exposure of positively charged functional groups, facilitating electrostatic interactions with ocular mucin and prolonging corneal retention. Compared to unmodified nanoparticles, SFB@(HB㊏EUD) exhibited a 1.55-fold improvement in transcorneal transport and a 2.46-fold higher vitreous accumulation. In the chick chorioallantoic membrane assay, a 17.33% reduction in neovascularization was observed, further demonstrating the potent anti-angiogenic effects. In streptozotocin (STZ)-induced DR mice, treatment with SFB@(HB㊏EUD) via topical eye drops significantly reduced vascular leakage, preserved retinal structure, and suppressed vascular endothelial growth factor (VEGF) expression by 32.1%, outperforming non-functionalized nanoparticles. Fundus imaging and fluorescein angiography confirmed restored retinal perfusion and minimal vascular abnormalities. These findings highlight the potential of SFB@(HB㊏EUD) as a non-invasive, targeted therapy for DR, leveraging EUD's mucoadhesive properties and sorafenib's anti-angiogenic activity.
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DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2018
·
IF 3.997
Heyu Li,Kailin Liu,Gareth R. Williams,Junzi Wu,Jianrong Wu,Haijun Wang,Shiwei Niu,Li-Min Zhu
We report a dual-responsive drug delivery system prepared by electrospinning. Blend fibers of poly(N-vinylcaprolactam) (PNVCL) and ethyl cellulose (EC) were first prepared, with the aim of developing thermoresponsive sustained release formulations. Eudragit L100-based fibers were then generated to yield pH-sensitive materials. Attempts to produce three-polymer fibers of EC , PNVCL and Eudragit were unsuccessful, and therefore hybrid mats containing two fiber populations (one made of PNVCL/EC, one comprising Eudragit) were instead fabricated by twin-jet electrospinning. Analogous drug-loaded versions of all the formulations were also prepared containing ketoprofen (KET). The fibers were largely smooth and homogeneous, and the addition of KET did not affect their morphology. The PNVCL-containing fiber mats changed from being hydrophilic to hydrophobic when the temperature was increased through the lower critical solution temperature of 33 °C. In vitro drug release profiles showed that the hybrid fiber mats were able to combine the properties of the three polymers, exhibiting both pH-sensitive and thermosensitive properties with sustained release. In addition, they were found to be nontoxic and suitable for cell growth. This study therefore demonstrates that PNVCL/EC/KET-Eudragit/KET multicomponent fiber mats comprise effective and biocompatible materials for targeted drug delivery.
研究领域:
药剂学
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材料科学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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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
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
·
2024
·
IF 3.7
Anqi Wang,Yuanyuan Liu,Wugui Xiong,Wei Li,Jin Li,Zhiqiang Yang,Zhongtao Zou,Yinjia Luo,Zhoujiang Chen,Hanmei Li,Chi Teng Vong,Liang Zou
Honokiol (HNK) is one of the bioactive ingredients from the well-known Chinese herbal medicine Magnolia officinalis , and its research interests is rising for its extensive pharmacological activities, including novel therapeutic effect on ulcerative colitis (UC). However, further application of HNK is largely limited by its unique physicochemical properties, such as poor water solubility, low bioavailability, as well as unsatisfied targeting efficacy for inflammatory lesions. In this study, we constructed galactosylation modified PLGA nanoparticles delivery system for efficient target delivery of HNK to the colitic lesions, which could lay a research foundation for the deep development of HNK for the treatment of UC. D-galactose was grafted by chemical coupling reactions with PLGA to prepare Gal-PLGA, which was used as a carrier for HNK (Gal-PLGA@HNK nanoparticles (NPs)). To improve the colon targeting efficiency by oral administration of the NPs, Eudragit S100 was used for wrapping on the surface of Gal-PLGA@HNK NPs (E/Gal-PLGA@HNK NPs). Our results showed that the encapsulation efficiency and drug loading capacity of E/Gal-PLGA@HNK NPs were 90.72 ± 0.54% and 8.41 ± 0.02%, respectively. Its average particle size was 242.24 ± 8.42 nm, with a PDI value of 0.135 ± 0.06 and zeta-potential of -16.83 ± 1.89 mV. The release rate of HNK from E/Gal-PLGA@HNK NPs was significantly decreased when compared with that of free HNK in simulated gastric and intestinal fluids, which displayed a slow-releasing property. It was also found that the cellular uptake of E/Gal-PLGA@HNK NPs was significantly increased when compared with that of free HNK in RAW264.7 cells, which was facilitated by D-galactose grafting on the PLGA carrier. Additionally, our results showed that E/Gal-PLGA@HNK NPs significantly improved colonic atrophy, body weight loss, as well as reducing disease activity index (DAI) score and pro-inflammatory cytokine levels in UC mice induced by DSS. Besides, the retention time of E/Gal-PLGA@HNK NPs in the colon was significantly increased when compared with that of other preparations, suggesting that these NPs could prolong the interaction between HNK and the injured colon. Taken together, the efficiency for target delivery of HNK to the inflammatory lesions was significantly improved by galactosylation modification on the PLGA carrier, which provided great benefits for the alleviation of colonic inflammation and injury in mice.
