INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2022
·
IF 6.51
Pengfei Wang,Juntong Zhao,Yuman Zhang,Zhongjie Zhu,Liyuan Liu,Hongwei Zhao,Xianchao Yang,Xiaonan Yang,Xiaohong Sun,Mingxia He
Cocrystal is constructed to improve physicochemical properties of active pharmaceutical ingredient and prevent polymorphism via intermolecular interactions. However, recent examples on cocrystal polymorphs display significantly different properties. Even though some analytical techniques have been used to characterize the cocrystal polymorphic system, it remains unclear how intermolecular interactions drive and stabilize the structure. In this work, we study the cocrystal polymorphs of nifedipine (NFD) and isonicotinamide (INA) using terahertz (THz) spectroscopy. Form I and form II of NFD-INA cocrystals show spectral fingerprints in THz region. Temperature-dependent THz spectra display distinguished frequency shifts of each fingerprint. Combined with solid-state density functional theory (DFT) calculations, the experimental fingerprints and their distinct responses to temperature are elucidated by specific collective vibrational modes. The vibrations of hydrogen bonding between dihydropyridine ring of NFD and INA are generally distributed below 1.5 THz, which play important roles in stabilizing cocrystal and preventing the oxidation of NFD. The rotations of methyl group in NFD are widely distributed in the range of 1.5–4.0 THz, which helps the steric recognition. The results demonstrate that THz spectroscopy is a sensitive tool to discriminate cocrystal polymorphs. It has the potential to be used as a non-invasive technique for pharmaceutical screening.
研究领域:
药物化学
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物理化学
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DOI
高影响因子
SENSORS AND ACTUATORS B-CHEMICAL
·
2023
·
IF 8.4
Yuxia Liu,Wensi Xu,Wenfeng Zhuge,Qing Huang,Gang Xiang,Jinyun Peng
Metal phthalocyanine-based porous organic polymers have gained increasing attention in numerous areas, but their application potential has yet to be comprehensively explored. In this study, a planar polymer (AlPc-CC POP) with excellent electrochemical capabilities was prepared using a straightforward substitution method. The electrocatalytic activity of AlPc-CC POP towards nifedipine (NIF) was investigated using electrochemical analysis. Under optimal conditions, the electrochemical sensor response to NIF was linearly positively correlated at concentrations ranging from 0.04 to 50 μM with a detection threshold of 0.0273 μM. Moreover, the sensor performed well in terms of reproducibility, stability, and selectivity. Notably, the constructed sensing platform enabled the determination of NIF levels in pharmaceuticals and human sera. This work provides a generalized platform for the detection of antihypertensive NIF and validates the potential of phthalocyanine-based porous organic polymer for sensing.
研究领域:
材料科学
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分析化学
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药物分析
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DOI
高影响因子
BULLETIN OF THE KOREAN CHEMICAL SOCIETY
·
2019
·Vol. 40
·期 3
·214-219
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IF 0.602
Jinyun Peng,Wenfeng Zhuge,Yingying Huang,Cuizhong Zhang,Wei Huang
In this study, a new photoelectrochemical (PEC) sensor based on the copper tetraamino-phthalocyanine-modified ITO electrode (CuTAPc/ITO) was designed for the determination of nifedipine. The prepared CuTAPc materials were characterized using UV–Visible spectrophotometry (UVS), Fourier transform infrared spectroscopy (FT-IR), and X-ray diffraction (XRD). Then, the CuTAPc solution was coated on the ITO electrode surface to fabricate a simple PEC sensing platform. Then, the photoelectrochemical behavior of nifedipine at the CuTAPc/ITO electrode was investigated by chronoamperometry under ultraviolet light irradiation. The obtained results indicated that the modified electrode showed a higher response signal than the blank electrode. The photocurrent of CuTAPc/ITO increased with the increasing concentration of nifedipine. The peak photocurrents were linearly dependent on the nifedipine concentration in the range of 0.25–18.0 μmol/L, thereby providing the detection limit of 0.15 μmol/L ( S / N = 3). Due to the good responses for the determination of nifedipine, this sensor can be used as an alternative analysis tool for the detection of nifedipine in various real samples with high sensitivity, low detection limit, and wide linearity range.
