MACROMOLECULAR BIOSCIENCE
·
2013
·Vol. 14
·期 2
·280-288
·
IF 3.742
Feifei Li,Bin Chen,Zhaohua Ping,Xiangxiang Jia,Xin Guo,Longqiang Xiao,Lijian Liu
Lipophilic 6- O -poly ( ϵ -caprolactone)- L -ascorbic acid (AA-6-PCL) is synthesized through ROP of ϵ -caprolactone (CL). The number of repeating CL units in the polymer chain varies from 6 to 19. AA-6-PCL loaded supramolecular polymer micelles (SMPMs) are constructed with β-cyclodextrin (β-CD) and PCL as blocks. Transmission electron microscopy images show a nanospheric morphology of the micelles with a size range of 43.3 ± 5.0 nm. The drug loading contents are 22.53–39.23% for AA-6-PCL. AA-6-PCL exhibits high radical scavenging capacity (93.96–96.73%) and efficient scavenging potency, and a cytotoxicity study proves the excellent cytocompatibility of AA-6-PCL loaded β-CD/PCL SMPMs, which altogether herald their potential application in the study of the induced pluripotent stem cells.
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JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE
·
2023
·
IF 4.1
Youwu Liao,Haiqiao Wang,Shuang Li,Yuanyuan Xue,Yunqiu Chen,Michael Adu-Frimpong,Ying Xu,Jiangnan Yu,Ximing Xu,Hugh D.C. Smyth,Yuan Zhu
Background Astaxanthin is approved by Food and Drug Administration (FDA) as a safe dietary supplement for humans. Astaxanthin, as a potent lipid-soluble keto-carotenoid, is widely used in food, cosmetics and pharmaceutical fields. However, the low solubility of astaxanthin limits its powerful biological activity and application in the aforementioned fields. This study aims to develop a delivery system to address the low solubility and bioavailability of astaxanthin and to enhance its antioxidant capacity. Results Astaxanthin-loaded Composite Micelles were successfully prepared via Coaxial Electrospray Technology. Astaxanthin was existed in the amorphous state in the electro-sprayed formulation with an approximate particle size of 186.28 nm with a polydispersity index of 0.243. In this delivery system, Soluplus and copovidone (PVPVA 64) were the main polymeric matrix for astaxanthin, which then released the drug upon contact with aqueous media, and results in an overall increase of drug solubility and a release rate of 94.08 %. Meanwhile, lecithin and PEG-g-CS could support the absorption of astaxanthin in the gastrointestinal tract and help the transmembrane transport. Consequently, the relative bioavailability reached about 308.33% and the ROS scavenging efficiency of formulation was 44.10 %, which was 1.57 times higher than that of free astaxanthin (28.10 %) when both were at the same concentration level based on astaxanthin. Conclusion It could be deduced that coaxial electrospray could be applied to prepare a composite micelles system for the delivery of poorly water-soluble active ingredients found in the fields of functional food, cosmetics and medicine. This article is protected by copyright. All rights reserved.
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International Journal of Nanomedicine
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2017
·
IF 4.3
Xiaoyan Wu,Weihong Ge,Tengfei Shao,Weijun Wu,Jian Hou,Li Cui,Jing Wang,Zhenghai Zhang
Biochanin A (BCA), a natural dietary isoflavone, has been reported to show anticancer activities. However, its low biological availability and poor aqueous solubility limit its usefulness as a chemotherapeutic agent. We developed BCA-loaded micelles with Pluronic F127 and Plasdone S630 (BCA-FS). The optimized, spherical-shaped BCA-FS was obtained at a ratio of 1:1 (F127:S630). The particle size was 25.17±1.2 nm, and the zeta potential was −10.9±0.24 mV. BCA solubility in water increased to 5.0 mg/mL after encapsulation, and the drug-loading efficiency was 5.88%±0.76%. In vitro release experiments showed a delayed release of BCA from the mixed micelles. Furthermore, the BCA absorption permeability across a Caco-2 cell monolayer from the apical side to the basolateral side increased by 54% in BCA-FS. A pharmacokinetics evaluation showed a 2.16-fold increase in the relative oral bioavailability of BCA-FS compared with raw BCA, indicating that the mixed micelles may promote absorption in the gastrointestinal tract. A gastrointestinal safety assay was used to assess the reliability and safety of BCA-FS. On the basis of these findings, we conclude that this simple nanomicelle system could be leveraged to deliver BCA and other hydrophobic drugs.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2019
·
IF 2.606
Jiangxiu Niu,Liye Wang,Ming Yuan,Jingxiao Zhang,Hong Chen,Yansong Zhang
Chemotherapeutics cannot effectively reach brain glioma due to the blood-brain barrier (BBB) and blood-brain tumour barrier (BBTB). To overcome these obstacles, dual-targeting DOX micelles (GF-DOX) were developed to deliver the drug across the BBB and reach the tumour site. In this study, we investigated the BBB targeting ability and the brain delivery of GF-DOX in mice. Results showed that the cellular uptake by brain microvascular endothelial cells (BMVECs) of GF-DOX was significantly higher than that by P105-DOX through caveolae- and clathrin-mediated endocytosis. An in vivo pharmacokinetic study in rats indicated that GF-DOX significantly increased the bioavailability of DOX (4.6-fold), as opposed to the control solution. The distribution of preparations in mice showed that GF-DOX could significantly increase the amount of DOX in the brain ( P < 0.05). The survival time of tumour-bearing mice of the GF-DOX group (32 days) was significantly longer than that of the free DOX group (19 days, P = 0.024), or other controls due to the dual-targeting effect of GF-DOX. In conclusion, the dual-targeting GF-DOX could improve the efficacy of anti-tumour drugs in the treatment of brain glioma in vitro and in vivo .
