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普朗尼克F127
JOURNAL OF DISPERSION SCIENCE AND TECHNOLOGY · 2020 · IF 1.701

Liposomes consisting of pluronic F127 and phospholipid: Effect of matrix on morphology, stability and curcumin delivery

Ziling Li,Yousheng Huang,Shengfeng Peng,Xing Chen,Liqiang Zou,Wei Liu,Chengmei Liu

We prepared liposomes consisting of different ratios of phospholipid and pluronic F127 (F127-Lps), then evaluated the effect of matrix on the morphology, stability and carriers’ property of liposomes. The particle size of liposomes was significantly decreased after pluronic F127 modification. Pluronic F127 at low ratio may incorporate into liposomes and form spherical and lamellar structure, while pluronic F127 at high ratio can form mixed aggregates with spherical micelles and lamellar vesicles. The membrane stability of liposomes was enhanced with increasing of pluronic F127 ratio. Curcumin was encapsulated into F127-Lps (cur-F127-Lps) with an entrapment efficiency of 89%. The higher the ratio of pluronic F127 was, the slower the release rate of curcumin. First order model was the main release mechanism for curcumin loaded liposomes. These results are useful for designing liposome-based food delivery systems that can be used in functional foods.

CAS / MDL: 458-37-7
研究领域: 食品科学 · 药剂学
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JOURNAL OF MICROENCAPSULATION · 2020 · IF 2.287

Novel folated pluronic F127 modified liposomes for delivery of curcumin: preparation, release, and cytotoxicity

Ziling Li,Xiangyuan Xiong,Shengfeng Peng,Xing Chen,Wei Liu,Chengmei Liu

Aim: A novel folated pluronic F127 (FA-F127) was synthesised, so as to modify liposomes with FA group on the surface, and evaluate the effects of FA-F127 modification on the properties of the modified liposomes.Methods: FA was linked to one end of pluronic F127, via the terminal OH group, to obtain FA-F127 and the structure was characterised. FA-F127 modified curcumin liposomes (cur-FA-F127-Lps) were prepared. The physicochemical characteristics of cur-FA-F127-Lps, including morphology and particle size, were studied. The in vitro cytotoxicity of cur-FA-F127-Lps against KB cancer cells was determined by MTT tests.Results: The effects of FA-F127 modification on the average particle size, PDI, curcumin encapsulation efficiency and microstructure were not significant. Compared with nonfolated F127 liposomes (cur-F127-Lps), cur-FA-F127-Lps exhibited significantly higher cytotoxicity towards KB cells.Conclusions: Folic acid modified liposomes provide a novel strategy to improve the chemotherapeutic efficacy of hydrophobic bioactive compounds.

CAS / MDL: 458-37-7
研究领域: 药剂学 · 药物递送系统 · 纳米技术 · 肿瘤学
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ARABIAN JOURNAL FOR SCIENCE AND ENGINEERING · 2025 · IF 2.9

pH- and Reduction-Responsive Supramolecular Hydrogels Based on Pluronic F127-Modified Hyaluronic Acid for the Targeted Delivery of Doxorubicin

Li Caixia,Zhou Qin,Chao Zhenzhen,Li Liang

In this study, the preparation of pH- and reduction-responsive doxorubicin (DOX)-loaded hyaluronate acid-F127 supramolecular hydrogels (DOX@Gels) with targeting ability due to the incorporation of hyaluronic acid is described. By combining Pluronic F127-modified hyaluronic acid (HA-F127), disulfide-modified β-cyclodextrin, α-cyclodextrin, and DOX, hydrogels were constructed through host–guest complexation and hydrogen bonding interactions, and a tailored platform for targeted drug delivery was provided. The chemical composition and rheological properties were comprehensively analyzed. Considering the controlled complexation between DOX and the hydrogel skeleton and the ability of HA to target cancer cells, controlled drug release from the hydrogel G[15,5,5] was investigated under various conditions in vitro. The cumulative amount of DOX released from hydrogel G[15,5,5] showed superior pH- and reduction-controlled release behavior. These results were likely caused by the HA-F127 ester bonds cleavage in acidic environments and the S‒S bond cleavage within the hydrogel networks in the presence of glutathione. Furthermore, the DOX release kinetics were analyzed using Higuchi and Korsmeyer-Peppas models. The results demonstrated that the experimental data was effectively fit with these two models, and the data fitted by using Korsmeyer-Peppas also indicated nonFickian diffusion kinetics of the DOX being released from hydrogels. Owing to the ability of HA to target SKOV-3 cells, the cytotoxicity experiments revealed that DOX@G[15,5,5] exhibited more significant anticancer effects than free DOX. Consequently, DOX@Gels containing HA have emerged as promising candidates for the targeted delivery and release of anticancer drugs.

