Pharmaceutics
·
2018
·Vol. 10
·期 3
·146
·
IF 3.746
Yifan Yang,Yunzhi Yin,Jun Zhang,Tiantian Zuo,Xiao Liang,Jing Li,Qi Shen
Oral delivery is considered the preferred route of administration due to its convenience and favorable compliance. Here, docetaxel (DTX) loaded polylactic-co-glycolic acid (PLGA) nanoparticles, coated with polyethyleneimine–folic acid (PEI-FA) and polyethyleneimine–borneol (PEI-BO), were designed to enhance oral absorption (FA/BO-PLGA-NPs). The FA/BO-PLGA-NPs were spherical and smooth with an average size of (137.0 ± 2.1) nm. Encapsulation efficiency (EE%) and drug loading (DL%) were (80.3 ± 1.8)% and (2.3 ± 0.3)%, respectively. In vitro release studies showed that approximately 62.1% of DTX was released from FA/BO-PLGA-NPs in media at pH 7.4. The reverted gut sac method showed that the absorption of FA/BO-PLGA-NPs in the intestines was approximately 6.0 times that of DTX. Moreover, cellular uptake suggested that the obtained FA/BO-PLGA-NPs could be efficiently internalized into Caco-2 cells via FA-mediated active targeting and BO-mediated P-glycoprotein (P-gp) inhibition. Pharmacokinetics study demonstrated that after oral administration of DTX at a dose of 10 mg/kg in FA/BO-PLGA-NPs, the bioavailability of FA/BO-PLGA-NPs was enhanced by approximately 6.8-fold compared with that of DTX suspension. FA/BO-PLGA-NPs caused no obvious irritation to the intestines. Overall, the FA/BO-PLGA-NP formulation remarkably improved the oral bioavailability of DTX and exhibited a promising perspective in oral drug delivery.Keywords:docetaxel;nanoparticles;dual-functional;folic acid;borneol;oral absorption
研究领域:
药学
·
纳米技术
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Analytical Methods
·
2015
·Vol. 7
·期 22
·9649-9654
·
IF 1.821
Shang Zhou,Danqun Huo,Changjun Hou,Mei Yang,Huanbao Fa,Cui Xia,Mei Chen
The monitoring of folate receptor levels in living cancer cells has attracted increasing interest; however, the present fluorescent probes used often suffer from interference from nonspecific adsorption on the surface of non-target cells. In the present study, the probe is readily prepared by using folic acid as a template molecule, a mesoporous silica nanoparticle as an imprinting material, and a CdTe quantum dot as a signal transducer for the recognition of folate receptors. This system is expected to offer specific recognition of folate receptors over other substances based on the high affinity of folic acid and folate receptors. The probe is stable and monodispersed in an aqueous suspension, and has little toxicity to living cells and thus can be utilized for targeted A549 cell imaging. The living cell imaging experiments further demonstrate its value in bioimaging cell-surface folate receptors by virtue of its superior biocompatibility, lower cytotoxicity and membrane permeability.
研究领域:
生物医学工程
·
纳米医学
·
癌症研究
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2014
·
IF 3.107
Jian Rong Zhang,Zhong Ling Wang,Fei Qu,Hong Qun Luo,Nian Bing Li
A highly sensitive folic acid (FA) detection method based on the fluorescence quenching of polyethylenimine-capped silver nanoclusters (PEI-AgNCs) was put forward. In the sensing system, FA and PEI-AgNCs were brought into close proximity to each other by electrostatic interaction, and a two-step electron-transfer process, in which the electron was transferred from FA to AgNCs through PEI molecule, led to fluorescence quenching. The fluorescence quenching efficiency of PEI-AgNCs was linearly related to the concentration of FA over the range from 0.1 nM to 2.75 μM. Good linear correlation (R2 = 0.9981) and a detection limit of 0.032 nM were obtained under optimum conditions. Moreover, the proposed method was used for the determination of FA in real samples with satisfactory results, and those coexistent substances could not cause any significant decrease in the fluorescence intensity of AgNCs. Therefore, the proposed research system is of practical significance and application prospects.
