AAPS PHARMSCITECH
·
2020
·Vol. 21
·期 5
·1-7
·
IF 2.401
Yan Na,Tang Zhan,Xu Yuqi,Li Xiumin,Wang Qiao
Ferulic acid is contained in some Chinese herbal medicines such as Ligusticum chuanxiong or Angelica sinensis. Studies have focused on the treatment of inflammatory diseases and pain using ferulic acid. However, little is known about its pharmacokinetics after transdermal administration. The present research investigated the pharmacokinetic behavior of ferulic acid in rat plasma and skin microdialysate after ferulic acid transdermal or intragastric administration. Samples collected at predetermined time points were determined by a simple and sensitive HPLC-UV method. The pharmacokinetic parameters were estimated using non-compartmental analysis with DAS 2.0 software. The values of AUC 0- t and C max after intragastric administration (20 mg/kg) in plasma were 281.47 ± 46.76 min mg/L and 12.20 ± 2.46 mg/L, respectively. After emulsion transdermal administration (117 mg/kg, 35 mg/4 cm 2 ), the values of AUC 0- t and C max in plasma and skin microdialysate were 953.90 ± 175.30 min mg/L, 7630.47 ± 1410.33 min mg/L, 3.00 ± 0.61 mg/L, and 19.08 ± 4.39 mg/L, respectively. Here, we show a promising delivery system for ferulic acid that could replace traditional administration, and a better understanding of the transdermal pharmacokinetics of ferulic acid, which may be helpful for further clinical and laboratory studies.
研究领域:
药理学
·
中药学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Lu Jin,Xiumin Li,Xu Chen,Xinghao Chen,Ye Liu,Haonan Xu,Qiao Wang,Zhan Tang
Puerarin (PUE), an isoflavonoid isolated from Pueraria lobata (Willd) Ohwi root, is a β -adrenergic receptor inhibitor used in treating glaucoma. The concentration range of gellan gum was determined based on the formulation viscosity and gelling capacity. PVP-K30 and gellan gum were used as variables, with the viscosity of formulation: STF = 40: 21, the 4 h permeation rate of rabbit isolated sclera, and 2 h in vitro release rate as response values. The JMP software was used to optimize the results, presenting that gellan gum was the main factor influencing viscosity. The in vitro release and permeation rate were primarily influenced by PVP-K30. The optimal prescription was 0.45% gellan gum and 6.0% PVP-K30. The in vitro release and permeation characteristics of puerarin in situ gel (PUE-ISG) were investigated using PUE solution as a control. The dialysis bag method results indicated that the release of the solution group leveled off after 4 h, while the PUE-ISG group had been continuously releasing. However, the cumulative release rates of the two were no longer significantly different at 10 h. The cumulative permeation rates of the ISG and solution groups were not significantly different ( P > 0.05) in the rabbit isolated sclera. The apparent permeability Papp and steady-state flux Jss of PUE-ISG were 0.950 ± 0.059 cm/h and 9.504 ± 0.587 mg·(cm·h), respectively. A sensitive and stable HPLC-MS/MS analytical method for quantifying aqueous humor concentrations of PUE was validated. A microdialysis technique was successfully used in the aqueous humor pharmacokinetics study to sample aqueous humor from rabbit eye continuously. The results revealed that PUE-ISG significantly increased the drug concentration in the aqueous humor, with C max and AUC (0-t) 3.77 and 4.40 times higher than those of the solution group, respectively. T max was also significantly prolonged, indicating good prospects for clinical application. The developed PUE-ISG preparation has the characteristics of rapid drug release and sustained permeation, and increase the drug concentration in aqueous humor, with all inactive ingredients remaining within the maximum allowable limits recommended by the FDA guideline.
研究领域:
药剂学
·
药物代谢动力学
·
眼科
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产品关联
DOI
PubMed
高影响因子
ANALYTICA CHIMICA ACTA
·
2025
·
IF 6
Jiaze Yan,Chao Jiang,Jiqi Zheng,Ming Guo
Background Microdialysis is an in vivo technique for dynamically analyzing biochemical components in tissues and fluids. Traditional microdialysis systems are primarily designed for low molecular weight polar compounds, resulting in lower recoveries for hydrophobic compounds. This study aimed to develop a greener, cost-effective, and enhanced microdialysis method for recovering eugenol, isoeugenol, and methyl isoeugenol, utilizing hydrophobic deep eutectic solvents as the perfusate, with the method's feasibility verified through in vivo experiments. Results Among the 19 types of deep eutectic solvents evaluated, thymol-levulinic acid was identified as the most suitable for eugenol compounds based on liquid-liquid microextraction and microdialysis experiments, showing an in vitro microdialysis recovery approximately 100 times higher than that of water. The optimization of microdialysis parameters was conducted, including molar ratio of HBA:HBD, temperature, flow rate, and semi-permeable membrane length. In the in vivo microdialysis experiments, the temporal concentration of eugenol, which was used as an anesthetic in Glyptocidaris crenularis, was detected by GC-MS/MS and calibrated using ex vivo recovery. When the concentration of eugenol in artificial seawater was maintained at 100 μg mL −1 , the eugenol levels in the coelomic fluid of Glyptocidaris crenularis rose from 0 to 6.89 ± 0.38 μg mL −1 within 60 min, then stabilized in next 80 min. Significance The findings demonstrate that deep eutectic solvents enhanced microdialysis provides high recoveries and enables real-time monitoring of drug concentration changes in biological systems, making this method a valuable tool for pharmacokinetic studies and environmental monitoring.