CAS / MDL: 9067-32-7 9003-11-6
研究领域: 药剂学 · 生物材料 · 肿瘤学
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Tissue Engineering Part A · 2021 · IF 3.845

Electrohydrodynamic 3D Printing Scaffolds for Repair of Achilles Tendon Defect in Rats

Hang Zhang,Zijie Pei,Changbao Wang,Mingshan Li,Hongtao Zhang,Jing Qu

Tissue engineering (TE) studies for Achilles tendon (AT) defects are a difficult and popular field in orthopedic medical practice. In this study, we applied electrohydrodynamic three-dimensional (3D) printing technology to construct scaffolds made of poly-(ɛ-ɛ-caprolactone) (PCL) and Pluronic F127 (F127) with different mass-volume ratios. The fibers and porous capabilities of the scaffolds were controlled using this technology. We found that F127 improved the hydrophilicity and degradation of PCL in vitro. The PCL scaffolds with 5% F127 were mostly favorable for cell adhesion and growth, suggesting that the scaffolds had good biocompatibility in vitro. Scaffolds with 5% F127 seeded with C3H10T1/2 cells were transplanted into AT defects in rats. A histological analysis indicated that the TE scaffolds were beneficial for the accumulation and arrangement of collagen fibers. Thus, this study provides fundamental experimental data for future clinical applications regarding TE for ATs.Impact statementElectrohydrodynamic three-dimensional (3D) printing can be used to construct tissue-engineered scaffolds with controllable fibers and good porosity. Pluronic-F127 (F127) improved the hydrophilicity and degradation of the poly-(ɛ-ɛ-caprolactone) (PCL), and a better microscale structure was obtained. The scaffolds with 5% F127, with good pore structures, were favorable for C3H10T1/2 cell growth and cellular morphology, indicating that they had good biocompatibility. In vivo transplantation experiments showed that scaffolds with 5% F127 improved the arrangement of collagen fibers, encouraging their potential application in the construction of future tissue-engineered tendons.

CAS / MDL: 64-19-7
研究领域: 骨科 · 组织工程 · 生物医学工程 · 再生医学
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ACS Omega · 2021 · IF 3.512

pH-Responsive Pluronic F127–Lenvatinib-Encapsulated Halogenated Boron-Dipyrromethene Nanoparticles for Combined Photodynamic Therapy and Chemotherapy of Liver Cancer

Jingjing Zong,Hao Peng,Xin Qing,Zhe Fan,Wenjing Xu,Xuanlong Du,Ruihua Shi,Yewei Zhang

Combination therapy such as photodynamic therapy (PDT)-enhanced chemotherapy is regarded as a promising strategy for cancer treatment. Boron-dipyrromethene (BODIPY), as close relatives of porphyrins, was widely used in PDT. However, poor water solubility, rapid metabolism by the body and lack of targeting limits its clinical application. Lenvatinib, as the first-line drug for molecular-targeted therapy of liver cancer, restricted its clinical application for its side effects. Herein, to achieve the synergy between PDT and chemotherapy, we synthesized two halogenated BODIPY, BDPBr2 and BDPCl2, which were prepared into self-assembly nanoparticles with lenvatinib, and were encapsulated with Pluronic F127 through the nanoprecipitation method, namely, LBPNPs (LBBr2 NPs and LBCl2 NPs). The fluorescence quantum yields of LBPNPs were 0.73 and 0.71, respectively. The calculated loading rates of lenvatinib for LBBr2 NPs and LBCl2 NPs were 11.8 and 10.2%, respectively. LBPNPs can be hydrolyzed under weakly acidic conditions (pH 5.0) to generate reactive oxygen species (ROS), and the release rate of lenvatinib reached 88.5 and 82.4%. Additionally, LBPNPs can be effectively taken up by Hep3B and Huh7 liver cancer cells, releasing halogenated BODIPY and lenvatinib in the acidic environment of tumor cells to enhance the targeting performance of chemotherapeutics. Compared with free lenvatinib and separate halogenated BODIPY, LBPNPs can inhibit tumor growth more effectively through pH-responsive chemo/photodynamic synergistic therapy and significantly promote the cascade of caspase apoptotic protease. This study shows that LBPNPs can be a promising nanotheranostic agent for synergetic chemo/photodynamic liver cancer therapy.

