International Journal of Pharmaceutics-X
·
2025
·
IF 6.4
Huaan Li,Bohan Lin,Shuangwu Wang,Ying Zhang,Zeming Zhou,Dingsheng Wen,Zhifeng Zhang,Xiaohua Feng,Lu Wen,Jun He,Gang Chen
Hearing loss, a global health concern, significantly impacts patients with delayed language development, impaired neurocognitive function, and severe social problems. The main cause is the cochlear hair cell damage induced by oxidative stress and inflammation from ototoxic drugs, noise exposure or diabetes. Glycyrrhizic acid (GA), derived from edible herb licorice, is widely utilized in traditional Chinese medicine and clinical treatments for liver diseases. However, its potential in preventing hearing loss remains largely unexplored. Herein, we propose GA as a novel otoprotective agent and demonstrate its capability to prevent hearing loss. Our results show that GA effectively reduces oxidative stress and inflammation induced by cisplatin, aminoglycosides, or even noise and diabetes, thereby protecting cochlear hair cells. In hearing loss models, two commonly used administration methods were compared, with tympanic injection providing better protective effects than oral administration of GA. To enhance oral bioavailability, GA is employed as both the medicine and excipient, and formulated into micelles with curcumin, another extensively used bioactive compound. Interestingly, formulation parameters such as feeding ratio and temperature have little impact on micelle size but significantly affect the drug loading efficiency. The carrier-free strategy can achieve a high drug loading capacity and significantly increase the drug concentration in blood, offering improved preventive efficacy. Notably, the micelles also exhibit protection on kidneys and liver, and do not compromise the antitumor activity of cisplatin. Therefore, GA holds promise as an otoprotective candidate, with potential clinical applications for oral prophylaxis of hearing loss using the micellar formulation.
研究领域:
药理学
·
耳科学
·
纳米医学
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DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2018
·
IF 8.097
Xiao-Ling Xu,Kong-Jun Lu,Meng-Lu Zhu,Yang-Long Du,Ya-Fang Zhu,Nan-Nan Zhang,Xiao-Juan Wang,Xu-Qi Kang,De-Min Xu,Xiao-Ying Ying,Ri-Sheng Yu,Chen-Ying Lu,Jian-Song Ji,Jian You,Yong-Zhong Du
Both targeted and stimuli-sensitive drug-delivery systems (DDSs) have been developed to augment antitumor effects. However, lack of knowledge regarding tumor tissue targeting and different effects of the stimuli-sensitive DDSs in orthotropic and ectopic tumors have impeded further advances in their clinical applications. Herein, we first reported a pH-triggered micelle with sialic acid (SA)-driven targeting ability (SA–poly(ethylene glycol)–hydrazone linker-doxorubicin (DOX), SPD). The SPD micelles encapsulated with DOX (SPDD) showed sustained drug release over 48 h in response to the pH gradient in vivo, slow under physical conditions and accelerated in the acid tumor microenvironment. In addition, the SPD micelles showed 2.3-fold higher accumulation in tumors after 48 h compared to the micelles lacking the SA moiety. The overexpression of E-selectin on the inflammatory vascular endothelial cells surrounding the tumors increased the accumulation of SPD micelles in tumor tissues, whereas that on the tumor cells increased the internalization of micelles. Consequently, SPDD micelles exerted remarkable antitumor effects in both orthotopic and ectopic models. Application of SPDD micelles in the in situ model reduced the tumor volume (77.57 mm3 vs 62.13 mm3) and metastasis after treatment for 25 days. These results suggest that SA-driven targeted DDS with a pH-responsive switch has the potential to treat hepatocarcinoma effectively both ectopically and orthotopically.
研究领域:
药剂学
·
肿瘤学
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DOI
PubMed
高影响因子
TALANTA
·
2019
·
IF 4.916
Xiaoyu Song,Rui Zhang,Yue Wang,Mengqing Feng,Honghua Zhang,Shuling Wang,Jun Cao,Tian Xie
A direct on-line complexion combined with micelle to solvent stacking method was proposed for simultaneous determination of metal ions by capillary electrophoresis coupled diode array detector. During the experiment, a plug of complexing agent was first injected to the inlet of capillary, followed by introducing the micelle-bound metal ions. Then the metal ions produced a micelle-to-solvent stacking effect and interacted with the complexing agent under a positive voltage. Continued application of voltage, the analytes were effectively focused and separated in the capillary zone electrophoresis . Repeatability was ranged from 1.89% to 1.94% for the migration time. The detection limits were 2.66–27.9 ng mL -1 for Ni 2+ , Co 2+ , Cu 2+ , Hg 2+ and Cd 2+ . Furthermore, the developed method showed a great potential for the determination of metal ions in the crayfish, beebread and Dendrobium officinale samples.
