Drug Delivery and Translational Research
·
2024
·
IF 5.7
Wang Yueli,Li Dongbo,Li Xiaojuan,Ren Dandan,Zhang Wei,Shu Gang,Lin Juchun,Li Haohuan,Xu Funeng,Peng Guangneng,Fu Hualin
Metamizole easily decomposes in the body and has a short action time and low bioavailability. Hence, frequent injection administrations are needed to maintain its plasma concentration. This study aimed to design and develop an in-situ gel based on poloxamer 407 and 188 to assess its long-acting antipyretic effects. The in-situ gel-forming systep00m with optimum sol–gel transition temperature of 35.9 °C to 36.3 °C could be formed using a combination of P407 at a ratio of 21–23% (w/v) and P188 at a ratio of 2–4% (w/v). In vitro erosion test showed that the in-situ gel’s erosion curve and the metamizole release rate both reached about 90% at 6 h, revealing a good linear relationship between the in-situ gel erosion and the drug release. In vitro release test with dialysis tube showed that the release of metamizole from the in-situ gel was remarkably slower than that from the metamizole solution. Approximately 85% of metamizole was released in the dialysis tube within 7 h, implying a good sustained release effect. Pharmacodynamic study showed that the in-situ gel injection extended the action time of metamizole relative to that when using the metamizole solution. Pharmacokinetic study revealed that the in-situ gel significantly increased the blood serum half-life and area under the curve), contributing to a sustained release and improved bioavailability. This study demonstrated that in-situ gel injection could prolong the action of metamizole in the body to reduce the number of administration times and has good clinical application. Graphical Abstract
研究领域:
药剂学
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药物传递系统
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
EUROPEAN POLYMER JOURNAL
·
2024
·
IF 5.8
Ze Xu,Jun Gao,Hongyu Zhang,Guojun Zheng,Jihong Hu,Junyao Li,Laidi Xu,Yong Kong
A thermosensitive hydrogel based on 6-deoxy-6-arginine grafted chitosan (DAC) and poloxamer 407 (P407) is prepared for wound repair. Since P407 is a thermosensitive polymer, the resultant DAC/P407-gel exhibits thermo-responsive sol–to–gel phase transition behaviors with a phase transition temperature (T sol/gel ) of ∼ 26.5 °C, making it an appropriate material for wound healing. The DAC/P407-gel has a three-dimensional (3D) network structure with large amounts of pores, and the good air permeability of the hydrogel makes it an attractive candidate as wound dressing. The introduction of DAC can not only increase the mechanical strength of the hydrogel but also significantly enhance its biological indexes including antibacterial activity, blood-clotting index (BCI) and hemocompatibility. The cytotoxicity test reveals that the developed DAC/P407-gel also shows outstanding cytocompatibility.
研究领域:
生物材料学
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医学工程
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药剂学
✓ 已验证
产品关联
DOI
高影响因子
MOLECULAR PHARMACEUTICS
·
2023
·
IF 4.9
Kehong Dong,Mei Zhang,Ying Liu,Xintao Gao,Xiaochen Wu,Dayong Shi,Chuanlong Guo,Jing Wang
Excessive acetaminophen (APAP) induces excess reactive oxygen species (ROS), leading to liver damage. Pterostilbene (PTE) has excellent antioxidant and anti-inflammatory activities, but poor solubility limits its biological activity. In this study, we prepared PTE-loaded Soluplus/poloxamer 188 mixed micelles (PTE-MMs), and the protective mechanism against APAP-induced liver injury was investigated. In vitro results showed that PTE-MMs protected H2O2-induced HepG2 cell proliferation inhibition, ROS accumulation, and mitochondrial membrane potential destruction. Immunofluorescence results indicated that PTE-MMs significantly inhibited H2O2-induced DNA damage and cGAS-STING pathway activation. For in vivo protection studies, PTE-MMs (25 and 50 mg/kg) were administered orally for 5 days, followed by APAP (300 mg/kg). The results showed that APAP significantly induced injury in liver histopathology as well as an increase in serum aspartate aminotransferase and alanine aminotransferase levels. Moreover, the above characteristics of APAP-induced acute liver injury were inhibited by PTE-MMs. In addition, APAP-induced changes in the activities of antioxidant enzymes such as SOD and GSH in liver tissue were also inhibited by PTE-MMs. Immunohistochemical results showed that PTE-MMs inhibited APAP-induced DNA damage and cGAS-STING pathway activation in liver tissues. For in vivo therapeutic effect study, mice were first given APAP (300 mg/kg), followed by oral administration of PTE-MMs (50 mg/kg) for 3 days. The results showed that PTE-MMs exhibited promising therapeutic effects on APAP-induced acute liver injury. In conclusion, our study shows that the Soluplus/poloxamer 188 MM system has the potential to enhance the biological activity of PTE in the protection and therapeutic of liver injury.
