PHARMACEUTICAL CHEMISTRY JOURNAL
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2024
·Vol. 58
·期 5
·765-774
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IF 0.8
Qiu Shouliang,Deng Xuezhen,Qian Kun,Yang Jie,Ma Yuexing
Drug-drug cocrystals can improve the physical and pharmaceutical properties of drugs and have been widely studied by many researchers. A new pharmaceutical cocrystal [C 16 H 18 FN 3 O 3 ][C 16 H 14 O 6 ] · 2(C 2 H 5 OH) (HSP-NOR) was synthesized by hesperetin (HSP) and norfloxacin (NOR) with the aim of improving the antibacterial activity and physicochemical properties. The single crystal structure shows that the asymmetric unit comprises both hesperetin and norfloxacin, as well as two ethanol molecules, in which norfloxacin exists as a zwitterion. The cocrystal formation improves the solubilities of hesperetin and norfloxacin in pure water. Preliminary antibacterial experiments showed that the antibacterial activities of the cocrystal on Streptococcus pneumoniae , Escherichia coli , Shigella dysenteriae , and Pseudomonas aeruginosa were stronger than those of norfloxacin. The in vivo study of acute toxicity showed that the minimum lethal dose of the cocrystal to mice was >3000 mg kg -1 BW, and there were no signs of toxicity after oral administration at this dosage.
研究领域:
药学
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生物化学
✓ 已验证
产品关联
DOI
高影响因子
NANOTECHNOLOGY
·
2014
·Vol. 25
·期 29
·295103
·
IF 3.672
Jun Chen,Xiao-Quan Yang,Yuan-Zheng Meng,Huan-Huan Huang,Meng-Yao Qin,Dong-Mei Yan,Yuan-Di Zhao,Zhi-Ya Ma
Probe bismuth sulfide modified with Pluronic F127 (Bi2S3-PF127), which has high biocompatibility and dispersibility, is synthesized using triblock copolymer Pluronic F127 to modify hydrophobic Bi2S3 nanoparticles that are prepared by a hot injection method. TEM results show that most of the probe has a length of about 14.85 ± 1.70 nm and a breadth of about 4.79 ± 0.63 nm. After injected into the tail vein of a mouse, the probe has obvious CT contrast enhancement capability from x-ray CT imaging results. Meanwhile, the probe's in vivo toxicity is also studied. It is found that hematoxylin and eosin stains of major organs have no change. A biochemical analysis (alanine aminotransferase and aspartate aminotransferase) prove the probe has no adverse effects. The results of a blood analysis (white blood cell count, red blood cell count, hemoglobin, and platelet count) are also normal. The biological distribution of Bi by ICP-AES shows that most of nanoparticles are cleaned out after injection 48 h, and the circulation half-life of the probe is 5.0 h, suggesting that Bi2S3-PF127 has a long circulation and indicating that the Bi2S3-PF127 probe has good biocompatibility and safety.
研究领域:
医学影像学
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纳米医学
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毒理学
✓ 已验证
DOI
高影响因子
Journal of Biomedical Nanotechnology
·
2017
·Vol. 13
·期 10
·1321-1332
·
IF 4.521
Liu Heng,Liu Yu,Chu Chengchao,Tong Haipeng,Xue Wei,Wang Junqing,Liu Gang,Zhang Weiguo
The aberrant tumor microenvironment (TME) characterized by hypoxia and acidification is closely associated with tumor malignant phenotypes and treatment resistance. Designing biocompatible TME-responsive nanoagents via convenient fabrication procedures are of particular interest for
specific and effective tumor theranostics. In this work, bovine serum albumin stabilized manganese dioxide (MnO2) nanostructures (BMnNSs) were synthesized via an environmental-friendly and facile one-step biomineralization process at physiological temperature, which possess suitable
size, good water dispersibility, and excellent biocompatibility. Then, the photosensitizer 2-devinyl-2-(1-hexyloxyethyl) pyropheophorbide (HPPH) was anchored onto BMnNSs with desirable loading efficiency, obtaining multifunctional BMnNSs-HPPH nanocomposites (BMnHNCs). The high reactivity of
MnO2 towards acidic pH/hydrogen peroxide (H2O2) was utilized to achieve TME responsive near-infrared fluorescence/magnetic resonance dual-modal imaging and improved photodynamic therapy. Owing to the efficient tumor accumulation of BMnHNCs mediated by the passive
targeting effect and generated oxygen in situ resulting from the reaction between MnO2 and endogenous H2O2 in tumor cells, the BMnHNCs exhibited remarkably enhanced tumor growth suppression compared with HPPH. Furthermore, tumor hypoxia and the vascular
endothelial growth factor expression were effectively attenuated by BMnHNCs. Notably, the BMnHNCs demonstrated no apparent in vivo toxicity upon intravenous administration. This biocompatible and biodegradable nanoformulation holds great potential for TME modulation and improved tumor
theranostics for clinical translation.
