INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
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2013
·
IF 2.206
Yan-Ling Luo,Li-Li Chen,Yan Miao,Feng Xu
Novel AB4-type polyurethane (PU) micelle-like amphiphilic block copolymers consisting of hydroxyl-functionalized carboxyl-terminated poly(butadiene-co-acrylonitrile) (f-CTBN) as the hydrophobic cores and methoxy poly(ethylene glycol) (MPEG) as the hydrophilic branched blocks were synthesized via esterification, followed by coupling reaction. Their chemical structure and molecular weight were characterized by FTIR, NMR, and SEC measurements. The block copolymers could easily self-assemble to form core–shell micelle nanoparticles in various media. The micelles bear a critical micelle concentration (CMC) in a range from 0.740 to 6.310 mg L–1 and were very stable even in PBS solutions. The TEM and DLS findings revealed that the micelles were almost spherical and narrow-size-distribution, with TEM mean diameters from 13 to 24 nm, and average hydrodynamic diameter about 124–151 nm. All these depended on chain lengths and compositional ratios of hydrophilic MPEG blocks. The drug loading and in vitro release indicated that the self-assembled micelle nanoparticles could effectively load hydrophobic prednisone, with encapsulation capacity of about 27–30%, and the drug release from the nanoparticles was dependent on MPEG chain lengths and the molar ratios of f-CTBN to MPEG. Cytotoxicity assays disclosed that the as-prepared block copolymer micelle nanoparticles exhibit good biocompatibility and could be employed as potential drug controlled release carriers.
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Analytical Methods
·
2014
·Vol. 6
·期 21
·8627-8632
·
IF 1.938
Jinjiao Shi,Ligang Chen
In this study, we investigated the possibility of reverse micelles which were used for the determination of rhodamine B in lipsticks followed by high performance liquid chromatography (HPLC). The reverse micelle of surfactant sodium 1,4-bis(2-ethylhexoxy)-1,4-dioxobutane-2-sulfonate (AOT) was formed in n-hexane. First, the samples were preprocessed by reverse micelle extraction, and then rhodamine B was extracted from the mixture with methanol by back-extraction. The effects of different parameters including the concentration of surfactant, pH, amount of potassium chloride, ultrasonic time and type of organic solvents were evaluated and optimized during reverse micelle formation. The limit of detection of rhodamine B was 0.01 μg g−1. The intra-day and inter-day precisions expressed as relative standard deviations were 3.6% and 4.5%, respectively. The recovery of rhodamine B obtained was 95.0%. The reverse micelle method proposed for the determination of rhodamine B in real samples of lipsticks has the advantages of simplicity, speed, high precision, low detection limit and the use of inexpensive equipment.
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International Journal of Nanomedicine
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2026
·
IF 8.7
Zhongcheng Ke,Tao Luo,Xiaoling Cheng,Xuwen Chai,Zitong Zhu,Zhusheng Huang,Zhen Wang
Purpose Gambogic acid (GA) shows potent inhibitory activity against various malignancies. However, achieving precise targeted delivery and spatiotemporal control of drug release at tumor sites remains a significant challenge. This study aimed to develop a hyaluronic acid (HA)-modified, redox-responsive drug delivery system based on a methoxy polyethylene glycol-linked GA prodrug (mPEG-ss-GA). Methods The amphiphilic prodrug, mPEG-ss-GA, was synthesized by conjugating GA to methoxy polyethylene glycol (mPEG) via a disulfide linkage. Subsequently, it spontaneously self-assembled with HA in an aqueous medium to form HA-modified mPEG-ss-GA micelles (HA/mPEG-ss-GA-M). The physicochemical properties of the micelles, including particle size, zeta potential, morphology, and in vitro release profiles, were systematically characterized. Cellular uptake in human non-small cell lung cancer cells (A549) was visualized using fluorescence microscopy. Furthermore, the in vitro pro-apoptotic effects were quantified using an Annexin V–propidium iodide (PI) binding assay. Finally, the in vivo anti-tumor efficacy was evaluated in a subcutaneous xenograft tumor model. Results The HA/mPEG-ss-GA-M micelles exhibited an average particle size of 251 nm with a zeta potential of −17.36 mV. The system demonstrated glutathione (GSH)-triggered drug release, with release kinetics that aligned well with the Higuchi model. In vitro studies revealed that HA/mPEG-ss-GA-M significantly enhanced cellular uptake, induced apoptosis, and suppressed cell migration. In vivo experiments showed that HA/mPEG-ss-GA-M achieved a tumor volume inhibition rate of 54.09%, compared to 29.56% for free GA. Conclusion HA/mPEG-ss-GA-M is a promising drug delivery system for targeted non-small cell lung cancer therapy and offers precise and efficient treatment options.