研究领域:
分析化学
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药物分析
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材料科学
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DOI
高影响因子
BIOCHEMICAL PHARMACOLOGY
·
2025
·
IF 5.6
Xiaohai Chen,Fengsheng Hong,Yuxin Shen,Hailun Xia,Lu Shi,Zheli Jiang,Ren-ai Xu
Tamoxifen, a selective estrogen receptor modulator (SERM) used in breast cancer therapy, requires metabolic activation by CYP3A4 to exert its biological effects. This study evaluated the effects of calcium channel blockers nimodipine, nitrendipine and felodipine on tamoxifen metabolism by studying their interactions with tamoxifen in vitro and in vivo . Rat liver microsomes (RLM) and human liver microsomes (HLM) were used in this study to evaluate the inhibitory potential of nimodipine, nitrendipine and felodipine on tamoxifen metabolism in vitro . A total of 28 cardiovascular drugs, including calcium channel blockers, were screened in an RLM incubation system in vitro . In RLM, nimodipine, nitrendipine and felodipine had half-maximum inhibitory concentration (IC 50 ) values of 5.55 µM, 11.86 µM and 7.71 µM, respectively. In HLM, the IC 50 values were increased to 20.38 µM, 30.06 µM, and 44.45 µM for nimodipine, nitrendipine and felodipine, respectively. The kinetic assays indicated that nimodipine and felodipine inhibited the metabolism of tamoxifen in a competitive way, whereas nitrendipine showed non-competitive inhibition in RLM. However, felodipine exhibited non-competitive inhibition, and nimodipine and nitrendipine showed competitive inhibition in HLM. Pharmacokinetic studies in rats revealed that pretreatment with nimodipine and nitrendipine significantly increased the systemic exposure of tamoxifen, as demonstrated by increasing the area under the curve (AUC), the maximum concentration (C max ) and decreasing the clearance (CL z/F ). Finally, molecular docking studies supported these findings, showing potential interactions at the active site of CYP3A4. These results suggested the necessity for careful monitoring and possible dose adjustments of tamoxifen when co-administered with calcium channel blockers in clinic.
研究领域:
药理学
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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
ELECTROCHIMICA ACTA
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2015
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IF 4.504
Qiang Zeng,Tianyan Wei,Min Wang,Xinjian Huang,Yishan Fang,Lishi Wang
ABSTRACT A sensitive and convenient electrochemical strategy is developed for the determination of nifedipine basing on a polyfurfural film modified glassy carbon electrode (GCE) by the one-step electropolymerization of furfural . The prepared polyfurfural film/GCE exhibits excellent electrocatalytic activity towards nifedipine. A series of experimental parameters including the pH of supporting electrolyte , accumulation time and potential for nifedipine is also considered and optimized. Under optimal conditions, the proposed nifedipine sensor has a wide linear detection range from 1 × 10 −8 to 7 × 10 −6 mol dm −3 , with a low detection limit of 5 × 10 −9 mol dm −3 . The proposed nifedipine sensor also displays excellent selectivity, stability and reproducibility. In particular, it shows splendid analytical performance for the determination of nifedipine in real pharmaceutical and human urine samples in practice.
研究领域:
分析化学
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电化学传感器
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药物分析
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DOI
高影响因子
ANALYTICAL AND BIOANALYTICAL CHEMISTRY
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2022
·Vol. 414
·期 26
·7675-7681
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IF 4.478
Sheng Yilun,Huang Zhongnan,Chen Yaling,Guo Xiaoyun,Chen Lan,Peng Huaping,Chen Wei
Monitoring of dihydropyridine drugs, such as nifedipine (NIF), has attracted considerable attention owing to the side effects arising from the consumption of such drugs. Herein, a highly sensitive and facile fluorescence-sensing platform based on a high-quantum-yield sulfur quantum dot (SQDs) probe for NIF detection is proposed. Based on the principle of the inner filter effect, the rapid detection of NIF with high sensitivity is successfully realized on the basis of the change in the fluorescence signal due to the quenching effect of NIF on SQDs. The results show a good linear relationship between the NIF concentration and fluorescence intensity within the range of 5–150 μmol/L, with a low detection limit of 1.63 μmol/L (S/N = 3). Moreover, because no surface modification or establishment of any coupling between the receptor and the fluorophore is necessary, this approach provides considerable flexibility and simplicity for the construction of a fluorescence sensor and substantially reduces the detection time. A systematic investigation was conducted to verify the applicability of this method for the analysis of pharmaceutical components in NIF tablets. This study not only promotes the design and development of a fluorescence analysis platform for NIF detection, but also facilitates the fabrication of novel SQD-based fluorescence-sensing systems for the molecular detection of drugs. Graphical abstract
Proposal for a facile nifedipine assay method based on the inner filter effect of nifedipine to high-quantum-yield sulfur quantum dots, and realizing nifedipine detection in tablets and human urine samples.