研究领域:
分析化学
·
生物医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
·
2018
·Vol. 34
·期 2
·203-211
·
IF 1.248
Song Shengmei,Li Minglu,Gong Xiaojuan,Han Hui,Zhou Yehong,Wang Li,Shuang Shaomin,Dong Chuan
In the paper, folic acid(FA)-mediated and β -cyclodextrin( β -CD) derivatives functionalized magnetic Fe 3 O 4 nanoparticles(MNPs) were successfully prepared as drug carriers for the targeted delivery and controlled release of water-insoluble anticancer drug. FA-sulfobutyl ether- β -CD-MNPs(FA-SBE- β -CD-MNPs), FA-hydroxypropyl- β -CD-MNPs(FA-HP- β -CD-MNPs) and FA-carboxymethyl- β -CD-MNPs(FA-CM- β -CD-MNPs) were fabricated, and the loading efficiency and relative entrapment rate of curcumin are 12.04 mg/g, 95.56% for FA-SBE- β -CD-MNPs, 9.6 mg/g, 81.63% for FA-HP- β -CD-MNPs and 7.88 mg/g, 85.28% for FA-CM- β -CD-MNPs, respectively. Meanwhile, at pH=5.0, the optimal release rate of curcumin is about 46.07% for FA-SBE- β -CD-MNPs in 5 h. Cellular uptake indicates that curcumin can be selectively transported to targeting site and released from the internalized carriers. The in vitro cytotoxicity reveals that non-toxic FA-SBE- β -CD-MNPs have excellent biocompatibility on HepG2 cells in the tested concentrations. Therefore, FA-SBE- β -CD-MNPs could provide a promising platform for the targeting delivery of water insoluble anti-cancer drugs for different treatment needs of cancer therapy.
研究领域:
药剂学
·
生物医学工程
·
肿瘤学
✓ 已验证
产品关联
DOI
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
·
肿瘤学
·
分子生物学
✓ 已验证
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
·
化学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMISTRY LETTERS
·
2015
·Vol. 44
·期 4
·471-473
·
IF 1.23
Sun Jiadi,Meng Long,Zhu Ye,Cui Yan,Liu Xiaoya
Herein, gels composed of nanoscaled particles were obtained via one-step self-assembly of poly(γ-glutamic acid) (γ-PGA) and folic acid (FA). The outcomes show that the amount of added FA plays a crucial role in the liquid–gel transition. The resulting gels revealed an increase in both storage modulus (G′) and loss modulus (G′′) with increasing amount of FA. This paper describes an effective and promising strategy to prepare gels based on self-assembly of copolymers or particles in an organic medium.
研究领域:
材料科学
·
生物化学
✓ 已验证
DOI
高影响因子
LUMINESCENCE
·
2025
·Vol. 40
·期 4
·e70175
·
IF 3
Jiaoyan Xie,Suqin Han
Folic acid (FA) is a crucial B vitamin for cell formation and maintenance, and its deficiency can lead to severe health disorders, highlighting the importance for accurate FA detection. Chemiluminescence (CL) provides a highly sensitive analytical approach, characterized by simple instrumentation, high accuracy, and low background interference. However, traditional CL techniques are often limited by weak signal intensity and poor robustness. This study presents a novel CL system using well-defined fluorescent Cl, S, N co-doped carbon dots (ClSN-CDs) integrated into the H 2 O 2 -KBrO 3 system. Under acidic conditions, the synergistic effect of H 2 O 2 and KBrO 3 induced ClSN-CDs to emit a strong CL signal, with the emitting species identified as excited-state ClSN-CDs. Trace amounts of FA significantly quenched the CL intensity of the ClSN-CDs-H 2 O 2 -KBrO 3 system, enabling rapid, sensitive, and selective FA detection. The system demonstrated a linear response to FA concentrations ranging from 0.02 to 1.0 μM, with a detection limit of 3.1 nM. Selectivity and recovery studies validated the system's robust analytical performance. Mechanistic investigations revealed that the CL reaction involved reactive oxygen species (ROS), and FA-mediated ROS consumption led to luminescence suppression.
研究领域:
分析化学
·
营养学
·
食品科学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Fang Xie,Nian Liu,Xiaoqing Liu,Xiaofang Feng,Zhaoxing Yang,Zhijun He,Jie Cai
Selenium nanoparticles (SeNPs) exhibit significant potential in antitumor therapy. However, challenges such as aggregation and lack of targeting capability limit their application. Herein, we developed selenium-loaded octenyl succinic anhydride starch (OSAS) micelles functionalized with folic acid (FA) for targeted tumor delivery. The FA-OSAS-SeNPs were synthesized through self-assembly, incorporating SeNPs into FA-conjugated OSAS micelles. Fourier Transform Infrared (FTIR) spectroscopy and UV–visible spectrophotometry confirmed the successful synthesis of FA-OSAS-SeNPs. The nanoparticles exhibited an average size of 131.66 ± 7.88 nm and a zeta potential of −19.54 ± 0.33 mV, with encapsulation efficiency and drug loading capacity of approximately 87.28 % and 8.96 %, respectively. FA-OSAS-SeNPs demonstrated good stability across various conditions, including different dilution ratios, temperatures, pH levels, and ionic strengths. In vitro studies showed that FA-OSAS-SeNPs exhibited significant targeted inhibitory effects on cervical cancer (HeLa) cells and markedly increased intracellular ROS levels, inducing apoptosis. This study presents a novel and effective strategy for targeted SeNPs delivery systems in tumor therapy, offering a valuable reference for future development of nanomaterials for clinical applications in cancer treatment.
