PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
·
2022
·
IF 3.915
Qingfa Guo,Fanyuan Kong,Xiaoru Pan,Shuhua Cao
Recent findings revealed that low-concentration paclitaxel(DTX) could enhance cytotoxicity by upregulating p53 expression in lung cancer cell lines. So, co-delivery of DTX and RFP-p53 gene with PEA nanoparticles (NPs) was studied. The prepared DTX loaded PEA NPs (PEA/DTX) were characterized by particle size distribution, morphology, zeta potential, and crystallography and cytotoxicity. Results showed that the PEA/DTX NPs had a mall particle size (≤100 nm), moderate zeta potential (≥40 mV) and drug loading of 9.0%, DTX was released from PEA/DTX NPs in an extended period in vitro. More important, agarose gel electrophoresis showed that PEA/DTX cationic NPs were able to completely bind RFP-p53 gene with mean particles size and zeta potential. Studies on cellular uptake of (PEA/DTX)/RFP-p53 NPs demonstrated that both drug and gene were effectively taken up by A549 tumor cells. It was found that intravenous injection of (PEA/DTX)/RFP-p53 NPs efficiently inhibited growth of subcutaneous A549 carcinoma in vivo (p < 0.05) and was significantly less side effect than that of mice treated with the other groups. Therefore, the (PEA/DTX)/RFP-p53 NPs might be a promising candidate for A549 cancer therapy.
研究领域:
药剂学
·
肿瘤学
·
分子生物学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2018
·
IF 3.862
Xiao Du,Shaoping Yin,Fang Zhou,Xu Du,Jianan Xu,Xiaochen Gu,Guangji Wang,Juan Li
Stimuli-responsive nanocarriers have demonstrated their potentials in optimizing chemotherapeutics and anticancer efficacy. In this study, a mixed micelle system (THSP) was prepared by combining reduction-sensitive hyaluronic acid-poly(lactide) (HA-ss-PLA) conjugates and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), with objective to achieve multiple functionalities of selective intracellular rapid release, active targeting capability and multidrug resistance reversal. The mixed micelle possessed desirable particle diameter of 124.32 nm and high entrapment efficiency at 87.97%. Importantly, the THSP mixed micelles demonstrated good stability in systemic circulation and rapidly released PTX in intracellular reductive environment. In vitro cellular uptake study and cytotoxicity assay indicated that the mixed micelles effectively increased drug accumulation in A549 cells and Taxol resistant A549/Taxol cells, and inhibited growth of tumor cells. In addition, the redox-responsive THSP micelles preferentially accumulated to the tumor site and improved anticancer drug activity in vivo, with a TIR of 69.08%. It was concluded that redox-sensitive mixed micelles THSP provided a potential vehicle for efficient anticancer drug delivery and enhancement in treating MDR tumor in the future.
研究领域:
纳米技术
·
药学
·
癌症研究
·
药物递送系统
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产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2026
·Vol. 31
·期 9
·1409
·
IF 5.1
Haojie Shi,Qianlong Xu,Fenglin Li,Caiyun Fan,Yi Han
Boron neutron capture therapy (BNCT) is a binary targeted radiotherapy that uses boron agents to treat refractory malignancies. This study developed a novel boronophenylalanine (BPA)-loaded liposome doped with o-carborane (CB) for BNCT. We applied response surface methodology (RSM) to identify factors affecting BPA loading and optimized encapsulation efficiency (EE) to minimize BPA loss. In in vitro experiments, these liposomes demonstrated promising characteristics for BNCT. The nanoparticle properties of CB-BPA-Lips remain stable for at least 48 h, and CB-BPA-Lips can effectively reduce the release of the agents loaded within them. Both cell viability assays and apoptosis assays have shown that CB-BPA-Lips have good biocompatibility and a lower inhibitory effect on cell viability than BPA. Cellular boron uptake peaked at 47.3642 ng B/106cells in A549 lung cancer cells and peaked at 38.8875 ng B/106cells in Bronchial Epithelium transformed with Ad12-SV40 2B (BEAS-2B) human normal bronchial epithelial cells at 24 h post-treatment, with both exceeding uptake in the BPA control group. Overall, this work presents an optimized liposomal formulation that enhances boron delivery to cancer cells and provides a potential candidate boron agent for BNCT pending in-depth in vivo studies.