研究领域:
分析化学
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药理学
·
海洋生物学
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产品关联
DOI
PubMed
高影响因子
ANALYTICAL CHEMISTRY
·
2020
·
IF 6.785
Lu Shi,Feifei Cao,Limin Zhang,Yang Tian
The development of switches responding to specific pH changes was particularly useful in wide application fields. Owing to flexible switches simulated by pH, i-motif DNAs are widely used as a pH sensor. But its character of structure transition strongly dependent on acidic pH severely hampers the application of i-motif DNA in physiological media. Herein, we report the stable i-motif structure formed at a physiological pH triggered by spatial confinement of silica nanochannels. Three classic DNA chains containing 21-mer i-motif domain base-pairs and a single-stranded multiply (T)n spacer, 5′-COOH-(T)n-CCCTAACCCTAACCCTAACCC-3′, were employed to evaluate the enhanced stability of i-motif structure. Compared to their free states in a dilute solution, the transition pH of all i-motif DNAs decorated in nanochannels remarkably shifts toward a neutral pH. Moreover, the transition midpoint can be tuned sensitively over the physiologically relevant pH range through slightly varying the length of T base spacer. Density functional theory (DFT) calculations validate that the increased proton density in a nanochannel triggers the formation of an i-motif structure under a neutral pH. Finally, this i-motif DNA based nanochannels electrode was successfully employed to monitor pH in brain microdialysates followed by cerebral ischemia. The present approach is not limited by fundamental investigation for DNA conformation but may extend toward the manipulation of i-motif based structures for artificial molecular machines and signaling systems.
研究领域:
生物化学
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分子生物学
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医学检测
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产品关联
DOI
PubMed
高影响因子
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
·
2016
·
IF 1.566
Wenqiang Ba,Zhou Li,Lisheng Wang,Ding Wang,Weiguo Liao,Wentao Fan,Yinai Wu,Fengyun Liao,Jianye Yu
The purpose of the present study was to prepare and optimize sinomenine (SIN) pluronic lecithin organogels system (PLO), and to evaluate the permeability of the optimized PLO in vitro and in vivo. Box–Behnken design was used to optimize the PLO and the optimized formulation was pluronic F127 of 19.61%, lecithin of 3.60% and SIN of 1.27%. The formulation was evaluated its skin permeation and drug deposition both in vitro and in vivo compared with gel. Permeation and deposition studies of PLO were carried out with Franz diffusion cells in vitro and with microdialysis in vivo. In vitro studies, permeation rate (Jss) of SIN from PLO was 146.55 ± 2.93 μg/cm2/h, significantly higher than that of gel (120.39 μg/cm2/h) and the amount of SIN deposited in skin from the PLO was 10.08 ± 0.86 μg/cm2, significantly larger than that from gel (6.01 ± 0.04 μg/cm2). In vivo skin microdialysis studies showed that the maximum concentration (Cmax) of SIN from PLO in “permeation study” and “drug-deposition study” were 150.27 ± 20.85 μg/ml and 67.95 μg/ml, respectively, both significantly higher than that of SIN from gel (29.66 and 6.73 μg/ml). The results recommend that PLO can be used as an advantageous transdermal delivery vehicle to enhance the permeation and skin deposition of SIN.
