Materials Chemistry Frontiers
·
2018
·Vol. 2
·期 8
·1529-1538
·
IF 0
Lijing Niu,Feiyan Zhu,Bowen Li,Lingling Zhao,Hongze Liang,Yinghua Yan,Hui Tan
A folate-conjugated and pH-sensitive polymeric micellar system for the co-delivery of DOX and PTX was studied. A doxorubicin conjugated prodrug was synthesized via Schiff's base reaction. Subsequently, folate was grafted onto the prodrug and PTX was encapsulated. Sustained drug release of both DOX and PTX from the polymeric micelles was observed and the release rate could be accelerated by decreasing the media pH. A cellular uptake assay revealed that the polymeric micelles were internalized in the cytoplasm via endocytosis by SW1353 cells, and the cellular uptake was enhanced for the folate-conjugated micelles due to an active FR-mediated endocytosis pathway, showing stronger red fluorescence compared to that of non-folate micelles. The in vitro anticancer efficiency of the polymeric micellar system was evaluated using a cytotoxicity assay by incubating different drug formulations with the SW1353 cells. Both free drugs and micellar formulations displayed inhibition of cell growth at different levels, while the folate-conjugated dual-drug loaded polymeric micelles (Folate–Oxd–DOX/PTX) displayed a much lower IC50 value than other drug formulations, indicating a desirable in vitro anticancer efficiency due to the synergistic effect of co-delivery and active targeting. Thus, the polymeric micellar system is a promising platform for targeted cancer chemotherapy.
研究领域:
药剂学
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肿瘤学
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生物材料
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产品关联
DOI
CURRENT MOLECULAR MEDICINE
·
2018
·Vol. 18
·期 6
·383-391
·
IF 2.254
Li Yue,Lin Yan,Liufu Chun,Tu Jiawei,Yang Chaopin,Chen ZhiYi
Objective: To study transfection efficiency of folate-modified chitosan (FACS) nanoparticles as a non-viral vector delivering pEGFP-C3plasmid (FA-CS/P) to 293T cells with or without the combination of ultrasound and microbubble. Method: pEGFP-C3 was used as a reporter gene and
FA-CS nanoparticles, which were prepared by complex coagulation method, were used as biological carriers. Transfection efficiency to 293T cells mediated by FA-CS/P nanoparticles, ultrasound (US) and microbubble (MB) was assessed by fluorescence microscopy and flow cytometry. Result: FA-CS/P
nanoparticles have a particle size of 355.1 nm and zeta potential of 10.4 mV. Significant green fluorescence could be observed in CS/P group, FA-CS/P group, US+MB/P group, US+FA-CS/P group, Liposome 2000 (L) group under an inverted fluorescence microscope, while for US+MB+FA-CS/P group, only
scattered fluorescence was observed. Result of flow cytometry showed that the transfection rate of US+MB+FA-CS/P group was (2.0±0.2)%, which was significantly lower than other groups (P<0.05). CCK-8 experiments showed that cell vitality of US+MB+FA-CS/P was groups (P<0.05). CCK-8
experiments showed that cell vitality of US+MB+FA-CS/P was (64.1±4.6)%, which was also lower than other groups (P<0.05). Conclusion: In this study, FA-CS was successfully synthesized. FA-CS could combine with pEGFP-C3 effectively forming nanoparticles with nanoparticle size,
well dispersion, high encapsulation efficiency and no significant toxicity to cells. The application of ultrasound increased the transfection rate of FA-CS/P. However, while being exposed to ultrasound and microbubble, the transfection rate of FA-CS/P decreased obviously, may indicate that
there was no synergistic effect for gene transfection by the combination of ultrasound, folate modified chitosan and microbubbles.
研究领域:
生物医学工程
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分子生物学
✓ 已验证
DOI
PubMed
高影响因子
Oncotarget
·
2016
·
IF 5.008
Tao Liu,Xidong Wu,Yigang Wang,Tao Zhang,Ting Wu,Fang Liu,Wansong Wang,Gang Jiang,Minqiang Xie
The co-delivery of drug and gene has become the primary strategy in cancer therapy. Based on our previous work, to co-deliver docetaxel (DOC) and MMP-9 siRNA more efficiently for HNE-1 nasopharyngeal carcinoma therapy, a folate-modified star-shaped copolymer (FA-CD-PLLD) consisting of β-cyclodextrin (CD) and poly(L-lysine) dendron (PLLD) was synthesized, and then used for DOC and MMP-9 co-delivery. Different from commonly used amphiphilic copolymers micelles, the obtained CD derivative could be used directly for the combinatorial delivery of nucleic acid and hydrophobic DOC without a complicated micellization process. In vitro and in vivo assays are carried out to confirm the effectiveness of the target strategy and combined treatment. It was found that the conjugation of CD-PLLD with FA could enhance the DOC/MMP-9 delivery effect obviously, inducing a more significant apoptosis and decreasing invasive capacity of HEN-1 cells. In vivo assays showed that FA-CD-PLLD/DOC/MMP-9 could inhibit HNE-1 tumor growth and decrease PCNA expression effectively, indicating a promising strategy for nasopharyngeal carcinoma therapy. Moreover, the in vivo distribution of DOC and MMP-9, blood compatibility and toxicity are also explored.
