INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2017
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IF 3.649
Yingqi Xu,Shengpeng Wang,Hon Fai Chan,Yuling Liu,Hui Li,Chengwei He,Zeyong Li,Meiwan Chen
Mitochondria are important targets for the intracellular delivery of drugs and DNA. For mitochondria-targeted delivery, a mitochondriotropic molecule, triphenylphosphonium (TPP), was applied to the synthesis of amphiphilic TPP-poly(ethylene glycol)-poly(ε-caprolactone) (TPP-PEG-PCL) polymers. The TPP-PEG-PCL polymer was used to prepare micelles using a solvent evaporation method for the delivery of gambogic acid (GA) (GA-TPP). The micelles were obtained with a favorable particle size of 150.07 ± 11.71 nm and an encapsulation efficiency of 80.78 ± 1.36%, and they displayed homogeneous spherical shapes. The GA-TPP micelles exerted enhanced cytotoxic and pro-apoptotic effect against A549 cells compared to free GA and GA-loaded PEG-PCL (GA-PP) micelles, due to the inhibition of the expression of apoptosis-related proteins and promotion of caspase 3/7 and caspase 9 activity. Notably, the mitochondria-targeting GA-TPP micelles selectively accumulated in the mitochondria, inducing the loss of mitochondrial membrane potential and the release of cytochrome c , thereby achieving improved mitochondria-targeting effects. In conclusion, the GA-TPP micelle system shows great promise for lung cancer treatment by inducing an apoptotic effect via the mitochondrial signaling pathway.
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JOURNAL OF NANOBIOTECHNOLOGY
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2021
·Vol. 19
·期 1
·1-15
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IF 10.435
Sun Changzhen,Lu Ji,Wang Jun,Hao Ping,Li Chunhong,Qi Lu,Yang Lin,He Bin,Zhong Zhirong,Hao Na
Background Nano-drug delivery systems show considerable promise for effective cancer therapy. Polymeric micelles have attracted extensive attention as practical nanocarriers for target drug delivery and controlled drug delivery system, however, the distribution of micelles and the release of the drug are difficult to trace in cancer cells. Therefore, the construction of a redox-sensitive multifunctional drug delivery system for intelligent release of anticancer drugs and simultaneous diagnostic imaging and therapy remains an attractive research subject.Results To construct a smart drug delivery system for simultaneous imaging and cancer chemotherapy, mPEG-ss-Tripp was prepared and self-assembled into redox-sensitive polymeric micelles with a diameter of 105 nm that were easily detected within cells using confocal laser scanning microscopy based on aggregation-induced emission. Doxorubicin-loaded micelles rapidly released the drug intracellularly when GSH reduced the disulfide bond. The drug-loaded micelles inhibited tumor xenografts in mice, while this efficacy was lower without the GSH-responsive disulfide bridge. These results establish an innovative multi-functional polymeric micelle for intracellular imaging and redox-triggered drug deliver to cancer cells.Conclusion sA novel redox-sensitive drug delivery system with AIE property was constructed for simultaneous cellular imaging and intelligent drug delivery and release. This smart drug delivery system opens up new possibilities for multifunctional drug delivery systems.