研究领域:
药剂学
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药物递送系统
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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
Pharmaceuticals
·
2023
·Vol. 16
·期 1
·90
·
IF 4.6
Haonan Xu,Ye Liu,Lu Jin,Xu Chen,Xinghao Chen,Qiao Wang,Zhan Tang
Brimonidine tartrate (BRT) is a highly selective α2 adrenergic receptor agonist as treatment for patients with open angle glaucoma and high intraocular pressure. The objective of this study was to formulate an ophthalmic ion-sensitive in situ gel (ISG) of BRT to increase the retention time of the drug and its bioavailability. The optimum formulation of 2 mg/mL BRT-ISG was obtained with 0.45% gellan gum as the gel matrix. In vitro release results showed that the water-soluble drug bromonidine tartrate in ocular in situ gels exhibited a high burst effect and fast release in solution. The results of dialysis membrane permeation showed that there was a significant difference between the commercially available and BRT-ISG groups after 45 min. The results of the pre-corneal retention study indicated that gellan gum can effectively prolong ocular surface retention. Preliminary stability results showed that it should be stored in a cool and dark place, and the formulation under long-term preservation can be basically stable. The pharmacokinetic study of the BRT-ISG in the anterior chamber of the rabbit eye was studied by microdialysis technique, and microdialysis samples were analyzed by LC-MS/MS. The pharmacokinetic study showed that the BRT-ISG reached Cmax (8.16 mg/L) at 93 min after administration, which was 2.7 times that of the BRT eye drops, and the AUC(0-t) (1397.08 mg·min/L) was 3.4 times that of the BRT eye drops. The optimal prescription can prolong the retention time of BRT in front of the cornea and significantly improve the bioavailability of BRT in the eye. Combined with the results of in vitro release, permeation and pre-corneal retention studies, the improvement of BRT-ISG bioavailability in rabbit eyes was found to be mainly due to the retention effect after the mixture of ISG and tears.Keywords:brimonidine tartrate;in-situ gel;ocular permeation;microdialysis
研究领域:
药剂学
·
眼科学
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ANALYTICAL CHEMISTRY
·
2015
·
IF 5.636
Limin Zhang,Yingying Han,Fan Zhao,Guoyue Shi,Yang Tian
Metals are essential components of all living cells, and in many cases cells trigger and utilize dynamic metal movements for signaling purposes. So, it is very critical to develop the biosensors for determination of metal ions in living systems with high selectivity and accuracy. In this work, taking Cu2+ as a model, an accurate and selective ratiometric electrochemical biosensor was developed. First, the specific molecule, 2,2′,2″-(2,2′,2″-nitrilotris(ethane-2,1-diyl)-tris((pyridin-2-ylmethyl)azanediyl)triethanethiol (TPAASH), was designed and synthesized for specific recognition of Cu2+. Meanwhile, electroactive molecule, 6-(ferrocenyl)hexanethiol (FcHT) was coimmobilized with TPAASH at one electrode as inner reference molecule to provide a built-in correction for avoiding the environmental effects. Thus, the developed biosensor demonstrated high accuracy and remarkable selectivity toward Cu2+ against other metal ions, amino acids, and so on. In addition, the biosensor also showed high sensitivity due to the electrocatalytic activity of the nanostructured gold flowers. As a result, the present ratiometric electrochemical biosensor was successfully applied in detection of Cu2+ in brain microdialysates of normal rat brain and that followed by global cerebral ischemia.
研究领域:
生物传感技术
·
神经科学
·
分析化学
✓ 已验证
DOI
PubMed
高影响因子
ANALYTICAL LETTERS
·
2015
·
IF 1.03
Rong-Xiang Chen,Li Wang,Jie Wang,Fu-Qiang Xu
A simple method was developed for the determination of hydrophilic whitening agents (ascorbyl glucoside, magnesium ascorbyl phosphate, arbutin, hydroquinone, and kojic acid) in bleaching cosmetics by high performance liquid chromatography with electrochemical detection. The samples were prepared using microdialysis and were separated within ten minutes using isocratic elution. Linear calibration was achieved for concentrations between 0.10 and 10.00 micromolar. The limits of detection were from 0.6 to 2.0 nanomolar; the recoveries were between 91.43 and 108.04 percent, and the relative standard deviation was less than 6.88 percent. This method was used to determine whitening compounds in several cosmetics with on-line microdialysis and the zero net flux method. The procedure was fast, simple, selective, and suitable for routine analysis.
研究领域:
分析化学
·
化妆品科学
✓ 已验证
DOI
高影响因子
International Journal of Analytical Chemistry
·
2019
·
IF 1.682
Lianghong Liu,Lian Zhu,Kaiyan Gong,Xinjun Zhi,Ying Guan,Wei Cai
Duhaldea nervosa (D. nervosa) has been used for treatment of bone fracture by external use. Thus, the percutaneous absorption was crucial to the effect of D. nervosa, especially the constituents of percutaneous absorption. However, the constituents in vivo were never investigated to date. In this study, an efficient method was developed for the identification of constituents of percutaneous absorption using UHPLC-Q-Exactive Orbitrap MS and microdialysis technique. A total of 20 constituents including 15 chlorogenic acid analogues, 3 amino acids, and 2 organic acids were unambiguously or tentatively identified based on high-resolution mass data including MS and MS2, chromatography retention time, and bibliography data. To the best of our knowledge, this is the first study to report the constituents of percutaneous absorption from D. nervosa, which will be very helpful for understanding the bioactive compounds and quality control.