研究领域:
生物医学工程
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纳米技术
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癌症治疗
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材料科学
✓ 已验证
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2022
·
IF 5.999
Yongli Shi,Xueyan Hou,ShaSha Yu,Xiaofei Pan,Mingbo Yang,Jie Hu,Xiao Wang
Doxorubicin (DOX) is widely used in the treatment of many tumors, but the dose-dependent toxicity limits its further application. In this study, a unique strategy was developed to improve the anti-tumor effects of free DOX and lower its in vivo toxicity by constructing novel glutathione (GSH)-sensitive poloxamer188-b-polycaprolactone-S-S-doxorubicin nanoparticles (PPSSD NPs). After uptake by tumor cells, the disulfide bonds in the PPSSD NPs would be cloven by reacting with GSH. Then, a lethal dose of DOX was released in tumor cells. The uptake of PPSSD NPs by 4T1 cells was proved using fluorescence microscopy by co-localization of PPSSD NPs and 4′, 6-diamidino-2-phenylindole (DAPI). Cell tests suggested that the PPSSD NPs showed high anti-tumor cells (4T1) activity but low cytotoxicity against normal cells (293 t). The in vivo toxicity and anti-tumor effects of the PPSSD NPs were studied with Kunming and Balb/c mice as models, respectively. The H&E slices, blood routine and biochemistry indexes of the PPSSD NPs treated mice indicated that the PPSSD NPs did not induce obvious in vivo toxicity. The PPSSD NPs showed higher in vitro anti-4T1 cells activity than free DOX. Furthermore, the in vivo anti-tumor study, TUNEL and H&E slices suggested that the PPSSD NPs exhibited excellent anti-tumor effects. In a word, the novel PPSSD NPs did not only improve the anti-tumor effect of DOX, but also decrease its cytotoxicity to normal tissues.
研究领域:
药理学
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肿瘤学
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纳米技术
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药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Nano Materials
·
2019
·
IF 0
Ying Liu,Yuxia Tang,Ying Tian,Jiang Wu,Jing Sun,Zhaogang Teng,Shouju Wang,Guangming Lu
Hydroxyapatite nanoparticles have drawn much attention in the development of multifunctional nanosystems because of their excellent biocompatibility. In the report, gadolinium-doped hydroxyapatite nanorods (NHA:Gd) were controlled synthesized through adjusting the amount of gadolinium. The NHA:Gd showed a high loading capacity for doxorubicin (118 μg per milligram) and a pH-responsive drug release ability. The r1 value of obtained doxorubicin (DOX)-loaded NHA:Gd (NHA:Gd-DOX) solution reached 0.0472 (μg/mL)−1 s–1 and was higher than that of commercial T1 contrast Gd-DTPA (0.0314 (μg/mL)−1 s–1). In vivo experiments demonstrated that NHA:Gd-DOX exhibited excellent MR imaging property. The results of therapeutic efficacy demonstrate that the tumor volume treated by NHA:Gd-DOX was significantly reduced compared to that treated by free DOX. In vivo toxicity experiments demonstrated no obvious damage to the major organs in NHA:Gd-DOX treated mice. Considering the excellent biocompatibility, T1WI contrast ability, and enhanced therapeutic efficacy, these NHA:Gd-DOX have great potential for applications as MR T1 contrast agents and drug carriers for cancer therapy.