研究领域:
药剂学
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肿瘤学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Scientific Reports
·
2022
·Vol. 12
·期 1
·1-16
·
IF 4.996
Lu Yi-heng,Chen Zong-lin,Lu Yu-wei
To inhibit the agglomeration of nanotitanium dioxide, a poly (vinyl chloride) (PVC) composite film doped with folic acid-modified titanium dioxide was synthesized and characterized using X-ray powder diffraction, X-ray photoelectron spectroscopy and thermogravimetric analysis coupled with Fourier transform infrared spectroscopy. The average grain size of the folic acid-modified titanium dioxide was found to decrease by 1.3 nm, indicating that the cohesiveness of the nanoparticles is decreased. The lowest temperature for 1.0% thermal decomposition of PVC was determined to be 230.0 °C. The decomposition rate at the peak temperature is found to be 39.6% lower than that of a control sample. The stability of the PVC is improved due to a lower number of surface chlorine atoms as well intermolecular attraction. A mechanism for folic acid modification of titanium dioxide-doped PVC is proposed. After doping, the ester groups in the plasticizer show a significant decrease in the vibration peak intensities observed at 1264 cm −1 , 1736 cm −1 and 1106 cm −1 . The doped PVC film suppresses the release of CO 2 , and the strongest vibration peak at 1264 cm −1 is found to be 17.2% lower than that for the blank sample, indicating that doping is beneficial for plasticizer recovery.
研究领域:
材料科学
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化学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2022
·
IF 5.988
Hairong Zeng,Chao Xia,Bei Zhao,Mengmeng Zhu,HaoYue Zhang,Die Zhang,Xin Rui,Huili Li,Yi Yuan
Bufalin (Buf), an active ingredient of the traditional Chinese medicine Chansu, is known to have anticancer effects for breast cancer. However, its poor solubility, high toxicity, and extensive side effects limit its use. Metal-organic frameworks (MOFs) are a class of promising drug delivery systems known for their high porosity. Here, we designed and constructed pH-sensitive and redox-responsive folic acid-modified MOFs as drug carriers of Buf (FA-MOF/Buf). Moreover, the anticancer activity of nanomedicines was also explored in vitro and in vivo . Compared to free Buf, the FA-MOF/Buf nanoparticles demonstrated improved water solubility and stability, higher intracellular uptake, and enhanced cytotoxicity in breast cancer cells in vitro . Furthermore, it displayed improved accumulation in the tumor site, enhanced anticancer activity, and reduced side effects in vivo . Our results demonstrated that FA-MOF could be developed as a potential delivery system for Buf to improve its antitumor activity for breast cancer treatment.