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DOI
PubMed
高影响因子
NANOTECHNOLOGY
·
2019
·Vol. 30
·期 26
·265102
·
IF 3.399
Shen Zhang,Hongying Lv,Jing Zhao,Meng Cheng,Shuqing Sun
Synergistic therapy of tumor has attracted the attention of an increasing number of researchers because of its higher efficiency compared to single therapy. Herein, 4-carboxyphenyl porphyrin-conjugated silica-coated gold nanorods (AuNR@SiO2-TCPP) were synthesized. The synergistic treatment of photothermal therapy and photodynamic therapy on A549 cancer was researched in vivo and in vitro. In the AuNR@SiO2-TCPP, Au NRs and TCPP act as photothermal agent and photosensitizer, respectively. The temperature of the AuNR@SiO2-TCPP (0.11 nmol L−1) rises to 56.8 °C for 10 min under the illumination of 808 nm laser (2 Wcm−2). In MTT assays, the viability of A549 cancer cell treated with AuNR@SiO2-TCPP (100 μg ml−1) is only 21%. In animal experiments, the relative tumor volumes in mice receiving AuNR@SiO2-TCPP (5 mg kg−1) with 660 and 808 nm irradiations were significantly inhibited and the average value is decreased to 0.78 while the average value of the control group is increased to 7.2. These results demonstrate that the AuNR@SiO2-TCPP is a potential nanomedicine against tumor for clinical application in the near future.
研究领域:
生物医学工程
·
纳米医学
·
肿瘤治疗
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DOI
高影响因子
Frontiers in Chemistry
·
2022
·
IF 5.545
Zeng Zhijun,Shen Huaxiang,Gao Wei,Guo Qifeng,Chen Mengjie,Yan Xiaojun,Liu Hongning,Ji Yanhua
In this study, we use cytarabine anticancer drug to synthesize a new rare earth complex with Europium ion. The study work is an attempt to investigate luminescence and biological properties of the Eu-based coordination polymers of cytarabine (Eu-CP-Ara) anticancer drug which have been prepared by us. Eu-CP-Ara has luminescence properties with emission centering at about 619 nm excited with 394 nm. We study cytarabine and Eu-CP-Ara in vitro cytotoxicity. Cytotoxicity of Eu-CP-Ara against lung cancer cells (A549) could even be comparable to the inhibitory effect of cytarabine ligands, showing the advantage of antitumor activity. In addition, Eu-CP-Ara showed lower cytotoxicity to normal liver cells (L02). At the same, from the CLSM images, Eu-CP-Ara has successfully entered the A549 cell. Hence, Eu-CP-Ara can be used as a potential anticancer drug. Eu-CP-Ara may be an effective strategy for the tracking cytarabine against tumours and might impart better accurate treatment effect and therapeutic efficiency.
研究领域:
药物化学
·
材料科学
·
肿瘤学
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2024
·
IF 5.3
Lei Shu,Peili Luo,Qingxin Chen,Jingyang Liu,Ying Huang,Chuanbin Wu,Xin Pan,Zhengwei Huang
Chemotherapy agents for lung cancer often cause apoptotic resistance in cells, leading to suboptimal therapeutic outcomes. FIN56 can be a potential treatment for lung cancer as it induces non-apoptotic cell death, namely ferroptosis. However, a bottleneck exists in FIN56-induced ferroptosis treatment; specifically, FIN56 fails to induce sufficient oxidative stress and may even trigger the defense system against ferroptosis, resulting in poor therapeutic efficacy. To overcome this, this study proposed a strategy of co-delivering FIN56 and piperlongumine to enhance the ferroptosis treatment effect by increasing oxidative stress and connecting with the autophagy pathway. FIN56 and piperlongumine were encapsulated into silk fibroin-based nano-disruptors, named FP@SFN. Characterization results showed that the particle size of FP@SFN was in the nanometer range and the distribution was uniform. Both in vivo and in vitro studies demonstrated that FP@SFN could effectively eliminate A549 cells and inhibit subcutaneous lung cancer tumors. Notably, ferroptosis and autophagy were identified as the main cell death pathways through which the nano-disruptors increased oxidative stress and facilitated cell membrane rupture. In conclusion, nano-disruptors can effectively enhance the therapeutic effect of ferroptosis treatment for lung cancer through the ferroptosis-autophagy synergy mechanism, providing a reference for the development of related therapeutics.
