COLLOIDS AND SURFACES B-BIOINTERFACES
·
2013
·
IF 3.554
Ping Luo,Yu Luo,Jin Huang,Wei Lu,Dajun Luo,Jiahui Yu,Shiyuan Liu
In this research, a reduction-degradable supramolecular micelle delivery system of camptothecin (CPT) was developed to enhance the stability of CPT in aqueous media. Firstly, Michael addition polymerization occurred between N, N ’-bis(acryloyl) cystamine (BAC) and mono(6-(2-aminoethyl)amino-6-deoxy)-β-cyclodextrin (CDen) to produce the reduction-degradable polymer of BAC-CDen. And adamantyl-modified polyethylene glycol monomethyl ether (mPEG-Ad) was further encapsulated into it to gain supramolecular micelles of mPEG-Ad@BAC-CDen. Then mPEG-Ad@BAC-CDen/CPT supramolecular micelles could be easily obtained by incorporation of CPT into mPEG-Ad@BAC-CDen via dialysis method. The particle size of supramolecular micelles increased from 106 nm (bare micelles) to 142 nm (CPT loaded micelles), suggesting their passive targeting potential to tumor tissue. Owing to the reduction degradability of disulfide linker in main chain of BAC-CDen, the CPT could be sustainably released from the above micelles with the gradual cleavage of polymer in the presence of dithiothreitol (DTT) at the concentration of simulating the intracellular condition. It was noted that the stability of CPT in aqueous media was remarkably improved in the mPEG-Ad@BAC-CDen supramolecular micelles, which effectively protected the active lactone ring of CPT from hydrolysis under physiological condition. Besides, compared with free CPT, the CPT-loaded supramolecular micelles showed much lower cytotoxicity against L929 cell line. All these results suggested the potential utilization of the mPEG-Ad@BAC-CDen supramolecular micelles as the carriers of hydrophobic drugs with better stability and lower cytotoxicity. And the resulted anti-tumor CPT supramolecular micelles can be delivered to tumor cells with a high selectivity.
研究领域:
药剂学
·
肿瘤学
·
生物化学
✓ 已验证
DOI
PubMed
高影响因子
POLYMER
·
2017
·
IF 3.684
Pengcheng Zhang,Zhenghe Zhang,Xiaoze Jiang,Leilei Rui,Yun Gao,Weian Zhang
A biotin-functionalized amphiphilic star-shaped block copolymer , POSS-(PCL- b -PDMAEMA) 8 -biotin, with an inorganic POSS nucleus, a hydrophobic poly( ɛ -caprolactone) (PCL) middle layer, a hydrophilic poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA) outer corona was synthesized for the targeting delivery and pH-responsive release of hydrophobic pheophorbide A (PPa) photosensitizers . In aqueous solution, this amphiphilic copolymer was able to form unimolecular micelles as determined by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The biotin-functionalized unimolecular micelles were responsive to pH and further utilized in encapsulation and release of PPa for photodynamic therapy (PDT). The PPa release from PPa-loaded unimolecular micelles could be enhanced at acidic condition. Additionally, confocal laser scanning microscopy (CLSM) and flow cytometry results revealed that PPa-loaded tumor-targeted unimolecular micelles could boost the internalization rate in HeLa cells effectively. Moreover, PPa-loaded unimolecular micelles showed low dark toxicity and high PDT efficacy towards HeLa cells according to the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Thus, PPa-loaded POSS-(PCL- b -PDMAEMA) 8 -biotin would have presented the potential application in PDT.