研究领域:
分析化学
·
环境科学
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DOI
PubMed
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 56
·32193-32199
·
IF 2.936
Yiyuan Tang,Kai Chen,Jiacheng Li,Yuhong Feng,Gaobo Yu,Longzheng Wang,Xinyu Zhao,Yang Peng,Quan Zhang
In this study, a pH-responsive amphiphilic alginate (Ugi-Alg) was synthesized via Ugi reaction without using a catalyst. The structure of Ugi-Alg was confirmed by FT-IR and 1H NMR spectroscopy. Amphiphilic alginate can form micelles in an aqueous medium due to it's amphiphilic nature.. The impacts of Na+ concentration and pH on the micelle size were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The dynamic light scattering observations showed that micelle size increases with the decrease in Na+ concentration in aqueous solution. However, the micelle size decreases first and then increases as the pH value decreases from 5.3 to 2.0. Transmission electron microscopy confirmed that the mean size of micelles is 30–200 nm. In addition, a model hydrophobic pesticide (acetamiprid) was loaded in the micelles. The encapsulation efficiency and release behavior of micelles were studied, which could be controlled by Na+ concentration and pH. The results indicated that encapsulation efficiency of acetamiprid increases from 55% to 96% due to the increase in Na+ concentration from 0.01 M to 0.3 M. Moreover, with the decrease in pH from 5.3 to 2.0, encapsulation efficiency increases from 55% to 80%. Furthermore, the data of acetamiprid release kinetics could be well-fitted by the Weibull model.
研究领域:
材料科学
·
环境科学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2019
·
IF 4.784
Mei Zhang,Sajid Asghar,Xin Jin,Ziyi Hu,Qineng Ping,Zhipeng Chen,Feng Shao,Yanyu Xiao
A micelle system based on hyaluronic acid (HA)-octadecylamine (OA) conjugate (HOA) functionalized with N -acetylcysteine (NAC) was constructed to yield NAC modified HOA conjugate (NHOA) for improving oral paclitaxel (PTX) delivery (PTX-NHOA). The average size of spherical PTX-NHOA micelles was 162.7 nm with a zeta potential of −27.6 mv. The encapsulation efficiency (EE) and drug loading (DL) of PTX-NHOA micelles were 92.64% and 6.96%, respectively. Additionally, NHOA micelles exihibited significantly higher cellular uptake in comparison with HOA micelles by caveolin-mediated and clathrin-mediated endocytosis. Higher permeation ability of NHOA micelles (2.75-fold and 1.32-fold, respectively) through cell monolayers of Caco-2/HT29 cells than that of Taxol and HOA micelles were also observed. The intestinal biodistribution result showed that NAC-modified micelles could enhance its adhesion to the intestinal surface and permeate deeply within the intestinal villi. The NHOA micelles were better absorbed in the duodenum, followed by the jejunum and the ileum. In vivo pharmacokinetic studies showed that AUC 0-t value of PTX-NHOA micelles was about 5.92-fold and 2.47-fold higher compared to that of Taxol and PTX-HOA micelles, respectively. In a word, NHOA micelles is a promising drug delivery system in improving the oral absorption of insoluble drugs.
研究领域:
药剂学
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
COLLOID AND POLYMER SCIENCE
·
2013
·Vol. 292
·期 1
·153-161
·
IF 2.161
Liu Jingcheng,Luo Jing,Liu Ren,Jiang Jinqiang,Liu Xiaoya
Photosensitive copolymer P(St- alt -MAn)- co -P(VM- alt -MAn) was synthesized and employed to disperse multi-wall carbon nanotubes (MWCNTs). It was found that copolymer could form micelles in aqueous solution and adsorb onto the surface of MWCNTs to produce micelle-encapsulated MWCNTs (e-MWCNTs) by in situ photo crosslinking after irradiation with ultraviolet light and a stable suspension of e-MWCNTs in aqueous solution was obtained. When deposited onto polyaniline (PANI)-modified glassy carbon electrodes, a thin film of e-MWCNTs composite was obtained and the performance of the e-MWCNTs/PANI electrode toward dopamine was then evaluated. The experimental results suggest that the hybrid film modified electrode exhibits a dramatic electrocatalytic effect on the oxidation of dopamine (DA), as evidenced by a marked enhancement of the current response. A series of CVs was obtained by modified glassy-carbon electrodes with different size of micelles was also researched. The result shows that the peak current increased with the increasing size of micelles. A linear calibration plot was obtained in a wide range of 1.0 × 10 −7 –1.0 × 10 −3 M and the detection limit was 5.0 × 10 −8 M. In addition, the interference from ascorbic acid (AA) was effectively suppressed due to the presence of the negatively charged carboxylate groups of copolymer on the outside of MWCNTs which repels AA anions and provides a transport channel only for DA cations.