研究领域:
药理学
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肿瘤学
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纳米医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF APPLIED POLYMER SCIENCE
·
2012
·Vol. 129
·期 2
·748-755
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IF 1.289
Xipan Liu,Dan Pan,Qian Guo,Yanjun Zhao,Zheng Wang
This study designed a photo-crosslinkable poly(ether-anhydride) nanocarrier with folate modification to achieve both biodegradability and active targeting. The nanocarrier consists of a hydrophobic polymer core and a shell of folate and hydrophilic poly(ethylene glycol). Nuclear magnetic resonance and Fourier transform infrared spectroscopy were used to verify the synthesis and relevant intermediate products. The nanocarrier was characterized in terms of morphology and diameter using transmission electron microscopy and dynamic light scattering. The results showed that the size of spherical nanocarriers located within 200–400 nm. The cellular uptake profile of nanocarriers in HeLa cells was examined using fluorescence microscope with the help of a fluorescent molecule and the folate-modified nanocarrier exhibited an enhanced uptake compared to that without modification. The nanocarrier degradation at physiological temperature was investigated gravimetrically and the in vitro release of model drug, paclitaxel (PTX) was examined via the dialysis method. The erosion rate of poly(ether-anhydride) network was controlled by the crosslinking density and the hydrolytic susceptibility; the folate modification slightly slowed the degradation process. The time scale of PTX release perfectly matched with that of nanocarrier erosion; after 6 h more than 50% weight loss of nanocarrier was observed and meanwhile the drug release profile got plateaued, indicating the dominant role of polymer erosion in the release of the active agent from the nanocarriers. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013
研究领域:
生物医学工程
·
药物递送
·
肿瘤治疗
·
材料科学
·
药剂学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Fengjie Liu,Fansu Meng,Xiaoshan Hong,Anil K. Giri,Mulazim Hussain Asim,Zhong Chen,Yiqi Chen,Yixuan Lin,Lulu He,Qiaowen Bu,Yong Huang,Xiaoli Sun,Zhenjiang Yang,Yu Cai
Background Baicalin (BA), a natural flavonoid compound, exhibits potential anti-breast cancer (BC) activity. However, its therapeutic efficacy is limited by biological membrane and tumor barriers. Albumin nanoparticles demonstrate excellent biocompatibility and ease of modification, making them highly advantageous for antitumor drug delivery. Despite these advantages, current preparation methods for albumin-based NPs have significant limitations, including the use of organic or toxic reagents, large and uneven particle size products, complex processes, etc. Objective The purpose of this study was to develop a novel method for preparing albumin nanoparticles (BSA NPs). Subsequently, BSA NPs were modified with folic acid (FA) and polymers and loaded with BA to construct a novel nanodrug delivery system (BA@mPEG-FA-BSA NPs) to improve the anti-breast cancer efficacy of BA. Methods Compared with the desolvation method and the thermal gelation method, the advantages of the new preparation method of BSA NPs are: less organic solvent and preparation time, greater yield, smaller particle size and uniform product. The preparation method of BSA NPs was investigated by single factor experiment. The encapsulation efficiency (EE) and drug loading (DL) of BA in BA@mPEG-FA-BSA NPs were detected by HPLC. The structural composition and physicochemical properties of the nanoparticles were characterized using transmission electron microscopy (TEM), infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), and X-ray diffraction (XRD). The anti-breast cancer efficacy of BA@mPEG-FA-BSA NPs was evaluated through cellular uptake, cytotoxicity, apoptosis, cell cycle analysis, and in vivo tumor-bearing mouse studies. Results According to the setting of process parameters, the established method can control the acquisition of uniform BSA NPs with a particle size between 20 and 300 nm. BA@mPEG-FA-BSA NPs exhibited a particle size of approximately 59.26 nm, a polydispersity index (PDI) < 0.3, EE of about 46.7 %, and DL of approximately 2.6 %. Cellular uptake experiments demonstrated that mPEG-FA-BSA NPs enhanced the uptake of free coumarin 6 in BT20 cells, with free FA showing competitive inhibition effects. Efficacy evaluation revealed that BA@mPEG-FA-BSA NPs exhibited cytotoxicity against BT20 cells, induced cell cycle arrest and apoptosis, and inhibited tumor growth in 4 T1 tumor-bearing mice. In most cases, the effects of BA@mPEG-FA-BSA NPs were superior to those of free BA, with a concentration- or dose-dependent manner observed. Conclusion This study established a novel preparation method for albumin nanoparticles, providing a new methodology for the construction of nano-drug delivery systems based on albumin materials. The developed BA@mPEG-FA-BSA NPs, with their relatively small particle size, demonstrated enhanced cellular uptake and anti-breast cancer activity of BA, highlight the potential for further optimization and clinical translation.
研究领域:
药学
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肿瘤学
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纳米医学
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产品关联
DOI
PubMed
高影响因子
Food Biophysics
·
2022
·Vol. 17
·期 3
·386-396
·
IF 3.34
Wang Yuhang,Fu Yuying,McClements David Julian,Ba Chujie,Li Teng
Propolis is a natural bioactive compound that is being explored as a nutraceutical because of its potential health benefits. In this study, propolis-loaded biopolymer nanoparticles were fabricated from folic acid-modified carboxymethyl chitosan (FA-CMCS) using the pH-driven method. The mean diameter of the propolis-loaded FA-CMCS nanoparticles was about 180 nm, and transmission electron microscopy showed they had a spherical shape. Fourier transform infrared spectroscopy analysis demonstrated that hydrogen bonding, electrostatic, and hydrophobic interactions were the major driving forces responsible for nanoparticle formation. The nanoparticles had good colloidal stability at pH 2.0, 3.0, 7.0, and 8.0 but exhibited some aggregation at intermediate pH values. The nanoparticles were also stable to salt addition up to 400 mM NaCl. Propolis-loaded FA-CMCS nanoparticles exhibited improved antioxidant properties compared to pure propolis and propolis-free nanoparticles. A simulated digestion model (fed state conditions) indicated that different amounts of propolis were released in different gastrointestinal regions: around 25%, 15%, and 25% in the stomach, small intestine, and colon, respectively. Our results suggest that the nanoparticles fabricated in this study have potential as colloidal delivery systems for sustained release of propolis in the human gut.