研究领域:
材料科学与工程
·
生物医药
·
纳米医学
✓ 已验证
DOI
高影响因子
CARBOHYDRATE POLYMERS
·
2014
·
IF 3.916
Jing-Xiao Chen,Miao Zhang,Wen Liu,Guo-Zhong Lu,Jing-Hua Chen
A novel micelle based on heparosan and deoxycholic acid (DOCA) conjugate (HD) as drug carrier was reported here. As the surface was negatively charged, this micelle could resist serum adsorption, showing favorable stability. Moreover, fluorescence observation confirmed that it was able to deliver model hydrophobic drug doxorubicin (DOX) into HeLa cells efficiently. The DOX-loaded micelles showed sustained release behavior at pH 7.4, and accelerated release behavior at pH 5.0 or in the presence of β-glucuronidase, which over-expressed in tumor cells. In vitro cytotoxicity assay demonstrated that the half-maximal inhibitory concentration (IC50) of DOX-loaded micelles against HeLa cells was much lower than that of COS7 cells, showing significant therapeutic distinction between tumor cells and normal cells. Combining with the good biocompatibility and biodegradability of heparosan, this micelle may be promising in clinical application for targeted drug delivery.
研究领域:
生物材料
·
药剂学
·
肿瘤学
✓ 已验证
DOI
PubMed
高影响因子
RSC Advances
·
2020
·Vol. 10
·期 50
·29668-29674
·
IF 3.119
Shuangxia Wu,Fengjie Geng,Suqin He,Wentao Liu,Hao Liu,Miaoming Huang,Chengshen Zhu
To increase the bioavailability and water solubility of hydrophobic medicine, an amphiphilic block copolymer, polycaprolactone-block-polyhydroxyethyl acrylamide (PCL-b-PHEAA), was synthesized. The copolymer can self-assemble into micelles by dialysis. The micelles were characterized by the Tyndall effect, static drop method, fluorescence spectrometry, dynamic light scattering, scanning electron microscopy and transmission electron microscopy. Ibuprofen was encapsulated inside the micelles by dialysis as a model medicine. The results show that the amphiphilic copolymer forms a uniform micelle system, with spherical micelles dispersed well in solution which have a low critical micelle concentration. In addition, the system shows good amphipathic behavior. Average particle size of a micelle is 104 nm, which increases a lot after drug loading and standing for half a month. In the first few hours, the cumulative release of the drug increases gradually; the rate of increase in the first ten hours is faster, then reaching a plateau which tends to be flat finally. It is similar under two different pH conditions. This biocompatible, biodegradable amphiphilic block copolymer has potential applications in the biomedical field.
研究领域:
生物材料
·
药剂学
·
高分子化学
✓ 已验证
DOI
PubMed
高影响因子
Science Bulletin
·
2015
·Vol. 60
·期 14
·1272-1280
·
IF 0
Lin Bingbing,Su Hongying,Jin Rongrong,Li Danyang,Wu Changqiang,Jiang Xin,Xia Chunchao,Gong Qiyong,Song Bin,Ai Hua
Multifunctional nanoparticles combining diagnostic and therapeutic agents into a single platform make cancer theranostics possible and have attracted wide interests in the field. In this study, a multifunctional nanocomposite based on dextran and superparamagnetic iron oxide nanoparticles (SPIO) was prepared for drug delivery and magnetic resonance imaging (MRI). Amphiphilic dextran was synthesized by grafting stearyl acid onto the carbohydrate backbone, and micelle was formed by the resulted amphiphilic dextran with low critical micelle concentration at 1.8 mg L −1 . Doxorubicin (DOX) and a cluster of the manganese-doped iron oxide nanoparticles (Mn-SPIO) nanocrystals were then coencapsulated successfully inside the core of dextran micelles, resulting in nanocomposites with diameter at about 100 nm. Cell culture experiments demonstrated the potential of these Mn-SPIO/DOX nanocomposites as an effective multifunctional nanoplatform for the delivery of anticancer drug DOX with a loading content (DLC) of 16 %. Confocal laser scanning microscopy reveals that the Mn-SPIO/DOX had excellent internalization ability against MCF-7/Adr cells after 2-h labeling compared with free DOX·HCl. Under a 3.0-T MRI scanner, Mn-SPIO/DOX nanocomposite-labeled cells in gelatin phantom show much darker images than the control. Their transverse relaxation ( T
2 ) rate is also significantly higher than that of the control cells (33.9 versus 2.3 s −1 ). Our result offers an effective strategy to treat MCF-7/Adr at optimized low dosages with imaging capability.