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Research
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2025
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IF 10.7
Xuan Wei,Jiamin Cheng,Meijuan Geng,Siyu Chen,Liyang Gong,Siyu Meng,Keying Chen,Ziyan Wang,Zhang Yuan,Kaiyong Cai,Liangliang Dai
The inhibition of dependent glutamine metabolism is an effective treatment for triple-negative breast cancer (TNBC) starvation, but it is limited by compensatory glycolysis and inadequate delivery efficiency. Herein, we construct a pH-responsive size/charge-reprogrammed micelle with hierarchical delivery characteristics for TNBC suppression with glutamine depletion and vessel blockade. It consists of a positively charged prodrug micelle chemically grafted with the glutamine transport inhibitor V9302 as the inner core layer, the neovascular disruptor CA4P adsorbed in the middle layer, and a pH-responsive peelable polymer as the outer shell. The nanosystem PPD/PPQV@C could effectively reduce size and reverse charge in response to the tumor acidic microenvironment by removing the outer polymer PPD, as accompanying the release of CA4P. Furthermore, the remaining PPQV could responsively release V9302 in the cytoplasm of tumor cells, improving the bioavailability of cargoes and overcoming permeability barrier through precise hierarchical release strategy. Importantly, V9302 and CA4P localized in the tumor intracellular and extracellular matrix could effectively block TNBC-dependent glutamine metabolism and inhibit compensatory nutrient by blocking angiogenesis, achieving the desired tumor suppression with prolonged survival time. This work exhibits a smart nanoplatform for efficient TNBC treatment via dual blockade of the dependent glutamine metabolism and angiogenesis.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Shuangjun Li,Ruyue Shi,Yankun Liu,Mingcong Niu,Zhicun Liu,Zhongjuan Wang,Jiwang Gao,Hongda Cai,Zhuyu Zhou,Shengnan Li,Xiuhua Zhao
Immune cells infiltrating tumors play a pivotal role in tumor progression regulation; however, their functionality is frequently suppressed by the acidic conditions of the tumor microenvironment (TME). Targeting and reversing tumor acidity holds significant potential for enhancing the efficacy of immunotherapy. Here, we present a proof-of-concept study on tumor acidity-reversal therapy mediated by bacterial cellulose-targeted micelles to promote M2 macrophage repolarization to M1 macrophages and restore the anti-tumor function of T cells. Our strategy utilizes a bacterial cellulose (BC) composite modified with folic acid (FA) and chrysin (BY), loaded with lactic acid-neutralizing chemotherapeutic vincristine (VCR) and lactate dehydrogenase inhibitor GNE-140, to self-assemble into tumor-targeted nanoparticles. Post-treatment, FA-BC-BY@VCR@GNE-140 demonstrated notable efficacy in reversing tumor acidity, inducing tumor cell death, mitigating immunosuppression, and stimulating host adaptive immunity. This approach represents an innovative strategy for synergizing chemotherapy and immunotherapy to combat tumor progression.
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NEW JOURNAL OF CHEMISTRY
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2024
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IF 2.7
Xiaoyi Song,Fan Yang,Ruixuan Ji,Bin Yang,Yin Lv,Zhong Wei
Traditional chemotherapy faces challenges related to limited drug efficacy and adverse reactions. Intelligent nanocarrier drug delivery systems (INDDSs) promise improved treatment outcomes with reduced toxicity. However, several clinical challenges persist in achieving rapid drug release and real-time monitoring. Herein, a ROS-responsive amphiphilic copolymer was synthesized: polyethylene glycol (mPEG-TK-OH) with ROS-responsive thioketal (TK) as the macromolecular initiator, and enzymatic ring-opening polymerization of caprolactone was performed. Small molecules of tetraphenylethylene (TPE) with aggregation-induced emission (AIE) properties were added to the polymer's terminus to enable fluorescence imaging and the ROS-responsive amphiphilic copolymer mPEG-TK-PCL-TPE with AIE properties is formed and enhances drug release monitoring through fluorescence resonance energy transfer (FRET) between TPE and the hydrophobic anti-cancer drug DOX. Leveraging distinct ROS levels between tumor and normal cells, these ROS-responsive nanomicelles effectively respond to high intracellular redox-active species and release DOX. The mPEG-TK-PCL-TPE micelles displayed a suitable size, high drug loading, and excellent imaging quality. In vitro cell experiments confirmed their biocompatibility and efficacy in inhibiting 4T1 tumor cells. This ROS-responsive amphiphilic copolymer, incorporating the AIE structure, introduces new opportunities for cancer treatment, enabling real-time drug release tracking and improving therapeutic outcomes.