研究领域:
肿瘤学
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药理学
·
纳米技术
·
细胞生物学
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产品关联
DOI
PubMed
高影响因子
ChemMedChem
·
2017
·Vol. 12
·期 19
·1600-1609
·
IF 3.225
Xinyu Hu,Yongmei Wang,Liangliang Zhang,Man Xu,Jianfa Zhang,Wei Dong
Graphical The power of attraction : Salecan-based composite hydrogels have magnetic-field-responsive properties due to the introduction of Fe 3 O 4 @SiO 2 nanoparticles into the hydrogel system. As a model anticancer drug, doxorubicin (DOX) was loaded into the composite hydrogels with high efficiency via strong electrostatic interactions between the amine group in DOX and carboxyl groups present in the hydrogels. These DOX-loaded salecan-g-PPH/Fe 3 O 4 @SiO 2 composite hydrogels show pH-responsive controlled drug release, and the liberated DOX can be effectively taken up by A549 cells. Salecan is a water-soluble extracellular β-glucan and has excellent physicochemical and biological properties for hydrogel preparation. In this study, a new pH/magnetic field dual-responsive hydrogel was prepared by the graft copolymerization of salecan with 4-pentenoic acid (PA) and N -hydroxyethylacrylamide (HEAA) in the presence of Fe 3 O 4 @SiO 2 nanoparticles for doxorubicin hydrochloride (DOX) release. Integration of Fe 3 O 4 @SiO 2 nanoparticles in salecan-g-poly(PA-co-HEAA) copolymers afforded magnetic sensitivity to the original material. DOX-loaded hydrogels exhibited a clear capacity for pH/magnetic field dual-responsive controlled drug release. Lowering the pH to acidic conditions or introducing an external magnetic field caused an enhancement in DOX release. This salecan-g-poly(PA-co-HEAA)/Fe 3 O 4 @SiO 2 composite hydrogel is a promising drug carrier for magnetically targeted drug delivery with enhanced DOX cytotoxicity against A549 cells.
研究领域:
材料科学
·
药学
·
生物医学工程
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产品关联
DOI
PubMed
高影响因子
IET Nanobiotechnology
·
2020
·Vol. 14
·期 7
·595-601
·
IF 1.859
Xinyu Xu,Ye Liu,Zhaoming Guo,Xue-Zhi Song,Xiuyu Qi,Zideng Dai,Zhenquan Tan
Metal-organic frameworks (MOFs) as drug carriers have many advantages than traditional drug carriers and have received extensive attention from researchers. However, how to regulate the microstructure of MOFs to improve the efficiency of drug delivery and sustained release behaviour is still a big problem for the clinical application. Herein, the authors synthesise surfactant-modified ZIF-8 nanoparticles with different microstructures by using different types of surfactants to modify ZIF-8. The surfactant-modified ZIF-8 nanoparticles have the larger specific surface area and total micropore volumes than the original ZIF-8, which enables doxorubicin (DOX) to be more effectively loaded on the drug carriers and achieve controlled drug sustained release. Excellent degradation performance of ZIF-8 nanoparticles facilitates the metabolism of drug carriers. The formulation was evaluated for cytotoxicity, cellular uptake and intracellular location in the A549 human non-small-cell lung cancer cell line. ZIF-8/DOX nano drugs exhibit higher cytotoxicity towards cells in comparison with free DOX, suggesting the potential application in nano drugs to cancer chemotherapy.
研究领域:
材料科学
·
药剂学
·
纳米技术
·
癌症研究
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DOI
高影响因子
ACS Applied Bio Materials
·
2020
·
IF 0
Yiyan Song,Ping Zhu,Zhihui Xu,Jin Chen
Multidrug resistance evoked by overusing pharmaceuticals of poor water solubility has posed a serious threat to public health, which urges the development of safe and efficacious therapeutic formulations. In this study, biomimetic nanospherical polydopamine (PDA) formed under mild conditions was modified using methoxypolyethylene glycol amine (m-PEG-NH2) to produce a polydopamine-based drug delivery platform. As characterized by various physicochemical methods, the PEGylated PDA with a uniform size distribution showed superior biocompatibility and efficient load capability for two hydrophobic anticancer drugs of paclitaxel and phytochemical curcumin, which exhibited synergistic cytotoxicity and a pH/ROS-responsive release behavior. Significantly, an enhanced effect of the encapsulated paclitaxel and curcumin was identified toward the drug-resistant A549/TAX cancer cells, which was correlated with the improved cellular internalization of hyperbranched PDA composites and distinctive cell cycle arrest of loaded drugs. The dual-drug-loaded spherical PDA nanocomposites hold enormous potential to tackle drug resistance from a chemotherapy perspective.