研究领域:
药剂学
·
医学影像
·
肿瘤学
✓ 已验证
DOI
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2021
·
IF 5.875
Siyu Sun,Xiyou Du,Manfei Fu,Abdur Rauf Khan,Jianbo Ji,Weidong Liu,Guangxi Zhai
In this study, galactosamine-modified poly(ethylene glycol)-poly(lactide) (Gal-PEG-PLA) polymers were synthesized and Gal-PEG-PLA/D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) micelles named as GPP micelles were designed to promote the oral absorption of a hydrophobic drug, curcumin (CUR). CUR-loaded Gal-PEG-PLA/TPGS micelles (CUR@GPP micelles) were fabricated using the thin-film dispersion method. CUR@GPP micelles had a size of about 100 nm, a near-neutral zeta potential , drug loading (DL) of 14.6%, and sustained release properties. GPP micelles with high Gal density (GPP3 micelles) were superior in facilitating uptake in epithelial cells and improving intestinal permeation. In situ intestinal absorption studies suggested that the jejunum and ileum were the best absorption segments in the intestinal tract. Additionally, biodistribution results revealed that GPP3 micelles could be remarkably taken up by the jejunum and ileum. Pharmacokinetics revealed that the maximum plasma concentration (C max ) and the area under the plasma concentration-time curve from 0 to 24 h (AUC 0–24 ) for CUR@GPP3 micelles were both significantly increased, and that the relative bioavailability of CUR@GPP3 micelles to CUR-loaded mPEG-PLA/TPGS micelles (CUR@PP micelles) was 258.8%. Furthermore, CUR-loaded micelles could reduce damage to the liver and intestinal tissues. This study highlights the importance of Gal content in the design of targeting nanocarrier Gal-modified micelles, which have broad prospects for oral delivery of hydrophobic drugs. Therefore, they could serve as a promising candidate for targeted delivery to the liver.
研究领域:
药剂学
·
生物医学工程
✓ 已验证
DOI
高影响因子
RSC Advances
·
2016
·Vol. 6
·期 112
·111217-111225
·
IF 3.289
Sijie Zhao,Huiru Yang,Cai Zuo,Lu Sun,Liwei Ma,Hua Wei
Star-shaped polymers are attractive as drug carriers due to the integration of relatively easy synthesis compared to the preparation of hyper-branched dendrimers and their potential ability to form unimolecular nanoparticles with enhanced stability to survive the high dilution-associated deformation and subsequently premature drug release in the body fluids and blood during circulation. Clearly, the star structure exerts a significant effect on their bioproperties and potential applications. In this study, three star-shaped amphiphilic copolymers with the same polymer compositions but different star structures were synthesized to investigate the effect of star architecture on their properties as well as potential applications as drug carriers. Three different branched alcohols, 2-(hydroxymethyl) propane-1,3-diol, pentaerythritol and dipentaerythritol with 3, 4, and 6 respective hydroxyl groups were chosen as the starting core to generate the target star-shaped amphiphilic block copolymers composed of hydrophobic poly(ε-caprolactone) (PCL) and hydrophilic poly(oligoethyleneglycol methacrylate) (POEGMA) with 3, 4, and 6 corresponding star arms by a combination of ring-opening polymerization (ROP) and atom transfer radical polymerization (ATRP). Dynamic light scattering (DLS) measurements and pyrene fluorescence probe technique confirmed the capability of the resultant star-shaped amphiphilic copolymers to form unimolecular micelles with average diameters smaller than 50 nm in an aqueous phase. A comparison of the drug loading capacity revealed that the micelles of 4-star-PCL–POEGMA (4s-PCL–POEGMA) exhibited the highest drug loading content (DLC) of all the three formulations. More importantly, in vitro doxorubicin (DOX) release study showed unique pH-mediated drug release behaviors, i.e., dramatically accelerated release at pH 6.0 but a much slower profile at pH 7.4, from these generally recognized “pH-insensitive” 4-arm star-shaped micelles. An acid-triggered degradation and an acid–base titration were performed to further reveal that such interesting pH-responsive drug release behaviors were attributed primarily to the hydrophilic corona of OEG brushes. This study is believed to provide a new insight into the structure–bioproperties relationship of star-shaped polymers, thus should be useful for the future design and development of novel star-shaped polymers for controlled drug delivery.