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Pharmaceutics
·
2026
·Vol. 18
·期 8
·1036
·
IF 6.9
Yu Zhang,Jian Guo,Haonan Qiu,Jiale Liu,Chi Zhang,Lutan Zhou,Chunfei Wang,Lihua Li,Xuefeng Hou
Background: Imperatorin (IPT) is a natural furanocoumarin featuring robust anti-inflammatory, antifibrotic and antioxidant activities. However, poor aqueous solubility and insufficient oral bioavailability restrict its clinical application. Multiple gastrointestinal barriers, including the mucus barrier, limited epithelial penetration and P-glycoprotein-triggered drug efflux, are major obstacles hindering IPT oral absorption.Methods: N-acetylcysteine (NAC)-functionalized TPGS conjugates were synthesized first. Using Pluronic®F108 and Lipoid®S-100 as a matrix, imperatorin@N-acetylcysteine-TPGS/Pluronic®F108/Lipoid®S-100 (IPT@NAC-TFS) micelles were fabricated. We characterized their physicochemical features and in vitro release behavior. The Caco-2/HT29-MTX-E12 co-culture cell model was adopted to explore mucus permeation, cellular uptake and transepithelial transport mechanisms. In vivo intestinal distribution and pharmacokinetic tests in rats were carried out to confirm the oral absorption-enhancing effect of micelles.Results: Optimized micelles displayed a uniform shape and favorable encapsulation efficiency. Low CMC maintained structural stability upon gastrointestinal dilution. NAC modification conferred mucus-penetrating capacity on micelles. TPGS simultaneously improved epithelial barrier permeability and inhibited drug efflux, switching IPT transport mode. The micelles effectively cleared intracellular ROS, recovered SOD activity and lowered MDA levels in BLM-impaired MLg fibroblasts. In vivo results revealed enhanced intestinal drug accumulation, with the relative oral bioavailability of IPT increased by 6.07-fold.Conclusions: IPT@NAC-TFS micelles overcome multiple gastrointestinal barriers for oral IPT delivery. Combining mucus penetration, efflux suppression and antioxidative capacity, this system offers a promising strategy to develop oral formulations of poorly soluble antifibrotic natural products.
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Pharmaceutics
·
2026
·Vol. 18
·期 4
·498
·
IF 6.9
Xingmeng Ma,Zhu Wang,Jingyi Wang,Xingyu Chen,Jinggang Zhang,Dengxue Yang,Shiyi Xu,Xueying Yan
Background/Objective : In lung cancer treatment, increasing the concentration of antitumor drugs at the tumor site, enhancing efficacy, and reducing systemic toxicity are significant challenges. This study aims to develop an intelligent responsive polymer micelle system (GPDD) that achieves efficient accumulation and controlled release of drugs at lung tumor sites through targeted and pH-responsive design. Methods : The GPDD system is formed by the self-assembly of GE11-PEG-hyd-DOX conjugates and co-loads free DOX. This system utilizes the targeting effect of the GE11 peptide with the epidermal growth factor receptor (EGFR) to accumulate at the tumor site, while the hydrazone bond serves as a pH-responsive linker that breaks in the acidic tumor microenvironment, triggering drug release. Experiments employed CCK-8 cytotoxicity assays and tumor-bearing nude mouse models (strain not specified) for in vitro and in vivo evaluations. Results : In vitro experiments showed that GE11-modified GPDD effectively inhibited tumor cell growth. In tumor-bearing nude mouse experiments, GPDD demonstrated more significant tumor suppression effects and lower systemic toxicity compared to free DOX and unmodified PDD. Conclusions : The GPDD nanocarrier integrates targeting and pH responsiveness, improving antitumor efficacy and reducing side effects, with translational potential. The novelty of the study lies in its dual-functional design and co-loading strategy, providing new insights for tumor-targeted delivery systems.