研究领域:
药学
·
纳米技术
·
肿瘤学
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产品关联
DOI
PubMed
MOLECULAR AND CELLULAR BIOCHEMISTRY
·
2020
·Vol. 476
·期 2
·1075-1082
·
IF 2.795
Zhang Xiaowei,Dong Yu,Gao Miao,Hao Minfeng,Ren Hui,Guo Ling,Guo Hua
The tumor necrosis factor receptor-associated protein 1 (TRAP1) is associated with the occurrence and development of various diseases, including inflammation and cancer. However, the role and mechanism of TRAP1 in the development of lung cancer need to be further explored. Therefore, the purpose of this study is to investigate the role of TRAP1 in the regulation of apoptosis by cisplatin and its special mechanism. The RT-qPCR and Western blot were used to detect the mRNA and protein expression of ANGPTL4 in A549 and H1299 cells, respectively. And the cell apoptosis and cell cycle were measured by flow cytometry (FCM). The expression of genes related to apoptosis and drug resistance as well as the cell cycle regulators, including MDM2, CyclinB1, and CDK1, were detected by Western blot. Finally, the reactive oxygen species (ROS) indicator DCFH-DA was performed to detect the generation of ROS, and the mitochondrial membrane potential (ΔΨm) was detected by JC-1 staining. The results showed that the expression of TRAP1 was significantly increased in A549/DDP and H1299/DDP than A549 and H1299 cells. Further research found that knockdown of TRAP1 induced apoptosis and caused G2/M cell cycle arrest in A549/DDP and H1299/DDP cells. What is more, siTRAP1 reduced the relative JC-1 polymer monomer fluorescence ratio and decreased the ΔΨm, up-regulated the expression of Cytochrome C. Importantly, siTRAP1 induces ROS-dependent mitochondrial dysfunction. It is suggested that that TRAP1 suppresses cisplatin-induced apoptosis by promoting ROS-dependent mitochondrial dysfunction.
研究领域:
肿瘤学
·
细胞生物学
·
药理学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF HETEROCYCLIC CHEMISTRY
·
2014
·Vol. 52
·期 2
·473-477
·
IF 0.873
Hongxia Liu,Libo Li,Shaikh Qurat-ul-ain,Tao Jiang
A series of novel 2,6-disubstituted purine derivatives were designed and synthesized from 2,6-dichloropurine. The structures of target compounds were determined by 1 H-NMR, 13 C-NMR, and HRMS. The synthesized compounds were evaluated for their inhibitory activities against lung cancer cell lines of A549 and liver cancer cell lines of Bel-7402. 2-(4-Benzyloxy-phenylamino)-6-(cyclohexylamino)purine( 3 ), 2-(4-chloro-phenylamino)-6-( n -butylamino)purine ( 5 ), 2-(4-morpholinoamino)-6-(4-hydroxy-phenylamino)purine ( 9 ), and 2-(4- O -galactosyl-phenylamino)-6-(cyclohexylamino)purine ( 12 ) exhibited moderate inhibitory activity.
研究领域:
药物化学
·
肿瘤学
·
有机合成
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2022
·
IF 6.51
Jinfeng He,Shuqian Yu,Ziyi Ma,Haotian Sun,Qinghua Yang,Zhiwei Liu,Xuan Wang,Xiaoyu Zhang,Longgang Wang
Gold nanoparticles are a kind of good photothermal agents. However, gold nanoparticle photothermal agents have low photothermal conversion efficiency and low tumor inhibiting ability. To overcome these problems, polymyxin E (PE) biomineralized and doxorubicin-loaded gold nanoflowers (DOX-SH@AuNFs) nanodrug was synthesized by the green synthesis method using the biological antimicrobial peptide PE as a stabilizer and grower of crystal seed, and doxorubicin-thiol (DOX-SH) was further loaded on the gold nanoparticles through the Au-S bond. The final DOX-SH@AuNFs displayed a wide absorption band in the UV–Vis spectra, and their photothermal conversion efficiency was 33.9%. Furthermore, the inhibition rate of DOX-SH@AuNFs on A549 cells was as high as 80.1% under the irradiation of near-infrared light at 808 nm. The tumor inhibition rate of DOX-SH@AuNFs was as high as 87.81% in vivo experiments. The high tumor suppression rate was attributed to the high photothermal conversion ability of DOX-SH@AuNFs and the delivery of doxorubicin. Taken together, the method of preparing DOX-SH@AuNFs provides a new idea for the treatment of cancer by photothermal therapy and chemotherapy synergistic system.
研究领域:
纳米技术
·
癌症研究
·
药学科学
·
材料科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）