研究领域:
药理学
·
分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PLoS One
·
2013
·Vol. 8
·期 11
·e79881
·
IF 3.73
Sha-Sha Li,Guo-Feng Li,Li Liu,Xiao Jiang,Bin Zhang,Zhi-Gang Liu,Xue-Ling Li,Li-Dong Weng,Ting Zuo,Qiang Liu
The aim of the present study was to design a novel topical skin-target drug-delivery system, the paeonol microsponge, and to investigate its drug-release patterns in dosage form, both in vitro and in vivo . Paeonol microsponges were prepared using the quasi-emulsion solvent-diffusion method. In vitro release studies were carried out using Franz diffusion cells, while in vivo studies were investigated by microdialysis after the paeonol microsponges were incorporated into a cream base. In vitro release studies showed that the drug delivered via microsponges increased the paeonol permeation rate. Ex vivo drug-deposition studies showed that the microsponge formulation improved drug residence in skin. In addition, in vivo microdialysis showed that the values for the area under the concentration versus time curve (AUC) for the paeonol microsponge cream was much higher than that of paeonol cream without microsponges. Maximum time (T max ) was 220 min for paeonol microsponge cream and 480 min for paeonol cream, while the half-life (t 1/2 ) of paeonol microsponge cream (935.1 min) was almost twice that of paeonol cream (548.6 min) in the skin (n = 3). Meanwhile, in the plasma, the AUC value for paeonol microsponge cream was half that of the paeonol cream. Based on these results, paeonol-loaded microsponge formulations could be a better alternative for treating skin disease, as the formulation increases drug bioavailability by lengthening the time of drug residence in the skin and should reduce side-effects because of the lower levels of paeonol moving into the circulation.
研究领域:
药剂学
·
皮肤科学
·
药物代谢动力学
✓ 已验证
DOI
PubMed
高影响因子
XENOBIOTICA
·
2017
·
IF 1.932
Yinai Wu,Fengyun Liao,Weiguo Liao,Jianye Yu,Xingyun Deng,Huazhu Zheng,YingJiao Meng,Lisheng Wang
1. In traditional Chinese medicine, Angelica sinensis is often coprescribed with Ligusticum chuanxiong Hort for the treatment of ischemic cerebrovascular diseases. Tetramethylpyrazine (TMP) is one of the most important active ingredients isolated from Ligusticum chuanxiong Hort; ferulic acid (FA) is the main water-soluble component of Angelica sinensis.2. The purpose of this study is to investigate the possible effect of FA on the brain pharmacokinetics of TMP in conscious Sprague-Dawley rats. The pharmacokinetic parameters of TMP were investigated in brain microdialysates after oral and intravenous administration of TMP (4 mg/kg) to rats in the absence and presence of FA (5 mg/kg). Samples were collected at timed intervals for the measurement of TMP by a rapid and sensitive UPLC-MS/MS method.3. The pharmacokinetic parameters were calculated by noncompartmental analysis for brain microdialysates. The brain pharmacokinetic data for TMP showed significant increases in Cmax, t1/2, AUC0–inf and MRT0–inf after combination with FA. After intragastric administration with FA, there were significant decreases in the Tmax (from 38.33 ± 5.77 to 21 ± 5.48 min; p < 0.01) of TMP. This study indicated that potential drug–drug interaction between TMP and FA should be taken into consideration and the combined administration is beneficial in improving the bioavailability of TMP in the brain.
研究领域:
药理学
·
中药学
·
神经科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ANALYTICAL CHEMISTRY
·
2020
·
IF 6.785
Na Li,Shumu Li,Tuo Li,Hui Yang,Yangyang Zhang,Zhenwen Zhao
The combination of microdialysis and mass spectrometry (MS) provides the potential for rapidly monitoring diverse metabolites in vivo. Unfortunately, the high concentration of salt in biological microdialysates hindered the sensitive and online detection of these small molecular compounds. In this study, we synthesized Co-incorporated mesoporous carbon material (Co-NC) and developed a Co-NC-assisted laser desorption/ionization (LDI) ion source as an online interface of in vivo microdialysis coupled with MS for the direct analysis of diverse metabolites in microdialysates. The Co-NC could be used as a matrix for surface-assisted laser desorption/ionization mass spectrometry (SALDI MS) analysis of small molecular compounds, even under high concentration salt conditions. The Co-NC possessed the adsorption ability for small molecular compounds, and it was believed that the adsorption ability of Co-NC might separate the analytes from the salt in microdialysates at a microscopic level, which might facilitate the desorption and ionization of the analytes and finally improved the salt-tolerance ability as a matrix. Furthermore, the Co-NC-assisted LDI ion source as a novel interface of in vivo microdialysis coupled with MS has been applied to the online monitoring of liver metabolites from the CCl4-induced liver injury rat model for the first time.
研究领域:
分析化学
·
生物医学工程
·
代谢组学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）