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SCIENCE AND TECHNOLOGY OF ADVANCED MATERIALS
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2026
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IF 6.6
Wei Ma,Hongyan Yang,Xinyue Ma,Jiao Huang,Li Chen,Atsushi Takahara
The development of polymer prodrugs with well-defined architectures capable of forming stable nanomicelles is important for achieving precise and efficient drug delivery. Compared with conventional linear systems, star-shaped copolymer prodrugs offer enhanced micellar stability owing to their covalently tethered architecture. However, many existing synthetic approaches rely on transition-metal catalyzed polymerization and customized monomers, which limit their sustainability and practical applicability. Herein, we report a pH-responsive doxorubicin (DOX)-conjugated benzaldehyde-functionalized star-shaped copolymer synthesized via an environmentally benign metal-free atom transfer radical polymerization (ATRP) strategy. A hydroxyl-functionalized star-shaped copolymer scaffold was first prepared from readily available monomers and subsequently modified to introduce pendant benzaldehyde groups, enabling DOX conjugation through acid-labile imine linkages. This approach affords well-controlled polymer architectures while avoiding transition-metal residues and the need for pre-functionalized monomers. The resulting DOX-conjugated star-shaped copolymers form unimolecular micelles with high colloidal stability and exhibit pH-triggered drug release under acidic conditions. In vitro studies further demonstrate effective cellular internalization and a moderated cytotoxic profile toward human large-cell lung carcinoma (H460) cells, supporting the functional viability of this micellar system as a polymer prodrug delivery platform.
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ACS Omega
·
2026
·
IF 5.2
Zhiyu Chen,Junhong Chen,Shuang Liu,Xu Zhou,Yichuan Zhang,Yunsheng Jiang,Xiao Liu,Yuan Zhang,Xiangling Pu,Hui Zhang
Osteosarcoma is the most prevalent primary bone cancer affecting children and adolescents, characterized by its high invasiveness and the challenges in treatment posed by multidrug resistance. Cancer stem cells significantly contribute to poor clinical outcomes; however, current targeted therapies remain limited in their effectiveness. In this study, we developed a novel dual-responsive nanomedicine designed to target the microenvironment of osteosarcoma cancer stem cells (OCSCs) and osteosarcoma itself, which selectively releases all-trans retinoic acid and paclitaxel, termed mPCDAP. Our findings indicate that mPCDAP rapidly releases all-trans retinoic acid to suppress stemness under conditions of elevated glutathione, subsequently increasing intracellular reactive oxygen species levels in tumor cells. This mechanism further facilitates the release of paclitaxel under conditions of highly reactive oxygen species, thereby inducing apoptosis in osteosarcoma cells. Additionally, mPCDAP was effectively internalized by both osteosarcoma cells and OCSCs, with in vitro and in vivo results demonstrating significant synergistic antitumor effects, promoting apoptosis and markedly reducing tumor stemness. This study presents a novel approach and promising prospects for targeted therapy of osteosarcoma and OCSCs.