研究领域:
药剂学
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肝脏病学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2019
·
IF 3.973
Yuxiang Sun,Fangfang Shi,Yajun Niu,Yu Zhang,Fei Xiong
Lipid deposition induced various diseases including nonalcoholic fatty liver and hyperlipemia. The excessive accumulation of triglyceride (TG) and the deposition of fat were the two most critical causes. Here, we developed Fe 3 O 4 @ [email protected] nanoparticles (NPs) with amphiphilic structures, which exhibited an excellent role in eliminating excess TG. Hydrophobic TG was adsorbed efficiently by Fe 3 O 4 @ [email protected] NPs through the “liposuction effect” and the formation of [email protected] complex was then conducted. The [email protected] complex was further enclosed by the endosome based on the endocytosis and subsequently was taken into the lysosome, degrading with the help of lipases. Meanwhile, the “nano-enzyme effect” of Fe 3 O 4 NPs recovered the lipid-regulated proteins including PPARα, further triggering biodegradation pathways of TG, although the lipid-regulated proteins were obviously inhibited in the high-fat hepatocytes models. These two mechanisms of Fe 3 O 4 @ [email protected] NPs together achieved the down-regulation of TG in vivo and in vitro. Therefore, our findings provided a novel thought in treating these diseases associated with lipid deposition, that is, nanoparticles modified by specific structure exhibit a superior TG removal.
研究领域:
纳米技术
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药理学
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肝病学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
ACS Omega
·
2023
·
IF 4.1
Zhijiang Sun,Zehua Yin,Mingyu Zhang,Dongli Guo,Fen Ran
At present, the design and fabrication of polymer membranes with high permeability and good retention ability are still huge challenges. In this study, the commercial Poloxamer 407 (Pluronic F127) is selected as a multifunctional additive, and polyvinylpyrrolidone is used as a pore-forming agent to modify the poly(ether sulfone) membrane by liquid–liquid phase conversion technology to prepare an ultrafiltration membrane with excellent performance. The hydrophobic poly(propylene oxide) segment in Poloxamer 407 guarantees that this copolymer can be firmly anchored to the poly(ether sulfone) matrix, and the hydrophilic poly(ethylene oxide) segments in Poloxamer 407 impart a stronger hydrophilic nature to the modified membrane surface. Therefore, the permeability and hydrophilicity of the modified membrane are significantly improved and the modified membrane also has good stability. When the amount of Poloxamer 407 added to the casting solution reached 0.6 g, the water flux of the modified membrane was as high as 368 L m–2 h–1, and the rejection rate of bovine serum albumin was close to 98%. In the test to isolate organic small molecule dyes, the retention rate of the modified membrane to Congo red is 94.27%. In addition, the modified membrane shows an excellent water flux recovery rate and antifouling ability. It performs well in subsequent cycle tests and long-term membrane life tests and can be used repeatedly. Our work has resulted in poly(ether sulfone) membranes with good performance, which show great potential in the treatment of biomedical wastewater and the removal of industrial organic dye wastewater, it provides ideas for the development and application of amphiphilic polymer materials.
研究领域:
材料科学
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膜技术
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环境工程
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
Journal of Pharmaceutical Innovation
·
2019
·Vol. 15
·期 1
·155-162
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IF 1.452
Huang Zhengwei,Wu Mingjun,Ma Cheng,Bai Xuequn,Zhang Xuejuan,Zhao Ziyu,Huang Ying,Pan Xin,Wu Chuanbin
Objective Solid lipid nanoparticles (SLN) mainly consist of lipids and surfactants. However, the toxicity of surfactant cannot be ignored, as the surfactant may cause unexpected side effect. This study established model SLN with different surfactants, Tween 80 (T80) and poloxamer 188 (P188). It was aimed to establish ultraviolet-visible (UV-Vis) spectroscopy methods for quantifying the contents of T80 and P188 in the model SLN. Methods The model SLN were produced by emulsification-precipitation method, and their particle size distribution was analyzed. The calibration curves for the contents of T80 and P188 were established. Surfactants in the model SLN were extracted by ultrasonication, and UV-Vis spectroscopy methods were utilized for quantification of surfactants in SLN. Results The deviation of precision and accuracy in P188 and T80 assay were acceptable, which indicated the method could be employed in sample quantification. Ten minutes was considered as the optimal ultrasonication time. And the contents of P188 and T80 were successfully measured by the established UV-Vis methods. Conclusion The UV-Vis spectroscopy methods were developed for the quantification of T80 and P188 in the model SLN. It is expected that the methods could be extended to more SLN systems and applied for the quantification of other surfactants.