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Polymer Chemistry
·
2017
·Vol. 8
·期 43
·6675-6687
·
IF 5.375
Da Huang,Yaqiang Wang,Fei Yang,Hong Shen,Zuquan Weng,Decheng Wu
Recently, nanoparticles self-assembled from amphiphilic supramolecular linear-dendritic block copolymers (LDBCs) have attracted great interest, since the combination of linear and dendritic polymers can incorporate the unique properties of the different segments but avoid some inherent drawbacks of dendrimers, not to mention that the components can be flexibly adjusted to enrich their functionality. In this study, LDBCs formed by host–guest recognition of polyacetal dendrimers with a β-cyclodextrin core and adamantane-terminated zwitterionic poly(sulfobetaine) could self-assemble into micelles and vesicles by varying the hydrophilic/hydrophobic ratio. Owing to the acid-labile characteristic of the dendritic segments, the micelles and vesicles were degradable and could release their payloads in a pH-responsive manner. The incorporation of zwitterionic linear segments gave the micelles and vesicles a charge-reversal ability and excellent resistivity to protein absorption, leading to higher affinity to cell membranes than conventional PEG-coated nanoparticles. In addition, the potential of these nanoparticles as anticancer drug carriers was preliminarily evaluated by using doxorubicin as a model drug and the results indicated that the DOX-loaded micelles and vesicles exhibited remarkable anticancer activity. This study cast a new light on the application of dendrimers and these micelles and vesicles constructed from LDBCs may be promising candidates as anticancer drug delivery platforms for cancer therapy.
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MACROMOLECULAR RAPID COMMUNICATIONS
·
2015
·Vol. 36
·期 15
·1402-1408
·
IF 4.941
Rui Qi,Yong Jin,Xinfeng Cheng,Baozhu Fan,Tongbing Sun,Shaojun Peng,Hanping Li
A novel rod-containing block copolymer is constructed by supramacromolecular self-assembly of α-cyclodextrin and a triblock copolymer with methoxy polyethylene glycol as the flanking chains and the midterm block alternately connected by 2,2-dimethylolbutyric acid and isophorone diisocyanate. The assembled rod-containing block copolymer shows an exciting phenomenon of concentration- and pH-dependent morphological switching of well-defined nanostructures. In the solutions at pH 9.2, spherical micelles, rod-like micelles, and hydrogel are observed successively with an increase of the concentration. Notably, the rod-like micelles are composed of spherical segments due to the combination of the crystalline cores of the spherical micelles. In addition, 1D nanostructures with different curvatures from linear rod-like micelles (pH 9.2) to ring-shaped micelles (pH 7.5) can be obtained by controlling the pH values of the assembled systems.
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MACROMOLECULAR CHEMISTRY AND PHYSICS
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2021
·Vol. 222
·期 13
·2000365
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IF 2.527
Qiong Guo,Jiangtao Liu,Hong Yang,Zhongli Lei
Stimuli-responsive chemical bonds have already been widely applied to construct nanomaterials, however, such materials rarely have great amounts of responsive groups and stable structures. Herein, a triple-stimuli-responsive interface-cross-linked (ICL) copolymer which is synthesized via Cu(I)-catalyzed azide-alkyne cycloaddition click polymerization and atom transfer radical polymerization (ATRP), is reported. N, N′-bis(bromoacetyl) cystamine is used for intramolecular crosslinking of the linear polymer chains. The ο-nitrobenzyl groups, peroxalate ester bonds, disulfide bonds, and triazole units are regularly and repeatedly arranged in the hydrophobic blocks, therefore enabling the polymer a large amount of responsive chemical bonds. The polymer self-assembles into spherical micelles with uniform size in deionized water. Using hydrophobic dye Nile red (NR) as a model drug to evaluate the effect of release in vitro, the multi-stimuli-sensitive release properties of the ICL micelles are investigated in detail by means of UV–vis, transmission electron microscopy, dynamic light scattering, and fluorescence spectrophotometry, and the results indicate the ICL micelles can respond to the photo, oxidation, or reduction responsiveness either independently or synergistically. Furthermore, the cross-linked structure enhances the stability of the micelles and rarely impacts the total amount of drug release. The research may have applications in the field of drug delivery systems for cancer therapy.