研究领域:
高分子药剂学
·
纳米医学
·
药物控释
·
生物材料
·
药剂学
·
肿瘤治疗
·
纳米载体
✓ 已验证
DOI
高影响因子
COLLOID AND POLYMER SCIENCE
·
2015
·Vol. 293
·期 8
·2291-2300
·
IF 1.865
Zhou Qing-Han,Lin Juan,Li Li-Dong,Shang Le
Biodegradable micelles based on disulfide-linked monomethoxy poly(ethylene glycol)- b -poly(methyl methacrylate) 2 (mPEG-SS-PMMA 2 ) miktoarm star block copolymers were synthesized through atom transfer radical polymerization procedure and applied to solubilization and delivery of methotrexate (MTX). The synthesized miktoarm star block copolymers were characterized by 1 H nuclear magnetic resonance, Fourier transform infrared spectra, and gel permeation chromatography. The block copolymers were able to self-assemble into spherical micelles in water with an average diameter up to 130 nm by transmission electron microscopy observation and dynamic light scattering measurements and have a critical micelle concentration of 0.91 mg/L. When MTX was incorporated into obtained micelles, high drug loading capacity was found attributed to the designed miktoarm star-shaped nanostructure. Interestingly, in presence of dithiothreitol, the micelles could be degraded into polymer chains by cleavage of the disulfide linkages. The in vitro release studies revealed that these micelles released over 95 % of MTX within 48 h under a reductive environment analogous to that of the cell comparing to minimal drug release (<22 %) under nonreductive conditions. Cell cytoxicity experiments showed that the obtained micelles exhibited nontoxic, and the drug-loaded micelles exhibited high anticancer efficacy and better biocompatibility as compared to free MTX. All of these results showed that mPEG-SS-PMMA 2 micelles are promising carriers for delivery of hydrophobic antitumor drugs.
研究领域:
药学
·
高分子科学
·
纳米技术
·
药物传递
·
生物化学
·
材料科学
✓ 已验证
DOI
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2017
·
IF 4.164
Xueli Wang,Changyu He,Qinglai Yang,Lianjiang Tan,Bingya Liu,Zhenggang Zhu,Bing Gong,Yu-Mei Shen
Redox-responsive linkages dispersed in the backbones of the synthetic polymers, while young in the current spectrum of the biomedical application, are rapidly extending into their niche. In the present work, triblock copolymer PEG-PLA-PEG synthesized and characterized by 1 H -NMR and SEC can self-assemble into redox-responsive micelles in aqueous media with nanosized 33 nm and 47 nm. And the copolymers PEG 2000 -PLA 3000 -PEG 2000 and PEG 2000 -PLA 5000 -PEG 2000 present lower CMC with 0.034 and 0.022 mg/mL, and higher DLC of 4.28% and 5.14% respectively, compared with that of diblock copolymer. Moreover, drug release from the micelles can be triggered and significantly accelerated in reductive environment. The low cytotoxicity of redox-responsive micelles was confirmed by MTT assay against NIH 3 T3 cells. All of these results demonstrated that these polymeric micelles self-assembled from double-disulfide tethered block copolymers are promising carriers for the redox-responsive intracellular delivery of hydrophobic anticancer drugs.