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Journal of Materials Chemistry B
·
2025
·
IF 5.7
Jia-Mi Li,Ya-Wen Ao,Junwei Yao,Wen-Ru Li,Bao-Jun Xie,Qian Wang,Shi-Wen Huang
Photodynamic therapy efficiency is constrained by tumor hypoxia and insufficient photosensitizer accumulation, to address these limitations, an oxygen-supplying nanoplatform was developed through function-oriented polymer design. Briefly, an amphiphilic copolymer (PFOC-PEI) was firstly synthesized by chemical conjugating perfluorooctanoic acid with branched polyethyleneimine, forming micelles capable of encapsulating chlorin e6 while alleviating hypoxia via fluorocarbon-mediated oxygen delivery. To enhance tumor-selective delivery for biocompatibility, a pH-responsive polyanion (PEI-DMMA) derived from 2,3-dimethylmaleic anhydride modification was integrated, yielding composite micelles (Ce6-PFOC-PEI/PEI-DMMA) with tumor stimulus responsiveness charge reversal and oxygen carrying capability. The nanocarrier maintained negative surface charge under physiological conditions to prolong blood circulation, while switching to positive charge at tumor sites through microenvironmental -triggered cleavage of acid-labile amide bonds, thereby enhancing tumor accumulation. In vitro studies demonstrated 1.5-fold higher cellular uptake of Ce6-PFOC-PEI/PEI-DMMA in acidic conditions compared to non-hydrolytic controls (Ce6-PFOC-PEI/PEI-SA), correlating with enhanced ROS generation in C6 glioma cells. The improved phototoxicity was evidenced by lower IC50 values against C6 cells. In vivo evaluation revealed 87% tumor growth inhibition in C6 tumor-bearing nude mice of Ce6-PFOC-PEI/PEI-DMMA, which is superior to that of Ce6-PFOC-PEI/PEI-SA (69%) and Ce6-PFOC-PEI (73%). This oxygen self-supplying platform integrates fluorocarbon-mediated oxygenation with pH-responsive charge reversal, demonstrating enhanced PDT efficacy while maintaining favorable biosafety.
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ACS Applied Bio Materials
·
2026
·
IF 4.7
Aolei Hu,Xilu Chen,Haimei Ling,Zhenzi Mi,Ruilian Yu,Yao Fu
Malignant melanoma has a high recurrence rate after surgical resection, conventional neoadjuvant chemotherapy (NAC) suffers from off-target toxicity and limited efficacy. Leveraging elevated tumor-specific reactive oxygen species (ROS), we designed a sequential therapeutic strategy combining ROS-responsive micelles and a multifunctional hydrogel to combat local recurrence. By conjugating 3-indoleacetic acid to chondroitin sulfate via a ROS-responsive thioketal linker, an amphiphile (CS-TK-IAA, CTI) was synthesized, significantly enhancing tumor-specific uptake and ROS-scavenging capacity. CTI self-assembled into micelles (CLT@CTI) encapsulating celastrol (CLT), achieving high encapsulation efficiency (92.3%) and drug loading capacity (25.2%). Postoperatively, an injectable chitosan-based hybrid hydrogel (CPG) with self-healing, tissue adhesion, and hemostatic properties was applied to the resection site, triggering a photothermal effect via near-infrared light. In a mouse melanoma recurrence model, neoadjuvant CLT@CTI therapy effectively suppressed primary tumor growth, while postoperative CPG gel-mediated photothermal ablation of residual tumors dramatically delayed recurrence and improved 60-day survival rates. This sequential therapeutic regimen, neoadjuvant chemotherapy with postoperative photothermal therapy, provides a promising and viable solution for preventing melanoma recurrence.
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
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2014
·
IF 3.552
Jia-Pei Wang,Jun-Sheng Chen,Guang-Jiu Zhao
In this work, we have reported our study on the controversial issue whether methanol molecules can be effectively encapsulated by surfactant AOT to form true reverse micelles. We compared the different photophysical properties of coumarin 153 (C153) in methanol/AOT/n-heptane reverse micelles and methanol/n-heptane binary mixture by means of steady-state absorption, fluorescence and time-resolved fluorescence spectroscopies. In the reverse micelles, the fluorescence emission spectra of C153 were dependent on the excitation wavelength, while in binary mixtures, the excitation wavelength dependence was not observed. The biexponential decay curves of C153 in reverse micelles give a further confirmation for the two different environments where C153 molecules reside in. In other words, C153 molecules can exist both inside the core of the reverse micelles and outside of it. These results proved that the methanol can be effectively encapsulated by AOT in n-heptane solvents to form stable methanol/AOT/n-heptane reverse micelles.