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TRIBOLOGY INTERNATIONAL
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2025
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IF 6.9
Mingyuan Dou,Qing Feng,Kangchun Li,Zhenpeng Li,Fuchuan Huang,Fukang Deng
The unique physicochemical properties and 2D layered structure of MXene make it a promising lubricant additive. However, its chemical instability limits its application in environmentally friendly and sustainable lubrication systems. Although various strategies have been explored to enhance the chemical stability and tribological properties of MXene aqueous solutions, these approaches often compromise MXene's chemical compatibility and require high-viscosity petroleum-based lubricants. In this study, choline hydroxide and amino acids were added to a Ti 3 C 2 T x aqueous solution, leading to the self-assembly of choline hydroxide and amino acids into ionic liquid micelles. These micelles effectively passivated the surface of Ti 3 C 2 T x and improved its chemical stability. The experimental and simulation results showed that the ionic liquid micelles facilitated the formation of hydrogen bonds and coordination bonds between the amino acid and the Ti 3 C 2 T x surface. This interaction increased the binding energy by 2.5 times, preventing oxidation and degradation for over 90 days of storage. Moreover, during frictional processes, a TiN/TiO 2 reaction film formed between choline hydroxide, amino acids, and Ti 3 C 2 T x contributed to improved tribological properties, reducing the friction coefficient by up to 39.18 % and the wear rate by up to 69.79 %, while ensuring long-term friction stability.
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ChemistrySelect
·
2025
·Vol. 10
·期 15
·e202501120
·
IF 2
Peipei Ji,Xiuwu Wang,Lianpei Zhou,Guiyang Zhou,Tao Chen
Graphical This study develops polymeric micelles with Brönsted acid and pybox-Ru(II) catalysts encapsulated in hydrophobic cores for efficient one-pot tandem catalysis of deacetalization-transfer hydrogenation. The micelles, prepared via self-assembly of block copolymers, demonstrate excellent catalytic efficiency, offering a simple and effective strategy for tandem catalysis. One-pot tandem catalysis has been favored by researchers for its ability to achieve the advantage of a shortened production process. In this paper, polymeric micelles containing Brönsted acid/pybox-Ru(II) in the hydrophobic cores were prepared for one-pot tandem catalysis of deacetalization-transfer hydrogenation reaction. First, block copolymer P[NHS] 30 - b -P[PEG 2000 ] 68 containing activated ester (NHS) in the suspended chain was successfully synthesized by ring-opening metathesis polymerization (ROMP) using a functional monomer containing norbornene group (NB-NHS) and polyethylene glycol containing norbornene group (NB-PEG 2000 ) as the raw materials. Then, block copolymer P[COOH] 30 - b -P[PEG 2000 ] 68 containing Brönsted acid catalyst and complex P[pybox-Ru] 30 - b -P[PEG 2000 ] 68 containing pybox-Ru(II) catalyst were prepared by the activated ester functionalization strategy. The copolymers and complexes were characterized using nuclear magnetic resonance spectroscopy (NMR), X-ray photoelectron spectroscopy (XPS), and gel permeation chromatography (GPC). Then, polymeric micelles with the catalysts encapsulated in hydrophobic cores were achieved by the self-assembly of the above copolymers in water. The prepared polymeric micelles as catalytic nanoreactors were successfully applied to one-pot tandem catalysis of the deacetalization-transfer hydrogenation reaction, demonstrating excellent catalytic efficiency. This study provided a facile and efficient strategy for tandem catalysis.