研究领域:
药剂学
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分析化学
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DOI
高影响因子
Materials Research Express
·
2020
·Vol. 7
·期 10
·105401
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IF 1.929
Qian Wu,Liang Li
In this paper, the composite gels based on poloxamer and chitosan with different contents were prepared for thermal sensitive mucosal drug delivery. The sol-gel transition temperature and rheological viscosity of the obtained gels were detected to select the optimum candidate for vaginal drug delivery. Electrochemistry impedance spectroscopy (EIS) was utilized to probe the hole structure in optimum hydrogel immersing in the vaginal fluid stimulant (VFS) for different time. The drug releasing rate of ethinyloestradiol loaded by the optimum hydrogel was examined. The drug releasing results suggested that the releasing rate satisfied with the Higuchi model, while the EIS results confirmed more pores in the composite gels would be formed during the immersing process in the VFS. The results indicated that the gel with the optimum formula met the requirements of vaginal medication. This research suggested poloxamer/chitosan might be an effective type of thermal gel for drug delivery in vagina.
研究领域:
药剂学
·
生物材料
✓ 已验证
DOI
高影响因子
Materials Today Bio
·
2025
·
IF 10.2
Ruifang Han,Haiyi Zhou,Xingshan Liang,Siyi He,Xiaoming Sun,Yongge Guan,Yang Song
Endometrium plays a key role in embryo implantation and maintenance of pregnancy. However, to repair endometrial injury is still a challenge. In recent years, hydrogel materials have been widely used as effective support matrices to prevent intrauterine adhesions after endometrial injury. They can also be used as preparation scaffolds for encapsulating MSCs and certain therapeutic drugs. This study aimed to develop a preparation scaffold with high tissue affinity, high viscoelasticity and controlled release for repair of endometrial injury. The scaffold utilized heparin poloxamer (HP) as the matrix material and ε-polylysine (EPL) as the functional excipient to prepare a hydrogel that is suitable for endometrial adhesion and further encapsulate BMSCs. Furthermore, a strategy of the thermo-sensitive EPL-HP hydrogel-encapsulated BMSCs were used for better homing of BMSC after transplantation into the rat endometrial injury model, so as to exert the potential of endometrial regeneration by activating Nrf2 to regulate SDF-1/CXCR4 axis.
研究领域:
生殖医学
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组织工程
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干细胞研究
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DOI
PubMed
高影响因子
MOLECULES
·
2022
·Vol. 27
·期 16
·5326
·
IF 4.927
Xianwen Song,Gang Lu,Jingxing Wang,Jun Zheng,Shanying Sui,Qiang Li,Yi Zhang
Polyacrylamide has promising applications in a wide variety of fields. However, conventional polyacrylamide is prone to hydrolysis and thermal degradation under high temperature conditions, resulting in a decrease in solution viscosity with increasing temperature, which limits its practical effect. Herein, combining molecular dynamics and practical experiments, we explored a facile and fast mixing strategy to enhance the thermal stability of polyacrylamide by adding common poloxamers to form the interpenetrating network hydrogel. The blending model of three synthetic polyacrylamides (cationic, anionic, and nonionic) and poloxamers was first established, and then the interaction process between them was simulated by all-atom molecular dynamics. In the results, it was found that the hydrogen bonding between the amide groups on all polymers and the oxygen-containing groups (ether and hydroxyl groups) on poloxamers is very strong, which may be the key to improve the high temperature resistance of the hydrogel. Subsequent rheological tests also showed that poloxamers can indeed significantly improve the stability and viscosity of nonionic polyacrylamide containing only amide groups at high temperatures and can maintain a high viscosity of 3550 mPa·S at 80 °C. Transmission electron microscopy further showed that the nonionic polyacrylamide/poloxamer mixture further formed an interpenetrating network structure. In addition, the Fourier transform infrared test also proved the existence of strong hydrogen bonding between the two polymers. This work provides a useful idea for improving the properties of polyacrylamide, especially for the design of high temperature materials for physical blending.