研究领域:
药剂学
·
生物医学工程
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Xiaohan Pan,Peng Wang,Jiahui Gu,Yuxiu Wang,Qingqing Li,Wenpeng Zhao,Shu Wang,Jingxin Gou,Xinyu Fan
Bladder instillation of chemo-therapeutic agents is common for bladder cancer (BC) treatment, however, due to the poor tissue selectivity of chemotherapeutic agents, this method suffers from bladder irritation or even chemical cystitis. Here, we designed a hydroxyethyl starch-based prodrug for epirubicin (EPI) using a pH-sensitive hydrazone linker and folate as the active targeting moiety (FA-HES-hyd-EPI) to achieve delivery selectivity. Prodrug micelles decorated with FA (FA-m), with diameter of 203.6 ± 7.1 nm and EPI loading of 5.80 ± 0.129 %, were prepared by self-assemble method. FA-m was found with improved cellular uptake and stronger cytotoxicity over EPI. An orthotopic BC model was established with FA receptor over-expression, and FA-m showed significantly higher accumulation at tissue and cell levels compared with the FA-free counterpart. Besides, the systemic exposure of FA-m was significantly lower than EPI (AUC 0-t : 28.11 ± 7.23 ng/mL/h versus 11.60 ± 4.27 ng/mL/h). More importantly, FA-m showed stronger in vivo tumor growth inhibition with average tumor weight of 0.26 ± 0.21 mg (EPI group: 1.695 ± 0.62 mg), and better safety according to body weight and HE staining data. Overall, the combination of active targeting and pH responsive prodrug strategies was a feasible way to achieve selective EPI delivery to BC via instillation that improved both therapeutic effect and safety.
研究领域:
药学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food Analytical Methods
·
2021
·Vol. 14
·期 8
·1637-1644
·
IF 3.366
He Yu,Wang Shuo,Wang Junping
Folic acid (FA) is a vitamin essential for human physiology; thus, rapid, accurate, and sensitive methods for its detection and quantification in different biological samples are necessary. A fluorescent ratiometric nanoprobe (the complex composed of quantum dots and carbon dots) based on carboxyl-modified quantum dots (QDs) and amino-modified graphene-based carbon dots (CDs) has been developed for the visual determination of folic acid (FA). The nanoprobe is the composition in which QDs were covalently bonded with CDs. Red and blue fluorescence of nanoprobe can be selectively quenched and enhanced by FA, respectively. Thus, the nanoprobe is capable to generate clearly visible fluorescence color change from pink to blue upon exposure to UV light. Depending on the color change and its intensity, FA can be identified, and their concentrations can be determined. The sensor prepared based on the nanoprobe demonstrated good selectivity and sensitivity toward FA with exceptionally low detection limit equal to 0.039 μM. We also prepared a paper-based sensor to demonstrate convenient and simple approach to visually detect FA. Thus, the nanoprobe demonstrated feasibility of rapid real-time quantitative FA detection; considering its simple, effective, and practicality, expectedly it can be used for practical application.
研究领域:
分析化学
·
生物医学工程
·
食品科学
✓ 已验证
产品关联
DOI
高影响因子
FOOD CHEMISTRY
·
2017
·
IF 4.529
Fenglian Wang,Minyi Cao,Nani Wang,Nadeem Muhammad,Shuchao Wu,Yan Zhu
Folic acid plays a significant role during periods of rapid cells division and growth. Pregnant women require folic acid daily, either from dietary supplements or folic acid tablets in order to prevent fetal neural tube defects. In this work, a simple coupled ultrahigh performance liquid chromatography and ion chromatography technique was developed for simultaneous determination of folic acid and inorganic anions in folic acid tablets. A reversed-phase C18 column was used as the pretreatment column for on-line separating inorganic anions from organics. Inorganic anions were concentrated in the concentration column. Under the optimal chromatographic conditions, good sensitivity and linear calibration-curves (r ≥ 0.9992) were obtained. Low detection limits were obtained in the range of 0.0032–0.40 mg L −1 for all analytes. Repeatability results were satisfactory with relative standard deviations less than 1.50% (n = 5). The developed method was utilized to analyze spiked folic acid tablet samples with good measured recoveries (92.4–107.4%).
研究领域:
分析化学
·
医学
·
药学
✓ 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）