研究领域:
材料科学
·
分析化学
·
生物医学工程
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DOI
高影响因子
Polymer Chemistry
·
2015
·Vol. 7
·期 4
·899-904
·
IF 5.52
Kaikai Ding,Liyan Shi,Ling Zhang,Tian Zeng,Yihua Yin,Ying Yi
A novel amphiphilic polymer–pesticide conjugate was synthesized by conjugation of PEG with the photolabile o-nitrobenzyl group followed by grafting dichlorophenoxyacetic acid (2,4-D), which can self-assemble into photoresponsive micelles in aqueous solutions for a controlled release of the herbicide. 1H NMR and FT-IR confirmed the structure of the synthesized conjugate. TEM observations showed that the micelles had a core–shell configuration. DLS and TEM measurements showed that the average diameters of the micelles decreased by about 40 nm after 365 nm UV irradiation. 1H NMR and UV-Vis studies confirmed that the photoresponse may be ascribed to the photolytic cleavage of o-nitrobenzyl as the connecting arm in the polymeric chain. No release of the micelles was detected without light, while the cumulative release rate from the micelles increased gradually upon solar-simulating radiation, reaching 99.6% in 8 h.
研究领域:
材料科学
·
农业科学
·
高分子化学
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产品关联
DOI
高影响因子
JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2021
·Vol. 102
·期 7
·2651-2659
·
IF 3.639
Tongtong Zhang,Khaing zar Myint,Yongmei Xia,Jing Wu
BACKGROUND Rebaudioside A (RA) and its monoglucosyl derivative, as like rebaudioside D (RD) are the most popular stevia glycosides but possess poor solubility in water, which limited their application as edible surfactants, the applications as in micellar solubilization and drug delivery. Meanwhile, effect of the monoglucosyl attached to RA moiety remains unclear. RESULTS Monoglucosyl rebaudioside A (RAG1) was synthesized via hydrolyzing the transglycosylation product of RA with 95% of RA converted. RAG1 content in raw reaction mixture was as high as 69.5% of total glycosides, and harvested with a content of 88.2% by simple filtration. The RAG1 exhibited an aqueous solubility of 87 folds of RA or 391 folds of RD at 25 °C. The surface activity of RAG1 solution was higher than RA and invincible to RD. The RAG1 micelles promoted aqueous solubility of idebenone (IDE) up to 500 folds higher at 25 °C. The cumulative release rate of IDE encapsulated in RAG1 micelles was 777.5% or 456.7% higher of that of free IDE in simulated gastric/intestinal fluids in 14 h, respectively. The RAG1-IDE remained the same in 98 days at 25 °C. CONCLUSION The α-linked glucosyl to RA induced higher hydrophilicity and surface activity than that resulted by β-linked glucosyl, making RAG1 not only dramatically raise the aqueous solubility of RA, but also endow IDE folds higher in bioaccessibility, yet making the capsule stable at storage. The results would provide a new edible delivery nanocarrier for encapsulation of hydrophobic bioactive components. © 2021 Society of Chemical Industry.
研究领域:
食品科学
·
药剂学
·
化学工程
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产品关联
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2011
·
IF 3.463
Xiujuan Huang,Yan Xiao,Meidong Lang
Micelles/sodium-alginate composite gel beads (micelles/SA beads) were constructed from SA matrix and indomethacin (IND) loaded six-arm block copolymer poly( ɛ -caprolactone)- block -(dimethylamino)ethyl methacrylate (S(PCL- b -PDMA) 6 ) micelles. The morphology, swelling property and drug loading level of the beads were investigated. The release behavior of IND from three matrices including micelles, SA beads and micelles/SA beads was evaluated at pH 1.2, 6.8 and 7.4, as well as in the simulated gastrointestinal (GI) tract. Significant differences in the release of IND from each matrix were observed in the acidic and near neutral pH fluids. The results suggested that IND could be protected by the micelles/SA beads from being released under acidic conditions in the stomach and would be mainly delivered to the small intestine and the colon. The release behavior was dependent on the initial concentrations of SA and calcium chloride (CaCl 2 ) due to the different crosslinking densities. The results demonstrated that these micelles/SA beads could represent a promising oral drug delivery system for drugs with poor water solubility.