研究领域:
材料科学
·
分子动力学
·
高分子化学
✓ 已验证
DOI
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2023
·
IF 5.2
Yue Lei,Yue Zhou,Yuheng Li,Yue Liu,Haiyan Gao,LiangLiang Lin,Hujun Xu
This study aimed to develop a temperature-sensitive perm agent that can reduce the risk of the active ingredient sodium thioglycolate (TGA(Na) in the perm agent to humans. We found that the loading of TGA(Na) in the pure poloxamer formulation reduces its gelation temperature and allows it to gel at room temperature , so we added cationic surfactants to increase its gelation temperature. The temperature-sensitive perm agent was prepared by adjusting the ratio of additives to the desired temperature, and it remained liquid below 32 °C and solidified on contact with the scalp (32 °C). The release behavior of sodium thioglycolate was studied by in vitro release studies and rheology, and the perm performance was investigated. The results showed that its perm efficiency was comparable to that of conventional perm agents, but its sodium thioglycolate transdermal volume was much lower than that of conventional perm agents, with a reduction of nearly 62 %. These results suggest the potential of the temperature-sensitive perm as a healthier alternative for perm design products.
研究领域:
药剂学
·
材料科学
✓ 已验证
DOI
高影响因子
CARBOHYDRATE POLYMERS
·
2022
·
IF 10.723
Rixiang Su,Peiyuan Li,Ying Zhang,Yingbin Lv,Fangzhou Wen,Wei Su
The design and development of smart shape-adaptable wound dressings with superior antimicrobial ability remain a challenge in therapeutic and clinical application. Herein, polydopamine/tannic acid/chitosan/poloxamer 407/188 hydrogel (PTCPP) was prepared with the aim of developing an in situ -formed antibacterial wound dressing with temperature stimulation and near-infrared radiation (NIR) responsive ability. PTCPP possessed injectability, photothermal stability, sustained release properties and cytocompatibility. In vitro antibacterial results showed that the bactericidal rates of PTCPP against Staphylococcus aureus ( S. aureus ) and Escherichia coli ( E. coli ) under NIR irradiation were 99.994 % and 99.91 %, respectively. In vivo experiments, PTCPP can adapt to shape of the wound, showing good adhesion, while promoting wound healing in bacterial infections. Therefore, PTCPP has potential application in the treatment of infectious wounds, and provides a strategic choice for developing antibacterial wound dressing combined with photothermal therapy.
研究领域:
材料科学
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生物医学工程
·
药学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Bioengineering and Biotechnology
·
2022
·
IF 6.064
Xiaojuan Peng,Chuanbo Ding,Yingchun Zhao,Mingqian Hao,Wencong Liu,Min Yang,Fengyan Xiao,Yinan Zheng
Ginsenoside Rg3 has shown beneficial effects in various skin diseases. The current interest in designing and developing hydrogels for biomedical applications continues to grow, inspiring the further development of drug-loaded hydrogels for tissue repair and localized drug delivery. The aim of the present study was to develop an effective and safe hydrogel (Rg3-Gel), using ginsenoside Rg3, and we evaluated the wound-healing potential and therapeutic mechanism of Rg3-Gel. The results indicated that the optimized Rg3-Gel underwent discontinuous phase transition at low and high temperatures. Rg3-Gel also exhibited good network structures, swelling water retention capacity, sustainable release performance, and excellent biocompatibility. Subsequently, the good antibacterial and antioxidant properties of Rg3-Gel were confirmed by in vitro tests. In full-thickness skin defect wounded models, Rg3-Gel significantly accelerated the wound contraction, promoted epithelial and tissue regeneration, and promoted collagen deposition and angiogenesis. In addition, Rg3-Gel increased the expression of autophagy proteins by inhibiting the MAPK and NF-KB pathways in vivo . It simultaneously regulated host immunity by increasing the abundance of beneficial bacteria and the diversity of the wound surface flora. From these preliminary evaluations, it is possible to conclude that Rg3-Gel has excellent application potential in wound-healing drug delivery systems.
研究领域:
药剂学
·
生物医学工程
·
伤口愈合
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药物递送系统
·
组织工程
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）