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
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2020
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IF 7.489
Tingting Yan,Binglei Song,Delun Du,Zhenggang Cui,Xiaomei Pei
Innovations in surfactant structures are a feasible way to prepare unique molecular aggregates with interesting properties. Herein, taking dehydroabietic acid as the starting material, a new amine oxide surfactant, abbreviated as R-8-AO, was synthesized. Cryogenic transmission electron microscopy (cryo-TEM) images and circular dichroism (CD) spectra reveal that at suitable concentrations, R-8-AO molecules form rarely discovered right-handed chiral wormlike micelles , which have a cross-sectional diameter of 5–6 nm. The overlap concentration of R-8-AO is approximately 8 mM, above which the wormlike micelles began to entangle in solutions. Due to the strong van der Waals forces between R-8-AO molecules, the scaling law gives an exponent of 7.88, which is higher than the theory predicted value. Gold nanoparticles were synthesized in-situ by irradiating mixed solutions of HAuCl 4 and wormlike micelles formed by R-8-AO with UV light . These ultrasmall spherical gold nanoparticles, which are located at the surface of wormlike micelles, have a uniform particle size of 3 ± 1 nm, as observed by TEM. In addition, the gold nanoparticles form a worm-like morphology induced by the wormlike micelles, showing soft-aggregate-directed nanoparticle assembly. This work is first to reveal the effectiveness of preparing ultrasmall gold nanoparticles with new morphological wormlike micelles as soft templates. The resulting organic-inorganic hybrid aggregates are also expected to find applications in catalysis and electronic fields.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
·
IF 8.5
Geng Lu,Lisha Zhang,Liang Liu,Yue Zhang,Siyuan Wen,Jing Luo,Xin Zhou,Jun Wang,Zhengliang Ma
Due to the skin's limited self-repair capacity after injury, developing effective wound dressings is crucial to accelerate wound closure and enhance tissue regeneration. In the work, a thermo-sensitive and tissue-adhesive hydrogel with an interpenetrating polymer network (QGNPI) was fabricated by using N-isopropylacrylamide (NIPAM), galactomannan, and chitin-lignin micelles. The abundant hydroxyl groups within galactomannan conferred enhanced adhesion properties to the hydrogel. To improve the stability of artesunate, it was encapsulated within the chitin-lignin micelles. Moreover, the QGNPI hydrogel exhibited excellent thermal responsiveness and strong tissue adhesion, enabling effective wound closure. It also demonstrated outstanding hemocompatibility and cytocompatibility, supporting its suitability for wound healing applications. In murine models, the QGNPI hydrogel functioned as an efficient sealant, achieving sutureless wound closure during initial healing. Moreover, it significantly accelerated tissue regeneration by reducing inflammatory cell infiltration, promoting organized collagen deposition, and stimulating robust angiogenesis. Collectively, these findings underscore the potential of QGNPI as a promising thermosensitive and adhesive hydrogel dressing for advanced wound management.
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Polymer Chemistry
·
2017
·Vol. 8
·期 9
·1540-1554
·
IF 5.375
Jian-Bin Qiao,Yoonjeong Jang,Qian-Qian Fan,Seung-Hee Chang,Lei Xing,Peng-Fei Cui,Yu-Jing He,Soomin Lee,Sunghyun Hwang,Myung-Haing Cho,Hu-Lin Jiang
Safe and efficient drug delivery systems have received great attention for cancer therapy due to their enhanced cancer-targeting efficiency and reduced undesirable side effects. Administration, safety, and effectiveness are the main issues for clinical trials in nanomedicine. Here, we develop a series of poly(lactic-co-glycolic acid)-co-polyspermine (PLGA-PSPE) copolymers via a simple polymerization reaction between activated carboxyl groups of poly(lactic-co-glycolic acid) (PLGA) and amine groups of polyspermine (PSPE) with different molecular weights (Mw) for safe and efficient lung cancer drug delivery. PLGA-PSPE can self-assemble into polymeric micelles with a low critical micelle concentration. PLGA-PSPE had very low cytotoxicity and hemolytic activity. In addition, PLGA-PSPE also had no potential systemic toxicity after aerosol delivery to mice. Dihydroergotamine tartrate (DHE), which could suppress lung cancer cell survival by induction of apoptosis and mitophagy in the latest study, was employed as the model hydrophobic drug and encapsulated into PLGA-PSPE polymeric micelles (PLGA-PSPE/DHE). PLGA-PSPE/DHE could be stored at 25 °C for 7 days, and showed a controlled and sustained drug release, and time and dose dependent cellular uptake. Moreover, PLGA-PSPE/DHE efficiently increased apoptosis and mitophagy in A549 lung cancer cells. Furthermore, PLGA-PSPE/DHE significantly reduced tumor sizes and numbers, and efficiently suppressed lung tumorigenesis in K-rasLA1 lung cancer model mice after aerosol delivery. These results indicate that PLGA-PSPE polymeric micelles have a potential as an anticancer drug delivery carrier for lung cancer therapy.