研究领域:
药剂学
·
材料科学
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
·
2018
·Vol. 20
·期 10
·1-11
·
IF 2.127
Feng Runliang,Deng Peizong,Zhou Feilong,Feng Sijia,Song Zhimei
To overcome honokiol’s poor water solubility and investigate its antifungal activity and pharmacokinetic property, Pluronic® F-127 (F127)-cyclodextrin conjugate was synthesized and employed to prepare honokiol-loaded micelles through emulsion-solvent evaporation method. The drug-loaded micelles were obtained with 92.30 ± 3.28% of encapsulation efficiency being higher than that obtained from F127 due to additional cyclodextrin inclusion. Fourier transformation infrared spectrometry and diffraction scanning calorimetry analysis tests demonstrated that honokiol was successfully encapsulated into the conjugate micelles in the amorphous or solid solution state because of their interactions. Meanwhile, in vitro antifungal activity experiment indicated that the MIC 90 of drug-loaded micelles was 64 μg/mL, showing the same antifungal activity as pure honokiol although it obviously retarded honokiol’s release. In vivo pharmacokinetic results confirmed that in vivo area under curve and apparent distribution volume of honokiol in drug-loaded micelles were 2- and 1.69-folds higher than that for pure honokiol, with its obvious prolonged mean retention time and half-life period, respectively. The clearance rate of honokiol was also shortened about 2-fold in comparison with pure honokiol when encapsulated into the micelles. These results suggest that the developed F127-cyclodextrin micellar formulation is a promising drug delivery system for antifungal drugs.
ᅟ
研究领域:
药剂学
·
生物医学
·
药物递送系统
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产品关联
DOI
高影响因子
Nano Research
·
2016
·Vol. 9
·期 12
·3828-3838
·
IF 8.893
Li Zhixiong,Liang Ruizheng,Xu Simin,Liu Wendi,Yan Dongpeng,Wei Min,Evans David G.,Duan Xue
Fluorescence resonance energy transfer (FRET) systems have broad applications in visual detection, intelligent materials, and biological imaging, all of which favor the transmission of light through multiple dimensions and in diverse directions. Herein, we have demonstrated multi-dimensional (0D and 2D) FRET within a multi-layer ultrathin film (UTF) by employing a layer-by-layer (LBL) assembly technique. The anionic block copolymer micelle poly(tert-butyl acrylate-co-ethyl acrylate-co-methacrylic acid) (PTBEM) is chosen as a molecular carrier for the incorporation of bis(8-hydroxyquinolate) zinc (Znq 2 ) and open-ring merocyanine (MC) (denoted as (Znq 2 /MC)@PTBEM). Alternatively, electrostatic assembly is performed with cationic layered double hydroxide (LDH) nanosheets (denoted as [(Znq 2 /MC)@PTBEM/LDH]
n
). This [(Znq 2 /MC)@PTBEM/LDH]
n
system offers a multi-dimensional propagation medium and ensures that the FRET donor and acceptor are located within their Förster radii in each direction. The system demonstrates a FRET process that can be switched via alternating ultraviolet/visible (UV/vis) irradiation, with tunable blue–green/red fluorescence, resulting in a FRET efficiency as high as 81.7%. It is expected that this assembly method, which uses 0D micelles on a 2D layered material, can be extended to other systems for further development of multi-dimensional FRET.
研究领域:
材料科学
·
生物成像
·
化学
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DOI
高影响因子
Food Analytical Methods
·
2015
·Vol. 9
·期 3
·699-705
·
IF 1.956
Yue Mei-E,Li Qian,Xu Jie,Jiang Ting-Fu
A rapid, simple, and sensitive method has been developed for the analysis of triazine herbicides in honey samples by using salt de-emulsification dispersive liquid-liquid microextraction and back-extraction (SD-DLLME-BE) coupled with sweeping in micellar electrokinetic chromatography (MEKC). In the newly developed method, chloroform can be generated by the reaction of chloral hydrate and sodium hydroxide, and the chloroform droplets dispersed into bulk aqueous solution can be swiftly carried to the bottom of the centrifuge tube with the addition of calcium chloride. Then, back-extraction was utilized to extract the analytes into an aqueous solution prior to capillary electrophoresis (CE) analysis. The advantages of the new in situ DLLME lie in dispersive solvent-free and no centrifugation operation compared with the conventional DLLME. Several important parameters influencing the preconcentration and extraction efficiency of SD-DLLME-BE such as sodium dodecyl sulfate (SDS) concentration, pH, chloral hydrate and sodium hydroxide content, extraction time, and calcium chloride content were optimized. Under the optimized conditions, the enrichment factors were achieved in the range from 459 to 636. The proposed method provided a good linearity, low limits of detection (8.56 ng/mL), and good repeatability of the extractions (relative standard deviations (RSDs) below 8.8 %, n = 6). Honey samples were analyzed by the proposed method, and obtained results indicated that the proposed method provides acceptable recoveries and precisions.
研究领域:
分析化学
·
食品科学
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产品关联
DOI
高影响因子