研究领域: 药学 · 纳米技术 · 癌症研究 · 生物医学工程
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MOLECULAR AND CELLULAR BIOCHEMISTRY · 2022 ·Vol. 478 ·期 2 ·241-247 · IF 3.842

Pluronic F127-liposome-encapsulated curcumin activates Nrf2/Keap1 signaling pathway to promote cell migration of HaCaT cells

Zhou Quan,Cai Xu,Huang Ying,Zhou Youliang

Curcumin (CUR) is an extract of Curcuma longa Linn., which has various pharmacological activities. The instability, low water solubility and bioavailability of CUR greatly limit its clinical application. This work prepared Pluronic F127-liposome-encapsulated curcumin (CUR-LIP-F127) and explored its functional role in wound healing. Liposome-encapsulated curcumin (CUR-LIP) and CUR-LIP-F127 were prepared. Human keratinocyte cell line (HaCaT) was treated with CUR, Pluronic F127-liposome (LIP-F127) and CUR-LIP-F127, or combined with ML385 (Nrf2 inhibitor). The expression of mRNAs and proteins was detected by quantitative real-time PCR and western blotting. MTT and wound healing assays were performed to detect cell viability and migration. CUR, LIP-F127 and CUR-LIP-F127 all had no influence on cell viability of HaCaT cells. CUR-LIP-F127 treatment significantly accelerated cell migration and enhanced the expression of nuclear factor erythroid-related factor 2 (Nrf2) and kelch-like erythroid cell-derived protein 1 (Keap1) in HaCaT cells with respect to CUR or LIP-F127 treatment. ML385 treatment impaired CUR-LIP-F127-mediated promotion of migration and up-regulation of Nrf2 and Keap1 in HaCaT cells. This work demonstrated that CUR-LIP-F127 activated Nrf2/Keap1 signaling pathway to promote migration of HaCaT cells, suggesting that CUR-LIP-F127 may contribute to wound healing.

研究领域: 药理学 · 细胞生物学 · 材料科学 · 生物医学工程
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ACS Nano · 2022 · IF 18.027

Insight into Drug Loading Regulated Micellar Rigidity by Nuclear Magnetic Resonance

Xi Hu,Yu Sun,Xiaoqi Zhou,Bo Zhang,Hanxi Guan,Fan Xia,Shuangying Gui,Xueqian Kong,Fangyuan Li,Daishun Ling

The rigidity of polymeric micelles plays an important role in their biological behaviors. However, how drug loading affects the rigidity of polymeric micelles remains elusive. Herein, the indomethacin (IMC)-loaded Pluronic F127 micelle is used as a model system to illustrate the impact of drug loading on the rigidity and biological behaviors of polymeric micelles. Against expectations, micelles with moderate drug loading show higher cellular uptake and more severe cytotoxicity as compared to both high and low drug loading counterparts. Extensive one- and two-dimensional nuclear magnetic resonance (NMR) measurements are employed to reveal that the higher drug loading induces stronger interaction between IMC and hydrophilic block to boost the micellar rigidity; consequently, the moderate drug loading imparts micelles with appropriate rigidity for satisfactory cellular uptake and cytotoxicity. In summary, NMR spectroscopy is an important tool to gain insight into drug loading regulated micellar rigidity, which is helpful to understand their biological behaviors.

研究领域: 药学 · 生物物理学 · 材料科学 · 核磁共振波谱学
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Biomolecules · 2022 ·Vol. 12 ·期 9 ·1263 · IF 6.064

Mucus-Penetrating Silk Fibroin-Based Nanotherapeutics for Efficient Treatment of Ulcerative Colitis