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Polymer Chemistry
·
2021
·Vol. 13
·期 7
·914-921
·
IF 5.582
Fei Deng,Menglin Yang,Yanli Zhang,Xiaohui Wu,Rujiang Ma,Feihe Ma,Linqi Shi
Refolding a denatured protein into its native form and stabilizing its structure are significant in the production and storage of protein products. The self-assembled mixed-shell polymeric micelle (MSPM) based nanochaperones closely mimic natural molecular chaperones in terms of structure and function and have been widely used to regulate the (re)folding of denatured proteins. However, the traditional manufacturing method of MSPM based nanochaperones is inconvenient with a very low concentration, which greatly restricts its large-scale applicability in practice. Here, we developed a one-pot strategy to synthesize high-concentration MSPMs for the mass preparation of nanochaperones to refold bulk denatured proteins and stabilize the structure of native proteins. The high-concentration MSPM is synthesized using two macro-RAFT agents to induce the polymerization and cross-linking of hydrophobic monomers. Through this one pot synthesis method, MSPMs with a concentration of 36.8 mg ml−1 are obtained, which is much higher than that obtained through the traditional method (0.5 mg ml−1). Moreover, the obtained MSPMs provide a good renaturation efficiency for the refolding of bulk denatured proteins and can stabilize native proteins for long-term storage. This strategy provides a simple method for the mass preparation of functional nanochaperones, which will promote its applications in practice.
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CARBOHYDRATE POLYMERS
·
2018
·
IF 5.158
Shuang Bai,Meili Hou,Xiaoxiao Shi,Jiucun Chen,Xiaoqian Ma,Yong-E Gao,Yajun Wang,Peng Xue,Yuejun Kang,Zhigang Xu
As one of the medical polymers approved by US Food and Drug Administration (FDA), poly(ethylene glycol) has low toxicity, high stability, good biocompatibility, unique physical and chemical properties. Cyclodextrin is an ideal candidate as a drug carrier due to its special structures and characteristics. These two materials were successfully assembled through chemosynthesis in combination with the hydrophilic poly(ethylene glycol) methyl ether methacrylate (OEGMA) chain and hydrophobic polymeric camptothecin (CPT) chain by atom transfer radical polymerization (ATRP). The introduction of disulfide bond of monomer was aimed to realize reduction agent-triggered release of active CPT. The obtained amphipathic prodrug [(Denoted as PC-PCPT- b -POEGMA (PCCO)] could form nano-sized polymeric micelles, which could release more than 85% of the loaded CPT via triggered cleavage of the disulfide linker. The cellular co-localization study revealed the potential pathway of drug internalization. Moreover, the PCCO micelles showed good biocompatibility in vivo after intravenous injection on a mouse model. This new CPT-loaded prodrug system could be prepared with low cost, and showed efficient and controlled drug release and favorable biocompatibility, demonstrating a promising potential as a stimuli-responsive polymeric prodrug for future clinical applications.