研究领域:
生物材料
·
药剂学
·
高分子化学
✓ 已验证
DOI
高影响因子
International Journal of Polymeric Materials and Polymeric Biomaterials
·
2026
·
IF 3.2
Hua Ma,Zimeng Wang,Yajie Ding,Xiuhong Duan,Hongzhou Shang,Lihua Liu,Ning Qiao,Xuepeng Zhang
In this study, a polymeric micelles material was prepared for tumor-targeted drug delivery using folic acid (FA) as targeting ligand. The polymeric material was prepared through combination of FA-modified methoxy polyethylene glycol (mPEG) and D-α-vitamin E succinate (VES) by pH-sensitive acetal bond, which was labeled as FA-PEG-OCO-VES. The prepared micelles were characterized by various testing methods. The results showed that the FA-PEG2000-OCO-VES micelles are in uniform spherical shape with diameter about 150 nm, which was selected for drug loading and release experiment. Quercetin (QU) was used as anticancer drug model in this study. The maximum encapsulation efficiency of FA-PEG2000-OCO-VES micelles was 72.49 ± 2.85%, and drug loading efficiency was 12.65 ± 0.48%. In vitro drug release experiments and release mechanism study showed that the accumulative release of QU was related to pH value. The hemolysis test and in vitro cytotoxicity assay displayed that the micelles have good biocompatibility. Targeting studies and in vitro anticancer activity experiments have shown that micelles could actively target overexpression receptors on the surface of tumor cells and enter breast cancer cells through endocytosis, inhibiting the proliferation of cancer cells after drug release. Therefore, FA-PEG2000-OCO-VES micelles are expected to be a promising drug carrier in the field of cancer therapy.
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Meiling Chen,Sijia Chen,Yi Sun,Yuyan Zheng,Wenhua Miao,Yadong Zhao,Bin Zheng,Shaimaa Hatab,Jin Zhu,Fei Liu
The aim of this work was to develop a novel fluorescent micelle using an amphiphilic cellulose-based functional material ( i.e. C- g -PLLA/AFC) to enable the visualization of drug loading and releasing, while enhancing the aqueous solubility and anti-tumor activity of paclitaxel (PTX). PTX was encapsulated in self-assembled C- g -PLLA/AFC micelles with optimal encapsulation efficiency and drug loading values of 90.40 % and 22.60 %, respectively. The fluorescence spectra showed an increase in fluorescence intensity with the increase of drug loading, confirming the successful loading of the PTX and enabling the visualization of PTX encapsulation. Meanwhile, The PTX-loaded micelles exhibited sustained release under simulated normal blood (pH 7.4) and tumor tissue microenvironment (pH 6.2) conditions, with cumulative drug release rates of 70.85 % and 90.20 % after 144 h, respectively. Fluorescence intensity increases during PTX release, which providing direct visualization of the process. Both drug loading and releasing are linked to changes in the aggregation state of fluorophores, enabling the visualization of these events. Anti-tumor cell experiments conducted with PTX-loaded micellar solutions demonstrated significant cytotoxicity against MCF-7 breast cancer cells. These findings highlight the potential of C- g- PLLA/AFC micelles as efficient carriers for hydrophobic drugs, offering visible monitoring capability for drug loading and releasing.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF APPLIED POLYMER SCIENCE
·
2025
·
IF 2.8
Xiuhong Duan,Zimeng Wang,Handa Liu,Hua Ma,Xuepeng Zhang,Lihua Liu,Hongzhou Shang,Ning Qiao
A predrug delivery system combining tumor-targeting and pH-responsive features was synthesized using baicalin (BAI), polyethylene glycol (PEG), and folic acid (FA). BAI and PEG were linked via esterification to create pH-sensitive ester bonds ( COO ) that facilitate drug release in acidic environments, while FA was attached to PEG through substitution. This system, named FA-PEG-COO-BAI (FPB), encapsulated curcumin (CUR) to form drug-loaded micelles. The impact of drug-loading conditions, such as sonication duration and initial drug dosage, on CUR/FA-PEG-COO-BAI encapsulation efficiency and drug release was investigated. In vitro studies demonstrated a maximum encapsulation rate of (73.09 ± 3.31)% and a drug-loading rate of (11.90 ± 0.69)%. Drug release from CUR/FA-PEG-COO-BAI micelles accelerated as pH decreased, confirming pH-responsive behavior. Cellular uptake and antitumor assays suggested effective tumor targeting and inhibition of proliferation. Hemolysis and cell viability assays indicated low toxicity. These findings underscore the potential of CUR/FA-PEG-COO-BAI micelles for controlled drug release and targeted therapy.
研究领域:
药剂学
·
肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）