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SAUDI PHARMACEUTICAL JOURNAL
·
2025
·Vol. 33
·期 5
·1-17
·
IF 3.4
Wang Ziheng,Xu Yuchen,Liu Manting,Yang Yuchang,Shi Wenjuan,Zhu Qian,Liu Juan,Yi Lisha,Wu Huimin,Yin Xingbin,Dong Xiaoxv,Ni Jian,Qu Changhai
This study aimed to establish a method for quantifying baicalin (BC) in rabbit ocular tissues and plasma, and evaluate the pharmacological efficacy and pharmacokinetic properties of BC and BC@HS15/DSPE-PEG2000-L-Val, a novel ocular formulation for dry eye treatment. BC@HS15/DSPE-PEG2000-L-Val or free BC was administered via eye drops to benzalkonium chloride (BAC)-induced dry eye mice. Corneal and conjunctival tissues were assessed for anti-dry eye efficacy. BC concentrations in cornea, conjunctiva, aqueous humor, and ocular plasma were quantified using LC–MS/MS. Noncompartmental pharmacokinetic parameters (AUC, Tmax) were calculated using DAS 2.0 software. The method demonstrated excellent linearity (0.50–500.00 ng/mL, r > 0.9905), precision (RSD < 10%), and accuracy (± 13%). Compared to free BC, BC@HS15/DSPE-PEG2000-L-Val significantly increased tear secretion, reduced MMP-3/MMP-9 expression, and preserved corneal epithelium integrity. In the micelle group, corneal and conjunctival Cmax values were 2.7- and 3.6-fold higher than the solution group, respectively. A sensitive and validated liquid chromatography-tandem mass spectrometry (LC–MS/MS) method was developed to measure baicalin concentrations in ocular plasma and tissues of rabbits. BC@HS15/DSPE-PEG2000-L-Val for treating dry eye demonstrated significantly superior outcomes. The nano-micelle notably enhanced BC concentration on the ocular surface and effectively prolonged its retention time. Graphical abstract
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JOURNAL OF APPLIED POLYMER SCIENCE
·
2023
·Vol. 140
·期 18
·e53805
·
IF 3
Dezhong Xu,Ao Li,Weijie Lin,Qiuxia Zou,Shuai Wu,Ajoy Kanti Mondal,Wangchuan Xiao,Fang Huang
In this study, pH and thermally responsive P(PFPHM 9 - b -DMAEMA- b -PEGMEA 480 ) was prepared by atom transfer radical polymerization (ATRP) using perfluoropolyether hydroxyethyl methacrylate (PFPHM) as hydrophobic core, 2-(Dimethylamino) ethyl methacrylate as pH and thermal response function segment, and poly (ethylene glycol) methyl ether acrylate 480 as hydrophilic shell, respectively. The chemical structure, critical micelle concentration (CMC), lower critical solution temperature (LCST), biological toxicity, stability of micelles, drug-loading performance and cumulative drug release rate of prepared P(PFPHM 9 - b -DMAEMA- b -PEGMEA 480 ) were analyzed by 19 F NMR, 1 H NMR, FTIR, DLS, UV–Vis, laser confocal microscopy and fluorescence spectrophotometer. The results show that P(PFPHM 9 - b -DMAEMA- b -PEGMEA 480 ) exhibites a CMC of 7.5 g/L, LCST of 37.6°C and excellent micelle stability. Moreover, the analysis of drug-loading indicates that the polymer displayed drug loading efficiency (DL) is 21.3% and the encapsulation efficiency (EE) is 90.0%. Its cumulative drug release rates at pH = 6.5 (42°C) is almost double of those at pH = 7.4 (42°C), pH = 6.5 (37°C) and pH = 7.4 (37°C). These results suggeste that the P(PFPHM 9 - b -DMAEMA- b -PEGMEA 480 ) at pH ranging from 6.5 to 7.4 and temperature ranging from 37 to 42°C are pH and temperature sensitive. It has great potential application as a drug loading for DOX.
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危险品化学品经营许可证（带存储）