研究领域:
药剂学
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生物材料
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营养学
✓ 已验证
DOI
高影响因子
Journal of Biomedical Nanotechnology
·
2018
·Vol. 14
·期 8
·1486-1495
·
IF 5.068
Wang Yonghong,Wen Baofang,Yu Hongli,Ding Dejun,Zhang JingJing,Zhang Yunxiang,Zhao Limin,Zhang Weifen
Nasopharyngeal carcinoma (NPC) is a common epithelial malignancy that occurs in the nasopharynx and it is one of the high incidences of malignant tumors in China. As previous reports, berberine hydrochloride (BH) possesses a repressive effect on the proliferation of various cancer types.
But the application of BH was hampered for a long time due to its hydrophobic properties, along with poor stability and bioavailability. In this study, folate acid modified chitosan nanoparticles loaded berberine hydrochloride (BH/FA-CTS NPs) were prepared by the ionic cross-linking technique,
the physicochemical properties and the influence of BH/FA-CTS NPs on proliferation, migration and apoptosis in human nasopharyngeal carcinoma CNE-1 cells were studied in vitro and in vivo. Results of scanning electron microscopy (SEM) images showed that BH/FA-CTS NPs were sphere
and the diameter was 258.2±9.1 nm. The drug loading and encapsulation efficiency were 8.17±1.12% and 87.73±4.21%, respectively. The drug release kinetics exhibited a slower and sustained release over a period of 48 h. Moreover, results of MTT assay and scratch assay displayed
that BH/FA-CTS NPs inhibited proliferation and migration of CNE-1 cells remarkably. BH/FA-CTS NPs promoted apoptosis and necrosis of CNE-1 cells. And BH/FA-CTS NPs displayed distinguished higher tumor inhibition than control group, free BH and BH/CTS NPs in vivo. Therefore, as a nanocomposite,
BH/FA-CTS NPs provide a new method and option for the treatment of nasopharyngeal carcinoma patients.
研究领域:
肿瘤学
·
药剂学
·
生物医学工程
✓ 已验证
DOI
PubMed
高影响因子
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
·
2025
·
IF 2.2
Yang Han,Junyong Fan,Wei Xia,Xiao Dong,Ying Ye
Primary liver cancer remains a major contributor to global cancer-related mortality. Echinacoside, a bioactive phenylethanoid glycoside isolated from traditional Chinese medicinal herbs, has shown potent anti-tumor effects. In this study, poly (lactic-co-glycolic acid) (PLGA) nanoparticles encapsulating echinacoside (E@PLGA and E@PLGA-FA) were synthesized via the double emulsification method. Their physicochemical properties, drug release kinetics, and anti-cancer efficacy were systematically evaluated through in vitro and in vivo models. Transmission electron microscopy (TEM) and dynamic light scattering (DLS) analyses revealed that the particle sizes of E@PLGA and E@PLGA-FA were approximately 91 nm and 100 nm, respectively, with zeta potentials of -22.50 mV and -31.89 mV. The polydispersity index (PDI) of E@PLGA and E@PLGA-FA was determined to be 0.16±0.01 and 0.19±0.01, respectively. The encapsulation efficiency and drug-loading capacity of echinacoside in E@PLGA-FA were 28.78% and 12.05%, respectively, slightly lower than those in E@PLGA nanoparticles (40.34% and 16.12%), likely due to folic acid modification altering PLGA solubility during formulation. In vitro release profiles demonstrated pH-dependent drug release: 22% at physiological pH (7.4) versus 67% under acidic conditions (pH 5.5) over 12 h, indicating tumor microenvironment-responsive behavior. Furthermore, E@PLGA-FA significantly inhibited the proliferation of HepG2 cells, induced apoptosis, caused cell cycle arrest at the G0/G1 phase, and suppressed cell mobility. Meanwhile, the protein levels of MMP2, MMP9 and Bax were increased after exposure to E@PLGA and E@PLGA-FA, whereas the protein levels of COL-Ⅰ, COL-Ⅱ, Bcl-2, Cyclin D1, and PCNA were decreased. In vivo, E@PLGA-FA effectively inhibited tumor growth, induced tumor cell apoptosis, and exhibited tumor-specific accumulation confirmed by fluorescence imaging. In addition, The E@PLGA-FA nanoparticle intervention did not induce pathological damage or inflammatory responses in murine liver and kidney tissues, suggesting a favorable safety profile for this compound. In conclusion, we engineered a novel tumor-targeted PLGA-based nanoparticle system for echinacoside delivery, which synergizes pH-responsive drug release, multi-mechanistic anti-cancer effects, and biosafety, offering a promising therapeutic platform for hepatocellular carcinoma.