研究领域:
分析化学
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药物化学
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生物医学工程
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DOI
PubMed
高影响因子
JOURNAL OF THE ELECTROCHEMICAL SOCIETY
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2022
·Vol. 169
·期 4
·046502
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IF 4.386
Yuxia Liu,Jinyun Peng,Wenfeng Zhuge,Qing Huang,Gang Xiang,Liying Wei
A conductive two-dimensional, phthalocyanine metal–organic framework material (CoPc-Cu MOF) was successfully modified onto a glassy carbon electrode (GCE) to construct an electrochemical sensor for the high-sensitivity detection of nifedipine (NIF). The 2D MOF was obtained by complexing (2,3,9,10,16,17,23,24-octahydroxyphthalocyaninato) cobalt(II) ([OH]8PcCo) with copper(II) ions (denoted as CoPc-Cu MOF). Under optimal conditions, the CoPc-Cu MOF/GCE sensor showed a wide linear range (0.01−92.55 μM) and a low detection limit (6.0 nM) for the determination of NIF. Moreover, the electrochemical sensor exhibited high repeatability, stability, and selectivity. The electrochemical sensing platform was applied to the real determination of NIF in tablets and showed satisfactory results.
研究领域:
分析化学
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材料科学
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DOI
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
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2020
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IF 5.88
Qiankun Jiang,Lingqiong Wu,Yue Zheng,Xiaojie Xia,Ping Zhang,Tong Lu,Jing Li
To combine the advantages of micelles and biomimetic silica materials, biomimetic micellar mesoporous silica xerogel (BM-SX) was initially established, biomimetic silica xerogel (B-SX) was also studied as control and nitrendipine (NDP) was taken as model drug. The content mainly focused on drug dissolution, systemic stability and cellular transmembrane transport of NDP loaded B-SX and NDP loaded BM-SX. With extra mesopores formed due to HPMC E50 micelles, the mean pore diameter, surface area and pore volume of BM-SX were all larger than B-SX. After loading NDP into the two carriers, crystal NDP changed to amorphous phase, leading to enhanced NDP dissolution. BM-SX presented superior abilities not only for its higher drug dissolution compared to B-SX but also for its capacity in remaining high amorphous drug phase and therefore no drug dissolution reduction can be observed. The dynamic contact angle result confirmed the strong power of HPMC E50 micelles in maintaining amorphous NDP in the carrier to improve high systemic stability. Both B-SX and BM-SX could increase drug absorption permeability and exert function as drug efflux inhibitor to inhibit the efflux effect of p-gp drug pump and promote NDP absorption and transport, and BM-SX was superior owing to micelles in the system.
研究领域:
药剂学
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材料科学
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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
CARBOHYDRATE POLYMERS
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2012
·
IF 3.628
Yuling Xie,Yanli Liu,Yan Wang,Siling Wang,Tongying Jiang
Three dimensionally ordered macroporous (3DOM) chitosan (3D-CS) matrix with interconnected pores in the nanometer range was developed as a drug carrier for the first time. 3D-CS was prepared using a template-assisted assembly and characterized by SEM, TGA, N 2 adsorption and FT-IR. As a model drug, nimodipine (NMDP) was incorporated into the pores of 3D-CS matrix. The solid state properties of NMDP-loaded samples were characterized by SEM, XRD, DSC and FT-IR. Dissolution studies showed that release behavior of the drug was markedly affected by the particle size of the matrix. With a relatively small matrix particle size, formulations of NMDP-3D-CS-0.5 and NMDP-3D-CS-1 exhibited rapid release patterns. However, on increasing the amount of carrier, release rate of the drug decreased. The pH-dependent slow-release characteristic of 3D-CS matrix delivery system was demonstrated by investigating the release behavior of NMDP at different pH values.