Dengchao Xie,Xin Zhou,Bo Xiao,Lian Duan,Zhenhua Zhu

Oral nanoparticles have been considered a prospective drug delivery carrier against ulcerative colitis (UC). To enhance the mucus-penetrating capacity and aqueous solubility, and strengthen the anti-inflammatory effect of resveratrol (RSV), we fabricated RSV-loaded silk fibroin-based nanoparticles with the functionalization of Pluronic F127 (PF-127). The obtained PF-127-functionalized RSV-loaded NPs had an average particle size around 170 nm, a narrow size distribution (polydispersity index < 0.2), and negative zeta potential (−20.5 mV). Our results indicated that the introduction of PF-127 strengthened the mucus-penetrating property of NPs. In vitro studies suggested that NPs with PF-127 enhanced the suppression of the secretion of proinflammatory cytokine TNF-α and reactive oxygen species (ROS) from RAW 264.7 macrophages under lipopolysaccharide stimulation in comparison with other counterparts. According to the evaluation of macro symptoms and main inflammatory cytokines, we further report preferable therapeutic outcomes achieved by PF-127 functionalized-NP-treated dextran sulphate sodium (DSS) groups in the colitis model compared with blank silk fibroin NPs and RSV-loaded NPs without the functionalization of PF-127. Taken together, this work suggests that the fabricated PF-127 NPs via the oral route are promising and useful RSV-loaded nanocarriers for UC treatment.Keywords:silk fibroin;resveratrol;nanoparticles;ulcerative colitis

研究领域: 药学 · 纳米技术 · 炎症 · 药物递送系统
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JOURNAL OF NANOBIOTECHNOLOGY · 2018 ·Vol. 16 ·期 1 ·1-15 · IF 5.294

RETRACTED ARTICLE: Injectable hydrogel encapsulating Cu2MnS2 nanoplates for photothermal therapy against breast cancer

Fu Ji-jun,Chen Ming-yue,Li Jie-xia,Zhou Jun-hua,Xie Sheng-nan,Yuan Ping,Tang Bo,Liu Cheng-cheng

Background In order to explore the possibility of treating breast cancer by local photo-therapy, a photothermal agents loaded in situ hydrogel was established. In detail, The Cu2MnS2 nanoplates were prepared by one-pot synthesis and, the thermosensitive Pluronic F127 was used as the hydrogel matrix. The Cu2MnS2 nanoplates and the hydrogel were characterized by morphous, particle size, serum stability, photothermal performance upon repeated 808 nm laser irradiation as well as the rheology features. The therapeutic effects of the Cu2MnS2 nanoplates and the hydrogel were evaluated qualitatively and quantitatively in 4T1 mouse breast cancer cells. The retention, photothermal efficacy, therapeutic effects and systemic toxicity of the hydrogel were assessed in tumor bearing mouse model.Results The Cu2MnS2 nanoplates with a diameter of about 35 nm exhibited satisfying serum stability, photo-heat conversion ability and repeated laser exposure stability. The hydrogel encapsulation did not negatively influence the above features of the photothermal agent. The nanoplates loaded in situ hydrogel shows a phase transition at body temperature and, as a result, a long retention in vivo.Conclusion sThe photothermal agent embedded hydrogel played a promising photothermal therapeutic effects in tumor bearing mouse model with low systemic toxicity after peritumoral administration.

研究领域: 肿瘤学 · 纳米医学 · 生物医学工程 · 材料科学
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International Journal of Nanomedicine · 2024 · IF 6.6

Utilization of Nitrogen-Doped Graphene Quantum Dots to Neutralize ROS and Modulate Intracellular Antioxidant Pathways to Improve Dry Eye Disease Therapy

Zixia Wu,Weibo Xia,Liling Ou,Ling Zheng,Bingying Hou,Tonghe Pan,Wenjie Sun,Leo H Koole,Yongqing Shao,Lei Qi