研究领域:
药剂学
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肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Biomedical Physics & Engineering Express
·
2015
·Vol. 1
·期 4
·045009
·
IF 0
Qiaoying Wang,Dan Wang,Danyang Li,Jian Lu,Qingrong Wei
Ovarian cancer has been the leading cause of death worldwide in gynecologic malignancy mainly due to the lack of ultrasensitive diagnosis approaches at its early stage and high cytotoxicity of anticancer drugs to normal cells. In an attempt to overcome the problems, a co-delivery system of folic acid (FA) modified nanoparticles were developed for early diagnosis and to maximize the therapeutic outcome. In the present study, we formulated a diblock copolymer of methoxy poly (ethylene glycol)-b-poly (-caprolactone)(mPEG-b-PCL) polymer micelles, and FA was further conjugated to endow micelles with active targeted capacity. Then paclitaxel (PTX) and superparamagnetic iron oxide (SPIO) were encapsulated in the core of micelles. The in vitro tumor cell targeting capability of FA-NP/SPIO/PTX and NP/ SPIO/PTX nanoparticles was assessed by confocal laser scanning microscopy (CLSM) with human ovarian cancer (SKOV3 cells) which overexpresses FA receptor. Quantitative analysis showed the amount of intracellular Fe in cells incubated with FA-NP/SPIO/PTX nanoparticles was about 13-fold higher than with NP/SPIO/PTX nanoparticles. The imaging contrast capability of FA-NP/SPIO/PTX nanoparticles as a sensitive MRI probe was evaluated by a 3 T clinical MR imaging scanner. The T2 -weighted imaging of cells incubated with targeting nanoparticles was found to have more sensitive imaging enhancement effect on the SKOV3 cells than non-targeting nanoparticles. Furthermore, the antitumor efficiency of targeting nanoparticles was approximately 5-fold higher than that of their counterparts, which further affirmed the feasibility of attaining the higher therapeutic efficacy of antitumor drugs while minimizing damage to healthy cells. The targeting nanoparticles exhibited the biphasic release characteristic in vitro. The results indicated that folate-modified nanoparticles could achieve high targeting specificity, high efficiency of delivery drug and excellent imaging enhancement. Therefore, the targeting nanoplatform has good prospects in non-invasively detecting early ovarian tumors, maximizing the therapeutic efficiency and real-time monitoring of therapeutic response, which can make it possible to lengthen patients' survival and ultimately achieve the goal of individualized medicine for ovarian cancer in the near future.
研究领域:
肿瘤学
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药剂学
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分子影像学
✓ 已验证
产品关联
DOI
Journal of Biomaterials and Tissue Engineering
·
2017
·Vol. 7
·期 8
·605-613
·
IF 1.383
Yang Bin,Gao Ge,Liu Lintao,Li Yang,Zhao Lihua,Xing Hua
In recent years, breast cancer attracts more and more attention because of its high mobility and high mortality for women. Phototherapy, including photothermal therapy (PTT) and photodynamic therapy (PDT), provides a new pathway to breast cancer therapy. Herein, we developed multifunctional
IR780 loaded nanoparticles based on folic acid modified chitosan (FASOC-IR780 NPs) for targeted imaging and phototherapy of cancer compatible with a single-nearinfrared (NIR) laser irradiation. In vitro characterizations demonstrated the self-assembled FASOC-IR780 NPs own narrow size
distribution and encouraging photothermal performance with enhanced generation of ROS under laser irradiation. The cytotoxicity studies on MDA-MB-231 cells showed enhanced toxicity upon NIR light irradiation. NIR small animal imaging demonstrated the significant tumor-selectivity of the nanoparticles
to breast cancer cells that over expressed folate receptor. In vivo treatments with FASOC-IR780 NPs resulted in effective tumor suppression. These results indicate that the multifunctional FASOC-IR780 NPs show notable targeting and theranostic potential in breast cancer therapy.
研究领域:
肿瘤学
·
纳米医学
·
生物材料科学
·
药剂学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）