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Acta Biomaterialia
·
2016
·
IF 6.008
Jiulong Zhang,Xiufeng Zhao,Qing Chen,Xiaoyi Yin,Xiu Xin,Kexin Li,Mingxi Qiao,Haiyang Hu,Dawei Chen,Xiuli Zhao
Multidrug resistance (MDR) of tumor cells is becoming the main reason for the failure of chemotherapy and P-glycoprotein (P-gp) mediated drug efflux has demonstrated to be the key factor for MDR. To address this issue, a novel pH-responsive mixed micelles drug delivery system composed of dextran-g-poly(lactide-co-glycolide)-g-histidine (HDP) and folate acid-D-α-tocopheryl polyethylene glycol 2000 (FA-TPGS2K) copolymers has been designed for the delivery of antitumor agent, paclitaxel (PTX) via FA-receptor mediated cell endocytosis , into PTX-resistant breast cancer MCF-7 cells (MCF-7/PTX). PTX-loaded FA-TPGS2K/HDP mixed micelles were characterized to have a small size distribution, high loading content and excellent pH-responsive drug release profiles. Compared with HDP micelles, FA-TPGS2K/HDP mixed micelles showed a higher cytotoxicity against MCF-7 and MCF-7/PTX cells due to the synergistic effect of FA-receptor mediated cell endocytosis, pH-responsive drug release and TPGS mediated P-gp inhibition. P-gp expression level, ATP content and mitochondrial membrane potential change have been measured, the results indicated blank FA-TPGS2K/HDP mixed micelles could inhibit the P-gp activity by reducing the mitochondrial membrane potential and depleting ATP content but not down-regulating the P-gp expression. In vivo antitumor activities demonstrated FA-TPGS2K/HDP mixed micelles could reach higher antitumor activity compared with HDP micelles for MCF-7/PTX tumor cells. Histological assay also indicated that FA-TPGS2K/HDP mixed micelles showed strongly apoptosis inducing effect, anti-proliferation effect and anti-angiogenesis effect. All these evidences demonstrated this pH-sensitive FA-TPGS2K/HDP micelle-based drug delivery system is a promising approach for overcoming MDR. Statement of Significance In this work, a novel FA-TPGS2K copolymer has been synthesized and used it to construct mixed micelles with HDP copolymer to overcome MDR effect. Furthermore, a series in vitro and in vivo evaluations have been made, which supported enough evidences for the efficient delivery of antitumor drug to MDR cells.
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DRUG DELIVERY
·
2023
·
IF 6
Ru Wang,Nuannuan Li,Tianyu Zhang,Yiying Sun,Xiaoyan He,Xiaoyan Lu,Liuxiang Chu,Kaoxiang Sun
Mitoxantrone (MX) can induce the immunogenic-cell death (ICD) of tumor cells and activate anti-tumor immune responses. However, it can also cause high expression of indole amine 2, 3-dioxygenase (IDO) during ICD, leading to T-cell apoptosis and a weakened immune response. An IDO inhibitor, 1-methyl tryptophan (1-MT), can inhibit the activity of IDO caused by MX, resulting in enhanced chemo-immunotherapy. Here, MX-1-MT was connected by ester bond which could be broken in an acidic tumor microenvironment. MX-1-MT was combined with polyethylene glycol (PEG) via a disulfide bond which could be reduced by glutathione overexpressed in tumors, thereby accelerating drug release at target sites. Folic acid-modified distearoyl phosphoethanolamine-polyethylene glycol (DSPE-PEG-FA) was introduced to form targeting micelles. The micelles were of uniform particle size, high stability, and high responsiveness. They could be taken-up by drug-resistant MCF-7/ADR cells, displayed high targeting ability, and induced enhanced cytotoxicity and ICD. Due to 1-MT addition, micelles could inhibit IDO. In vivo studies demonstrated that micelles could accumulate in the tumor tissues of nude mice, resulting in an enhanced antitumor effect and few side-effects.
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EUROPEAN POLYMER JOURNAL
·
2025
·
IF 6.3
Ruizhen Zhang,Chengwen Jin,Pengjie Xie,Tao Chen
The coordinated release of multiple substances presents a significant technical challenge, primarily due to their distinct release kinetics and potential intermolecular interactions. To address this, we developed a composite nanoreactor and strategically selected two hydrophobic fluorescent dyes, Coumarin 102 and Nile Red, as model payloads. Firstly, a photoresponsive block copolymer, P(DMA 50 - b -SPMA 60 ) ( P1 ), containing carbamate spiropyran methacrylate units, and a thermoresponsive block copolymer with an Upper Critical Solution Temperature (UCST), P(DMA 50 - b -SBMA 48 ) ( P2 ), were synthesized via reversible addition-fragmentation chain transfer (RAFT) polymerization. These copolymers self-assembled into micelles, which encapsulated Coumarin 102 and Nile Red within the hydrophobic cores of P1 and P2 , respectively. The individual stimulus-responsive release profiles were monitored via fluorescence spectroscopy. Composite nanoreactors were then prepared by physical blending the two loaded micelle types. The stability of the composite system was verified by fluorescence spectroscopy, transmission electron microscopy (TEM), and differential scanning calorimetry (DSC). Upon exposure to specific stimuli (light or temperature), selective release of the respective hydrophobic molecules was achieved: UV irradiation triggered a 80% release of Coumarin 102 from M3 micelles, while heating above the UCST induced a 75% release of Nile Red from M4 micelles. The composite micelles thus integrate multiple orthogonal stimulation responses with precise selective release control, offering a promising platform for advanced controlled-release applications in nanotechnology and biotechnology.
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