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Molecular Therapy-Nucleic Acids
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2021
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IF 8.886
Jing Miao,Xiqin Yang,Xuwei Shang,Zhe Gao,Qian Li,Yun Hong,Jiaying Wu,Tingting Meng,Hong Yuan,Fuqiang Hu
Hepatitis B (HB) is a viral infectious disease that seriously endangers human health, and since there are no radical drugs to counter this, effective and safe therapies urgently need to be developed. HB virus (HBV) mainly infects hepatocytes (HCs), while the drugs are easily phagocytosed by Kupffer cells (KCs). In this study, the glutathione concentration difference between HCs and KCs was examined and utilized in an ideal drug-release strategy. Here, galactosylated chitosan-oligosaccharide-SS-octadecylamine (Gal-CSSO) was prepared to accurately deliver 10-23 DNAzyme DrzBC (blocking HBeAg expression) or DrzBS (blocking HBsAg expression) in targeted HB therapy. In vitro Gal-CSSO systems exhibited low cytotoxicity, endosomal escape, and glutathione responsiveness. The HBeAg and HBsAg secretion of HepG2.2.15 was significantly decreased by Gal-CSSO systems, and the maximum inhibition rates were 1.82-fold and 2.38-fold greater than those of commercial Lipofectamine 2000 (Lipo2000) systems. In vivo Gal-CSSO systems exhibited HC targeting and HC microenvironmental responsiveness without noticeable hepatotoxicity or systemic toxicity. The HBeAg and HBsAg titers of the HBV-infected mice were evidently decreased by Gal-CSSO systems, and the inhibition rates were 1.52-fold and 1.22-fold greater than those of Lipo2000 systems. This study presents a kind of glycolipid-like polymer micelles that promise efficient and safe gene therapy of HB.
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ACS Applied Materials & Interfaces
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2017
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IF 7.504
Danni Ran,Jiani Mao,Changyou Zhan,Cao Xie,Huitong Ruan,Man Ying,Jianfen Zhou,Wan-Liang Lu,Weiyue Lu
Compared to that of other tumors, various barriers, such as the blood–brain barrier (BBB), enzymatic barriers, and the blood–brain tumor barrier, severely impede the successful treatment of gliomas. Peptide ligands were frequently used as targeting moieties to mediate brain tumor-targeted drug delivery. LWSW (SYPGWSW) is a recently reported quorum-sensing (QS) peptide that is able to efficiently cross the BBB. Even though linear LWSW traverses the BBB in vitro, its in vivo targeting ability has been greatly impaired due to proteolysis. Here, we developed a stable peptide, DWSW (DWDSDWDGDPDYDS), using the retro-inverso isomerization technique to achieve an enhanced antiglioma effect. In vitro studies have demonstrated that both the LWSW and DWSW peptides possessed excellent tumor-homing properties and barrier-penetration abilities, whereas DWSW exhibited exceptional stability in serum and maintained its targeting ability after serum preincubation. In vivo, DWSW-modified probes and micelles accumulated more efficiently in the glioma region in comparison with LWSW-modified probes and micelles because of full resistance to proteolysis in blood circulation. As expected, DWSW-modified paclitaxel (PTX)-loaded micelles (DWSW Micelle/PTX) exhibited the longest median survival time among glioma-bearing nude mice. Our results suggested that the QS peptide appears to be a promising targeting moiety, with potential applications in glioma-targeted drug delivery.
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