研究领域:
药学
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纳米技术
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药物递送系统
·
炎症性肠病
✓ 已验证
产品关联
DOI
PubMed
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
BIOMEDICINE & PHARMACOTHERAPY
·
2023
·
IF 7.5
Guohui Xue,Huifang Xiong,Shixiu Wang,Yingjun Fu,Yong Xie
Objective Tripterygium glycoside (TG) is a fat-soluble extract of Tripterygium wilfordii, with anti-inflammatory properties associated with TLR signaling pathways. This study constructed a targeted delivery system for experimental colitis, namely, eudragit (EuL)-coated chitosan (Ch)-TG conjugate microspheres (Ch-TG-MS/EuL), and evaluated its therapeutic efficacy and underlying mechanisms. Methods Ch-TG-MS was fabricated using emulsification cross-linking technique and then coated with EuL to create Ch-TG-MS/EuL. Drug release properties were assessed using a dialysis model. Additionally, the therapeutic benefits of Ch-TG-MS/EuL on colonic inflammation and its specific effect on TLR4/NF-κB signaling in intestinal mucosa were evaluated in vivo using a DSS-induced murine colitis model. Results The Ch-TG-MS/EuL microspheres appeared as yellow powders with a slightly enlarged shape, rough surface, and adhesions. The Ch-TG-MS/EuL formulations also exhibited high entrapment efficiency and drug loading rate. High-performance liquid chromatography revealed that Ch-TG-MS/EuL exhibited a less intense peak than free TG, confirming that the drug is contained within the formulation. Free TG displayed explosive release within the first 5 h of administration, while Ch-TG-MS/EuL prevented the pre-mature release of TG and exhibited controllable release up to 24 h. In vivo, noticeable amelioration of intestinal mucosal tissue destruction was achieved with Ch-TG-MS/EuL compared to free TG. Additionally, immunohistochemical and western blotting results revealed that Ch-TG-MS/EuL markedly down-regulated the expression of intestinal mucosal TLR4, MyD88, and NF-κB p65. Hence, Ch-TG-MS/EuL may ameliorate the colon inflammatory response by inhibiting the hyperactivation of TLR4/NF-κB signaling. Conclusion Novel Ch-TG-MS/EuL preparation may represent a colonic delivery system for UC therapeutics by inhibiting TLR4/NF-κB hyperactivation. Data availability All experimental data supporting the conclusions of this study are available from the corresponding author on reasonable request.
研究领域:
药学
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药理学
·
免疫学
·
药物递送系统
·
炎症性肠病
✓ 已验证
DOI
PubMed
高影响因子
SOLAR ENERGY MATERIALS AND SOLAR CELLS
·
2014
·
IF 5.03
Changzhong Chen,Xiaodi Liu,Wenmin Liu,Mengfei Ma
In this work, the influence of type of supporting materials on the performance of form stable phase change materials (FSPCMs) was investigated. Two kinds of FSPCMs containing myristic acid (MA) were prepared using an inorganic material (bentonite) and a polymer (Eudragit L100) individually as the supporting material. The morphology, composition, crystalline properties, phase transition properties and heat storage/release performances of MA/bentonite FSPCMs (abbreviated as FSPCM-B) and MA/Eudragit L100 FSPCMs (abbreviated as FSPCM-E) were researched comparatively. The results show that the maximum MA content of FSPCM-B and FSPCM-E without melt MA leakage is 50 wt% and 70 wt%, respectively. All the prepared FSPCMs have good thermal reliability and reusability , and phase transition enthalpies of FSPCM-B are obviously lower than those of FSPCM-E with the same MA mass fraction. Due to the high thermal conductivity of bentonite, the heat transfer rate of FSPCM-B is exactly higher than that of FSPCM-E. This study will provide insights into the design and application of FSPCMs with inorganic matrix and polymeric matrix .
研究领域:
材料科学
·
储能技术
·
热工工程
✓ 已验证
DOI
高影响因子
FOOD HYDROCOLLOIDS
·
2025
·
IF 12.4
Yangrui Wang,Yingxue Yue,Shengjun Yang,Sufang Duan,Yuning Yang,Zhaozhi Wang,Xuetong Li,Bailiang Li,Yupeng Wang
Probiotics, which play a crucial role in regulating intestinal homeostasis and maintaining host health, face significant challenges in maintaining their survival rate after processing, storage, and oral administration, posing a substantial hurdle in probiotic use. In this study, electrospinning technology was employed to prepare polyvinyl alcohol (PVA)/Pullulan (PUL) nanofibers and Eudragit® S100 (ES100)/PVA/PUL core-shell nanofibers. The effects of different PVA, PUL, and ES100 solution concentrations, applied voltage, collector distance, and feed rate on the morphology and diameter of nanofibers were investigated by scanning electron microscopy. The fibers were characterized using fourier transform infrared spectroscopy, X-ray diffraction, and thermal analysis. Additionally, the storage stability and resistance to gastrointestinal stress of the nanofibers loaded with Lactiplantibacillus plantarum KLDS1.0386 were investigated. The results indicate that the prepared PVA/PUL nanofibers and ES100/PVA/PUL core-shell nanofibers exhibit smooth surfaces, uniform diameters, and excellent thermal stability. Compared with free L. plantarum KLDS1.0386, the survival rate of PVA/PUL nanofiber-encapsulated bacteria increased by 25.07% after 21 days of storage at 4 °C and by 33.21% at 25 °C, respectively. Experiments simulating gastrointestinal digestion showed that the survival rates of PVA/PUL nanofibers and ES100/PVA/PUL nanofiber-coated L. plantarum KLDS1.0386 were 9.11% and 15.73% higher in simulated gastric juice compared to free L. plantarum KLDS1.0386, respectively. Additionally, 13.15% and 13.92% higher in simulated intestinal fluid, respectively. The nanofibers prepared in this study can be used as delivery carriers for probiotics. They enhance the storage stability and improve the tolerance of probiotics to the harsh gastrointestinal environment.
研究领域:
生物技术
·
食品科学
·
材料科学
✓ 已验证
产品关联
DOI
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
危险品化学品经营许可证（带存储）