研究领域:
纳米技术
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医学成像
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癌症治疗
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材料科学
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药学
✓ 已验证
产品关联
DOI
PROCESS BIOCHEMISTRY
·
2022
·
IF 4.885
Yanzhang Liu,Yongxiao Dong,Xiaoli Pu,Xiaoyan Yin
Diabetic cataract (DC) is a major cause of visual impairment for diabetic patients. There are limited range of drug delivery approaches and pharmacologic interventions available to control the diabetic cataract progressions, specifically the eye drops related non-invasive strategies. The reported studies in diabetic cataract designate that non-enzymatic glycosylation and oxidative damages of the crystalline lens played a vital role in the formation cataract pathogenesis. In the present investigation, we developed a novel combination of anti-oxidant curcumin (CUR) and cerium oxide nanoparticles (CeO 2 NPs) entrapped poly lactic-co-glycolic acid (PLGA) copolymeric nanoformulations (CCNPs) to improve auto-regenerative redox and anti-glycation potential to treat diabetic cataract complications. The analytical methods exhibited successful entrapments of curcumin and CeO 2 NPs into the PLGA formulations under X-ray diffraction pattern (XRD), Fourier-transform infrared (FTIR) spectrum and scanning electron microscope (SEM) observations. We investigated and found that prepared CCNPs nanoformulation could have effective anti-oxidant and anti-glycation potential to protect lens epithelial (HLE-B3) cells by prominent prevention of repetitive reactive oxygen species (ROS) generations. In vivo toxicity analysis results indicated that CCNPs have no any inflammation abnormalities and less Ce ions caring on major organs of rat by subcutaneous (SC) injection procedure. We expecting that this developed approach would provide capable therapeutic potential for the treatment of diabetic cataract.
研究领域:
药学
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纳米技术
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眼科学
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糖尿病研究
✓ 已验证
产品关联
DOI
高影响因子
NEW JOURNAL OF CHEMISTRY
·
2020
·Vol. 44
·期 39
·16741-16751
·
IF 3.288
Jiacheng Wang,Wenshu Qiao,Haitian Zhao,Jianjun Cheng,Ying Han,Xin Yang
The development and application of nano-drug carrier systems have opened up unprecedented opportunities for tumor treatment. However, eliminating the related liver toxicity is still very challenging because hepatotoxicity is the most severe adverse effect of chemotherapy and nanotherapy. Herein, a highly atom-economical bioactive nanocarrier delivery system is shown. This carrier is assembled from oleanolic acid (OA), which is abundantly present in Chinese medicinal plants and has shown potent antioxidant, antitumor, and hepatoprotective properties. Molecular simulation and experimental characterization have demonstrated that the assembly process of OA-encapsulated paclitaxel (PTX) to form OA–PTX nanoparticles is mainly through hydrophobic interactions and hydrogen bonding interactions. In vitro and in vivo experiments confirmed that OA and PTX have synergistic antitumor effects due to their different antitumor mechanisms. As expected, liver injury induced by PTX was significantly reduced due to the hepatoprotective activity of OA. The prepared nanomedicine has high drug loading capacity and excellent targeting, as well as good biocompatibility and low in vivo toxicity, which ensure the effectiveness of the tumor treatment and the safety of the body. The present study provides new ideas for the development of nanocarriers and avenues for active natural products in reducing drug side effects.
研究领域:
药学
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纳米技术
·
癌症研究
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毒理学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
ACS Applied Materials & Interfaces
·
2023
·
IF 9.5
Nini Li,Xiaohong Ji,Somnath Mukherjee,Bing Yang,Yuqing Ren,Changhao Wang,Yashao Chen
In recent years, sunscreens’ adverse impacts on the environment and biology have gained wide attention. The improvement of sunscreen safety has become one of the major priorities in skin photoprotection research. It is an effective strategy to develop bionic photoprotective materials by simulating the photoprotective mechanism existing in nature. Inspired by the photoprotective mechanisms of skin and plant leaves, the bionic photoprotective material CS-SA-PDA nanosheet was developed using the free radical grafting method and Michael addition, with natural melanin analogue polydopamine (PDA) nanoparticles and plant sunscreen molecular sinapic acid (SA) as sun protection factors and natural polymer chitosan (CS) as the connecting arm. The results show that CS-SA-PDA can effectively shield UVB and UVA due to the possible synergistic effect between PDA and SA. The introduction of polymer CS significantly improved the photostability of SA and reduced the skin permeability of PDA nanoparticles. The CS-SA-PDA nanosheet can also effectively scavenge photoinduced free radicals. Furthermore, in vivo toxicity and anti-UV evaluations confirm that CS-SA-PDA has no skin irritation and is excellent against skin photodamage, which makes it an ideal skin photoprotective material.
研究领域:
材料科学
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纳米技术
·
生物医学工程
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环境科学
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药学
·
化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子