研究领域:
药剂学
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生物材料
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产品关联
DOI
PubMed
高影响因子
LUMINESCENCE
·
2022
·Vol. 37
·期 9
·1547-1556
·
IF 2.613
Like Zhou,Hui Zhou,Huilong Xiao,Zihang Zhang,Ziyun Xiong,Xun Tuo,Hui Guo
Nifedipine (NDP), a dihydropyridine calcium antagonist, is widely used for the treatment of hypertension and angina pectoris. Catalase is a key antioxidant enzyme that is closely relevant to the level of reactive oxygen specie in vivo . Here, the research explored the effects of NDP on the conformation and catalytic function of bovine liver catalase (BLC) through enzymatic reaction kinetic techniques, multispectroscopic analysis, and computer simulation methods. Kinetic studies clarified that the NDP reduced the activity of BLC using a noncompetitive inhibition mechanism. Based on trial data, a static quenching mechanism functioned in quenching the intrinsic fluorescence of BLC. The binding constant value was (4.486 ± 0.008) × 10 4 M −1 (298 K) and BLC had one binding site for NDP. Tyr was prone to be exposed more to a hydrophilic environment in wake of a shift in fluorescence value. The binding reaction of BLC to NDP caused a conformational change in BLC, which in turn led to increase in the α-helix content and a decline in the β-sheet content. Furthermore, several amino acids residues interacted with NDP by means of van der Waals forces, whereas Gln397, Asn368, Gln371, Asn384, and Pro377 formed several hydrogen bonds with NDP.
研究领域:
生物化学
·
药物学
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产品关联
DOI
PubMed
高影响因子
MICROPOROUS AND MESOPOROUS MATERIALS
·
2020
·
IF 4.551
Ping Zhang,Qiankun Jiang,Yue Zheng,Jing Li
To further explore the wonder of nano technology in drug delivery system, the combination of micelles and mesoporous silica was conducted for delivering poorly water soluble nifedipine (NFP). Double-nano silica xerogel (DN-SX) with both micelles and nanopores was prepared and silica xerogel with only nanopores (SN-SX) was made for comparison. Characteristics of DN-SX and SN-SX, including morphology, porous structure and crystalline state were investigated and pharmaceutical performances of drug loaded carriers were studied. The micelles in DN-SX contributed to achieve larger mesopores and enhanced NFP dissolution better than SN-SX. How responses of drug release amount and reduced drug release amount reacted as changing each influencing factor was elucidated by Box–Behnken experimental design. With the DN-SX obtained by optimization, in vivo pharmacokinetic study result demonstrated that the relative bioavailability of NFP loaded DN-SX and NFP loaded SN-SX were 216.84% and 161.14%, respectively. Therefore, the optimized DN-SX with double-nano structure was of great value for designing poorly water soluble drug delivery system.
研究领域:
药剂学
·
纳米技术
·
药物动力学
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产品关联
DOI
高影响因子
Bio-Design and Manufacturing
·
2023
·
IF 7.9
Lu Jingyi,Sun Miao,Zhang Jingyu,Yang Xiaofu,Dong Minyi,He Huihui,Liu An,Yu Mengfei,Wang Baixiang,Wang Huiming
Regeneration and reconstruction of bone tissue is always a challenge for clinicians due to the uncertainty of bone repair materials in terms of long-term and efficient effects on osteoblasts. Here, we propose a novel strategy combining benidipine, an antihypertensive drug and nanoparticles to synergistically promote the healing of bone defects. Loose and porous benidipine-loaded magnesium silicate nanoparticles were prepared and validated for their biosafety. The nanoparticles were efficiently taken up by preosteoblasts and uniformly distributed around the nucleus. After internalization into cells, the nanosystem is degraded by lysosomes, and the effect of promoting osteogenic differentiation is reflected by the continuous release of benidipine, silicon and magnesium ions. Our results clearly evaluated that the nanoflower-like magnesium silicate delivering benidipine tends to be more appropriate for the bone regeneration in preosteoblasts, indicating that it might be a potential approach in guiding bone repair in clinical applications. Graphic abstract
研究领域:
生物医学工程
·
材料科学
·
组织工程
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）