Purpose Patients afflicted with dry eye disease (DED) experience significant discomfort. The underlying cause of DED is the excessive accumulation of ROS on the ocular surface. Here, we investigated the nitrogen doped-graphene quantum dots (NGQDs), known for their ROS-scavenging capabilities, as a treatment for DED.Methods NGQDs were prepared by using citric acid and urea as precursors through hydrothermal method. The antioxidant abilities of NGQDs were evaluated through: scavenging the ROS both extracellular and intracellular, regulating the nuclear factor-erythroid 2-related factor (Nrf2) antioxidant pathway of human corneal epithelial cells (HCECs) and their transcription of inflammation related genes. Furthermore, NGQDs were modified by Arg-Gly-Asp-Ser (RGDS) peptides to obtain RGDS@NGQDs. In vivo, both the NGQDs and RGDS@NGQDs were suspended in 0.1% Pluronic F127 (w/v) and delivered as eye drops in the scopolamine hydrobromide-induced DED mouse model. Preclinical efficacy was compared to the healthy and DPBS treated DED mice.Results These NGQDs demonstrated pronounced antioxidant properties, efficiently neutralizing free radicals and activating the intracellular Nrf2 pathway. In vitro studies revealed that treatment of H2O2-exposed HCECs with NGQDs induced a preservation in cell viability. Additionally, there was a reduction in the transcription of inflammation-associated genes. To prolong the corneal residence time of NGQDs, they were further modified with RGDS peptides and suspended in 0.1% Pluronic F127 (w/v) to create RGDS@NGQDs F127 eye drops. RGDS@NGQDs exhibited superior intracellular antioxidant activity even at low concentrations (10 μg/mL). Subsequent in vivo studies revealed that RGDS@NGQDs F127 eye drops notably mitigated the symptoms of DED mouse model, primarily by reducing ocular ROS levels.Conclusion Our findings underscore the enhanced antioxidant benefits achieved by modifying GQDs through nitrogen doping and RGDS peptide tethering. Importantly, in a mouse model, our novel eye drops formulation effectively ameliorated DED symptoms, thereby representing a novel therapeutic pathway for DED management.

研究领域: 眼科 · 材料科学 · 药学 · 细胞生物学
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Journal of Biomedical Nanotechnology · 2020 ·Vol. 16 ·期 10 ·1463-1470 · IF 4.483

Anti-Inflammatory Efficacy of Fabricated Rhein Micelles

Ding Xiangyu,Wang Yuan,Wen Chunmei,Wang Silu,Ruan Qingqing,Li Zhaofeng,Xu Jinzhong,Xu Zheng,Deng Jie

Rhein is a potential anti-inflammatory agent, but its poor water solubility significantly restricts its clinical application. In this study, rhein micelles (RMs) with improved water solubility were fabricated on Pluronic F127 (F-127). Transmission electron microscopy showed that the as-prepared RMs displayed a mean diameter of approximately 20 nm and a spherical morphology. The encapsulation efficiency of the micelles towards drugs varied from 81.38 ± 4.35% to 24.87 ± 4.32%. The RMs exhibited a burst release during the first 6 h and a following sustained release up to 96 h with a biphasic drug release pattern as suggested by the drug release assay. Cytotoxicity assessment showed that the RMs caused no change in cell viability at drug concentrations below 40 μM after 24 and 48 h of incubation. In RAW264.7 macrophages, the RMs inhibited the lipopolysaccharide-induced activation of p65/NF-κB, which in turn suppressed the transcription of its downstream inducible nitric oxide synthase, and cytokine genes such as interleukin-1β and tumor necrosis factor-α . Simultaneously, the RMs led to reduced cytokine secretions, including cyclooxygenase-2, prostaglandin E2, nitric oxide, and interleukin-6 in a dose-dependent manner. The RMs reported herein may be a promising candidate for developing anti-inflammatory therapeutic formulations.

研究领域: 药学 · 纳米技术 · 炎症研究
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Frontiers in Pharmacology · 2019 · IF 3.845

Synergistic Effect of Retinoic Acid Polymeric Micelles and Prodrug for the Pharmacodynamic Evaluation of Tumor Suppression

Zhu Yan-Hua,Ye Ning,Tang Xin-Feng,Khan Malik Ihsanullah,Liu Hong-Liang,Shi Ning,Hang Li-Feng

All-trans retinoic acid (ATRA) is an effective agent that induces differentiation, inhibits cell proliferation, and acts as an anticancer agent. ATRA was successfully conjugated with Pluronic F127 via esterification to enhance its anticancer effects. Pluronic-ATRA showed high cytotoxicity and inhibitory concentrations (IC50) 50% lower than those of ATRA in various breast cancer cell lines (4T1:31.16–8.57 μg/mL; EMT6: 50.48–7.08 μg/mL; MDA-MB-231:37.58–8.99 μg/mL; BT474:25.27–9.09 μg/mL). In combination with chemotherapy, Pluronic-ATRA synergistically enhanced the cytotoxic effects of cisplatin (CDDP). Pluronic-ATRA combined with CDDP effectively suppressed breast tumor growth in vivo. The results of this study demonstrate the potential of Pluronic-ATRA as an anticancer agent that can be used in combination therapy against solid tumors.

CAS / MDL: 1122-58-3 25952-53-8
研究领域: 药理学 · 肿瘤学 · 纳米技术 · 药物递送系统
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